抗体药物复合物（ADCs）正处于癌症领域药物开发革命的前沿。由抗体、连接分子和细胞毒性药物（"载体"）三个主要组成部分组成，ADCs具有将细胞毒性药物传递给表达特定抗原的细胞的独特能力，这是传统化疗方法所不能及的一大进步，传统化疗方法具有广泛的非特异性作用。可以使用多种药物载体，包括最常用的微管抑制剂（auristatins和maytansinoids），以及拓扑异构酶抑制剂和烷基化剂。最后，连接分子在ADCs的效果中起着关键作用，作为可切割部分，连接分子对特异位点激活和旁观杀伤效应产生影响，这一点在常常表达多种抗原的实体瘤中尤为重要。虽然ADCs最初用于血液恶性肿瘤，但它们已证明在多种实体肿瘤恶性肿瘤中具有实用性，包括乳腺癌、胃肠道肿瘤、肺癌、宫颈癌、卵巢癌和尿路上皮肿瘤。目前，有六种ADCs获得FDA批准用于固体肿瘤的治疗：ado-trastuzumab emtansine和trastuzumab deruxtecan，两者都是抗HER2的；enfortumab-vedotin，瞄准nectin-4；sacituzuzmab govitecan，瞄准Trop2；tisotumab vedotin，瞄准组织因子；和mirvetuximab soravtansine，瞄准叶酸受体-α。尽管它们展示了实用性和可耐受的安全性概况，由于肿瘤细胞发生进化以避免表达特定的目标抗原，ADCs可能会变得无效。此外，当前ADCs的成本可能限制了其应用范围。在这里，我们回顾了ADCs的结构和功能，以及正在进行的有关新型ADCs的临床研究和其作为固体恶性肿瘤治疗的潜力。

Antibody-drug conjugates (ADCs) are at the forefront of the drug development revolution occurring in oncology. Formed from three main components-an antibody, a linker molecule, and a cytotoxic agent ("payload"), ADCs have the unique ability to deliver cytotoxic agents to cells expressing a specific antigen, a great leap forward from traditional chemotherapeutic approaches that cause widespread effects without specificity. A variety of payloads can be used, including most frequently microtubular inhibitors (auristatins and maytansinoids), as well as topoisomerase inhibitors and alkylating agents. Finally, linkers play a critical role in the ADCs' effect, as cleavable moieties that serve as linkers impact site-specific activation as well as bystander killing effects, an upshot that is especially important in solid tumors that often express a variety of antigens. While ADCs were initially used in hematologic malignancies, their utility has been demonstrated in multiple solid tumor malignancies, including breast, gastrointestinal, lung, cervical, ovarian, and urothelial cancers. Currently, six ADCs are FDA-approved for the treatment of solid tumors: ado-trastuzumab emtansine and trastuzumab deruxtecan, both anti-HER2; enfortumab-vedotin, targeting nectin-4; sacituzuzmab govitecan, targeting Trop2; tisotumab vedotin, targeting tissue factor; and mirvetuximab soravtansine, targeting folate receptor-alpha. Although they demonstrate utility and tolerable safety profiles, ADCs may become ineffective as tumor cells undergo evolution to avoid expressing the specific antigen being targeted. Furthermore, the current cost of ADCs can be limiting their reach. Here, we review the structure and functions of ADCs, as well as ongoing clinical investigations into novel ADCs and their potential as treatments of solid malignancies.