New Life of Topoisomerase I Inhibitors as Antibody-Drug Conjugate Warheads

拓扑异构酶I抑制剂作为抗体药物偶联物弹头的新用途

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Abstract

Antibody-drug conjugates (ADC) allow the delivery of cytotoxic chemotherapeutic agents to tumors. Two ADC delivering topoisomerase I (TOP1) poisons (Enhertu and Trodelvy) have recently been FDA-approved for Her2- and Trop2-expressing solid tumors. In a recent study, a TOP1-anti B7-H4 ADC was described and shown to be synergistic with a novel PARP1-selective inhibitor. See related article by Kinneer et al., p. 1086.

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