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Adjusted LOA
ML Risk
GSK2798745 Micronized API without SLS and hypermellose · 1 trial · 1 indication
AUC will be determined following a single oral dose of GSK2798745 under fasted conditions (Treatment periods 1-3) and fed conditions (Treatment period 4)
Cmax will be determined following a single oral dose of GSK2798745 under fasted conditions (Treatment periods 1-3) and fed conditions (Treatment period 4)
| Arm | Type | Description |
|---|---|---|
| GSK2798745 ABCD treatment sequence | EXPERIMENTAL | Subjects will be given 2.4 mg single oral doses of GSK2798745 (micronized API without SLS and hypromellose) in fasted state (treatment A), 2.4 mg of GSK2798745 (micronized API with SLS and hypromellose) in fasted state (treatment B), GSK2798745 (milled API with SLS and hypromellose) in fasted state (treatment C), and GSK2798745 tablet in fed state (treatment D) in either treatment periods 1, 2, or 3; the three treatment periods will each be separated by a minimum washout period of 7 days |
| GSK2798745 CABD treatment sequence | EXPERIMENTAL | Subjects will be given 2.4 mg GSK2798745 (milled API with SLS and hypromellose) in fasted state (treatment C), 2.4 mg single oral doses of GSK2798745 (micronized API without SLS and hypromellose) in fasted state (treatment A), 2.4 mg of GSK2798745 (micronized API with SLS and hypromellose) in fasted state (treatment B), and GSK2798745 tablet in fed state (treatment D) in either treatment periods 1, 2, or 3; the three treatment periods will each be separated by a minimum washout period of 7 days |
| GSK2798745 ACBD treatment sequence | EXPERIMENTAL | Subjects will be given 2.4 mg single oral doses of GSK2798745 (micronized API without SLS and hypromellose) in fasted state (treatment A), 2.4 mg GSK2798745 (milled API with SLS and hypromellose) in fasted state (treatment C), 2.4 mg of GSK2798745 (micronized API with SLS and hypromellose) in fasted state (treatment B), and GSK2798745 tablet in fed state (treatment D) in either treatment periods 1, 2, or 3; the three treatment periods will each be separated by a minimum washout period of 7 days |
| GSK2798745 BACD treatment sequence | EXPERIMENTAL | Subjects will be given 2.4 mg of GSK2798745 (micronized API with SLS and hypromellose) in fasted state (treatment B), 2.4 mg of GSK2798745 (micronized API without SLS and hypromellose) in fasted state (treatment A), 2.4 mg GSK2798745 (milled API with SLS and hypromellose) in fasted state (treatment C), and GSK2798745 tablet in fed state (treatment D) in either treatment periods 1, 2, or 3; the three treatment periods will each be separated by a minimum washout period of 7 days |
| GSK2798745 BCAD treatment sequence | EXPERIMENTAL | Subjects will be given 2.4 mg of GSK2798745 (micronized API with SLS and hypromellose) in fasted state (treatment B), 2.4 mg GSK2798745 (milled API with SLS and hypromellose) in fasted state (treatment C), 2.4 mg single oral doses of GSK2798745 (micronized API without SLS and hypromellose) in fasted state (treatment A), and GSK2798745 tablet in fed state (treatment D) in either treatment periods 1, 2, or 3; the three treatment periods will each be separated by a minimum washout period of 7 days |
| GSK2798745 CBAD treatment sequence | EXPERIMENTAL | Subjects will be given 2.4 mg GSK2798745 (milled API with SLS and hypromellose) in fasted state (treatment C), 2.4 mg of GSK2798745 (micronized API with SLS and hypromellose) in fasted state (treatment B), 2.4 mg single oral doses of GSK2798745 (micronized API without SLS and hypromellose) in fasted state (treatment A), and GSK2798745 tablet in fed state (treatment D) in either treatment periods 1, 2, or 3; the three treatment periods will each be separated by a minimum washout period of 7 days |
| Name | Type | Description |
|---|---|---|
| GSK2798745 Micronized API without SLS and hypermellose (Tablet A) | DRUG | This is an immediate release tablet containing 2.4 mg of micronized GSK2798745 API; to be administered orally with 240 mL of water under fasted/fed conditions |
| GSK2798745 Micronized API with SLS and hypermellose (Tablet B) | DRUG | This is an immediate release tablet containing 2.4 mg of micronized GSK2798745 API with SLS and hypermellose; to be administered orally in fasted/fed conditions with 240 mL of water |
| GSK2798745 milled API without SLS and hypermellose (Tablet C) | DRUG | This is an immediate release tablet containing 2.4 mg of milled GSK2798745 API with SLS and hypermellose; to be administered orally in fasted/fed conditions, with 240 mL of water |
Inclusion Criteria: * Between 18 and 75 years of age inclusive, at the time of signing the informed consent * Healthy as determined by the investigator or medically qualified designee based on a medical evaluation including medical history, physical examination, laboratory tests and cardiac monitor...
GSK2798745 Micronized API without SLS and hypermellose is an investigational small molecule tablet formulation developed by GSK plc. It is being studied in congestive heart failure and is also known as GSK2798745 Micronized API without SLS and hypermellose (Tablet A). It is not approved and remains in Phase 1 clinical development.
GSK2798745 Micronized API without SLS and hypermellose is being studied for congestive heart failure, a cardiovascular condition. The clinical program is at Phase 1, so the drug is investigational and has not been approved for any use. Its only recorded trial enrolled healthy adult volunteers rather than patients.
GSK2798745 Micronized API without SLS and hypermellose targets TRPV4, a transient receptor potential cation channel. It acts as a TRPV4 antagonist, meaning it is designed to block activity at that receptor. TRPV4 antagonism is the mechanism under study in the cardiovascular setting of congestive heart failure.
GSK2798745 Micronized API without SLS and hypermellose is made by GSK plc, which trades under the ticker GSK. GSK is the developer of the compound and the sponsor of its clinical program. The asset is a small molecule TRPV4 antagonist tablet formulation.
GSK2798745 Micronized API without SLS and hypermellose is in Phase 1 development. It is investigational and has not been approved by the FDA. One Phase 1 trial has been completed, and no trials are currently active, so the recorded clinical work for this formulation has finished.
GSK2798745 Micronized API without SLS and hypermellose has been studied in one completed Phase 1 trial, NCT02925546, titled A Phase I Study to Assess the Pharmacokinetics of GSK2798745 Tablets. It enrolled 18 healthy adult volunteers in the United States, was randomized and controlled, and was not double blind.