Table 6.
Kinase Inhibitor | Food Effect | CYP 3A4 inducer | CYP 3A4 Inhibitor | Effect on Concurrent Medications | Proton Pump Inhibitor | Statin | Warfarin |
---|---|---|---|---|---|---|---|
Axitinib | No | Decrease KI level; avoid inducer | Increase KI level; Reduce KI dose | Does not inhibit CYP3A4 | No adjustment | ||
Bosutinib | With food | Decrease KI level; avoid inducer | Increase KI level; Avoid inhibitor | Decrease KI level; use antacid, H2 2 hr later | |||
Cabozantinib | Empty Stomach | Decrease KI level; avoid inducer | Increase KI level; Avoid inhibitor | CYP3A4 substrate increase | |||
Crizotinib | No | Decrease KI level; avoid inducer | Increase KI level; Avoid inhibitor | CYP3A4 substrate increase | |||
Dasatinib | No | Decrease KI level; increase KI dose | Increase KI level; Reduce KI dose | CYP3A4 substrate increase | Do not use PPI, H2; use antacid 2 hr later | Simvastatin's AUC increase | |
Erlotinib | Empty stomach | Decrease KI level; increase KI dose | Increase KI level; Reduce KI dose | CYP3A4 substrate increase | Do not use PPI; take erlotinib 10 hr later or 2 hr before H2; use antacid 2 hr later | High INR | |
Gefitinib | No | Decrease KI level; increase dose to 500 mg | Increase KI level; Avoid inhibitor | H2 reduced AUC | |||
Imatinib | With food | Decrease KI level; increase KI dose | Increase KI level; Avoid inhibitor | CYP3A4 substrate increase | Simvastatin's AUC increase | ||
Lapatinib | Empty stomach | Decrease KI level; increase KI dose | Increase KI level; Reduce KI dose | CYP3A4 substrate increase | Esomeprazole did not reduce KI level | ||
Nilotinib | Empty stomach | Decrease KI level; avoid inducer | Increase KI level; Reduce KI dose | CYP3A4 substrate increase | Decrease KI level;use antacid, H2, 2 hr later; gastrectomy decrease KI level | No change | |
Pazopanib | Empty Stomach | Decrease KI level; avoid inducer | Increase KI level; Reduce KI dose | CYP3A4 substrate change | No change | ||
Regorafenib | With food | Decrease KI level; avoid inducer | Increase KI level; Avoid inhibitor | CYP3A4 substrate increase | |||
Ruxolitinib | No | No adjustment | Increase KI level; Reduce KI dose | ||||
Sorafenib | Empty stoma ch | Decrease KI level; avoid inducer | Ketoconazole, no effect | Not inhibit CYP3A4 | |||
Sunitinib | No | Decrease KI level; increase KI dose | Increase KI level; Reduce KI dose | No effect on major CYP | |||
Vandetanib | No | Decrease KI level; avoid inducer | Itraconazole, no effect | Avoid; QT prolonging/ar rhythmic | |||
Vemurafenib | No | Decrease KI level; avoid inducer | Increase KI level; Avoid inhibitor | CYP3A4 substrate change | Warfarin AUC 18% increase | ||
Vismodegib | No | No effect | No effect | PPI, H2, and antacid may decrease KI level | |||
Ponatinib | No | avoid inducer | Increase KI level; Reduce to 30mg | No effect on major CYP | Not evaluated; antiacid may reduce KI level |
Abbreviations: AUC, area under the curve; H2, Histamine H2 receptor blocker; HR, hour; KI, kinase inhibitor