ZEN003694 + talazoparib

ZEN003694 + talazoparib is an investigational oral combination therapy consisting of the BET bromodomain inhibitor ZEN003694 (also known as ZEN-3694) and the PARP inhibitor talazoparib. ZEN003694 inhibits the bromodomain and extra-terminal (BET) family of proteins, disrupting cancer cell transcription and sensitizing tumors to DNA damage by downregulating homologous recombination repair gene expression. Talazoparib inhibits PARP, a key enzyme involved in DNA damage repair, leading to accumulation of lethal DNA breaks in tumor cells. The combination aims to enhance anti-cancer activity in patients with advanced or metastatic solid tumors, notably those with triple negative breast cancer (TNBC) or other cancers with DNA repair pathway abnormalities, particularly in the absence of germline BRCA1/2 mutations. This regimen is under investigation in Phase 1b/2 and Phase 2 clinical trials, where it has shown preliminary antitumor activity and a manageable safety profile, with thrombocytopenia as the most common dose-limiting toxicity[1][2][3][4][5][7][9].

Brand names

Talzenna

Other names

ZEN-3694 + talazoparib