A drug conjugate consists of a cytotoxic drug bound via a linker to a targeted ligand, allowing the targeted delivery of the drug to one or more tumor sites. This approach simultaneously reduces drug toxicity and increases efficacy, with a powerful combination of efficient killing and precise targeting. Antibody‒drug conjugates (ADCs) are the best-known type of drug conjugate, combining the specificity of antibodies with the cytotoxicity of chemotherapeutic drugs to reduce adverse reactions by preferentially targeting the payload to the tumor. The structure of ADCs has also provided inspiration for the development of additional drug conjugates. In recent years, drug conjugates such as ADCs, peptide‒drug conjugates (PDCs) and radionuclide drug conjugates (RDCs) have been approved by the Food and Drug Administration (FDA). The scope and application of drug conjugates have been expanding, including combination therapy and precise drug delivery, and a variety of new conjugation technology concepts have emerged. Additionally, new conjugation technology-based drugs have been developed in industry. In addition to chemotherapy, targeted therapy and immunotherapy, drug conjugate therapy has undergone continuous development and made significant progress in treating lung cancer in recent years, offering a promising strategy for the treatment of this disease. In this review, we discuss recent advances in the use of drug conjugates for lung cancer treatment, including structure-based drug design, mechanisms of action, clinical trials, and side effects. Furthermore, challenges, potential approaches and future prospects are presented.

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用于治疗肺癌的药物偶联物：从药物发现到临床实践

药物缀合物由通过接头与靶向配体结合的细胞毒性药物组成，允许将药物靶向递送至一个或多个肿瘤位点。这种方法同时降低了药物毒性并提高了疗效，将高效杀伤和精确靶向相结合。抗体药物偶联物（ADC）是最知名的药物偶联物类型，它将抗体的特异性与化疗药物的细胞毒性相结合，通过优先将有效负载靶向肿瘤来减少不良反应。ADC 的结构也为其他药物缀合物的开发提供了灵感。近年来，ADC、肽药物偶联物（PDC）和放射性核素药物偶联物（RDC）等药物偶联物已获得美国食品药品监督管理局（FDA）的批准。药物偶联物的范围和应用不断扩大，包括联合治疗和精准药物递送，并且出现了多种新的偶联技术概念。此外，工业界还开发了基于新结合技术的药物。除化疗、靶向治疗和免疫治疗外，药物结合疗法近年来在肺癌治疗方面不断发展并取得了显着进展，为肺癌的治疗提供了一种有前景的策略。在这篇综述中，我们讨论了使用药物缀合物治疗肺癌的最新进展，包括基于结构的药物设计、作用机制、临床试验和副作用。此外，还提出了挑战、潜在方法和未来前景。