tosedostat

Tosedostat is an orally bioavailable small molecule inhibitor of the M1 family of aminopeptidases, including puromycin-sensitive aminopeptidase (PSA) and leukotriene A4 hydrolase (LTA4H). It is converted in vivo to its active metabolite CHR-79888. Tosedostat exerts antiproliferative, pro-apoptotic, and anti-angiogenic effects against a range of tumor cell lines by blocking protein degradation pathways critical for cancer cell survival. It has demonstrated activity as a single agent and in combination with cytotoxic agents such as carboplatin and paclitaxel. Tosedostat has been primarily investigated for the treatment of hematological malignancies such as acute myeloid leukemia (AML), relapsed/refractory AML, multiple myeloma, pancreatic cancer, and other solid tumors[1][2][3][4][5][7].