Background and aims <p>Trophoblast cell-surface antigen 2 (TROP2) is a cell surface glycoprotein that plays a significant role in the self-renewal, proliferation, invasion and transformation of tumor cells, and is highly expressed in a variety of tumors. At present, TROP2 has become an important target for the research and development of Antibody-drug conjugates (ADCs) in the field of lung cancer. Although sacituzumab govitecan, datopotamab deruxtecan and sacituzumab tirumotecan are all TROP2-targeted ADCs, there are certain differences in their drug structures. These differences may have led to the distinctions in their anti-tumor activity and safety. This study aims to review the similarities and differences among these three drugs, with the expectation of providing some assistance for the selection of clinical medication.</p> Methods <p>The key words Sacituzumab govitecan/IMMU-132, Datopotamab deruxtecan/DS-1062a and Sacituzumab tirumotecan/SKB264 retrieved Medline/PubMed, Google Scholar, Web of Science and ScienceDirect databases until September 25, 2025. Articles about pharmacokinetics, pharmacodynamics, drug safety and other aspects were selected to systematically summarize.</p> Results <p>These three TROP2 ADCs have many similarities in terms of pharmacokinetics, pharmacodynamics and common treatment-related adverse events. However, there are some differences in the efficacy of combination with immunotherapy drugs and treatment-related adverse events over grade 3.</p> Conclusion <p>There are differences in pharmacological effects, efficacy, and incidence of adverse events among sacituzumab govitecan, datopotamab deruxtecan, and sacituzumab tirumotecan. For patients with EGFR-mutated progression after targeted therapy or driver gene negative advanced non-small cell lung cancer, the individualized optimization of TROP2 ADCs treatment can obtain the greatest benefit.</p>