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Disitamab vedotin + pertuzumab is a combination therapy under clinical investigation for the treatment of HER2-positive cancers, particularly breast cancer. Disitamab vedotin is an antibody-drug conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2); it consists of a monoclonal antibody with high binding affinity for HER2, conjugated via a cathepsin-cleavable valine-citrulline linker to monomethyl auristatin E (MMAE), a potent microtubule inhibitor that induces cell death upon internalization and cleavage in tumor cells[2][4][8]. Pertuzumab is a humanized monoclonal antibody that binds to a distinct epitope (subdomain II) of the HER2 receptor, inhibiting HER2 heterodimerization with other HER family receptors and downstream signaling, as well as promoting antibody-dependent cellular cytotoxicity (ADCC)[6]. This dual HER2 blockade is designed to synergistically suppress HER2-driven signaling and enhance antitumor activity[3][9].
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