Major
Established
描述
Cyclosporine significantly increases apixaban exposure through inhibition of CYP3A4 and P-glycoprotein, elevating bleeding risk.
机制
Apixaban is metabolised by CYP3A4 and transported by P-gp; cyclosporine inhibits both pathways, substantially increasing apixaban AUC and Cmax.
临床意义
FDA labeling recommends dose reduction of apixaban when combined with strong dual inhibitors; bleeding risk increases proportionally to AUC.
处理措施
Reduce apixaban to 2.5 mg BID when strong dual CYP3A4/P-gp inhibitors such as cyclosporine are used; monitor closely for bleeding.