Not provided
| ID | Type | Description | Link |
|---|---|---|---|
| 2018-001175-21 | EudraCT Number |
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
This is a first time in human (FTIH), 2-period study, to assess the relative bioavailability of a mesylate salt capsule of GSK3640254, compared to a bis- hydrochloride salt capsule of GSK3640254, in healthy subjects, administered following a moderate calorie and fat meal. The subjects will be randomized to 2 sequences, Regimen AB or Regimen BA. For Regimen AB: The Regimen A, which will include oral administration of GSK3640254 bis-hydrochloride Capsule 200 milligram (mg) (reference), which will be administered, in Period 1 and Regimen B will include GSK3640254 Mesylate salt capsule (test), 200 mg, which will be administered in Period 2. For the regimen BA, the regimen B, will be administered, in Period 1 and regimen A, in Period 2. Each of the regimens will be given orally as 2 capsules in the morning, as per randomization sequence. There will be a minimum washout of 7 days between each dose of study treatment. A total, of 14 subjects, are planned to be enrolled in the study. The maximum duration of the study from screening to follow-up is approximately 7 weeks.
Not provided
Not provided
Not provided
Not provided
Not provided
| Label | Type | Description | Intervention Names |
|---|---|---|---|
| GSK3640254 Bis-hydrochloride followed by GSK3640254 mesylate | Experimental | The subjects in this arm will receive an oral administration of 200 mg, as 2 GSK3640254 bis-hydrochloride salt Capsules(reference), as single oral dose, on the morning of Day 1 during Period 1 of the study. This will be followed by an oral administration of 200 mg, as 2 GSK3640254 Mesylate salt capsule (test), as single oral dose, on the morning of Day 1, during Period 2 of the study. The drug will be administered following a moderate calorie and fat meal. There will be a minimum washout of 7 days between each dose of study treatment. |
|
| GSK3640254 Mesylate followed by GSK3640254 Bis-hydrochloride | Experimental | The subjects in this arm will receive an oral administration of 200 mg as 2 GSK3640254 Mesylate salt capsule (test), as single oral dose, on the morning of Day 1 during Period 1 of the study. This will be followed by an oral administration of 200 mg, as 2 GSK3640254 bis-hydrochloride salt Capsule, 100 mg (reference), as single oral dose, on the morning of Day 1 during Period 2, of the study. The drug, will be administered following a moderate calorie and fat meal. There will be a minimum washout of 7 days between each dose of study treatment. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| GSK3640254 bis-hydrochloride salt capsule | Drug | Administered orally (as single dose) on morning of Day 1, as 2 capsules of 100 mg following a moderate calorie and fat meal during Period 1 and Period 2, at the specified sequence, as per study. |
| Measure | Description | Time Frame |
|---|---|---|
| Area Under the Concentration-time Curve From Time Zero (Pre-dose) Extrapolated to Infinite Time (AUC[0-infinity]) of GSK3640254 Following Single Oral Dose in Healthy Participants | Blood samples were collected at designated timepoints. Pharmacokinetic (PK) parameters of GSK3640254 were calculated using non-compartmental methods. Geometric mean and percentage (%) geometric coefficient of variation have been presented. | Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48 and 72 hours post-dose in each treatment period |
| Area Under the Concentration-time Curve From Zero to Time of Last Sample Taken (AUC[0-t]) of GSK3640254 Following Single Oral Dose in Healthy Participants | Blood samples were collected at designated timepoints. PK parameters of GSK3640254 were calculated using non-compartmental methods. Geometric mean and % geometric coefficient of variation have been presented. Statistical analysis of PK parameters was done using mixed effect model for evaluation of relative bioavailability (Frel). Point estimate and 90% confidence interval (CI) for the ratio of geometric least square mean of the test mesylate salt capsule to the reference Hydrochloride capsule were calculated for AUC(0-t). | Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, and 72 hours post-dose in each treatment period |
| Maximum Observed Concentration (Cmax) of GSK3640254 Following Single Oral Dose in Healthy Participants | Blood samples were collected at designated timepoints. PK parameters of GSK3640254 were calculated using non-compartmental methods. Geometric mean and % geometric coefficient of variation have been presented. Statistical analysis of PK parameters was done using mixed effect model for evaluation of Frel. Point estimate and 90% CI for the ratio of geometric least square mean of the test mesylate salt capsule to the reference Hydrochloride capsule were calculated for Cmax. | Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, and 72 hours post-dose in each treatment period |
