Drug intelligence / Profile preview

GSK376501 + midazolam

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Intranasal, Sublingual, Rectal, Buccal
01

Overview

GSK376501 + midazolam is a **combination drug** consisting of GSK376501, a partial agonist of the peroxisome proliferator-activated receptor gamma (PPARγ), and midazolam, a short-acting benzodiazepine. GSK376501 is an investigational small molecule developed by GSK for treating type 2 diabetes and obesity, acting as a PPARγ partial agonist to modulate glucose and lipid metabolism[4][2]. Midazolam is a widely used benzodiazepine with hypnotic, sedative, anxiolytic, muscle relaxant, anticonvulsant, and amnesic properties, primarily acting as a positive allosteric modulator of the GABA-A receptor[3][5]. Clinically, midazolam is employed for procedural sedation, anesthesia, and acute agitation, and can be administered via multiple routes. The combination of these drugs likely would be relevant for drug-interaction studies or special procedural use, but is not a marketed fixed-dose combination.

Other names
midazolamGSK376501GSK-376501GSK 376501
02

Targets

PPARA (Peroxisome proliferator-activated receptor alpha)GABRR (GABA-A receptor subunit rho)PPARG (Peroxisome proliferator-activated receptor gamma)CYP3A4 (Cytochrome P450 3A4)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP2C8 (Cytochrome P450 2C8)

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