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GSK3542503

Phase 1

Hypertension | Small molecule | Cardiovascular |GSK plc|Last Updated: May 7, 2021

Success Probability

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Market & Valuation

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Trial Design

RandomizedCONTROLLED
Total Trials1
Total Enrollment42

FDA Designations

No designations recorded

Clinical trial landscape

GSK3542503 · 1 trial · 1 indication

Phase 1 1
NCT03031496Bioequivalence Study Between GSK3542503 Hydrochlorothiazide + Amiloride Hydrochloride 50 mg: 5 mg Tablets and Reference Product in Healthy Adult Participants Under Fasting ConditionsHypertension
COMPLETED42 Analytics
PHASE1COMPLETED
Bioequivalence Study Between GSK3542503 Hydrochlorothiazide + Amiloride Hydrochloride 50 mg: 5 mg Tablets and Reference Product in Healthy Adult Participants Under Fasting Conditions
HypertensionUnlock trial analytics

Study Endpoints

Primary Endpoints

Area Under the Curve (AUC) From Time Zero to the Time of the Last Quantifiable Concentration (AUC [0-t]) of Hydrochlorothiazide and Amiloride Hydrochloride
Pre-dose, 0.33, 0.67, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 7.0, 8.0, 10, 12,14, 16 hours post-dose on Day 1, 24 and 36 hours post dose on Day 2 and 48 hours post-dose on Day 3

Blood samples were collected at indicated time points under fasting conditions for pharmacokinetic (PK) analysis of hydrochlorothiazide and amiloride. Bioequivalence of test product and reference product was assessed based on the 90 percent confidence intervals (CIs) for estimates of the geometric mean ratios between the AUC (0-t) of the test and reference products in relation to the conventional bioequivalence range. An analysis of variance was used with sequence, subject (sequence), treatment and period as fixed effects.

Maximum Observed Concentration (Cmax) of Hydrochlorothiazide and Amiloride Hydrochloride in Plasma
Pre-dose, 0.33, 0.67, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 7.0, 8.0, 10, 12,14, 16 hours post-dose on Day 1, 24 and 36 hours post dose on Day 2 and 48 hours post-dose on Day 3

Blood samples were collected at indicated time points under fasting conditions for pharmacokinetic (PK) analysis of hydrochlorothiazide and amiloride. Bioequivalence of test product and reference product was assessed based on the 90 percent CIs for estimates of the geometric mean ratios between the Cmax of the test and reference products in relation to the conventional bioequivalence range. An analysis of variance was used with sequence, subject (sequence), treatment and period as fixed effects.

Secondary Endpoints

AUC From Time Zero to Infinity (AUC[0-inf]) of Hydrochlorothiazide and Amiloride Hydrochloride in Plasma
Pre-dose, 0.33, 0.67, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 7.0, 8.0, 10, 12,14, 16 hours post-dose on Day 1, 24 and 36 hours post dose on Day 2 and 48 hours post-dose on Day 3
Time of Occurrence of Cmax (Tmax) of Hydrochlorothiazide and Amiloride Hydrochloride in Plasma
Pre-dose, 0.33, 0.67, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 7.0, 8.0, 10, 12,14, 16 hours post-dose on Day 1, 24 and 36 hours post dose on Day 2 and 48 hours post-dose on Day 3
Percentage of AUC(0-inf) Obtained by Extrapolation (Percent AUCex) of Hydrochlorothiazide and Amiloride Hydrochloride in Plasma
Pre-dose, 0.33, 0.67, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 7.0, 8.0, 10, 12,14, 16 hours post-dose on Day 1, 24 and 36 hours post dose on Day 2 and 48 hours post-dose on Day 3
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Test A followed by Ref B of HCTZ 50mg+ Amiloride HCl 5mgEXPERIMENTALEligible participants following an overnight fast of at least 10 hours, will be administered the study drug orally with 240 mL (8 fluid ounces) of water. No food will be allowed for at least 4 hours post-dose. Water will be allowed as desired except for one hour before and after drug administration.
Ref B followed by test A of HCTZ 50mg + Amiloride HCl 5mgEXPERIMENTALEligible participants following an overnight fast of at least 10 hours, will be administered the study drug orally with 240 mL (8 fluid ounces) of water. No food will be allowed for at least 4 hours post-dose. Water will be allowed as desired except for one hour before and after drug administration.

Interventions

NameTypeDescription
GSK3542503 (HCTZ 50mg/Amiloride HCl 5mg tablets)DRUGGSK3542503 (HCTZ 50mg/Amiloride HCl 5mg tablets) are cream-colored, circular, flat faced uncoated tablets with beveled edges having break line on one side and "BD" embossed on the other side.
Moduretic (HCTZ 50mg/Amiloride HCl 5mg tablets)DRUGModuretic (HCTZ 50mg/Amiloride HCl 5mg tablets) tablets are peach-colored, half scored, diamond shaped tablets marked "MSD917".
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Eligibility Criteria

Age Range18 Years to 65 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Participants must be between18 and 65 years of age inclusive, at the time of signing the informed consent. * Healthy, non-smoker, as determined by the investigator or medically qualified designee based on a medical evaluation including medical history, physical examination, la...

Countries:South Africa
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Frequently asked questions about GSK3542503

What is GSK3542503 used for?

GSK3542503 is an investigational small molecule being developed for hypertension, a cardiovascular condition. It is currently in Phase 1 clinical development and is not approved by the FDA. The drug is being studied for its potential use in treating high blood pressure.

Who makes GSK3542503?

GSK3542503 is being developed by GSK plc, a pharmaceutical company traded on the stock exchange under the ticker GSK. The company is conducting clinical research to evaluate the drug's safety and efficacy in patients with hypertension.

What phase is GSK3542503 in?

GSK3542503 is in Phase 1 clinical development. It is an investigational drug, meaning it has not been approved by regulatory authorities. The drug is being studied for the treatment of hypertension, and its safety and tolerability are being evaluated in early-stage clinical trials.

What clinical trials is GSK3542503 in?

GSK3542503 has one completed Phase 1 clinical trial registered under NCT03031496. This study was a bioequivalence trial comparing GSK3542503, a combination of hydrochlorothiazide and amiloride hydrochloride 50 mg:5 mg tablets, to a reference product in healthy adult participants under fasting conditions. The trial enrolled 42 participants in South Africa.

Is GSK3542503 the same as hydrochlorothiazide and amiloride?

GSK3542503 is a combination product containing hydrochlorothiazide and amiloride hydrochloride. The Phase 1 trial NCT03031496 was designed to assess the bioequivalence of GSK3542503 tablets compared to a reference product of the same combination in healthy volunteers.