2024年2月8日 · A DNA-encoded library screen leveraging electron microscopy-optimized constructs, differential enrichment, and an orthosteric-blocking compound led to the identification of RLY-2608, a first-in-class allosteric mutant-selective inhibitor of PI3Kα.

2024年5月29日 · RLY-2608, a novel, oral allosteric PI3Kα inhibitor, is designed to overcome these limitations via mutant- and isoform-selective PI3Kα inhibition for greater target coverage, improved tolerability, and anti-tumor activity.

RLY-2608 achieves maximum efficacy in both kinase and helical domain PIK3CA mutant in vivo xenograft models with significantly reduced elevation of insulin levels compared to orthosteric inhibitors

RLY-2608 is a first-in-class PI3Kα inhibitor that demonstrates mutant-selective efficacy in the clinic. These features have the potential to improve outcomes in patients with PIK3CA-mutant tumors, in monotherapy, and in combination with other targeted therapies.

• RLY-2608 is a first-in-class allosteric mutant-selective PI3Kα inhibitor. • RLY- 2608 potently inhibits aberrant PI3Kα signaling driven by expression of PIK3CA H1047R and restores gene expression to a physiological non-disease state in endothelial cells.

RLY-2608 is an oral, mutant-selective PI3Kα allosteric inhibitor discovered by Relay Therapeutics that targets a cryptic pocket near the ATP-binding site.

2024年9月9日 · RLY-2608 is the lead program in Relay Therapeutics’ efforts to discover and develop mutant selective inhibitors of PI3Kα, the most frequently mutated kinase in all cancers, with oncogenic mutations detected in about 14% of patients with solid tumors.

multi-center, dose escalation/expansion study of RLY-2608 monotherapy includes adult pts with advanced solid tumors who are refractory or intolerant to, or have declined, standard therapy.

2022年6月2日 · RLY-2608, a novel oral allosteric PI3Kα inhibitor, is uniquely designed to overcome these limitations via mutant- and isoform-selective PI3Kα inhibition for greater target coverage, improved tolerability and antitumor activity.

RLY-2608 works by targeting and blocking a protein called PI3K, which promotes cancer growth and spread in people with a PIK3CA mutation. RLY-2608 is a capsule that is taken orally (by mouth). Fulvestrant is a standard hormonal treatment for certain types of breast cancer and is given by injection. Who Can Join