Table 2.

Major Drug Interactions with Regorafenib

Inducers of CYP3A4*	Inhibitors of CYP3A4^	CYP2C9 Inhibition#	UGT1A1 Inhibitor&
Carbamazepine Isoniazid Phenobarbital Phenytoin/fosphenytoin Rifampin St. John’s wort (Hypericum perforatum)	Boceprevir Clarithromycin Conivaptan Grapefruit juice Ketoconazole Indinavir Itraconazole Nefazodone Nelfinavir Posaconazole Ritonavir Saquinavir Telaprevir Telithromycin Voriconazole	Warfarin	Irinotecan

Notes: *Inducers of CYP3A4 may decrease exposure to regorafenib and exposure to M-2 and M-5 metabolites may increase. ^{^}Inhibitors of CYP3A4 may increase exposure to regorafenib and exposure to M-2 and M-5 metabolites may decrease. ^#Regorafenib inhibits CYP2C9; concomitant administration of drugs that are CYP2C9 substrates may result in increased exposure of that drug. ^&Regorafenib is a UGT1A1 inhibitor: concomitant use with irinotecan may result in increased irinotecan exposure.