Cabometyx and Alcohol/Food Interactions

ADJUST DOSING INTERVAL: Food may alter the oral bioavailability of cabozantinib. When healthy subjects were given a single 140 mg oral dose with a high-fat meal, cabozantinib peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 41% and 57%, respectively, relative to administration under fasting conditions. In clinical studies, patients were administered cabozantinib without food.

GENERALLY AVOID: Coadministration with grapefruit juice is likely to increase the plasma concentrations of cabozantinib, which is primarily metabolized by CYP450 3A4. However, the interaction has not been studied. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.

MANAGEMENT: Cabozantinib should be administered at least one hour before or two hours after a meal. The consumption of grapefruit, grapefruit juice, and supplements that contain grapefruit extract should be avoided.

cabozantinib - hypertension

The use of cabozantinib causes hypertension. Blood pressure should be well-controlled prior to initiating cabozantinib and monitored and treated as needed with standard anti-hypertensive therapy. It is recommended to reduce the dose in case of persistent hypertension despite use of anti-hypertensive medications and to discontinue therapy if hypertension is severe and persistent despite these measures. Discontinue cabozantinib therapy for severe hypertension that cannot be controlled with anti-hypertensive therapy and if there is evidence of hypertensive crisis or severe hypertension despite optimal medical management. Close monitoring is recommended.