| Time to Reach Maximum Observed Concentration (Tmax) of GSK3640254 Following Single Oral Dose in Healthy Participants |
| Measure | Description | Time Frame |
|---|---|---|
| Number of Participants With Non-serious Adverse Events (Non-SAEs) and Serious Adverse Events (SAEs) | An adverse event (AE) is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. SAE is 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 disability/incapacity, is a congenital anomaly/birth defect and other situations according to medical or scientific judgement. |
Not provided
Inclusion Criteria:
Exclusion Criteria:
Not provided
Not provided
Not provided
Not provided
Not provided
| Name | Affiliation | Role |
|---|---|---|
| GSK Clinical Trials | ViiV Healthcare | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| GSK Investigational Site | Nottingham | NG11 6JS | United Kingdom |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 33200887 | Derived | Joshi SR, Fernando D, Igwe S, McKenzie L, Krishnatry AS, Halliday F, Zhan J, Greene TJ, Xu J, Ferron-Brady G, Lataillade M, Min S. Phase I evaluation of the safety, tolerability, and pharmacokinetics of GSK3640254, a next-generation HIV-1 maturation inhibitor. Pharmacol Res Perspect. 2020 Dec;8(6):e00671. doi: 10.1002/prp2.671. |
Not provided
Not provided
IPD for this study will be made available via the Clinical Study Data Request site.
IPD will be made available, within 6 months of publishing the results of the primary endpoints of the study.
Access is provided, after a research proposal is submitted and has submitted approval from the Independent Review Panel and after a Data Sharing Agreement is in place. Access is provided, for an initial period of 12 months but an extension can be granted, when justified for up to another 12 months.
Participants received treatment in one of the two sequences; regimen A (GSK3640254 hydrochloride salt capsule) followed by regimen B (GSK3640254 mesylate salt capsule) or vice versa in each of the treatment period 1 and 2. A total of 14 participants were enrolled in the study.
This was a single center, open-label, randomized, two-period crossover study to assess the relative bioavailability of a mesylate salt capsule of GSK3640254 compared to a hydrochloride salt capsule in healthy participants.
Not provided
| ID | Title | Description |
|---|---|---|
| FG000 | GSK3640254 200 Mg-hydrochloride Salt Followed by Mesylate Salt | Eligible participants received a single dose of GSK3640254 200 milligram (mg) bis-hydrochloride salt (100 mg x 2 capsules) administered orally on Day 1 in treatment period 1 after a moderate fat meal. It was followed by a washout period of minimum 7 days. Participants received GSK3640254 200 mg mesylate salt (100 mg x 2 capsules) administered orally on Day 1 in treatment period 2 after a moderate fat meal. |
| FG001 | GSK3640254 200 Mg-mesylate Salt Followed by Hydrochloride Salt | Eligible participants received a single dose of GSK3640254 200 mg mesylate salt (100 mg x 2 capsules) administered orally on Day 1 in treatment period 1 after a moderate fat meal. It was followed by a washout period of minimum 7 days. Participants received GSK3640254 200 mg bis-hydrochloride salt (100 mg x 2 capsules) administered orally on Day 1 in treatment period 2 after a moderate fat meal. |
| Title | Milestones | Reasons Not Completed | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Treatment Period 1 (4 Days) |
| |||||||||||||
| Washout Period (7 Days) |
| |||||||||||||
| Treatment Period 2 (4 Days) |
|
Not provided
Not provided
| ID | Title | Description |
|---|---|---|
| BG000 | All Participants | Eligible participants received a single dose of GSK3640254 200 mg bis-hydrochloride salt (100 mg x 2 capsules) followed by GSK3640254 200 mg mesylate salt (100 mg x 2 capsules) or vice versa, administered orally on Day 1 in each treatment period 1 and 2 following a moderate fat meal. The washout period was of minimum 7 days between the treatment periods. |
| 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 | Area Under the Concentration-time Curve From Time Zero (Pre-dose) Extrapolated to Infinite Time (AUC[0-infinity]) of GSK3640254 Following Single Oral Dose in Healthy Participants | Blood samples were collected at designated timepoints. Pharmacokinetic (PK) parameters of GSK3640254 were calculated using non-compartmental methods. Geometric mean and percentage (%) geometric coefficient of variation have been presented. | PK Population comprising of participants in the Safety Population for whom at least one PK sample was obtained, analyzed and evaluable drug concentrations reported. Only those participants with data available at the specified data points were analyzed. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hour*microgram per milliliter | Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48 and 72 hours post-dose in each treatment period |
|
SAEs and non-serious AEs were collected from the start of study treatment up to 25 days.
