simurosertib

Simurosertib is an orally bioavailable small molecule inhibitor of cell division cycle 7-related protein kinase (CDC7), a serine/threonine kinase that plays a critical role in the initiation of DNA replication and regulation of cell cycle progression. By inhibiting CDC7, simurosertib prevents the initiation of DNA replication during mitosis, leading to cell cycle arrest and apoptosis in tumor cells that overexpress CDC7. This mechanism results in antiproliferative effects across various cancer types, including colorectal, lung, ovarian, and pancreatic cancers. Simurosertib was developed by Takeda Oncology for use as an antineoplastic agent but has been discontinued for all investigated indications after reaching phase I/II clinical trials for several advanced solid tumors.[1][2][3][5][6]

Other names

2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-onesimurosertib hemihydrate