oprozomib + midazolam

Oprozomib + midazolam is a drug combination primarily utilized in clinical pharmacology studies to assess the drug-drug interaction (DDI) potential of oprozomib. Oprozomib (formerly PR-047) is an orally bioavailable, irreversible inhibitor of the 20S proteasome, specifically targeting the chymotrypsin-like activity of the β5 subunit (PSMB5). It was developed by Onyx Pharmaceuticals (an Amgen subsidiary) for the treatment of hematologic malignancies like multiple myeloma. Midazolam is a short-acting benzodiazepine that acts as a positive allosteric modulator of the GABA-A receptor. In this specific combination context, midazolam serves as a sensitive probe substrate for the Cytochrome P450 3A4 (CYP3A4) enzyme. Clinical trials have evaluated how oprozomib affects the pharmacokinetics of midazolam to determine if oprozomib acts as an inhibitor or inducer of CYP3A4, which informs safety guidelines for co-administration with other CYP3A4-metabolized drugs.

Other names

PR-047 + midazolam