Lapatinib Ditosylate and Food

Take lapatinib on an empty stomach 1 hour before or 1 hour after a meal unless otherwise directed by your doctor. This will make it easier for your body to absorb the medication. The lapatinib dose is administered once daily and should not be divided. The usual dose of lapatinib is equal to 5 tablets. You may swallow each tablet one at a time, but take the entire lapatinib dose at the same time each day. If you are receiving therapy with lapatinib you should be advised to avoid grapefruits and grapefruit juice. Grapefruit can raise the levels of lapatinib in your body and lead to dangerous side effects.

GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of lapatinib. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits.

ADJUST DOSING INTERVAL: Food can significantly increase the oral bioavailability of lapatinib. According to the manufacturer, lapatinib peak plasma concentration (Cmax) was approximately 2.5- and 3-fold higher and systemic exposure (AUC) 3- and 4-fold higher when administered with a low fat meal (5% fat; 500 calories) or with a high-fat meal (50% fat; 1000 calories), respectively, compared to fasting. Dividing the daily dose also resulted in an approximately 2-fold higher systemic exposure at steady state compared to the same total dose administered once daily.

MANAGEMENT: Patients treated with lapatinib should preferably avoid the consumption of grapefruit or grapefruit juice. The manufacturer recommends that lapatinib be administered at least one hour before or one hour after a meal. The lapatinib dose is administered once daily and should not be divided.