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Xeritinib (also known as HMPL-005) is an orally bioavailable, potent, and highly selective small molecule inhibitor of the Epidermal Growth Factor Receptor (EGFR) tyrosine kinase. Developed by HUTCHMED (formerly Hutchison Whampoa Pharmaceuticals), xeritinib was designed to target tumors characterized by EGFR overexpression or gene amplification. The drug entered Phase 1 clinical development in China, where it was evaluated in patients with advanced malignant solid tumors, including specific cohorts for esophageal cancer, head and neck squamous cell carcinoma, and non-small cell lung cancer (NSCLC). A primary focus of its development was EGFR-amplified esophageal cancer, a population with significant unmet medical need. While it demonstrated a favorable safety profile and target engagement in early studies, xeritinib is no longer listed in the developer's active clinical pipeline as of 2024.
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