Drug intelligence / Profile preview

BMS-986166 + gemfibrozil

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

BMS-986166 is an orally administered small molecule prodrug developed by Bristol Myers Squibb. It is a highly potent, selective modulator of sphingosine-1-phosphate receptor 1 (S1P1), modulating immune cell trafficking by causing lymphocyte sequestration through S1P1 receptor agonism. The active metabolite is BMS-986166-P, which displays reduced cardiotoxicity compared to other S1P modulators and shows efficacy in preclinical models of autoimmune diseases, particularly multiple sclerosis. Gemfibrozil is a lipid-regulating agent of the fibrate class, primarily acting as an agonist of peroxisome proliferator-activated receptor alpha (PPAR-α), reducing triglycerides and raising HDL cholesterol for disorders like hypertriglyceridemia. The combination denotes concurrent administration of these two oral agents, potentially for drug-drug interaction evaluation or pharmacokinetic studies, as gemfibrozil is a known CYP2C8 inhibitor and may alter the metabolism of drugs like BMS-986166[1][2][5].

Other names
BMS-986166BMS986166BMS 986166BMS-986166-04BMS986166-04BMS 986166-04S1PR1 modulatorS-1PR1 modulatorS 1PR1 modulatorgemfibrozil
02

Targets

EDG1 (Sphingosine-1-phosphate receptors)

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