GLR203101 / Gan & Lee Pharma - LARVOL DELTA

Discovery of GLR203101, a selective and orally bioavailable PROTAC of SMARCA2 for the treatment of SMARCA4 mutant tumors (AACR 2025) - "Few SMARCA2 selective compounds have entered clinical trials, including PROTAC molecule PRT-3789 administered by intravenous injection in phase 2 clinical trials.Herein, we report the discovery of a selective and orally bioavailable SMARCA2 PROTAC degrader, GLR203101. After 24 hours of oral administration of GLR203101, a robust degradation of SMARCA2 while sparing SMARCA4 was observed in transplanted tumors in the xenograft model. GLR203101 is being evaluated as a preclinical candidate."

Oncology • SMARCA2 • SMARCA4