This week in therapeutics




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Baculoviral IAP repeat-containing 2
(BIRC2; cIAP1); x-linked inhibitor of apoptosis (XIAP)

Mouse and cell culture studies identified bicyclic octahydropyrrolo[1,2-a]pyrazine-based inhibitors of cIAP1 that could help treat cancer. In a human breast cancer cell line, the most potent compound inhibited cell growth at nanomolar concentrations. In a mouse xenograft model of human breast cancer, the most potent compound caused dose-dependent tumor regression. Researchers did not disclose next steps, which could include testing the lead inhibitor in models of additional cancer indications.
Takeda Pharmaceutical Co. Ltd. has the lead cIAP1 inhibitor in preclinical development.
At least eight companies have compounds that inhibit IAP proteins in Phase II testing or earlier to treat various cancers.

SciBX 6(5); doi:10.1038/scibx.2013.110
Published online Feb. 7, 2013

Patent application filed covering use in cancer; licensing status undisclosed

Hashimoto, K. et al. J. Med. Chem.; published online Jan. 8, 2013;
Contact: Tomoyasu Ishikawa, Takeda Pharmaceutical Co. Ltd., Kanagawa, Japan
Contact: Bunnai Saito, same affiliation as above