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| ID | Type | Description | Link |
|---|---|---|---|
| BUS-P1-12 | Other Identifier | Bellus Health Inc |
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This is a phase 1, 2-part, open-label, fixed-sequence study evaluating potential drug-drug interactions between gemfibrozil (part 1) or dabigatran etexilate (part 2) and camlipixant (BLU-5937) 50 mg tablet in healthy participants under fasting conditions.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part 1: Camlipixant 50 mg + Gemfibrozil 600 mg | Experimental | Participants received a single oral dose of camlipixant 50 milligram (mg) tablet on Day 1, followed by repeat oral doses of gemfibrozil 600 mg tablet twice daily (BID), every 12 hours, (total daily dose of 1200 mg) on Days 5 to 11, with co-administration of a single oral dose of camlipixant 50 mg tablet with the gemfibrozil on Day 9. There was a washout of at least 4 days between the dose of camlipixant on Day 1 and the dose of gemfibrozil on Day 5. |
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| Part 2: Dabigatran etexilate 150 mg + camlipixant 50 mg | Experimental | Participants received single oral dose of dabigatran etexilate 150 mg capsule on Day 1, followed by repeated oral doses of camlipixant 50 mg tablet twice daily (BID) (total daily dose of 100 mg) from Days 5 to 9, with co-administration of a single oral dose of dabigatran etexilate 150 mg capsule with the morning dose of camlipixant on Day 10. There was a washout of at least 4 days between the dose of dabigatran etexilate on Day 1 and the dose of camlipixant on Day 5. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Camlipixant | Drug | Camlipixant will be administered |
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| Measure | Description | Time Frame |
|---|---|---|
| Part 1: Area Under the Concentration-time Curve From Time Zero to Infinity (AUC-inf) of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
| Part 1: Area Under the Concentration-time Curve From Time Zero Until the Last Observed Concentration (AUC[0-t]) of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
| Part 1: Maximal Observed Concentration (Cmax) of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
| Part 2: AUC(0-Infinity) of Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: AUC(0-t) of Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Measure | Description | Time Frame |
|---|---|---|
| Part 1: Time to Reach Maximum Observed Concentration (Tmax) of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
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Inclusion Criteria:
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| GSK Investigational Site | Québec | Quebec | G1P 0A2 | Canada |
A total of 45 participants were enrolled in the study (25 participants in Part 1 and 20 participants in Part 2). Only 32 participants (13 participants were never dosed) were dosed into the study to receive either camlipixant + gemfibrozil or dabigatran etexilate+ camlipixant creating the Safety Population. (The safety population included all participants who received at least one dose of any study drug).
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| ID | Title | Description |
|---|---|---|
| FG000 | Part 1: Camlipixant 50 mg + Gemfibrozil 600 mg | Participants received a single oral dose of camlipixant 50 milligram (mg) tablet on Day 1, followed by repeat oral doses of gemfibrozil 600 mg tablet twice daily (BID), every 12 hours, (total daily dose of 1200 mg) on Days 5 to 11, with co-administration of a single oral dose of camlipixant 50 mg tablet with the gemfibrozil on Day 9. There was a washout of at least 4 days between the dose of camlipixant on Day 1 and the dose of gemfibrozil on Day 5. |
| FG001 | Part 2: Dabigatran Etexilate 150 mg + Camlipixant 50 mg | Participants received single oral dose of dabigatran etexilate 150 mg capsule on Day 1, followed by repeated oral doses of camlipixant 50 mg tablet twice daily (BID) (total daily dose of 100 mg) from Days 5 to 9, with co-administration of a single oral dose of dabigatran etexilate 150 mg capsule with the morning dose of camlipixant on Day 10. There was a washout of at least 4 days between the dose of dabigatran etexilate on Day 1 and the dose of camlipixant on Day 5. |
| Title | Milestones | Reasons Not Completed | ||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Part 1 (Up to Day 21) |
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| Part 2 (Up to Day 22) |
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Baseline characteristics are reported for the Safety Population which consisted of all participants who received at least one dose of any study drug.