SAEs and Non-SAEs were reported by treatment for the Safety Population which comprised of all randomized participants who received at least 1 dose of study treatment.
Not provided
| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | GSK3640254 200 mg Hydrochloride Salt | Eligible participants received a single dose of GSK3640254 200 mg bis-hydrochloride salt (100 mg x 2) administered orally on Day 1 in either treatment period 1or 2 as per randomization. |
Not provided
| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Abdominal pain | Gastrointestinal disorders | MedDRA 21.0 | Systematic Assessment |
Not provided
| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| GSK Response Center | ViiV Healthcare | 866-435-7343 | GSKClinicalSupportHD@gsk.com |
Not provided
| Type | Includes Protocol | Includes SAP | Includes ICF | Document Label | Document Date | Document Uploaded Date | Document File Name |
|---|---|---|---|---|---|---|---|
| Prot | Yes | No | No | Study Protocol | May 29, 2018 | Jul 24, 2019 | Prot_000.pdf |
| SAP | No | Yes | No | Statistical Analysis Plan | Nov 21, 2018 | Jul 24, 2019 | SAP_001.pdf |
Not provided
| ID | Term |
|---|---|
| D015658 | HIV Infections |
| ID | Term |
|---|---|
| D000086982 | Blood-Borne Infections |
| D003141 | Communicable Diseases |
| D007239 | Infections |
| D015229 | Sexually Transmitted Diseases, Viral |
Not provided
Not provided
Subjects will receive GSK3640254 bis-hydrochloride salt capsule followed by mesylate salt capsule or vice versa in two treatment periods.
Not provided
Not provided
This is an open-label study.
Not provided
| GSK3640254 Mesylate Salt Capsule | Drug | Administered orally (as single dose) on morning of Day 1, as 2 capsules of , 100 mg following a moderate calorie and fat meal during Period 1 and Period 2, at the specified sequence, as per study. |
|
Blood samples were collected at designated timepoints. PK parameters of GSK3640254 were calculated using non-compartmental methods. Median and full range of Tmax have been presented. |
| Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, and 72 hours post-dose in each treatment period |
| Concentration at 24 Hours Post-dose (C24h) of GSK3640254 Following Single Oral Dose in Healthy Participants | Blood samples were collected at designated timepoints. PK parameters of GSK3640254 were calculated using non-compartmental methods. Geometric mean and % geometric coefficient of variation have been presented. | Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12 and 24 hours post-dose in each treatment period |
| Up to 25 days |
| Change From Baseline in Clinical Chemistry Parameters; Alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP) and Aspartate Aminotransferase (AST) | Blood samples were collected to analyze the clinical chemistry parameters; ALT, ALP and AST. Day-1 was considered as Baseline. Change from Baseline was calculated by subtracting Baseline value from the post-Dose visit value. Mean and standard deviation have been presented. | Baseline (Day -1) and Day 3 |
| Change From Baseline in Clinical Chemistry Parameters; Bicarbonate, Calcium, Chloride, Glucose (Fasting), Potassium, Sodium and Urea | Blood samples were collected to analyze the clinical chemistry parameters; Bicarbonate, Calcium, Chloride, Glucose (fasting), Potassium, Sodium and Urea. Day-1 was considered as Baseline. Change from Baseline was calculated by subtracting Baseline value from the post-Dose visit value. Mean and standard deviation have been presented. | Baseline (Day -1) and Day 3 |
| Change From Baseline in Clinical Chemistry Parameters; Bilirubin, Creatinine and Direct Bilirubin | Blood samples were collected to analyze the clinical chemistry parameters; Bilirubin, Creatinine and Direct Bilirubin. Day-1 was considered as Baseline. Change from Baseline was calculated by subtracting Baseline value from the post-Dose visit value. Mean and standard deviation have been presented. | Baseline (Day -1) and Day 3 |
| Change From Baseline in Clinical Chemistry Parameter; Protein | Blood samples were collected to analyze the clinical chemistry parameter; Protein. Day-1 was considered as Baseline. Change from Baseline was calculated by subtracting Baseline value from the post-Dose visit value. Mean and standard deviation have been presented. | Baseline (Day -1) and Day 3 |
