Antibody-drug conjugates (ADCs) are a promising class of cancer therapies that combine monoclonal antibodies with cytotoxic drugs, offering targeted treatment with reduced toxicity. This review summarizes the clinical efficacy and safety of FDA-approved ADCs in human cancers. As of now, 13 ADCs have received FDA approval, with over 100 in clinical trials. ADCs are composed of three main components: a monoclonal antibody, a linker, and a cytotoxic drug. The antibody targets cancer cells, allowing the drug to be delivered specifically to the tumor, minimizing damage to healthy cells. Several ADCs have shown significant efficacy in treating various cancers. Gemtuzumab ozogamicin (GO) is the first FDA-approved ADC, used for acute myeloid leukemia (AML). Despite initial safety concerns, it was later reapproved at a lower dose. Brentuximab vedotin (BV) targets CD30-positive cancers, including Hodgkin lymphoma and anaplastic large cell lymphoma, and has shown good efficacy and safety. Trastuzumab emtansine (T-DM1) is effective in HER2-positive breast cancer, with improved outcomes compared to traditional therapies. Inotuzumab ozogamicin (InO) is used for acute lymphoblastic leukemia (ALL), showing high response rates and improved survival. Moxetumomab pasudotox (MP) is approved for hairy cell leukemia, and polatuzumab vedotin (PV) is used for diffuse large B-cell lymphoma. Enfortumab vedotin (EV) targets Nectin-4 in bladder cancer, showing promising results. Trastuzumab deruxtecan (T-DXd) is effective in HER2-positive breast cancer, with improved outcomes. Sacituzumab govitecan (SG) is used for metastatic triple-negative breast cancer and bladder cancer. Disitamab vedotin (RC48) is approved for gastric cancer and has shown efficacy in combination with immunotherapy. Loncastuximab tesirine (LT) is used for lymphomas, and tisotumab vedotin (TV) is effective in cervical cancer. Mirvetuximab soravtansin (MIRV) is used for ovarian cancer. Despite their benefits, ADCs still face challenges, including off-target toxicity and the need for further research to optimize their use. Future studies aim to improve the safety and efficacy of ADCs, making them more effective and accessible for cancer patients.Antibody-drug conjugates (ADCs) are a promising class of cancer therapies that combine monoclonal antibodies with cytotoxic drugs, offering targeted treatment with reduced toxicity. This review summarizes the clinical efficacy and safety of FDA-approved ADCs in human cancers. As of now, 13 ADCs have received FDA approval, with over 100 in clinical trials. ADCs are composed of three main components: a monoclonal antibody, a linker, and a cytotoxic drug. The antibody targets cancer cells, allowing the drug to be delivered specifically to the tumor, minimizing damage to healthy cells. Several ADCs have shown significant efficacy in treating various cancers. Gemtuzumab ozogamicin (GO) is the first FDA-approved ADC, used for acute myeloid leukemia (AML). Despite initial safety concerns, it was later reapproved at a lower dose. Brentuximab vedotin (BV) targets CD30-positive cancers, including Hodgkin lymphoma and anaplastic large cell lymphoma, and has shown good efficacy and safety. Trastuzumab emtansine (T-DM1) is effective in HER2-positive breast cancer, with improved outcomes compared to traditional therapies. Inotuzumab ozogamicin (InO) is used for acute lymphoblastic leukemia (ALL), showing high response rates and improved survival. Moxetumomab pasudotox (MP) is approved for hairy cell leukemia, and polatuzumab vedotin (PV) is used for diffuse large B-cell lymphoma. Enfortumab vedotin (EV) targets Nectin-4 in bladder cancer, showing promising results. Trastuzumab deruxtecan (T-DXd) is effective in HER2-positive breast cancer, with improved outcomes. Sacituzumab govitecan (SG) is used for metastatic triple-negative breast cancer and bladder cancer. Disitamab vedotin (RC48) is approved for gastric cancer and has shown efficacy in combination with immunotherapy. Loncastuximab tesirine (LT) is used for lymphomas, and tisotumab vedotin (TV) is effective in cervical cancer. Mirvetuximab soravtansin (MIRV) is used for ovarian cancer. Despite their benefits, ADCs still face challenges, including off-target toxicity and the need for further research to optimize their use. Future studies aim to improve the safety and efficacy of ADCs, making them more effective and accessible for cancer patients.