R&D background and application of selective RET inhibitor platinib (Pujihua)

Pralsetinib is a selective RET (rearranged translocation oncogene) kinase inhibitor, mainly used to treat RET-driven tumors. RETGene rearrangements or mutations account for a certain proportion in non-small cell lung cancer (NSCLC), papillary thyroid cancer and certain other solid tumors, and are important drivers of tumor occurrence and progression. Traditional chemotherapy and non-selective multi-target tyrosine kinase inhibitors (TKI) have limited efficacy against RET driven tumors and have high adverse reactions. Therefore, there is an increasingly urgent need for the development of highly selective RET inhibitors.

Platinib was developed to address the limitations of existing treatments in terms of efficacy and safety. As a third-generation RET inhibitor, Platinib is highly selective and can target tumors driven by RET gene fusions or mutations while reducing non-specific inhibition of other kinases, thereby reducing the risk of adverse reactions. The drug showed good tumor inhibitory activity in preclinical experiments, providing a solid foundation for its entry into clinical trials.

In terms of clinical application, Platinib is mainly used to treat patients with RET fusion-positive non-small cell lung cancer, and patients with RET mutation- or fusion-driven papillary thyroid cancer. Clinical trial data show that platinib can significantly improve the objective response rate (ORR) and progression-free survival (PFS), and also shows efficacy in patients who have relapsed after previously receiving chemotherapy or other targeted drug treatments. Its good tolerability and controllable side effects make it an important treatment option for patients with RET-driven tumors.

In addition, platinib is gradually expanding in market applications. In addition to monotherapy, researchers are also exploring combinations with immunotherapy, chemotherapy and other targeted drugs in order to further improve the efficacy. With the launch and promotion at home and abroad, platinib provides precise and efficient targeted treatment options for patients with RET-driven tumors, providing a new direction for the development of personalized cancer treatment.

Reference link:https://www.drugs.com