Sunitinib - Overall Recommendations
Sunitinib CANNOT be Co-Administered with the Following Agents1-4
- Strong CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole, grapefruit)
- Strong CYP3A4 inducers (e.g. dexamethasone, phenytoin, carbamazepine, rifampicin, rifabutin, rifapentin, phenobarbital, St John's wort)
- QTc interval-prolonging drugs (e.g. 5HT3 antagonists, antibiotics, antifungals and over-the-counter drugs (e.g. domperidone)
Additional Important Information when Prescribing Sunitinib2,4,5
If co-administration of strong CYP3A4 inhibitors is necessary, consider reducing the sunitinib dose to a minimum of 37.5 mg daily for GIST and mRCC or 25 mg daily for pNET, based on careful monitoring of tolerability.2
If co-administration of CYP3A4 inducers is necessary, consider increasing the sunitinib dose in 12.5 mg increments (up to 87.5 mg per day for GIST and mRCC or 62.5 mg per day for pNET), based on careful monitoring of tolerability.2,3,5
If co-administration of QTc interval-prolonging drugs is necessary, obtain an ECG 24-48 hours before, and 1 week after, the start of concomitant treatment.3
Consider increasing the dose of sunitinib to 75 mg over 24 hours if co-administering with rifampicin.4
Considering decreasing the dose of imatinib to 25 mg over 24 hours if co-administering with ketoconazole.4
- Food and Drug Administration. Sunitinib (Sutent) Prescribing information. 2015.
- European Medicines Agency. Sunitinib (SUTENT). Summary of Product Characteristics. 2015.
- 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.
- Pajares B, Torres E, Trigo JM et al. Tyrosine kinase inhibitors and drug interactions: a review with practical recommendations. Clin Transl Oncol 2012; 14: 94-101.
- Teo YL, Ho HK, Chan A. Metabolism-related pharmacokinetic drug-drug interactions with tyrosine kinase inhibitors: current understanding, challenges and recommendations. Br J Clin Pharmacol 2015; 79: 241-253.