SYHA1815

SYHA1815 is a novel, orally active small molecule inhibitor that selectively targets the rearranged during transfection (RET) receptor tyrosine kinase. It demonstrates potent inhibition of both wild-type RET and gatekeeper V804 mutant forms with subnanomolar to low nanomolar IC50 values. The drug exhibits approximately 20-fold selectivity for RET over KDR (VEGFR2) and more than 100-fold selectivity over a broad panel of other kinases. Mechanistically, SYHA1815 induces G1 cell-cycle arrest in RET-driven cancer cells by downregulating c-Myc expression, leading to antiproliferative effects. Preclinical studies have shown efficacy against RET-aberrant cancers both in vitro and in vivo, including overcoming resistance mutations such as V804M/L. Developed by Shanghai Runshi Pharmaceutical and CSPC Pharmaceutical Group, it is currently undergoing phase I/II clinical trials for solid tumors in China[1][3][4][5].