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ERAS-601 is an investigational, orally administered small molecule inhibitor targeting Src homology region 2 domain-containing phosphatase-2 (SHP2). SHP2 is a key oncogenic tyrosine phosphatase that transduces receptor tyrosine kinase signaling in the RAS/MAPK pathway via regulation of guanine nucleotide exchange factors. By inhibiting SHP2, ERAS-601 aims to disrupt multiple cancer-driving processes, particularly in tumors dependent on RAS/MAPK signaling. The drug is being developed by Erasca and was originally licensed from NiKang Therapeutics. It has been evaluated as monotherapy and in combination with cetuximab (an EGFR inhibitor) for advanced solid tumors, including chordoma and other cancers such as colorectal cancer, head and neck cancer, non-small-cell lung cancer, squamous cell carcinoma, pancreatic cancer, gastric cancer, rectal cancer, and duodenal cancers[4][3][7]. Early clinical data suggest promising antitumor activity with manageable safety profiles[3][6].
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