molecules of the month


CDC7 serine/threonine kinase inhibitor

oral 50 mg QD, Ph. II in solid tumors compl.

from homology model pharmacophore + opt.

Sci. Adv., May 21, 2021

Takeda Pharmaceutical, Kanagawa, JP

2 mins read

The Takeda CDC7 serine/threonine kinase inhibitor, simurosertib (TAK-931), is the first orally active CDC7-selective inhibitor and recently had its Ph. I study results in solid tumors posted. The drug was dosed as a single agent in one study at 50 mg QD with 7-day rest periods on 21-day cycles, and in another study at varying levels with varying rest schedules, suggestive of anticipated on-target tox. Neutropenia and GI adverse events appear to be drug-related (NCT02699749), and most patients did not complete the study due to progressive disease. Though the single-agent results are discouraging, the team published this paper describing their efforts to find a combination regimen and/or cancer subtype where CDC7 inhibition might be effective. Finding the right combination or right…

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