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| ID | Title | Description |
|---|---|---|
| BG000 | Part 1: Camlipixant 50 mg + Gemfibrozil 600 mg | Participants received a single oral dose of camlipixant 50 milligram (mg) tablet on Day 1, followed by repeat oral doses of gemfibrozil 600 mg tablet twice daily (BID), every 12 hours, (total daily dose of 1200 mg) on Days 5 to 11, with co-administration of a single oral dose of camlipixant 50 mg tablet with the gemfibrozil on Day 9. There was a washout of at least 4 days between the dose of camlipixant on Day 1 and the dose of gemfibrozil on Day 5. |
| Units | Counts |
|---|---|
| Participants |
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| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age, Customized | Count of Participants |
| Type | Title | Description | Population Description | Reporting Status | Anticipated Posting Date | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Time Frame | Units Analyzed | Denominator Units Selected | Arm/Group Information | Denominators | Classes | Analyses | |||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Primary | Part 1: Area Under the Concentration-time Curve From Time Zero to Infinity (AUC-inf) of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 9 PK profiles of the camlipixant could be adequately characterized, specifically, when administered alone and in combination with gemfibrozil (Part 1) | Posted | Geometric Mean | Geometric Coefficient of Variation | Hours*nanograms per milliliter | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
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Part1(Day1 postdose until Day5 predose of gemfibrozil [Camlipixant 50mg];from Day5 dosing until Day9 predose of camlipixant[Gemfibrozil 600mg];from camlipixant dosing on Day9 until end of study[Day21] [Camlipixant 50mg+Gemfibrozil 600mg]) and Part2(Day1 postdose until Day5 predose of camlipixant[Dabigatran etexilate 150mg];from Day5 dosing until Day10 predose of dabigatran[Camlipixant 50mg];from dabigatran dosing on Day10 until end of study [Day22] [Dabigatran etexilate 150mg+camlipixant 50mg])
Safety Population comprised of all participants who received at least one dose of any study drug. AEs were reported treatment-wise.
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| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | Part 1: Camlipixant 50 mg | Participants received a single oral dose of 50 mg camlipixant tablet on Day 1. |
| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Hepatic enzyme increased | Investigations | v26.0 | Systematic Assessment |
| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Palpitations | Cardiac disorders | v26.0 | Systematic Assessment |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| GSK Response Center | GlaxoSmithKline | 866-435-7343 | GSKClinicalSupportHD@gsk.com |
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| Type | Includes Protocol | Includes SAP | Includes ICF | Document Label | Document Date | Document Uploaded Date | Document File Name |
|---|---|---|---|---|---|---|---|
| Prot | Yes | No | No | Study Protocol | Jun 29, 2023 | Oct 11, 2024 | Prot_000.pdf |
| SAP | No | Yes | No | Statistical Analysis Plan | Nov 27, 2023 | Oct 11, 2024 | SAP_001.pdf |
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| ID | Term |
|---|---|
| D003371 | Cough |
| ID | Term |
|---|---|
| D012120 | Respiration Disorders |
| D012140 | Respiratory Tract Diseases |
| D012818 | Signs and Symptoms, Respiratory |
| D012816 | Signs and Symptoms |
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| ID | Term |
|---|---|
| D000069604 | Dabigatran |
| D015248 | Gemfibrozil |
| ID | Term |
|---|---|
| D011725 | Pyridines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D001562 | Benzimidazoles |
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| Dabigatran etexilate | Drug | Dabigatran etexilate will be administered |
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| Gemfibrozil | Drug | Gemfibrozil will be administered. |
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| Part 2: Cmax of Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: AUC(0-Infinity) of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: AUC(0-t) of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: Cmax of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 1: Terminal Elimination Half-Life (T1/2) Following Administration of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
| Part 1: Percentage of AUC0-Infinity Due to Extrapolation From the Time of the Last Observed Concentration to Infinity (%AUC Extrapolation) of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. Percentage of AUC extrapolation was calculated as [1 - (AUC0-t/AUC0-inf)] * 100. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
| Part 1: Terminal Elimination Rate Constant of Camlipixant (Kel) | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
| Part 1: Apparent Clearance (CL/F) of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
| Part 1: Apparent Volume of Distribution (Vz/F) of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
| Part 2: Tmax of Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: T1/2 Following Administration Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: Percentage of AUC0-Infinity Due to Extrapolation From the Time of the Last Observed Concentration to Infinity (%AUC Extrapolation) of Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. Percentage of AUC extrapolation was calculated as [1 - (AUC0-t/AUC0-inf)] * 100. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: Kel Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: CL/F Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: Vz/F Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: Tmax of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: T1/2 Following Administration of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: Percentage of AUC0-Infinity Due to Extrapolation From the Time of the Last Observed Concentration to Infinity (%AUC Extrapolation) of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. Percentage of AUC extrapolation was calculated as [1 - (AUC0-t/AUC0-inf)] * 100. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: Kel of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: CL/F of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 2: Vz/F of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