| Number of Participants With Worst Case Hematology Results by Potential Clinical Importance (PCI) Criteria | Blood samples were collected to analyze the hematology parameters; Hematocrit (Hct), Hemoglobin (Hb), Leukocytes, Lymphocytes, Neutrophils and Platelets. PCI ranges were Hct (Male and Female [high: >0.54 proportion of red blood cells in blood]), Hb (Male and Female [high: >180 grams per liter]), lymphocytes (low: <0.8x10^9 cells per liter), neutrophils (low: <1.5x10^9 cells per liter), platelets (low: <100x10^9 cells per liter and high: >550x10^9 cells per liter) and leukocytes (low: <3x10^9 cells per liter and high: >12x10^9 cells per liter). Participants were counted in the worst case category such that their value changed to (low, normal or high). If values were unchanged (example: High to High), or whose value became normal, were recorded in the 'To Normal or No Change' category. | Up to 22 days |
| Number of Participants With Urinalysis Results by Dipstick Method by Visit | Urine samples were collected to assess urine bilirubin, urine glucose, urine ketones, urine leukocyte esterase (LE), urine nitrite, urine occult blood, urine protein, urobilinogen and monitor urine potential of hydrogen (pH). The dipstick test gave results in a semi-quantitative manner, and results for urinalysis parameters were recorded as negative, trace and positive, indicating proportional concentrations in the urine sample. All the numeric result values >0 have been considered as "positive". | Day -1 and Day 3 |
| Number of Participants With Clinically Significant Abnormal Findings for Electrocardiogram (ECG) Parameters | A single 12-lead ECGs was obtained using an ECG machine that automatically calculates the heart rate and measures PR, QRS, QT, QT corrected (QTc) and QT interval corrected for heart rate according to Fridericia's formula (QTcF) intervals. Clinically significant abnormal ranges were: PR: lower: <120 milliseconds (msec) and upper: >200 msec; QRS: lower: <60 msec and upper: >120 msec and QTcF: lower: <320 msec and upper: >450 msec. The number of participants with clinically significant abnormal findings for ECG parameters have been presented. | Day -1, pre-dose, 2, 4, 6, 24 and 72 hours post-dose in each treatment period |
| Diastolic Blood Pressure (DBP) and Systolic Blood Pressure (SBP) at Indicated Time-points | Vital signs including DBP and SBP were measured at the indicated time-points and summarized during the study to evaluate the safety of the participants. Mean and standard deviation have been presented. | Day -1, pre-dose, 2, 4, 6, 24 and 72 hours post-dose in each treatment period |
| Pulse Rate (PR) at Indicated Time-points | Vital sign including PR was measured at the indicated time-points and summarized during the study to evaluate the safety of the participants. Mean and standard deviation have been presented. | Day -1, pre-dose, 2, 4, 6, 24 and 72 hours post-dose in each treatment period |
| Respiratory Rate (RR) at Indicated Time-points | Vital sign including RR was measured at the indicated time-point and summarized during the study to evaluate the safety of the participants. Mean and standard deviation have been presented. | Day -1, pre-dose, 2, 4, 6, 24 and 72 hours post-dose in each treatment period |
| Temperature at Indicated Time-points | Vital sign including temperature was measured at the indicated time-points and summarized during the study to evaluate the safety of the participants. Mean and standard deviation have been presented. | Day -1, pre-dose, 2, 4, 6, 24 and 72 hours post-dose in each treatment period |
| Number of Participants With the Indicated Assessment Events of Suicidal Behavior (SB) and Suicidal Ideation (SI) Via the Columbia Suicide Severity Rating Scale (C-SSRS) | Assessment of suicidality was conducted using the C-SSRS, a brief questionaire designed to assess severity and change in suicidality by integrating both behavior and ideation using a semi-structured interview to probe participant responses. | Day 3 in each treatment period |
| NOT COMPLETED |
|
| NOT COMPLETED |
|
| Years |
|
| Sex: Female, Male | Count of Participants | Participants |
|
| Race/Ethnicity, Customized | Number | Participants |
|
Eligible participants received a single dose of GSK3640254 200 mg bis-hydrochloride salt (100 mg x 2) administered orally on Day 1 in either treatment period 1or 2 as per randomization.
