Drug intelligence / Profile preview

talazoparib + rifampin

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

This entry refers to the combination of **talazoparib**, a potent poly(ADP-ribose) polymerase (PARP) inhibitor used primarily as an antineoplastic agent, and **rifampin**, a well-known antibiotic and a strong inducer of cytochrome P450 (CYP) enzymes and P-glycoprotein (P-gp) transporter. Talazoparib inhibits PARP1 and PARP2, promoting synthetic lethality in tumor cells with homologous recombination repair deficiency, such as BRCA-mutated cancers. Rifampin is primarily used for the treatment and prophylaxis of tuberculosis and as an inducer in drug-drug interaction studies. When used together, rifampin as a P-gp inducer can alter the pharmacokinetics of talazoparib, specifically increasing the maximum plasma concentration (Cmax) of talazoparib by about 37%, while not significantly impacting its area under the curve (AUC)[1][2][3][4][5]. This combination has been studied for drug-drug interaction, rather than for a therapeutic indication.

Brand names
TalzennaRifadin
Other names
talazoparibBMN 673BMN673BMN-673rifampinrifampicin
02

Targets

CYP3A4 (Cytochrome P450 3A4)ABCB1 (P-glycoprotein)rpoB (DNA-directed RNA polymerase subunit beta)ABCG2 (Breast cancer resistance protein)MRP (Multidrug resistance-associated protein family)PARP2 (Poly (adp-ribose) polymerase 2)PXR (Pregnane X receptor)

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