| Part 1: Number of Participants With Treatment-emergent Adverse Events (TEAEs), Treatment-emergent Serious Adverse Events (TESAEs) and Treatment-emergent Adverse Events of Medical Interest (TEAEMIs) | An adverse event (AE) is defined as any untoward medical occurrence in a participant who is administered a pharmaceutical product and which does not necessarily have a causal relationship with the treatment. Serious adverse events (SAEs) are defined as any untoward medical occurrence that; at any dose: results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, other situations as per medical and scientific judgement. Adverse events of medical interest (AEMIs) are AEs of scientific interest specific to the drug class. AEMIs for this study includes the following, but not limited to taste disturbances (dysgeusia, hypogeusia, ageusia), oral paresthesia and oral hypoesthesia Treatment-emergent events (i.e., TEAEs, TESAEs and TEAEMIs) were defined as events that commence on or after the time of first study drug administration | Day 1 post-dose until Day 5 pre-dose of gemfibrozil [camlipixant 50mg]; from Day 5 dosing until Day 9 pre-dose of camlipixant [gemfibrozil 600mg]; from camlipixant dosing on Day 9 until end of study [Day 21] [camlipixant 50mg+gemfibrozil 600mg] |
| Part 2: Number of Participants With TEAEs, TESAEs and TEAEMIs | An adverse event (AE) is defined as any untoward medical occurrence in a participant who is administered a pharmaceutical product and which does not necessarily have a causal relationship with the treatment. Serious adverse events (SAEs) are defined as any untoward medical occurrence that; at any dose: results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, other situations as per medical and scientific judgement. Adverse events of medical interest (AEMIs) are AEs of scientific interest specific to the drug class. AEMIs for this study includes the following, but not limited to: taste disturbances (dysgeusia, hypogeusia, ageusia), oral paresthesia and oral hypoesthesia Treatment-emergent events (i.e., TEAEs, TESAEs and TEAEMIs) were defined as events that commence on or after the time of first study drug administration. | Day1 postdose until Day5 predose of camlipixant [dabigatran etexilate 150mg];from Day5 dosing until Day10 predose of dabigatran [camlipixant 50mg];from dabigatran dosing on Day10 until end of study [Day 22][dabigatran etexilate 150mg+camlipixant 50mg] |
| Part 1: Number of Participants With Abnormal Clinically Significant Changes in 12-Lead Electrocardiogram (ECG) Findings | A 12-lead ECG was recorded with the participant in a semi-recumbent or supine position, after 5 minutes of rest using an ECG machine. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant 12-Lead ECG findings have been presented. | Day 5, Day 9 pre-dose and 1 hour post-dose, Day 12 |
| Part 2: Number of Participants With Abnormal Clinically Significant Changes in 12-Lead ECG Findings | A 12-lead ECG was recorded with the participant in a semi-recumbent or supine position, after 5 minutes of rest using an ECG machine. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant 12-Lead ECG findings have been presented. | Day 5, Day 10 and Day 13 |
| Part 1: Number of Participants With Abnormal Clinically Significant Changes in Vital Signs: Diastolic Blood Pressure (DBP), Systolic Blood Pressure (SBP), and Heart Rate | Vital signs including DBP, SBP, and heart rate were measured in a sitting position after resting for at least 5 minutes. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant changes for vital signs have been presented. | Day 9 and Day 12 |
| Part 2: Number of Participants With Abnormal Clinically Significant Changes in Vital Signs: DBP, SBP, and Heart Rate | Vital signs including DBP, SBP, and heart rate were measured in a sitting position after resting for at least 5 minutes. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant changes for vital signs have been presented. | Day 10 and Day 13 |
| Part 1: Number of Participants With Abnormal Clinically Significant Changes in Vital Signs: Respiratory Rate and Oral Temperature | Vital signs including respiratory rate and oral temperature were measured after resting for at least 5 minutes in a sitting position. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant changes for vital signs have been presented. | Day 12 |
| Part 2: Number of Participants With Abnormal Clinically Significant Changes in Vital Signs: Respiratory Rate and Oral Temperature | Vital signs including respiratory rate and oral temperature were measured after resting for at least 5 minutes in a sitting position. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant changes for vital signs have been presented. | Day 13 |
| Part 1: Number of Participants With Abnormal Clinically Significant Changes During Physical Examination | Physical examination included assessment of the head, eyes, ears, nose, throat, neck, chest, lungs, abdomen, musculoskeletal, dermatological, cardiovascular/peripheral vascular, and general neurological examination. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant changes in physical examination has been presented. | Up to Day 12 |
| Part 2: Number of Participants With Abnormal Clinically Significant Changes During Physical Examination | Physical examination included assessment of the head, eyes, ears, nose, throat, neck, chest, lungs, abdomen, musculoskeletal, dermatological, cardiovascular/peripheral vascular, and general neurological examination. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant changes in physical examination has been presented. | Up to Day 13 |
| Part 1: Number of Participants With Abnormal Clinically Significant Changes in Hematology Parameters | Blood samples were collected to analyze hematology parameters: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Hematocrit, Hemoglobin, Platelets, and Erythrocytes. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of participants with abnormal clinically significant changes in hematology parameters were reported. | Up to Day 12 |
