GenSci145 / GeneScience - LARVOL DELTA

A phase I/II study of GenSci145 as monotherapy or combination therapy in PIK3CA-mutated advanced solid tumors (ESMO 2026) - No abstract available

Combination therapy • Metastases • Monotherapy • P1/2 data • Oncology • Solid Tumor • PIK3CA

GenSci145 as Monotherapy or in Combination Therapy, in Participants With PIK3CA-mutated, Locally Advanced or Metastatic Solid Tumors. (clinicaltrials.gov) - P1 | N=186 | Recruiting | Sponsor: Changchun GeneScience Pharmaceutical Co., Ltd. | Not yet recruiting ➔ Recruiting

Enrollment open • Monotherapy • Breast Cancer • Colorectal Cancer • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • ER • HER-2 • PGR • PIK3CA

GenSci145: A mutant selective PI3Kα inhibitor overcoming brain metastasis treatment barriers (AACR 2026) - "It significantly inhibited proliferation (T47D IC50: 120.6 nM, selectivity 28.6-fold) and pAKT signaling (IC50: 67.5 nM, selectivity 11.3-fold) in mutant cells, with no significant effects on other PI3K subtypes or off-target kinases.In in-vivo experiments, GenSci145 showed dose-dependent anti-tumor effects in HR-positive, HER2-negative breast cancer CDX/PDX models, with significant synergy when combined with fulvestrant...For intracranial tumors, the CFB was 4.78 at 25 mg/kg and 1.71 at 100 mg/kg, which was superior to STX-478 (100 mg/kg, CFB=9.56)... GenSci145 is a highly selective PI3Kα mutant inhibitor that mechanistically avoids the metabolic side effects of traditional inhibitors. Preclinical studies have shown significant anti-tumor effects in various PIK3CA mutant tumor models, with excellent blood-brain barrier penetration and effective inhibition of brain metastases. Overall, GenSci145 is expected to overcome the clinical limitations of existing PI3Kα..."

Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • HER-2 • PIK3CA

GenSci145 as Monotherapy or in Combination Therapy, in Participants With PIK3CA-mutated, Locally Advanced or Metastatic Solid Tumors. (clinicaltrials.gov) - P1 | N=186 | Not yet recruiting | Sponsor: Changchun GeneScience Pharmaceutical Co., Ltd.

Monotherapy • New P1 trial • Breast Cancer • Colorectal Cancer • Solid Tumor • ER • HER-2 • PGR • PIK3CA