Drug intelligence / Profile preview

bortezomib + rifampicin

Development stage
Phase 1
Lead developer
Takeda
Modality
Small Molecules
Administration
Intravenous (bortezomib), Oral (rifampicin)
01

Overview

Bortezomib + rifampicin is a combination of two small molecule drugs. Bortezomib is a reversible inhibitor of the 26S proteasome and is primarily used as an antineoplastic agent in the treatment of multiple myeloma and mantle cell lymphoma. It induces apoptosis in cancer cells by disrupting protein degradation pathways. Rifampicin (also known as rifampin) is a potent antibiotic that acts by inhibiting DNA-dependent RNA polymerase in bacteria and is widely used to treat tuberculosis and other bacterial infections. When co-administered, rifampicin acts as a strong inducer of cytochrome P450 3A4 (CYP3A4), which significantly increases the metabolism of bortezomib. This interaction leads to reduced plasma concentrations (AUC) and peak levels (Cmax) of bortezomib—by approximately 45%—potentially reducing its clinical efficacy against cancer[1][3][4]. Therefore, this combination should generally be avoided unless no alternatives exist.

Brand names
Bortezomib Fresenius Kabi
Other names
bortezomib + rifampin
02

Targets

rpoB (DNA-directed RNA polymerase subunit beta)PSMB5 (Proteasome subunit beta Type-5)

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