Drug intelligence / Profile preview

talazoparib

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

Overview

Talazoparib is an orally available small molecule inhibitor of poly(ADP-ribose) polymerase (PARP), specifically targeting PARP1 and PARP2 enzymes involved in DNA repair. By inhibiting these enzymes, talazoparib prevents the repair of single-strand DNA breaks via the base excision repair pathway and induces cytotoxicity in cancer cells with defects in homologous recombination repair genes such as BRCA1 and BRCA2. It also exerts a potent "PARP trapping" effect, stabilizing PARP-DNA complexes and further impairing DNA replication and cell survival. Talazoparib is primarily indicated for the treatment of HER2-negative locally advanced or metastatic breast cancer with deleterious or suspected deleterious germline BRCA mutations, as well as for HRR gene-mutated metastatic castration-resistant prostate cancer (in combination with enzalutamide). The drug was developed by Pfizer.

Brand names
TalzennaTalzenna Liquid-Filled
Other names
talazoparibMDV3800MDV-3800MDV 3800
02

Targets

PARP2 (Poly (adp-ribose) polymerase 2)

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