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EP-0146 is a potent and highly selective small molecule inhibitor of the RET (Rearranged during Transfection) tyrosine kinase, developed by Easton Biopharmaceuticals. It is designed to target oncogenic RET alterations, including chromosomal rearrangements (fusions) and point mutations, which are key drivers in various cancers such as non-small cell lung cancer (NSCLC) and medullary thyroid cancer (MTC). By inhibiting RET kinase activity, EP-0146 blocks downstream signaling pathways, such as MAPK/ERK and PI3K/AKT, that promote tumor cell proliferation and survival. The drug is currently being evaluated in Phase 1 clinical trials for patients with advanced solid tumors harboring RET gene alterations.
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