Drug Interactions between clofazimine and pexidartinib

Consumer information for this interaction is not currently available.

GENERALLY AVOID: Coadministration of pexidartinib with moderate CYP450 3A4 inhibitors may significantly increase the plasma concentrations and the incidence and severity of adverse effects of pexidartinib, including potentially fatal hepatotoxicity. The proposed mechanism is inhibition of CYP450 3A4, the primary isoenzyme responsible for the metabolic clearance of pexidartinib. Concomitant administration of itraconazole, a strong CYP450 3A4 inhibitor, increased pexidartinib peak plasma concentration (Cmax) and systemic exposure (AUC) by 48% and 70%, respectively. No data are available regarding the effects that other, less potent CYP450 3A4 inhibitors may have on the pharmacokinetics of pexidartinib.

MANAGEMENT: The use of pexidartinib with a moderate CYP450 3A4 inhibitor should generally be avoided. If concomitant use is required, the dose of pexidartinib should be reduced according to the manufacturer's recommendations. If concomitant use of a moderate CYP450 3A4 inhibitor is discontinued, the dose of pexidartinib may be increased, after 3 plasma half-lives of the moderate CYP450 3A4 inhibitor, to the dose that was used prior to starting the moderate CYP450 3A4 inhibitor.