Vemurafenib - Overall Recommendations

Vemurafenib CAN be Co-Administered with the Following Agents, IF Administered with Caution1,2

  • Agents with narrow therapeutic windows that are metabolised by CYP1A2, CYP2D6 and CYP3A4
  • The CYP2C9 substrate warfarin
  • Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, saquinavir, telithromycin, ritonavir, indinavir, nelfinavir, voriconazole)
  • Strong CYP3A4 inducers (e.g., phenytoin, carbamazepine, rifampin, rifabutin, rifapentine, phenobarbital)

Additional Important Information when Prescribing Vermurafenib1-3

If co-administration of CYP1A2, CYP2D6 and CYP3A4 substrate drugs cannot be avoided, exercise caution and consider a dose reduction of the concomitant CYP1A2 and CYP2D6 substrate drug.


  1. European Medicines Agency. Vemurafenib (ZELBORAF). Summary of Product Characteristics. 2015.
  2. Food and Drug Administration. Vemurafenib (ZELBORAF) Prescribing information. 2015.
  3. van Leeuwen RW, van Gelder T, Mathijssen RH, Jansman FG. Drug-drug interactions with tyrosine-kinase inhibitors: a clinical perspective. Lancet Oncol 2014; 15: e315-326.
Last update: 21 July 2015