Drug interactions of Axitinib

In vitro data indicate that axitinib is metabolized primarily by CYP3A4/5 and, to a lesser extent,  CYP1A2, CYP2C19, and uridine diphosphate-glucuronosyltransferase (UGT) 1A1.

1 CYP3A4/5 Inhibitors  

Co-administration of ketoconazole, a strong inhibitor of CYP3A4/5, increased the plasma  exposure of axitinib in healthy volunteers. Co-administration of INLYTA with strong CYP3A4/5 inhibitors should be avoided. Grapefruit or grapefruit juice may also increase axitinib plasma  concentrations and should be avoided. Selection of concomitant medication with no or minimal  CYP3A4/5 inhibition potential is recommended. If a strong CYP3A4/5 inhibitor must be coadministered, the INLYTA dose should be reduced.

2 CYP3A4/5 Inducers  

Co-administration of rifampin, a strong inducer of CYP3A4/5, reduced the plasma exposure of  axitinib in healthy volunteers. Co-administration of INLYTA with strong CYP3A4/5 inducers  (e.g., rifampin, dexamethasone, phenytoin, carbamazepine, rifabutin, rifapentin, phenobarbital,  and St. John’s wort) should be avoided. Selection of concomitant medication with no or minimal  CYP3A4/5 induction potential is recommended . Moderate CYP3A4/5 inducers (e.g., bosentan, efavirenz,  etravirine, modafinil, and nafcillin) may also reduce the plasma exposure of axitinib and should  be avoided if possible.

FDA，2012.01