AZD2461

AZD2461 is an orally bioavailable small molecule inhibitor of poly(ADP-ribose) polymerase (PARP), developed as a next-generation PARP inhibitor following olaparib. It selectively binds to PARP enzymes, preventing PARP-mediated DNA repair of single-strand DNA breaks via the base-excision repair pathway, leading to accumulation of double-strand breaks and cell death in susceptible tumor cells. Unlike olaparib, AZD2461 was designed with lower affinity for drug transporters such as P-glycoprotein (Pgp), allowing it to circumvent resistance mechanisms seen in some tumors. It also has a different inhibitory profile for PARP isoforms, particularly showing lower affinity for PARP3 compared to other inhibitors. The drug has been evaluated primarily in Phase 1 clinical trials for refractory solid tumors[1][2][4][5][6][7][8].

Other names

4-(4-fluoro-3-(4-methoxypiperidine-1-carbonyl)benzyl)phthalazin-1(2H)-one1174043-16-3UNII-3K288XF5XJUNII3K288XF5XJUNII 3K288XF5XJCHEMBL4098253CHEMBL-4098253CHEMBL 4098253