| OG001 | GSK3640254 Capsule 200 mg Mesylate Salt | Eligible participants received a single dose of GSK3640254 200 mg mesylate salt (100 mg x 2) administered orally on Day 1 in either treatment period 1or 2 as per randomization. |
|
|
| Primary | Area Under the Concentration-time Curve From Zero to Time of Last Sample Taken (AUC[0-t]) of GSK3640254 Following Single Oral Dose in Healthy Participants | Blood samples were collected at designated timepoints. PK parameters of GSK3640254 were calculated using non-compartmental methods. Geometric mean and % geometric coefficient of variation have been presented. Statistical analysis of PK parameters was done using mixed effect model for evaluation of relative bioavailability (Frel). Point estimate and 90% confidence interval (CI) for the ratio of geometric least square mean of the test mesylate salt capsule to the reference Hydrochloride capsule were calculated for AUC(0-t). | PK Population | Posted | Geometric Mean | Geometric Coefficient of Variation | Hour*microgram per milliliter | Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, and 72 hours post-dose in each treatment period |
|
|
|
|
| Primary | Maximum Observed Concentration (Cmax) of GSK3640254 Following Single Oral Dose in Healthy Participants | Blood samples were collected at designated timepoints. PK parameters of GSK3640254 were calculated using non-compartmental methods. Geometric mean and % geometric coefficient of variation have been presented. Statistical analysis of PK parameters was done using mixed effect model for evaluation of Frel. Point estimate and 90% CI for the ratio of geometric least square mean of the test mesylate salt capsule to the reference Hydrochloride capsule were calculated for Cmax. | PK Population | Posted | Geometric Mean | Geometric Coefficient of Variation | Microgram per milliliter | Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, and 72 hours post-dose in each treatment period |
|
|
|
|
| Primary | Time to Reach Maximum Observed Concentration (Tmax) of GSK3640254 Following Single Oral Dose in Healthy Participants | Blood samples were collected at designated timepoints. PK parameters of GSK3640254 were calculated using non-compartmental methods. Median and full range of Tmax have been presented. | PK Population | Posted | Median | Full Range | Hours | Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, and 72 hours post-dose in each treatment period |
|
|
|
| Primary | Concentration at 24 Hours Post-dose (C24h) of GSK3640254 Following Single Oral Dose in Healthy Participants | Blood samples were collected at designated timepoints. PK parameters of GSK3640254 were calculated using non-compartmental methods. Geometric mean and % geometric coefficient of variation have been presented. | PK Population | Posted | Geometric Mean | Geometric Coefficient of Variation | Microgram per milliliter | Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12 and 24 hours post-dose in each treatment period |
|
|
|
| Secondary | Number of Participants With Non-serious Adverse Events (Non-SAEs) and Serious Adverse Events (SAEs) | An adverse event (AE) is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. SAE is 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 disability/incapacity, is a congenital anomaly/birth defect and other situations according to medical or scientific judgement. | Safety Population comprising of all randomized participants who received at least one dose of study treatment. | Posted | Count of Participants | Participants | Up to 25 days |
|
|
|
| Secondary | Change From Baseline in Clinical Chemistry Parameters; Alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP) and Aspartate Aminotransferase (AST) | Blood samples were collected to analyze the clinical chemistry parameters; ALT, ALP and AST. Day-1 was considered as Baseline. Change from Baseline was calculated by subtracting Baseline value from the post-Dose visit value. Mean and standard deviation have been presented. | Safety Population. Only those participants with data available at the specified data points were analyzed (represented by n=X in the category titles). | Posted | Mean | Standard Deviation | International units per liter | Baseline (Day -1) and Day 3 |
