molecules of the month

The Bayer DNA-PK inhibitor, BAY-8400, is an orally active and selective DNA-PK kinase inhibitor that synergistically enhances the efficacy of radiotherapeutics in xenograft models. The program started with a campaign to identify ATR inhibitors, which resulted in hits against ATR, ATM, and DNA-PK, all of which are of interest due to their roles in DNA damage repair. It will be interesting to watch this active space to see whether ATR, ATM, or DNA-PK inhibition can improve therapeutic indexes or efficacy of various DNA-damaging treatments clinically.