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MPS-216 is an orally bioavailable small molecule inhibitor of the MET (Hepatocyte Growth Factor Receptor) tyrosine kinase. Discovered by Nerviano Medical Sciences and developed by Fondazione Ricerca Traslazionale (FoRT), it was primarily investigated for the treatment of advanced non-small cell lung cancer (NSCLC), particularly in patients whose tumors exhibit MET amplification or mutations. MET signaling is a known driver of oncogenesis and resistance to EGFR inhibitors in NSCLC. MPS-216 aims to block the autophosphorylation of MET and its downstream signaling pathways, thereby inhibiting tumor cell proliferation and survival. Clinical development reached Phase I/II but was terminated in 2016.
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