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Selective next-generation RET inhibitor
APS03118 is a second generation selective RET inhibitor independently developed by APS. Preclinical data indicated that APS03118 is RET highly selective and scarcely influence on other targets. APS03118 shows remarkable potency against various RET fusion and mutations at the nanomolar level including gatekeeper V804 and solvent frontier G810 mutation that induces the resistance of the first generation of selective RET inhibitors. Dose-dependent antitumor activity and well tolerability of APS03118 were observed in mice models, especially in mice intracranial tumor model with complete regression of brain tumor and 100% mice survival.


                                                                           Physiological an Oncogenic Acdtivation of RET Kinase 

Selective next-generation RET inhibitor(图1)

                                                                     Oncogenic activation of RET occurs via two genetic mechanisms:

                                                               somatic RET fusion, somatic and germline RET mutations

                                                                                                2020. Carcinogenesis

                                                         Resistance Mechanism of Selective RET Inhibitors 

Selective next-generation RET inhibitor(图2)

Selective next-generation RET inhibitor(图3)

                                                                              RET solvent front mutation RET G810R/S/C/V block 

                                                                     the binding of first generation RET inhibitors 

                                                                                               2020 . J Thorac Oncol ; 2020. NACLC


APS03118 has therapeutic potential for RET altered cancers not limited by tumor type. RET fusion and rearrangement occur in approximately 1-2% of NSCLC patients , particularly in young, non-smoking lung adenocarcinoma patients with an incidence of up to 7-17%. RET mutations are detected in 90% of medullary thyroid cancers and RET fusion in 10-20% of thyroid cancer. In addition, less than 1% of other solid tumors such as pleural mesothelioma, colorectal cancer, esophageal cancer, breast cancer, pancreatic cancer, and pancreatic cancer are driven by  RET aberration. About 70,000 to 80,000 patients worldwide with advanced solid tumors can benefit from monotherapy with RET inhibitors according to 2019 global data. RET inhibitors also have shown synergy with other targeted therapies, such as RET mutations after resistance to EGFR inhibitors, and becomes the optimal choice for unresponsive and refractory RET positive patients.



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