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| ID | Type | Description | Link |
|---|---|---|---|
| J2G-OX-JZJP | Other Identifier | Eli Lilly and Company | |
| LOXO-RET-18014 | Other Identifier | Loxo Oncology, Inc. |
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| Name | Class |
|---|---|
| Loxo Oncology, Inc. | INDUSTRY |
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The main purpose of this study is to assess the effect of itraconazole and rifampin on how fast selpercatinib gets into the blood stream and how long it takes the body to remove it when administered in healthy participants. Information about safety and tolerability will be collected. The study is conducted in two parts and it will last up to 54 days (part 1) and 59 days (part 2), respectively, inclusive of screening period.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part 1 - 160 mg Selpercatinib + 200 mg Itraconazole | Experimental | Participants received a single oral dose of 160 milligrams (mg) selpercatinib on Day 1 of Period 1. In Period 2, participants received an oral dose of 200 mg itraconazole administered once daily (QD) for 11 consecutive days (Days -4 to 7) with a single oral dose of 160 mg selpercatinib co-administered on Day 1 of Period 2. There was a washout period of at least 7 days between the dose of selpercatinib in Period 1 and the first dose of itraconazole in Period 2. |
|
| Part 2 - 160 mg Selpercatinib + 600 mg Rifampin | Experimental | Participants received a single oral dose of 160 mg selpercatinib on Day 1 of Period 1. In Period 2, participants received an oral dose of 600 mg rifampin administered QD for 16 consecutive days (Days 1 to 16) with a single oral dose of 160 mg selpercatinib co-administered on Day 1 and Day 10 of Period 2. There was a washout period of at least 7 days between the dose of selpercatinib in Period 1 and the first dose of rifampin and selpercatinib in Period 2. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Selpercatinib | Drug | Administered orally. |
|
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib | PK: AUC0-t of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.) | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
| PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib | PK: AUC0-inf of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.) | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
| PK: Percentage of AUC0-inf Extrapolated (AUC%Extrap) of Selpercatinib | PK: AUC%extrap of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.) | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
| PK: Maximum Observed Concentration (Cmax) of Selpercatinib |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Call 1-877-CTLILLY (1-877-285-4559) or 1-317-615-4559 Mon - Fri 9 AM - 5 PM Eastern time (UTC/GMT - 5 hours, EST) | Eli Lilly and Company | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Celerion | Tempe | Arizona | 85283 | United States |
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| ID | Title | Description |
|---|---|---|
| FG000 | Part 1 - 160 mg Selpercatinib + 200 mg Itraconazole | Participants received a single oral dose of 160 milligrams (mg) selpercatinib on Day 1 of Period 1. In Period 2, participants received an oral dose of 200 mg itraconazole administered once daily (QD) for 11 consecutive days (Days -4 to 7) with a single oral dose of 160 mg selpercatinib co-administered on Day 1 of Period 2. There was a washout period of at least 7 days between the dose of selpercatinib in Period 1 and the first dose of itraconazole in Period 2. |
| FG001 | Part 2 - 160 mg Selpercatinib + 600 mg Rifampin | Participants received a single oral dose of 160 mg selpercatinib on Day 1 of Period 1. In Period 2, participants received an oral dose of 600 mg rifampin administered QD for 16 consecutive days (Days 1 to 16) with a single oral dose of 160 mg selpercatinib co-administered on Day 1 and Day 10 of Period 2. There was a washout period of at least 7 days between the dose of selpercatinib in Period 1 and the first dose of rifampin and selpercatinib in Period 2. |
| Title | Milestones | Reasons Not Completed | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Period 1 |
| ||||||||||||||||
| Period 2 |
|
All participants who received at least one dose of study drug.
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| ID | Title | Description |
|---|---|---|
| BG000 | Part 1 - 160 mg Selpercatinib + 200 mg Itraconazole | Participants received a single oral dose of 160 mg selpercatinib on Day 1 of Period 1. In Period 2, participants received an oral dose of 200 mg itraconazole administered QD for 11 consecutive days (Days -4 to 7) with a single oral dose of 160 mg selpercatinib co-administered on Day 1 of Period 2. There was a washout period of at least 7 days between the dose of selpercatinib in Period 1 and the first dose of itraconazole in Period 2. |
| Units | Counts |
|---|---|
| Participants |
|
| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age, Continuous | Mean |
| 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 | Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib | PK: AUC0-t of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.) | All participants who received at least one dose of selpercatinib with evaluable PK data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanogram *hour per milliliter (ng*h/mL) | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
|
Baseline Up To 50 Days
All participants who received at least one dose of study drug. Gender specific events occurring only in male or female participants have had the number of participants at risk adjusted accordingly. Per pre-specified analysis, adverse events were reported as per the treatment regimen received.
