Issues

In this volume of Molecular Cancer Therapeutics, Roulston and colleagues disclose a novel, highly potent and selective oral ATR inhibitor, RP-3500 (NCT04497116), with efficacy as a monotherapy and in combination with PARP inhibitors in BRCA and ATM deficient preclinical models. Intermittent dosing of RP-3500 (green squares) maintains efficacy without inducing anemia, a dose-limiting toxicity observed clinically for ATR inhibitors. Furthermore, concomitant intermittent administration of RP-3500 with PARP inhibitors (purple filled triangles) provides greater efficacy and reduced toxicity compared to sequential administration (purple open triangles), providing an opportunity to maximize clinical benefit for this class of anti-cancer agent. Read the full article on page 245.