| Part 2: Number of Participants With Abnormal Clinically Significant Changes in Hematology Parameters | Blood samples were collected to analyze hematology parameters: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Hematocrit, Hemoglobin, Platelets, and Erythrocytes. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of participants with abnormal clinically significant changes in hematology parameters were reported. | Up to Day 13 |
| Part 1: Number of Participants With Abnormal Clinically Significant Changes in Clinical Chemistry Parameters | Blood samples were collected to analyze clinical chemical parameters: albumin, alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase, calcium, chloride, creatinine kinase, creatinine, gamma glutamyl transferase, glucose, phosphate, potassium, sodium, total, direct, and indirect bilirubin, protein, urea, and urate. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of Participants with abnormal clinically significant changes in clinical chemistry parameters were reported. | Up to Day 12 |
| Part 2: Number of Participants With Abnormal Clinically Significant Changes in Clinical Chemistry Parameters | Blood samples were collected to analyze clinical chemical parameters: albumin, alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase, calcium, chloride, creatinine kinase, creatinine, gamma glutamyl transferase, glucose, phosphate, potassium, sodium, total, direct, and indirect bilirubin, protein, urea, and urate. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of Participants with abnormal clinically significant changes in clinical chemistry parameters were reported. | Up to Day 13 |
| Part 1: Number of Participants With Abnormal Clinically Significant Changes in Coagulation Parameters | Blood samples were collected to analyze coagulation parameters: activated partial thromboplastin time, prothrombin time international normalized ratio (INR), and prothrombin time. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of Participants with abnormal clinically significant changes in coagulation parameters were reported. | Up to Day 12 |
| Part 2: Number of Participants With Abnormal Clinically Significant Changes in Coagulation Parameters | Blood samples were collected to analyze coagulation parameters: activated partial thromboplastin time, prothrombin time international normalized ratio (INR), and prothrombin time. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of Participants with abnormal clinically significant changes in coagulation parameters were reported. | Up to Day 13 |
| Part 1: Number of Participants With Abnormal Clinically Significant Changes in Urinalysis | Urine samples were collected to analyze urinalysis parameters: specific gravity and potential of hydrogen (pH). Bilirubin, blood (occult), glucose, ketones, leukocyte esterase, nitrite, protein, urobilinogen were analyzed by dipstick. The dipstick test gives results in a semi-quantitative manner, and results can be read as Negative, Trace, 1+, 2+ indicating proportional concentrations in the urine sample. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of Participants with abnormal clinically significant changes in urinalysis parameters were reported. | Up to Day 12 |
| Part 2: Number of Participants With Abnormal Clinically Significant Changes in Urinalysis | Urine samples were collected to analyze urinalysis parameters: specific gravity and potential of hydrogen (pH). Bilirubin, blood (occult), glucose, ketones, leukocyte esterase, nitrite, protein, urobilinogen were analyzed by dipstick. The dipstick test gives results in a semi-quantitative manner, and results can be read as Negative, Trace, 1+, 2+ indicating proportional concentrations in the urine sample. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of Participants with abnormal clinically significant changes in urinalysis parameters were reported. | Up to Day 13 |
| COMPLETED |
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| NOT COMPLETED |
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| BG001 | Part 2: Dabigatran Etexilate 150 mg + Camlipixant 50 mg | Participants received single oral dose of dabigatran etexilate 150 mg capsule on Day 1, followed by repeated oral doses of camlipixant 50 mg tablet twice daily (BID) (total daily dose of 100 mg) from Days 5 to 9, with co-administration of a single oral dose of dabigatran etexilate 150 mg capsule with the morning dose of camlipixant on Day 10. There was a washout of at least 4 days between the dose of dabigatran etexilate on Day 1 and the dose of camlipixant on Day 5. |
| BG002 | Total | Total of all reporting groups |
| Participants |
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| Sex: Female, Male | Count of Participants | Participants |
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| Race/Ethnicity, Customized | "All Other Races" category (Black and Asian where 0\ | Count of Participants | Participants |
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| Primary | Part 1: Area Under the Concentration-time Curve From Time Zero Until the Last Observed Concentration (AUC[0-t]) of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 9 PK profiles of the camlipixant could be adequately characterized, specifically, when administered alone and in combination with gemfibrozil (Part 1) | Posted | Geometric Mean | Geometric Coefficient of Variation | Hours*nanograms per milliliter | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
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| Primary | Part 1: Maximal Observed Concentration (Cmax) of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 9 PK profiles of the camlipixant could be adequately characterized, specifically, when administered alone and in combination with gemfibrozil (Part 1) | Posted | Geometric Mean | Geometric Coefficient of Variation | Nanograms per milliliter | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