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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 Period 1: 160 mg Selpercatinib | Participants received a single oral dose of 160 mg selpercatinib on Day 1 of Period 1. |
Not provided
| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Abdominal pain | Gastrointestinal disorders | MedDRA 21.0 | Systematic Assessment |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Chief Medical Officer | Eli Lilly and Company | 8005455979 | ClinicalTrials.gov@lilly.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 11, 2018 | Aug 21, 2025 | Prot_000.pdf |
| SAP | No | Yes | No | Statistical Analysis Plan | Sep 7, 2018 | Aug 20, 2025 | SAP_001.pdf |
Not provided
| ID | Term |
|---|---|
| C000656166 | selpercatinib |
| D017964 | Itraconazole |
| D012293 | Rifampin |
| ID | Term |
|---|---|
| D014230 | Triazoles |
| D001393 | Azoles |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
Not provided
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| Itraconazole | Drug | Administered orally. |
|
| Rifampin | Drug | Administered orally. |
|
PK: Maximum observed concentration (Cmax) of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
| (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
| PK: Time to Reach Cmax (Tmax) of Selpercatinib | PK: Tmax of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.) | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
| PK: Apparent First-order Terminal Elimination Rate Constant (Kel) of Selpercatinib | PK: Kel of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.) | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
| PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Selpercatinib | PK: CL/F of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.) | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
| PK: Apparent First-order Terminal Elimination Half-life (t½) of Selpercatinib | PK: t½ of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.) | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
| Part 2 - PK: Area Under the Concentration-Time Curve From Time 0 to 24 Hours (AUC0-24) of Selpercatinib Post Dose Day 1 | PK: AUC0-24 of Selpercatinib in Part 2 was reported. | Part 2, Periods 1 and 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose. |
| COMPLETED |
|
| NOT COMPLETED |
|
| BG001 | Part 2 - 160 mg Selpercatinib + 600 mg Rifampin | Participants received a single oral dose of 160 mg selpercatinib on Day 1 of Period 1. In Period 2, participants received an oral dose of 600 mg rifampin administered QD for 16 consecutive days (Days 1 to 16) with a single oral dose of 160 mg selpercatinib co-administered on Day 1 and Day 10 of Period 2. There was a washout period of at least 7 days between the dose of selpercatinib in Period 1 and the first dose of rifampin and selpercatinib in Period 2. |
| BG002 | Total | Total of all reporting groups |
| years |
|
| Sex: Female, Male | Count of Participants | Participants | No |
|
| Ethnicity (NIH/OMB) | Count of Participants | Participants | No |
|
| Race (NIH/OMB) | Count of Participants | Participants | No |
|
| Region of Enrollment | Count of Participants | Participants | No |
|
Participants received a single oral dose of 160 mg selpercatinib on Day 1 of Period 1. |
| OG001 | Part 1 Period 2: 160 mg Selpercatinib + 200 mg Itraconazole | Participants received an oral dose of 200 mg itraconazole administered QD for 11 consecutive days (Days -4 to 7) with a single oral dose of 160 mg selpercatinib co-administered on Day 1 of Period 2. |
| OG002 | Part 2 Period 1: 160 mg Selpercatinib | Participants received a single oral dose of 160 mg selpercatinib on Day 1 of Period 1. |
| OG003 | Part 2 Period 2: 160 mg Selpercatinib on Day 1 + 600 mg Rifampin | Participants received an oral dose of 600 mg rifampin administered QD for 16 consecutive days (Days 1 to 16) with a single oral dose of 160 mg selpercatinib co-administered on Day 1 of Period 2. |
| OG004 | Part 2 Period 2: 160 mg Selpercatinib on Day 10 + 600 mg Rifampin | Participants received an oral dose of 600 mg rifampin administered QD for 16 consecutive days (Days 1 to 16) with a single oral dose of 160 mg selpercatinib co-administered on Day 10 of Period 2. |
|
|
| Primary | PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib | PK: AUC0-inf of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.) | All participants who received at least one dose of selpercatinib with evaluable PK data. | Posted | Geometric Mean | Geometric Coefficient of Variation | ng*hr/mL | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
|
|
|
| Primary | PK: Percentage of AUC0-inf Extrapolated (AUC%Extrap) of Selpercatinib | PK: AUC%extrap of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.) | All participants who received at least one dose of selpercatinib with evaluable PK data. | Posted | Geometric Mean | Geometric Coefficient of Variation | percentage of AUC0-inf extrapolated | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
|
|
|
