tofacitinib + ketoconazole

tofacitinib + ketoconazole refers to the co-administration of the Janus kinase (JAK) inhibitor tofacitinib (formerly known as tasocitinib or CP-690,550) and the potent CYP3A4 inhibitor ketoconazole. This combination was specifically evaluated by Pfizer in Phase 1 pharmacokinetic studies to assess the impact of CYP3A4 inhibition on the systemic exposure of tofacitinib. Tofacitinib is an oral small molecule that primarily inhibits JAK1 and JAK3, thereby blocking the signaling of various cytokines involved in the pathogenesis of inflammatory diseases like rheumatoid arthritis. Because tofacitinib is primarily metabolized by the CYP3A4 enzyme, co-administration with strong inhibitors like ketoconazole can significantly increase its plasma concentrations, necessitating dose adjustments. Tofacitinib is approved for the treatment of rheumatoid arthritis, psoriatic arthritis, ulcerative colitis, and ankylosing spondylitis, while ketoconazole is a broad-spectrum antifungal agent.

Brand names

XeljanzNizoral

Other names

tasocitinib + ketoconazole