GSC002639 / GeneScience - LARVOL DELTA

GSC002639, a brain penetrating and mutant-selective PI3Kα inhibitor, exhibits potent mono- and combination therapy against PI3CA mutant tumors (AACR 2025) - "Our study also revealed a notable observation: In an HR-positive and HER2-negative PI3Kα H1047X CDX model, the combination of GSC002639 with Fulvestrant exhibited greater efficacy than the combinations of either Alpelisib or Inavolisib with Fulvestrant. In this report, we present the identification and characterization of GSC002639, a selective inhibitor targeting the PI3Kα H1047X mutation. GSC002639 demonstrates high specificity, the ability to cross the blood-brain barrier, and robust in vivo efficacy, while avoiding the insulin elevation. The promising pharmacokinetic and toxicological profiles of GSC002639 suggest its potential as a safe and effective cancer therapy."

Combination therapy • Breast Cancer • Colorectal Cancer • Endometrial Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor • HER-2 • PIK3CA • PIK3CB • PIK3CD • PIK3CG