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| Primary | Part 2: AUC(0-Infinity) of Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hours*nanograms per milliliter | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Primary | Part 2: AUC(0-t) of Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hours*nanograms per milliliter | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Primary | Part 2: Cmax of Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | Nanograms per milliliter | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Primary | Part 2: AUC(0-Infinity) of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hours*nanograms per milliliter | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Primary | Part 2: AUC(0-t) of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hours*nanograms per milliliter | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Primary | Part 2: Cmax of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | Nanograms per milliliter | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Secondary | Part 1: Time to Reach Maximum Observed Concentration (Tmax) of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 9 PK profiles of the camlipixant could be adequately characterized, specifically, when administered alone and in combination with gemfibrozil (Part 1) | Posted | Median | Full Range | Hours | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
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| Secondary | Part 1: Terminal Elimination Half-Life (T1/2) Following Administration of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 9 PK profiles of the camlipixant could be adequately characterized, specifically, when administered alone and in combination with gemfibrozil (Part 1) | Posted | Geometric Mean | Geometric Coefficient of Variation | Hours | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
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| Secondary | Part 1: Percentage of AUC0-Infinity Due to Extrapolation From the Time of the Last Observed Concentration to Infinity (%AUC Extrapolation) of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. Percentage of AUC extrapolation was calculated as [1 - (AUC0-t/AUC0-inf)] * 100. | The PK parameter Population included all participants for whom the Day 1 and Day 9 PK profiles of the camlipixant could be adequately characterized, specifically, when administered alone and in combination with gemfibrozil (Part 1) | Posted | Geometric Mean | Geometric Coefficient of Variation | Percentage of AUC extrapolation | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
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| Secondary | Part 1: Terminal Elimination Rate Constant of Camlipixant (Kel) | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 9 PK profiles of the camlipixant could be adequately characterized, specifically, when administered alone and in combination with gemfibrozil (Part 1) | Posted | Geometric Mean | Geometric Coefficient of Variation | h^-1 | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
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| Secondary | Part 1: Apparent Clearance (CL/F) of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 9 PK profiles of the camlipixant could be adequately characterized, specifically, when administered alone and in combination with gemfibrozil (Part 1) | Posted | Geometric Mean | Geometric Coefficient of Variation | Liters per hour | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
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| Secondary | Part 1: Apparent Volume of Distribution (Vz/F) of Camlipixant | Blood samples were collected at indicated time points for PK analysis of Camlipixant. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 9 PK profiles of the camlipixant could be adequately characterized, specifically, when administered alone and in combination with gemfibrozil (Part 1) | Posted | Geometric Mean | Geometric Coefficient of Variation | Liters | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 15, 18, 24, 48, 72 hours post-dose on Day 1 and Day 9 |
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| Secondary | Part 2: Tmax of Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Median | Full Range | Hours | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Secondary | Part 2: T1/2 Following Administration Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hours | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Secondary | Part 2: Percentage of AUC0-Infinity Due to Extrapolation From the Time of the Last Observed Concentration to Infinity (%AUC Extrapolation) of Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. Percentage of AUC extrapolation was calculated as [1 - (AUC0-t/AUC0-inf)] * 100. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | Percentage of AUC extrapolation | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Secondary | Part 2: Kel Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | h^-1 | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Secondary | Part 2: CL/F Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | Liters per hour | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Secondary | Part 2: Vz/F Free Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | Liters | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Secondary | Part 2: Tmax of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Median | Full Range | Hours | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Secondary | Part 2: T1/2 Following Administration of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hours | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Secondary | Part 2: Percentage of AUC0-Infinity Due to Extrapolation From the Time of the Last Observed Concentration to Infinity (%AUC Extrapolation) of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. Percentage of AUC extrapolation was calculated as [1 - (AUC0-t/AUC0-inf)] * 100. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | Percentage of AUC extrapolation | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Secondary | Part 2: Kel of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | h^-1 | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Secondary | Part 2: CL/F of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | Liters per hour | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Secondary | Part 2: Vz/F of Total Dabigatran | Blood samples were collected at indicated time points for PK analysis of Dabigatran. PK analysis was conducted using standard non-compartmental methods. | The PK parameter Population included all participants for whom the Day 1 and Day 10 PK profiles of the dabigatran could be adequately characterized, specifically, when administered alone and in combination with camlipixant (Part 2). Only those participants who were measured and analyzed (i.e., contributed data reported in table) were included in 'Overall Number of Participants Analyzed' field. | Posted | Geometric Mean | Geometric Coefficient of Variation | Liters | Pre-dose, 0.25 , 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 16, 24, 36, 48, 60, 72 hours post-dose on Day 1 and Day 10 |
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| Secondary | Part 1: Number of Participants With Treatment-emergent Adverse Events (TEAEs), Treatment-emergent Serious Adverse Events (TESAEs) and Treatment-emergent Adverse Events of Medical Interest (TEAEMIs) | An adverse event (AE) is defined as any untoward medical occurrence in a participant who is administered a pharmaceutical product and which does not necessarily have a causal relationship with the treatment. Serious adverse events (SAEs) are defined as any untoward medical occurrence that; at any dose: results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, other situations as per medical and scientific judgement. Adverse events of medical interest (AEMIs) are AEs of scientific interest specific to the drug class. AEMIs for this study includes the following, but not limited to taste disturbances (dysgeusia, hypogeusia, ageusia), oral paresthesia and oral hypoesthesia Treatment-emergent events (i.e., TEAEs, TESAEs and TEAEMIs) were defined as events that commence on or after the time of first study drug administration | Safety Population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Day 1 post-dose until Day 5 pre-dose of gemfibrozil [camlipixant 50mg]; from Day 5 dosing until Day 9 pre-dose of camlipixant [gemfibrozil 600mg]; from camlipixant dosing on Day 9 until end of study [Day 21] [camlipixant 50mg+gemfibrozil 600mg] |
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| Secondary | Part 2: Number of Participants With TEAEs, TESAEs and TEAEMIs | An adverse event (AE) is defined as any untoward medical occurrence in a participant who is administered a pharmaceutical product and which does not necessarily have a causal relationship with the treatment. Serious adverse events (SAEs) are defined as any untoward medical occurrence that; at any dose: results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, other situations as per medical and scientific judgement. Adverse events of medical interest (AEMIs) are AEs of scientific interest specific to the drug class. AEMIs for this study includes the following, but not limited to: taste disturbances (dysgeusia, hypogeusia, ageusia), oral paresthesia and oral hypoesthesia Treatment-emergent events (i.e., TEAEs, TESAEs and TEAEMIs) were defined as events that commence on or after the time of first study drug administration. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Day1 postdose until Day5 predose of camlipixant [dabigatran etexilate 150mg];from Day5 dosing until Day10 predose of dabigatran [camlipixant 50mg];from dabigatran dosing on Day10 until end of study [Day 22][dabigatran etexilate 150mg+camlipixant 50mg] |
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| Secondary | Part 1: Number of Participants With Abnormal Clinically Significant Changes in 12-Lead Electrocardiogram (ECG) Findings | A 12-lead ECG was recorded with the participant in a semi-recumbent or supine position, after 5 minutes of rest using an ECG machine. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant 12-Lead ECG findings have been presented. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Day 5, Day 9 pre-dose and 1 hour post-dose, Day 12 |
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| Secondary | Part 2: Number of Participants With Abnormal Clinically Significant Changes in 12-Lead ECG Findings | A 12-lead ECG was recorded with the participant in a semi-recumbent or supine position, after 5 minutes of rest using an ECG machine. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant 12-Lead ECG findings have been presented. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Day 5, Day 10 and Day 13 |
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| Secondary | Part 1: Number of Participants With Abnormal Clinically Significant Changes in Vital Signs: Diastolic Blood Pressure (DBP), Systolic Blood Pressure (SBP), and Heart Rate | Vital signs including DBP, SBP, and heart rate were measured in a sitting position after resting for at least 5 minutes. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant changes for vital signs have been presented. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Day 9 and Day 12 |
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| Secondary | Part 2: Number of Participants With Abnormal Clinically Significant Changes in Vital Signs: DBP, SBP, and Heart Rate | Vital signs including DBP, SBP, and heart rate were measured in a sitting position after resting for at least 5 minutes. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant changes for vital signs have been presented. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Day 10 and Day 13 |
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| Secondary | Part 1: Number of Participants With Abnormal Clinically Significant Changes in Vital Signs: Respiratory Rate and Oral Temperature | Vital signs including respiratory rate and oral temperature were measured after resting for at least 5 minutes in a sitting position. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant changes for vital signs have been presented. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Day 12 |
