molecules of the month

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…