Regorafenib has 18 known drug interactions based on U.S. FDA drug labeling data. 15 are classified as major interactions requiring close medical supervision. Notable interactions include combinations with Carbamazepine, Clarithromycin, Grapefruit Juice. Patients taking Regorafenib should inform their healthcare provider of all current medications — including over-the-counter drugs and supplements — to avoid potentially harmful combinations. Data sourced from OpenFDA and the NIH National Library of Medicine.
- Total
- 18
- Major
- 15
- Moderate
- 3
Major (15)
- Regorafenib + Carbamazepine— Strong CYP3A4 inducer that decreases regorafenib plasma concentrations and may lead to decreased efficacy.
- Regorafenib + Clarithromycin— Strong CYP3A4 inhibitor that increases regorafenib plasma concentrations and may lead to increased toxicity.
- Regorafenib + Grapefruit Juice— Strong CYP3A4 inhibitor that increases regorafenib plasma concentrations and may lead to increased toxicity.
- Regorafenib + Itraconazole— Strong CYP3A4 inhibitor that increases regorafenib plasma concentrations and may lead to increased toxicity.
- Regorafenib + Ketoconazole— Strong CYP3A4 inhibitor that increases regorafenib plasma concentrations and may lead to increased toxicity.
- Regorafenib + Nefazodone— Strong CYP3A4 inhibitor that increases regorafenib plasma concentrations and may lead to increased toxicity.
- Regorafenib + Phenobarbital— Strong CYP3A4 inducer that decreases regorafenib plasma concentrations and may lead to decreased efficacy.
- Regorafenib + Phenytoin— Strong CYP3A4 inducer that decreases regorafenib plasma concentrations and may lead to decreased efficacy.
- Regorafenib + Posaconazole— Strong CYP3A4 inhibitor that increases regorafenib plasma concentrations and may lead to increased toxicity.
- Regorafenib + Rifampin— Strong CYP3A4 inducer that decreases regorafenib plasma concentrations and may lead to decreased efficacy.
- Regorafenib + Rosuvastatin— Combination increases rosuvastatin exposure. Limit rosuvastatin dose to 10 mg once daily.
- Regorafenib + Rosuvastatin Calcium— Increases rosuvastatin exposure. Limit rosuvastatin dose to 10 mg once daily.
- Regorafenib + St. John'S Wort— Strong CYP3A4 inducer that decreases regorafenib plasma concentrations and may lead to decreased efficacy.
- Regorafenib + Telithromycin— Strong CYP3A4 inhibitor that increases regorafenib plasma concentrations and may lead to increased toxicity.
- Regorafenib + Voriconazole— Strong CYP3A4 inhibitor that increases regorafenib plasma concentrations and may lead to increased toxicity.
Moderate (3)
- Regorafenib + Atorvastatin— BCRP substrate whose plasma concentrations increase with regorafenib; monitor for exposure-related toxicity.
- Regorafenib + Fluvastatin— BCRP substrate whose plasma concentrations increase with regorafenib; monitor for exposure-related toxicity.
- Regorafenib + Methotrexate— BCRP substrate whose plasma concentrations increase with regorafenib; monitor for exposure-related toxicity.