Iniparib, also known as SAR-240550; NSC-746045; BSI-201; IND-71677; NIBA; INO-2BA, is a small-molecule prodrug inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase-1 (PARP-1) with potential chemosensitizing, radiosensitizing and antineoplastic activities. In vivo, PARP-1 inhibitor BSI-201 is converted to the active drug, which selectively binds to PARP-1 and inhibits PARP-1- mediated DNA repair. Consequently, this agent may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. In addition, PARP-1 inhibitor BSI-201 may exhibit direct antineoplastic activity against cancers defective in DNA repair.
相关文献及参考
Liang, H. et al.: IDrugs, 13, 646 (2010); Liang, H. et al.: Curr. Breat Cancer Rep., 3, 44 (2011); O'Shaughnessy, J. et al.: N. Eng. J. Med., 364, 205 (2011);
安全信息
Warnings
IRRITANT
Storage condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).