venadaparib

Venadaparib is a potent, selective, and orally active small molecule inhibitor of poly(ADP-ribose) polymerase 1 and 2 (PARP1/2). It exhibits high selectivity for PARP1 and PARP2 with IC50 values in the low nanomolar range (approximately 0.8–1.4 nM for PARP1 and 1.0–3 nM for PARP2), while showing minimal activity against other PARPs such as PARP3 or tankyrases[1][2][6]. By inhibiting these enzymes, venadaparib prevents the repair of DNA single-strand breaks via base excision repair pathways, leading to synthetic lethality in tumor cells deficient in homologous recombination repair mechanisms—such as those with BRCA mutations[5][6]. Venadaparib has demonstrated potent antitumor activity in preclinical models and is under clinical investigation primarily for advanced solid tumors that have progressed after standard therapies[5]. The drug shows favorable pharmacokinetic properties, broad tissue distribution, improved safety margins compared to earlier-generation PARP inhibitors like olaparib, and promising efficacy especially in homologous recombination-deficient cancers[6].

Other names

4-((3-((3-((cyclopropylamino)methyl)-1-azetidinyl)carbonyl)-4-fluorophenyl)methyl)-1(2h)-phthalazinone