HER2-targeted antibody-drug conjugates

HER2-targeted antibody-drug conjugates (HER2-ADCs) are a class of cancer therapeutics that combine monoclonal antibodies targeting human epidermal growth factor receptor 2 (HER2) with potent cytotoxic payloads connected by specialized linkers. These drugs work by binding to HER2 receptors overexpressed on cancer cell surfaces, triggering internalization of the ADC-HER2 complex. Inside the cell, the payload is released through linker cleavage, causing cell death through various mechanisms depending on the specific payload (such as microtubule inhibition or DNA damage). Some HER2-ADCs also demonstrate bystander effects, affecting neighboring cancer cells with lower HER2 expression. This class includes approved drugs like trastuzumab emtansine (T-DM1) and trastuzumab deruxtecan (T-DXd), as well as investigational agents like disitamab vedotin (RC48) and trastuzumab duocarmazine (SYD985).

Other names

HER2-ADCHER-2-ADCHER 2-ADCanti-HER2 antibody-drug conjugatesanti-HER-2 antibody-drug conjugatesanti-HER 2 antibody-drug conjugates