SY-5007

SY-5007 is a potent, highly selective, small-molecule inhibitor of the RET (Rearranged during Transfection) tyrosine kinase, developed by Shouyao Holdings (Beijing) Co., Ltd. It is designed to target oncogenic RET alterations, including chromosomal rearrangements (fusions) and point mutations, which are key drivers in several malignancies. The drug is primarily being developed for the treatment of RET-fusion positive non-small cell lung cancer (NSCLC), medullary thyroid cancer (MTC) harboring RET mutations, and RET-fusion positive papillary thyroid cancer (PTC). By inhibiting the RET kinase activity, SY-5007 blocks downstream signaling cascades such as the MAPK/ERK and PI3K/AKT pathways, thereby suppressing tumor cell proliferation and survival. It is administered orally and has demonstrated promising antitumor activity in preclinical models and early-phase clinical trials.