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. 2021 May 26;8:477–492. doi: 10.2147/JHC.S251729

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.