| Primary | PK: Maximum Observed Concentration (Cmax) of Selpercatinib | PK: Maximum observed concentration (Cmax) of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. | All participants who received at least one dose of selpercatinib with evaluable PK data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanograms per milliliter (ng/mL) | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
|
|
|
| Primary | PK: Time to Reach Cmax (Tmax) of Selpercatinib | PK: Tmax of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.) | All participants who received at least one dose of selpercatinib with evaluable PK data. | Posted | Median | Full Range | hours (h) | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
|
|
|
| Primary | PK: Apparent First-order Terminal Elimination Rate Constant (Kel) of Selpercatinib | PK: Kel of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.) | All participants who received at least one dose of selpercatinib with evaluable PK data. | Posted | Mean | Standard Deviation | 1/hour | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
|
|
|
| Primary | PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Selpercatinib | PK: CL/F of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.) | All participants who received at least one dose of selpercatinib with evaluable PK data. | Posted | Mean | Standard Deviation | Liters/hour | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
|
|
|
| Primary | PK: Apparent First-order Terminal Elimination Half-life (t½) of Selpercatinib | PK: t½ of Selpercatinib was reported. Outcome measure timeframe: Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.) | All participants who received at least one dose of selpercatinib with evaluable PK data. | Posted | Mean | Standard Deviation | h | (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. |
|
|
|
| Primary | Part 2 - PK: Area Under the Concentration-Time Curve From Time 0 to 24 Hours (AUC0-24) of Selpercatinib Post Dose Day 1 | PK: AUC0-24 of Selpercatinib in Part 2 was reported. | All participants in Part 2 who received at least one dose of selpercatinib on Day 1 of either period with evaluable PK data. | Posted | Geometric Mean | Geometric Coefficient of Variation | ng*h/mL | Part 2, Periods 1 and 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose. |
|
|
|
| 0 |
| 12 |
| 0 |
| 12 |
| 1 |
| 12 |
| EG001 | Part 1 Period 2: 160 mg Selpercatinib + 200 mg Itraconazole | Participants received an oral dose of 200 mg itraconazole administered QD for 11 consecutive days (Days -4 to 7) with a single oral dose of 160 mg selpercatinib co-administered on Day 1 of Period 2. | 0 | 12 | 0 | 12 | 4 | 12 |
| EG002 | Part 2 Period 1: 160 mg Selpercatinib | Participants received a single oral dose of 160 mg selpercatinib on Day 1 of Period 1. | 0 | 12 | 0 | 12 | 3 | 12 |
| EG003 | Part 2 Period 2: 160 mg Selpercatinib + 600 mg Rifampin | Participants received an oral dose of 600 mg rifampin administered QD for 16 consecutive days (Days 1 to 16) with a single oral dose of 160 mg selpercatinib co-administered on Day 1 and Day 10 of Period 2. | 0 | 12 | 0 | 12 | 5 | 12 |
| Abdominal pain lower | Gastrointestinal disorders | MedDRA 21.0 | Systematic Assessment |
|
| Constipation | Gastrointestinal disorders | MedDRA 21.0 | Systematic Assessment |
|
| Diarrhoea | Gastrointestinal disorders | MedDRA 21.0 | Systematic Assessment |
|
| Lip swelling | Gastrointestinal disorders | MedDRA 21.0 | Systematic Assessment |
|
| Nausea | Gastrointestinal disorders | MedDRA 21.0 | Systematic Assessment |
|
| Axillary pain | General disorders | MedDRA 21.0 | Systematic Assessment |
|
| Nodule | General disorders | MedDRA 21.0 | Systematic Assessment |
|
| Ear canal injury | Injury, poisoning and procedural complications | MedDRA 21.0 | Systematic Assessment |
|
| Laceration | Injury, poisoning and procedural complications | MedDRA 21.0 | Systematic Assessment |
|
| Weight decreased | Investigations | MedDRA 21.0 | Systematic Assessment |
|
| Decreased appetite | Metabolism and nutrition disorders | MedDRA 21.0 | Systematic Assessment |
|
| Myalgia | Musculoskeletal and connective tissue disorders | MedDRA 21.0 | Systematic Assessment |
|
| Headache | Nervous system disorders | MedDRA 21.0 | Systematic Assessment |
|
| Pollakiuria | Renal and urinary disorders | MedDRA 21.0 | Systematic Assessment |
|
| Dysmenorrhoea | Reproductive system and breast disorders | MedDRA 21.0 | Systematic Assessment |
|
| Nasal congestion | Respiratory, thoracic and mediastinal disorders | MedDRA 21.0 | Systematic Assessment |
|
| Oropharyngeal discomfort | Respiratory, thoracic and mediastinal disorders | MedDRA 21.0 | Systematic Assessment |
|
| Erythema | Skin and subcutaneous tissue disorders | MedDRA 21.0 | Systematic Assessment |
|
| Seborrhoeic dermatitis | Skin and subcutaneous tissue disorders | MedDRA 21.0 | Systematic Assessment |
|
| Flushing | Vascular disorders | MedDRA 21.0 | Systematic Assessment |
|
Not provided
| D010879 |
| Piperazines |
| D012294 | Rifamycins |
| D006576 | Heterocyclic Compounds, 4 or More Rings |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| D047029 | Lactams, Macrocyclic |
| D047028 | Macrocyclic Compounds |
| D011083 | Polycyclic Compounds |