PH050 / Suzhou Puhe Pharma - LARVOL DELTA

MAT2A inhibition enhances the anti-tumor efficacy of combined pan-RAS(ON) and PRMT5 inhibition in MTAP-deficient pancreatic tumors (AACRPanCa 2026) - "Here we present the discovery of a highly brain-penetrant and potent MAT2A inhibitor, PH050, and report that its combination with PH033, a molecular glue pan-RAS(ON) inhibitor with tumor-enriched distribution properties, enhanced the anti-tumor activity.Objective&Comprehensive in vitro and in vivo PD studies have been conducted to demonstrate the potency of PH050, and combination effect of PH050 with PH033, with or without PRMT5MTA inhibitor (MRTX1719). PH050 is a potent, selective and brain penetrant MAT2A inhibitor. The preclinical studies indicate that the combination of PH050 and pan-RAS(ON) inhibitor (with or without PRMT5MTA inhibitor) has the potential to exert profound and durable therapeutic benefit in patients with MTAP-deleted pancreatic cancer.Citation Format:Bin Liu, Lu Li, Yulai Zhang, Changhong Jia, Shuang Wang, Lu Chang, Yulun Wu, Zhizhong Li, Amy Guan, Yongqi Guo. MAT2A inhibition enhances the anti-tumor efficacy of combined pan-RAS(ON) and PRMT5..."

Clinical • Idiopathic Arthritis • Oncology • Pancreatic Cancer • Solid Tumor • Targeted Protein Degradation • MAT2A • MTAP