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Drug interactions of Rezurock

1. Effect of Other Drugs on Rezurock

Strong CYP3A Inducers

Coadministration of Rezurock with strong CYP3A inducers decreases belumosudil exposure, which may reduce the efficacy of Rezurock. Increase the dosage of Rezurock when coadministered with strong CYP3A inducers.

Proton Pump Inhibitors

Coadministration of Rezurock with proton pump inhibitors decreases belumosudil exposure, which may reduce the efficacy of Rezurock. Increase  the dosage of Rezurock when coadministered with proton pump inhibitors.

2. Effect of Rezurock on Other Drugs

Certain UTG1A1 substrates

Avoid coadministration of Rezurock with UGT1A1 substrates, for which minimal concentration changes may lead to serious toxicities. If coadministration cannot be avoided, decrease the UGT1A1 substrates dosage(s) in accordance with the respective Prescribing  Information.

Rezurock is an inhibitor of UGT1A1. Coadministration of Rezurock with a UGT1A1 substrate decreased plasma concentrations of the glucuronide metabolite, which may increase the risk of adverse reactions related to sensitive  substrates of UGT1A1.

Certain P-gp, OATP1B1, and BCRP substrates

Avoid coadministration of Rezurock with P-gp, OATP1B1, and BCRP substrates, for which  minimal concentration changes may lead to serious toxicities. If coadministration cannot be avoided, decrease the P-gp, OATP1B1, and BCRP substrates dosage(s) in accordance with the respective Prescribing Information.

Rezurock is an inhibitor of P-gp, OATP1B1, and BCRP. Coadministration of Rezurock with P-gp, OATP1B1, and BCRP substrates increased their plasma concentrations, which may increase the risk of adverse reactions related to these  substrates.

from FDA，2024.04