Drug intelligence / Profile preview

selexipag + rifampicin

Development stage
Unknown
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**Selexipag + rifampicin** is a combination of two pharmaceutical agents: selexipag, a selective prostacyclin (IP) receptor agonist indicated for the treatment of pulmonary arterial hypertension (PAH), and rifampicin, a potent antibiotic and strong CYP2C8 inducer often used in the treatment of tuberculosis and related infections. Selexipag acts by stimulating the IP receptor, leading to vasodilation, anti-proliferative, and anti-fibrotic effects in pulmonary vasculature with minimal activity at other prostanoid receptors[1][5]. Rifampicin, as a strong inducer of CYP2C8 (and other enzymes), markedly increases the metabolism of selexipag, reducing exposure to selexipag’s active metabolite, and consequently may necessitate dose adjustments of selexipag in clinical use to maintain efficacy[2][4][5]. The combination is not a marketed product, but represents a pharmacokinetic and drug-interaction scenario of clinical relevance.

Other names
selexipagrifampicinUPTRAVIRifadin
02

Targets

ABCB1 (P-glycoprotein)CXADR (Coxsackievirus and adenovirus receptor)CYP3A4 (Cytochrome P450 3A4)PTGIR (Prostanoid IP Receptor)PXR (Pregnane X receptor)CYP2C8 (Cytochrome P450 2C8)

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