darexaban + ketoconazole

This is a **combination of darexaban, an oral direct factor Xa inhibitor, and ketoconazole, a strong inhibitor of CYP3A4 and P-glycoprotein**. Darexaban (code name YM150) acts as an anticoagulant by inhibiting factor Xa, an important enzyme in the coagulation cascade, and was developed for prevention of thromboembolic events. Ketoconazole is an antifungal medication that also strongly inhibits the activity of CYP3A4 and P-glycoprotein, affecting the metabolism and excretion of many drugs, including direct oral anticoagulants. A study demonstrated that **co-administration of ketoconazole with darexaban does not significantly affect the pharmacokinetics of the main active metabolite, darexaban glucuronide; PK changes were not deemed clinically relevant**[2]. The primary mechanism of interaction would be through ketoconazole's inhibition of darexaban's metabolic and transporter pathways, but in studies, no dosing adjustment was found necessary for the combination[2]. Darexaban was developed by Astellas, but its development was discontinued and it is not approved for clinical use. Ketoconazole is widely available as both oral and topical antifungal medication.

Other names

darexaban + ketoconazole