Drug intelligence / Profile preview

ozanimod + rifampin

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

Overview

Ozanimod + rifampin is a combination of ozanimod, a selective sphingosine-1-phosphate receptor (S1P) modulator, and rifampin, a broad-spectrum antibiotic and strong inducer of several hepatic drug-metabolizing enzymes. - **Ozanimod** binds with high affinity to S1P receptor subtypes 1 and 5, blocking lymphocyte egress from lymph nodes and thereby reducing immune cell-mediated inflammation, primarily indicated for relapsing forms of multiple sclerosis and moderately to severely active ulcerative colitis. Its mechanism involves sphingosine-1-phosphate receptor 1 (S1P1) and sphingosine-1-phosphate receptor 5 (S1P5) modulation, leading to immunosuppression. - **Rifampin** is primarily used as an antibacterial agent against Mycobacterium tuberculosis and other bacteria. It acts as a strong inducer of cytochrome P450 enzymes (notably CYP3A and moderate CYP2C8), as well as P-glycoprotein transporters, which accelerates the metabolism of concomitant drugs. When ozanimod is co-administered with rifampin, rifampin markedly increases the metabolic clearance of ozanimod and its active metabolites, resulting in a reduction of ozanimod’s pharmacological efficacy and exposure. This combination is generally contraindicated due to decreased efficacy of ozanimod in the presence of rifampin[1][3][4].

Brand names
ZeposiaZeposia 7-day Starter PackZeposia7-day Starter PackZeposia-7-day Starter PackZeposia Starter Kit
Other names
ozanimodumrifampicin
02

Targets

S1PR5 (Sphingosine-1-phosphate receptor 5)

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