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SHR-A1201 is an antibody-drug conjugate (ADC) designed for the treatment of HER2-positive cancers, particularly advanced or metastatic breast cancer. It consists of a humanized anti-HER2 monoclonal antibody (trastuzumab, IgG1) chemically linked via a lysine-SMCC linker to DM1 (maytansine), a potent microtubule inhibitor. The ADC specifically targets HER2-expressing tumor cells, where it binds to the HER2 antigen on the cell surface, is internalized, and releases DM1 intracellularly to inhibit microtubule polymerization and induce cell death. SHR-A1201 has demonstrated safety and tolerability in phase I clinical trials with encouraging antitumor activity in heavily pretreated patients with advanced HER2-positive breast cancer[1][3][5]. The drug exhibits pharmacokinetic properties typical of ADCs and shows dose-proportional exposure over tested ranges[8].
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