Drug intelligence / Profile preview

GSK1292263 + atorvastatin

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GSK1292263 + atorvastatin is an **oral combination** of GSK1292263, a selective small molecule agonist of the G protein-coupled receptor 119 (GPR119), and atorvastatin, a statin that inhibits HMG-CoA reductase. GSK1292263 was developed to improve glucose metabolism and modulate gut hormone secretion, showing a significant increase in peptide YY (PYY) levels but no substantial effect on glucose control in type 2 diabetes mellitus. Atorvastatin is widely used for the treatment of hyperlipidemia and prevention of cardiovascular events by lowering LDL cholesterol. This combination was specifically investigated for its effects in dyslipidemic patients and for drug-drug interactions. No unique brand name or fixed-dose combination product is approved or marketed; the combination has only been studied as co-administration in clinical trials[3][5][9].

02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)ABCG2 (Breast cancer resistance protein)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)CYP3A4 (Cytochrome P450 3A4)GPR119 (Glucose-dependent insulinotropic receptor)

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