|
|
|
| Secondary | Change From Baseline in Clinical Chemistry Parameters; Bicarbonate, Calcium, Chloride, Glucose (Fasting), Potassium, Sodium and Urea | Blood samples were collected to analyze the clinical chemistry parameters; Bicarbonate, Calcium, Chloride, Glucose (fasting), Potassium, Sodium and Urea. Day-1 was considered as Baseline. Change from Baseline was calculated by subtracting Baseline value from the post-Dose visit value. Mean and standard deviation have been presented. | Safety Population. Only those participants with data available at the specified data points were analyzed (represented by n=X in the category titles). | Posted | Mean | Standard Deviation | Millimoles per liter | Baseline (Day -1) and Day 3 |
|
|
|
| Secondary | Change From Baseline in Clinical Chemistry Parameters; Bilirubin, Creatinine and Direct Bilirubin | Blood samples were collected to analyze the clinical chemistry parameters; Bilirubin, Creatinine and Direct Bilirubin. Day-1 was considered as Baseline. Change from Baseline was calculated by subtracting Baseline value from the post-Dose visit value. Mean and standard deviation have been presented. | Safety Population. Only those participants with data available at the specified data points were analyzed (represented by n=X in the category titles). | Posted | Mean | Standard Deviation | Micromoles per liter | Baseline (Day -1) and Day 3 |
|
|
|
| Secondary | Change From Baseline in Clinical Chemistry Parameter; Protein | Blood samples were collected to analyze the clinical chemistry parameter; Protein. Day-1 was considered as Baseline. Change from Baseline was calculated by subtracting Baseline value from the post-Dose visit value. Mean and standard deviation have been presented. | Safety Population | Posted | Mean | Standard Deviation | Grams per liter | Baseline (Day -1) and Day 3 |
|
|
|
| Secondary | Number of Participants With Worst Case Hematology Results by Potential Clinical Importance (PCI) Criteria | Blood samples were collected to analyze the hematology parameters; Hematocrit (Hct), Hemoglobin (Hb), Leukocytes, Lymphocytes, Neutrophils and Platelets. PCI ranges were Hct (Male and Female [high: >0.54 proportion of red blood cells in blood]), Hb (Male and Female [high: >180 grams per liter]), lymphocytes (low: <0.8x10^9 cells per liter), neutrophils (low: <1.5x10^9 cells per liter), platelets (low: <100x10^9 cells per liter and high: >550x10^9 cells per liter) and leukocytes (low: <3x10^9 cells per liter and high: >12x10^9 cells per liter). Participants were counted in the worst case category such that their value changed to (low, normal or high). If values were unchanged (example: High to High), or whose value became normal, were recorded in the 'To Normal or No Change' category. | Safety Population | Posted | Count of Participants | Participants | Up to 22 days |
|
|
|
| Secondary | Number of Participants With Urinalysis Results by Dipstick Method by Visit | Urine samples were collected to assess urine bilirubin, urine glucose, urine ketones, urine leukocyte esterase (LE), urine nitrite, urine occult blood, urine protein, urobilinogen and monitor urine potential of hydrogen (pH). The dipstick test gave results in a semi-quantitative manner, and results for urinalysis parameters were recorded as negative, trace and positive, indicating proportional concentrations in the urine sample. All the numeric result values >0 have been considered as "positive". | Safety Population. Only those participants with data available at the specified data points were analyzed (represented by n=X in the category titles). | Posted | Count of Participants | Participants | Day -1 and Day 3 |
|
|
|
