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SPH5030 is an orally bioavailable, selective, and irreversible small molecule inhibitor of the receptor tyrosine kinase human epidermal growth factor receptor 2 (HER2; also known as ERBB2). It was developed using a molecular hybridization strategy to optimize selectivity and potency against both wild-type and mutant forms of HER2. Compared to other irreversible HER2 inhibitors like neratinib and pyrotinib, SPH5030 demonstrates higher selectivity for HER2 with reduced off-target effects. Preclinical studies showed potent antitumor activity in models harboring common HER2 mutations. Clinically, it is being evaluated for the treatment of advanced solid tumors that overexpress or harbor mutations in HER2, including biliary cancer and colorectal cancer[1][3][4][5][6][7].
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