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ZV0203 is a first-in-class antibody-drug conjugate (ADC) that utilizes a biosimilar of pertuzumab as its targeting antibody, directed against HER2-positive tumor cells. The ADC is constructed with a microtubule inhibitor payload, DUO5 (a Dolastatin 10 derivative), attached via a stable and protease-cleavable valine-citrulline linker. ZV0203 specifically binds to the domain II of the HER2 receptor, blocking both homodimerization and heterodimerization with other members of the EGFR family (HER2/EGFR, HER2/HER3, HER2/HER4). Preclinical studies demonstrated superior antitumor activity compared to Kadcyla (ado-trastuzumab emtansine) in multiple xenograft models without noticeable toxicity. In phase 1 clinical trials for patients with advanced solid tumors overexpressing HER2, ZV0203 showed manageable safety and encouraging antitumor activity in heavily pretreated patients[1][4][5]. The drug is administered intravenously every three weeks.
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