RGT-490 / Regor - LARVOL DELTA

Discovery and characterization of RGT-490, a mutant selective PI3Kα inhibitor (AACR 2026) - "Clinical use and efficacy of the approved PI3Kα inhibitors alpelisib and inavolisib are limited by the side effects associated with wild-type (WT) PI3Kα inhibition, prominently hyperglycemia, rash, stomatitis and GI toxicities. With potent activity and excellent selectivity, RGT-490 provides opportunity to reduce WT PI3Kα-associated toxicities, enable deeper target coverage and achieve further improved clinical efficacy in PI3Kα mutant patients. RGT-490 phase 1 study is planned 1H2026."

Breast Cancer • Colorectal Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • PIK3CA