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| Secondary | Part 2: Number of Participants With Abnormal Clinically Significant Changes in Vital Signs: Respiratory Rate and Oral Temperature | Vital signs including respiratory rate and oral temperature were measured after resting for at least 5 minutes in a sitting position. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant changes for vital signs have been presented. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Day 13 |
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| Secondary | Part 1: Number of Participants With Abnormal Clinically Significant Changes During Physical Examination | Physical examination included assessment of the head, eyes, ears, nose, throat, neck, chest, lungs, abdomen, musculoskeletal, dermatological, cardiovascular/peripheral vascular, and general neurological examination. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant changes in physical examination has been presented. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Up to Day 12 |
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| Secondary | Part 2: Number of Participants With Abnormal Clinically Significant Changes During Physical Examination | Physical examination included assessment of the head, eyes, ears, nose, throat, neck, chest, lungs, abdomen, musculoskeletal, dermatological, cardiovascular/peripheral vascular, and general neurological examination. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for the number of participants with abnormal clinically significant changes in physical examination has been presented. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Up to Day 13 |
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| Secondary | Part 1: Number of Participants With Abnormal Clinically Significant Changes in Hematology Parameters | Blood samples were collected to analyze hematology parameters: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Hematocrit, Hemoglobin, Platelets, and Erythrocytes. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of participants with abnormal clinically significant changes in hematology parameters were reported. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Up to Day 12 |
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| Secondary | Part 2: Number of Participants With Abnormal Clinically Significant Changes in Hematology Parameters | Blood samples were collected to analyze hematology parameters: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Hematocrit, Hemoglobin, Platelets, and Erythrocytes. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of participants with abnormal clinically significant changes in hematology parameters were reported. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Up to Day 13 |
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| Secondary | Part 1: Number of Participants With Abnormal Clinically Significant Changes in Clinical Chemistry Parameters | Blood samples were collected to analyze clinical chemical parameters: albumin, alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase, calcium, chloride, creatinine kinase, creatinine, gamma glutamyl transferase, glucose, phosphate, potassium, sodium, total, direct, and indirect bilirubin, protein, urea, and urate. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of Participants with abnormal clinically significant changes in clinical chemistry parameters were reported. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Up to Day 12 |
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| Secondary | Part 2: Number of Participants With Abnormal Clinically Significant Changes in Clinical Chemistry Parameters | Blood samples were collected to analyze clinical chemical parameters: albumin, alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase, calcium, chloride, creatinine kinase, creatinine, gamma glutamyl transferase, glucose, phosphate, potassium, sodium, total, direct, and indirect bilirubin, protein, urea, and urate. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of Participants with abnormal clinically significant changes in clinical chemistry parameters were reported. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Up to Day 13 |
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| Secondary | Part 1: Number of Participants With Abnormal Clinically Significant Changes in Coagulation Parameters | Blood samples were collected to analyze coagulation parameters: activated partial thromboplastin time, prothrombin time international normalized ratio (INR), and prothrombin time. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of Participants with abnormal clinically significant changes in coagulation parameters were reported. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Up to Day 12 |
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| Secondary | Part 2: Number of Participants With Abnormal Clinically Significant Changes in Coagulation Parameters | Blood samples were collected to analyze coagulation parameters: activated partial thromboplastin time, prothrombin time international normalized ratio (INR), and prothrombin time. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of Participants with abnormal clinically significant changes in coagulation parameters were reported. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Up to Day 13 |
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| Secondary | Part 1: Number of Participants With Abnormal Clinically Significant Changes in Urinalysis | Urine samples were collected to analyze urinalysis parameters: specific gravity and potential of hydrogen (pH). Bilirubin, blood (occult), glucose, ketones, leukocyte esterase, nitrite, protein, urobilinogen were analyzed by dipstick. The dipstick test gives results in a semi-quantitative manner, and results can be read as Negative, Trace, 1+, 2+ indicating proportional concentrations in the urine sample. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of Participants with abnormal clinically significant changes in urinalysis parameters were reported. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Up to Day 12 |