| Secondary | Number of Participants With Clinically Significant Abnormal Findings for Electrocardiogram (ECG) Parameters | A single 12-lead ECGs was obtained using an ECG machine that automatically calculates the heart rate and measures PR, QRS, QT, QT corrected (QTc) and QT interval corrected for heart rate according to Fridericia's formula (QTcF) intervals. Clinically significant abnormal ranges were: PR: lower: <120 milliseconds (msec) and upper: >200 msec; QRS: lower: <60 msec and upper: >120 msec and QTcF: lower: <320 msec and upper: >450 msec. The number of participants with clinically significant abnormal findings for ECG parameters have been presented. | Safety Population | Posted | Count of Participants | Participants | Day -1, pre-dose, 2, 4, 6, 24 and 72 hours post-dose in each treatment period |
|
|
|
| Secondary | Diastolic Blood Pressure (DBP) and Systolic Blood Pressure (SBP) at Indicated Time-points | Vital signs including DBP and SBP were measured at the indicated time-points and summarized during the study to evaluate the safety of the participants. Mean and standard deviation have been presented. | Safety Population | Posted | Mean | Standard Deviation | Millimeters of mercury | Day -1, pre-dose, 2, 4, 6, 24 and 72 hours post-dose in each treatment period |
|
|
|
| Secondary | Pulse Rate (PR) at Indicated Time-points | Vital sign including PR was measured at the indicated time-points and summarized during the study to evaluate the safety of the participants. Mean and standard deviation have been presented. | Safety Population. | Posted | Mean | Standard Deviation | Beats per minute | Day -1, pre-dose, 2, 4, 6, 24 and 72 hours post-dose in each treatment period |
|
|
|
| Secondary | Respiratory Rate (RR) at Indicated Time-points | Vital sign including RR was measured at the indicated time-point and summarized during the study to evaluate the safety of the participants. Mean and standard deviation have been presented. | Safety Population. Only those participants with data available at the specified data points were analyzed (represented by n=X in the category titles). | Posted | Mean | Standard Deviation | Breaths per minute | Day -1, pre-dose, 2, 4, 6, 24 and 72 hours post-dose in each treatment period |
|
|
|
| Secondary | Temperature at Indicated Time-points | Vital sign including temperature was measured at the indicated time-points and summarized during the study to evaluate the safety of the participants. Mean and standard deviation have been presented. | Safety Population | Posted | Mean | Standard Deviation | Celsius | Day -1, pre-dose, 2, 4, 6, 24 and 72 hours post-dose in each treatment period |
|
|
|
| Secondary | Number of Participants With the Indicated Assessment Events of Suicidal Behavior (SB) and Suicidal Ideation (SI) Via the Columbia Suicide Severity Rating Scale (C-SSRS) | Assessment of suicidality was conducted using the C-SSRS, a brief questionaire designed to assess severity and change in suicidality by integrating both behavior and ideation using a semi-structured interview to probe participant responses. | Safety Population | Posted | Count of Participants | Participants | Day 3 in each treatment period |
|
|
|
| 0 |
| 14 |
| 0 |
| 14 |
| 3 |
| 14 |
| EG001 | GSK3640254 Capsule 200 mg Mesylate Salt | Eligible participants received a single dose of GSK3640254 200 mg mesylate salt (100 mg x 2) administered orally on Day 1 in either treatment period 1or 2 as per randomization. | 0 | 14 | 0 | 14 | 6 | 14 |
| Flatulence | Gastrointestinal disorders | MedDRA 21.0 | Systematic Assessment |
|
| Gingival bleeding | Gastrointestinal disorders | MedDRA 21.0 | Systematic Assessment |
|
| Arthralgia | Musculoskeletal and connective tissue disorders | MedDRA 21.0 | Systematic Assessment |
|
| Pain in extremity | Musculoskeletal and connective tissue disorders | MedDRA 21.0 | Systematic Assessment |
|
| Headache | Nervous system disorders | MedDRA 21.0 | Systematic Assessment |
|
| Epistaxis | Respiratory, thoracic and mediastinal disorders | MedDRA 21.0 | 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.
| D012749 | Sexually Transmitted Diseases |
| D016180 | Lentivirus Infections |
| D012192 | Retroviridae Infections |
| D012327 | RNA Virus Infections |
