Iniparib

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Description

Iniparib (BSI-201) is a potent small-molecule Poly(ADP-ribose) polymerase (PARP1) inhibitor for cancer treatment. Poly(ADP-ribose) polymerase (PARP) is a critical DNA repair enzyme involved in DNA single-strand break repair via the base excision repair pathway. PARP1 is activated by DNA damage. BSI-201 was the first putative PARP inhibitor to commence phase III clinical trials. Iniparib (BSI-201) produces rapid apoptosis in various cancer cell lines with IC50 values ranging from 40-128 μM and is not toxic in Syrian hamsters at doses as high as 200 mg/kg. BSI-201 was well tolerated and there were no changes in blood counts at the end of treatment. Antitumor activity of Iniparib (BSI-201) was confirmed by Caspace-3 and TUNEL staining of OVCAR-3 tumors. The combination of Iniparib and topotecan produced significant antitumor activity (P<0.001) and increased the percentage of complete tumor regression compared with topotecan alone. In addition, PARP-1 inhibitor BSI-201 may exhibit direct antineoplastic activity against cancers defective in DNA repair.

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