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HJ-002-03 is an orally bioavailable, small molecule tyrosine kinase inhibitor (TKI) developed by Heking Pharmaceutical Technology (Shanghai) Co., Ltd. It is specifically designed to target the epidermal growth factor receptor (EGFR), with potent activity against EGFR exon 20 insertion mutations. These mutations are a distinct class of oncogenic drivers in non-small cell lung cancer (NSCLC) that are typically resistant to first-, second-, and many third-generation EGFR inhibitors. HJ-002-03 functions by irreversibly binding to the ATP-binding site of the mutated EGFR kinase domain, thereby blocking downstream signaling pathways such as MAPK/ERK and PI3K/AKT that promote tumor cell proliferation and survival. The drug is currently undergoing Phase 1 clinical evaluation in patients with advanced solid tumors, particularly those with NSCLC harboring specific EGFR mutations.
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