| D014777 | Virus Diseases |
| D000091662 | Genital Diseases |
| D000091642 | Urogenital Diseases |
| D007153 | Immunologic Deficiency Syndromes |
| D007154 | Immune System Diseases |
| ALP, Day 3, n=14,14 |
|
|
| AST, Day 3, n=13,14 |
|
|
| Calcium, Day 3, n=14,14 |
|
|
| Chloride, Day 3, n=14,14 |
|
|
| Glucose (fasting), Day 3, n=12,14 |
|
|
| Potassium, Day 3, n=14,14 |
|
|
| Sodium, Day 3, n=14,14 |
|
|
| Urea, Day 3, n=14,14 |
|
|
| Creatinine, Day 3, n=14,14 |
|
|
| Direct Bilirubin, Day 3, n=0,1 |
|
|
| Hct, To high |
|
| Hb, To low |
|
| Hb, To normal or no change |
|
| Hb, To high |
|
| Leukocytes, To low |
|
| Leukocytes, To normal or no change |
|
| Leukocytes, To high |
|
| Lymphocytes, To low |
|
| Lymphocytes, To normal or no change |
|
| Lymphocytes, To high |
|
| Neutrophils, To low |
|
| Neutrophils, To normal or no change |
|
| Neutrophils, To high |
|
| Platelets, To low |
|
| Platelets, To normal or no change |
|
| Platelets, To high |
|
| Bilirubin, Day -1, Trace, n=14,14 |
|
|
| Bilirubin, Day -1, Positive, n=14,14 |
|
|
| Bilirubin, Day 3, Negative, n=14,14 |
|
|
| Bilirubin, Day 3, Trace, n=14,14 |
|
|
| Bilirubin, Day 3, Positive, n=14,14 |
|
|
| Glucose, Day -1, Negative, n=14,14 |
|
|
| Glucose, Day -1, Trace, n=14,14 |
|
|
| Glucose, Day -1, Positive, n=14,14 |
|
|
| Glucose, Day 3, Negative, n=14,14 |
|
|
| Glucose, Day 3, Trace, n=14,14 |
|
|
| Glucose, Day 3, Positive, n=14,13 |
|
|
| Ketones, Day -1, Negative, n=14,14 |
|
|
| Ketones, Day -1, Trace, n=14,14 |
|
|
| Ketones, Day -1, Positive, n=14,14 |
|
|
| Ketones, Day 3, Negative, n=14,14 |
|
|
| Ketones, Day 3, Trace, n=14,14 |
|
|
| Ketones, Day 3, Positive, n=14,14 |
|
|
| LE, Day -1, Negative, n=14,14 |
|
|
| LE, Day -1, Trace, n=14,14 |
|
|
| LE, Day -1, Positive, n=14,14 |
|
|
| LE, Day 3, Negative, n=14,14 |
|
|
| LE, Day 3, Trace, n=14,14 |
|
|
| LE, Day 3, Positive, n=14,14 |
|
|
| Nitrite, Day -1, Negative, n=14,14 |
|
|
| Nitrite, Day -1, Trace, n=14,14 |
|
|
| Nitrite, Day -1, Positive, n=14,14 |
|
|
| Nitrite, Day 3, Negative, n=14,14 |
|
|
| Nitrite, Day 3, Trace, n=14,14 |
|
|
| Nitrite, Day 3, Positive, n=14,14 |
|
|
| Occult blood, Day -1, Negative, n=14,14 |
|
|
| Occult blood, Day -1, Trace, n=14,14 |
|
|
| Occult blood, Day -1, Positive, n=14,14 |
|
|
| Occult blood, Day 3, Negative, n=14,14 |
|
|
| Occult blood, Day 3, Trace, n=14,14 |
|
|
| Occult blood, Day 3, Positive, n=14,14 |
|
|
| pH, Day -1, Negative, n=14,14 |
|
|
| pH, Day -1, Trace, n=14,14 |
|
|
| pH, Day -1, Positive, n=14,14 |
|
|
| pH, Day 3, Negative, n=14,14 |
|
|
| pH, Day 3, Trace, n=14,14 |
|
|
| pH, Day 3, Positive, n=14,14 |
|
|
| Protein, Day -1, Negative, n=14,14 |
|
|
| Protein, Day -1, Trace, n=14,14 |
|
|
| Protein, Day -1, Positive, n=14,14 |
|
|
| Protein, Day 3, Negative, n=14,14 |
|
|
| Protein, Day 3, Trace, n=14,14 |
|
|
| Protein, Day 3, Positive, n=14,14 |
|
|
| Urobilinogen, Day -1, Negative, n=14,14 |
|
|
| Urobilinogen, Day -1, Trace, n=14,14 |
|
|
| Urobilinogen, Day -1, Positive, n=14,14 |
|
|
| Urobilinogen, Day 3, Negative, n=14,14 |
|
|
| Urobilinogen, Day 3, Trace, n=14,14 |
|
|
| Urobilinogen, Day 3, Positive, n=14,14 |
|
|
| 2 hours |
|
| 4 hours |
|
| 6 hours |
|
| 24 hours |
|
| 72 hours |
|
| DBP, 2 hours |
|
| DBP, 4 hours |
|
| DBP, 6 hours |
|
| DBP, 24 hours |
|
| DBP, 72 hours |
|
| SBP, Day -1 |
|
| SBP, Pre-dose |
|
| SBP, 2 hours |
|
| SBP, 4 hours |
|
| SBP, 6 hours |
|
| SBP, 24 hours |
|
| SBP, 72 hours |
|
| 2 hours |
|
| 4 hours |
|
| 6 hours |
|
| 24 hours |
|
| 72 hours |
|
| Pre-dose, n=14,14 |
|
|
| 2 hours, n=14,14 |
|
|
| 4 hours, n=14,14 |
|
|
| 6 hours, n=14,14 |
|
|
| 24 hours, n=13,14 |
|
|
| 72 hours, n=14,14 |
|
|
| 2 hours |
|
| 4 hours |
|
| 6 hours |
|
| 24 hours |
|
| 72 hours |
|
| SI- Method, but no intent or plan |
|
| SI- Method and intent, but no plan |
|
| SI- Method, intent, and plan |
|
| SB- Preparatory acts or behaviour |
|
| SB- Aborted attempt |
|
| SB- Interrupted attempt |
|
| SB- Non-fatal actual suicide attempt |
|
| SB- Completed suicide |
|