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GSK3640254 bis- salt

Phase 1

HIV Infections | Small molecule | Infectious Disease |GSK plc|Last Updated: Sep 6, 2019

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Market & Valuation

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Trial Design

RandomizedCONTROLLED
Total Trials1
Total Enrollment14

FDA Designations

No designations recorded

Clinical trial landscape

GSK3640254 bis- salt · 1 trial · 1 indication

Phase 1 1
NCT03575962A Study to Compare the Relative Bioavailability of Two Different Formulations of GSK3640254HIV Infections
COMPLETED14 Analytics
PHASE1COMPLETED
A Study to Compare the Relative Bioavailability of Two Different Formulations of GSK3640254
HIV InfectionsUnlock trial analytics

Study Endpoints

Primary Endpoints

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
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

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.

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
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

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).

Maximum Observed Concentration (Cmax) of GSK3640254 Following Single Oral Dose in Healthy Participants
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

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.

Time to Reach Maximum Observed Concentration (Tmax) of GSK3640254 Following Single Oral Dose in Healthy Participants
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

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.

Concentration at 24 Hours Post-dose (C24h) of GSK3640254 Following Single Oral Dose in Healthy Participants
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12 and 24 hours post-dose in each treatment period

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.

Secondary Endpoints

Number of Participants With Non-serious Adverse Events (Non-SAEs) and Serious Adverse Events (SAEs)
Up to 25 days
Change From Baseline in Clinical Chemistry Parameters; Alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP) and Aspartate Aminotransferase (AST)
Baseline (Day -1) and Day 3
Change From Baseline in Clinical Chemistry Parameters; Bicarbonate, Calcium, Chloride, Glucose (Fasting), Potassium, Sodium and Urea
Baseline (Day -1) and Day 3
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
GSK3640254 Bis-hydrochloride followed by GSK3640254 mesylateEXPERIMENTALThe 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-hydrochlorideEXPERIMENTALThe 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.

Interventions

NameTypeDescription
GSK3640254 bis-hydrochloride salt capsuleDRUGAdministered 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.
GSK3640254 Mesylate Salt CapsuleDRUGAdministered 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.
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Eligibility Criteria

Age Range18 Years to 55 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Subject must be 18 to 55 years of age inclusive, at the time of signing the informed consent * Subjects who are overtly healthy as determined by medical evaluation including medical history, physical examination, laboratory tests, and cardiac monitoring. * Body weight \>= 50 k...

Countries:United Kingdom
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Frequently asked questions about GSK3640254 bis- salt

What is GSK3640254 bis- salt used for?

GSK3640254 bis- salt is an investigational small molecule being developed for the treatment of HIV Infections. It is currently in Phase 1 clinical development and has not been approved by regulatory authorities.

Who makes GSK3640254 bis- salt?

GSK3640254 bis- salt is being developed by GSK plc, a pharmaceutical company listed on the stock exchange under the ticker symbol GSK.

What phase is GSK3640254 bis- salt in?

GSK3640254 bis- salt is in Phase 1 clinical development. It is an investigational drug and has not yet been approved for any use. A Phase 1 study has been completed to evaluate its properties.

What clinical trials is GSK3640254 bis- salt in?

GSK3640254 bis- salt has one completed clinical trial, NCT03575962, titled 'A Study to Compare the Relative Bioavailability of Two Different Formulations of GSK3640254'. This Phase 1 study enrolled 14 participants in the United Kingdom and included healthy volunteers.

Is GSK3640254 bis- salt the same as GSK3640254?

GSK3640254 bis- salt is a specific salt form of the compound GSK3640254. The clinical trial NCT03575962 compares different formulations of GSK3640254, including the bis- salt form, to assess their relative bioavailability.