Sichuan Huiyu Pharmaceutical Co., Ltd (SHA: 688553), a China-based pharmaceutical company, has announced that the National Medical Products Administration (NMPA) has accepted a clinical trial filing for its Category 1 investigational drug, HYP-2090PTSA. This small molecule drug candidate targets KRAS G12C and PI3K and is under review for potential use in treating advanced solid tumors with the KRAS G12C mutation, including non-small cell lung cancer (NSCLC), colorectal cancer, and pancreatic cancer.
Preclinical Studies Highlight Synergistic Effects and Resistance Overcoming
Preclinical studies have demonstrated that HYP-2090PTSA can simultaneously inhibit both KRAS G12C and PI3K, effectively blocking the downstream signaling pathways mediated by these targets. This dual inhibition approach achieves synergistic effects and has the potential to overcome drug resistance. In vitro study results indicate that HYP-2090PTSA maintains significant anti-proliferative activity against tumor cell lines that have developed both primary and acquired resistance to sotorasib and adagrasib, which are KRAS G12C inhibitors already listed abroad. Furthermore, HYP-2090PTSA’s monotherapy effect is significantly superior to the combination of KRAS G12C inhibitors and PI3K inhibitors.
In Vivo Studies Show Promise in Overcoming Resistance
Animal models from in vivo pharmacodynamic studies have shown that HYP-2090PTSA has significant potential to overcome drug resistance in multiple mouse models that are resistant to both sotorasib and adagrasib. This indicates that HYP-2090PTSA could offer a new treatment option for patients with advanced solid tumors who have not responded to existing KRAS G12C inhibitors.-Fineline Info & Tech