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| Secondary | Part 2: Number of Participants With Abnormal Clinically Significant Changes in Urinalysis | Urine samples were collected to analyze urinalysis parameters: specific gravity and potential of hydrogen (pH). Bilirubin, blood (occult), glucose, ketones, leukocyte esterase, nitrite, protein, urobilinogen were analyzed by dipstick. The dipstick test gives results in a semi-quantitative manner, and results can be read as Negative, Trace, 1+, 2+ indicating proportional concentrations in the urine sample. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Number of Participants with abnormal clinically significant changes in urinalysis parameters were reported. | Safety population consisted of all participants who received at least one dose of any study drug. | Posted | Count of Participants | Participants | Up to Day 13 |
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|
|
| 0 |
| 16 |
| 0 |
| 16 |
| 1 |
| 16 |
| EG001 | Part 1: Gemfibrozil 600 mg | Participants received repeated oral doses of gemfibrozil 600 mg tablet twice daily (BID), every 12 hours, (total daily dose of 1200 mg) on Days 5 to 11. | 0 | 16 | 0 | 16 | 6 | 16 |
| EG002 | Part 1: Camlipixant 50 mg+ Gemfibrozil 600 mg | Participants received repeated oral doses of gemfibrozil 600 mg tablet twice daily (BID), every 12 hours, (total daily dose of 1200 mg) on Days 5 to 11, with co-administration of a single oral dose of camlipixant 50 mg tablet with the gemfibrozil on Day 9. Participants were followed up for adverse events until end of study (up to Day 21) | 0 | 16 | 1 | 16 | 5 | 16 |
| EG003 | Part 2: Dabigatran Etexilate 150 mg | Participants received single oral dose of dabigatran etexilate 150 mg capsule on Day 1 | 0 | 16 | 0 | 16 | 4 | 16 |
| EG004 | Part 2: Camlipixant 50 mg | Participants received repeated oral doses of camlipixant 50 mg tablet twice daily (BID) (total daily dose of 100 mg) from Days 5 to 10. | 0 | 15 | 0 | 15 | 6 | 15 |
| EG005 | Part 2: Dabigatran Etexilate 150 mg+ Camlipixant 50 mg | Participants received repeated oral doses of camlipixant 50 mg tablet twice daily (BID) (total daily dose of 100 mg) from Days 5 to 9, with co-administration of a single oral dose of dabigatran etexilate 150 mg capsule with the morning dose of camlipixant on Day 10. Participants were followed up for adverse events until end of study (up to Day 22). | 0 | 14 | 0 | 14 | 0 | 14 |
| Abdominal pain upper | Gastrointestinal disorders | v26.0 | Systematic Assessment |
|
| Thyroxine free decreased | Investigations | v26.0 | Systematic Assessment |
|
| Dysgeusia | Nervous system disorders | v26.0 | Systematic Assessment |
|
| Headache | Nervous system disorders | v26.0 | Systematic Assessment |
|
| Affect lability | Psychiatric disorders | v26.0 | Systematic Assessment |
|
| Constipation | Gastrointestinal disorders | MedDRA v26.0 | Systematic Assessment |
|
| Abdominal pain | Gastrointestinal disorders | MedDRA v26.0 | Systematic Assessment |
|
| Aphthous ulcer | Gastrointestinal disorders | MedDRA v26.0 | Systematic Assessment |
|
| Faeces soft | Gastrointestinal disorders | MedDRA v26.0 | Systematic Assessment |
|
| Flatulence | Gastrointestinal disorders | MedDRA v26.0 | Systematic Assessment |
|
| Gastrointestinal sounds abnormal | Gastrointestinal disorders | MedDRA v26.0 | Systematic Assessment |
|
| Feeling hot | General disorders | MedDRA v26.0 | Systematic Assessment |
|
| Chest discomfort | General disorders | MedDRA v26.0 | Systematic Assessment |
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| Feeling abnormal | General disorders | MedDRA v26.0 | Systematic Assessment |
|
| Alanine aminotransferase increased | Investigations | MedDRA v26.0 | Systematic Assessment |
|
| Aspartate aminotransferase increased | Investigations | MedDRA v26.0 | Systematic Assessment |
|
| Blood pressure increased | Investigations | MedDRA v26.0 | Systematic Assessment |
|
| Heart rate increased | Investigations | MedDRA v26.0 | Systematic Assessment |
|
| Back pain | Musculoskeletal and connective tissue disorders | MedDRA v26.0 | Systematic Assessment |
|
| Diarrhoea | Gastrointestinal disorders | MedDRA v26.0 | Systematic Assessment |
|
| Gastrooesophageal reflux disease | Gastrointestinal disorders | MedDRA v26.0 | Systematic Assessment |
|
| Nausea | Gastrointestinal disorders | MedDRA v26.0 | Systematic Assessment |
|
| Gamma-glutamyltransferase increased | Investigations | MedDRA v26.0 | Systematic Assessment |
|
| SARS-CoV-2 test positive | Investigations | MedDRA v26.0 | Systematic Assessment |
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| Somnolence | Nervous system disorders | MedDRA v26.0 | Systematic Assessment |
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| Dry eye | Eye disorders | MedDRA v26.0 | Systematic Assessment |
|
| Photophobia | Eye disorders | MedDRA v26.0 | Systematic Assessment |
|
| Procedural dizziness | Injury, poisoning and procedural complications | MedDRA v26.0 | Systematic Assessment |
|
| Pollakiuria | Renal and urinary disorders | MedDRA v26.0 | Systematic Assessment |
|
| Hand dermatitis | Skin and subcutaneous tissue disorders | MedDRA v26.0 | Systematic Assessment |
|
GSK agreements may vary with individual investigators, but will not prohibit any investigator from publishing. GSK supports the publication of results from all centers of a multi-center trial but requests that reports based on single site data not precede the primary publication of the entire clinical trial.
| D013568 | Pathological Conditions, Signs and Symptoms |
| D006574 |
| Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| D058607 | Fibric Acids |
| D058610 | Isobutyrates |
| D002087 | Butyrates |
| D000144 | Acids, Acyclic |
| D002264 | Carboxylic Acids |
| D009930 | Organic Chemicals |
| D010421 | Pentanoic Acids |
| D014631 | Valerates |
| D010647 | Phenyl Ethers |
| D004987 | Ethers |
| D010636 | Phenols |
| D001555 | Benzene Derivatives |
| D006841 | Hydrocarbons, Aromatic |
| D006844 | Hydrocarbons, Cyclic |
| D006838 | Hydrocarbons |
| D005232 | Fatty Acids, Volatile |
| D005227 | Fatty Acids |
| D008055 | Lipids |
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