HSK40118

HSK40118 is an investigational small molecule PROTAC (Proteolysis Targeting Chimera) designed to target and degrade the epidermal growth factor receptor (EGFR). Developed by Haisco Pharmaceutical Group, it is being evaluated as an oral therapy for patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring EGFR mutations. Unlike traditional EGFR inhibitors that block the receptor's activity, HSK40118 induces degradation of the EGFR protein itself via recruitment of E3 ubiquitin ligase, leveraging the cell’s natural proteasome system. This approach aims to overcome resistance mechanisms associated with conventional tyrosine kinase inhibitors by eliminating both wild-type and mutant forms of EGFR. As of June 2025, HSK40118 is in phase 1 clinical trials assessing its safety, tolerability, pharmacokinetics/pharmacodynamics, and preliminary efficacy in NSCLC patients who have progressed on prior EGFR-targeted therapies[1][2][6][7][9].