Sichuan Huiyu Pharmaceutical Co., Ltd (SHA: 688553), a China-based pharmaceutical company, has announced that it has received clinical trial approval from the National Medical Products Administration (NMPA) for its investigational drug HYP2090PTSA. This small molecule KRAS G12C/PI3K inhibitor is intended for the treatment of advanced solid tumors with KRAS G12C mutation, including non-small cell lung cancer, colorectal cancer, and pancreatic cancer.
Preclinical Studies and Synergistic Effects
Preclinical studies have demonstrated that HYP2090PTSA, a Category 1 chemical drug, can simultaneously inhibit both KRAS G12C and PI3K, achieving synergistic effects and potentially overcoming drug resistance. In vitro results indicate that HYP-2090PTSA maintains significant anti-proliferative activity against tumor cell lines that have developed primary and acquired resistance to marketed KRAS G12C inhibitors sotorasib and adarasib. Moreover, the monotherapy effect of HYP-2090PTSA is significantly superior to the combination of KRAS G12C inhibitors and PI3K inhibitors.
In Vivo Pharmacodynamics and Overcoming Drug Resistance
Animal models have shown that HYP-2090PTSA has significant potential to overcome drug resistance in multiple mouse models that are resistant to both sotorasib and adarasib. This suggests that HYP2090PTSA may offer a new therapeutic option for patients with advanced solid tumors who have not responded to or have developed resistance to existing treatments.
Conclusion
The approval to proceed with clinical trials is a significant step forward for Sichuan Huiyu Pharmaceutical as it seeks to develop HYP2090PTSA as a novel treatment for patients with KRAS G12C mutated tumors. The drug’s ability to overcome resistance and its synergistic effects in preclinical studies position it as a promising candidate in the fight against advanced solid tumors.-Fineline Info & Tech
