Drug Interactions between belumosudil and pralsetinib

Pralsetinib should be taken on an empty stomach, at least 2 hours after or 1 hour before a meal. Do not consume grapefruit, grapefruit juice, or any supplements that contain grapefruit extract during treatment with pralsetinib unless directed otherwise by your doctor. Grapefruit juice can increase the blood levels of pralsetinib. This may increase the risk and/or severity of serious side effects such as lung problems, high blood pressure, liver problems, bleeding, fatigue, muscle pains, or constipation. Talk to your doctor if you have any questions or concerns. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

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Consumer information for this interaction is not currently available.

ADJUST DOSING INTERVAL: Administration with food increases the oral bioavailability of belumosudil. The mechanism has not been described. Administration of belumosudil (200 mg single oral dose) in healthy subjects, with a fatty and calorie-rich meal (approximately half of the calories were contained in the fat) increased the mean belumosudil peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) by 120% and 100%, respectively, compared to administration under fasting conditions. The time to reach peak concentration (Tmax) was delayed by 30 minutes. Administration of oral belumosudil 200 mg once daily with food in patients with chronic graft-versus-host disease (chronic GVHD) lead to steady-state concentrations of the drug with an accumulation ration of 1.4.

MANAGEMENT: To ensure maximal oral absorption, belumosudil should be administered with a meal, every day at the same time.