Antibody-drug conjugates (ADCs) are a unique class of drugs that combine the power of cytotoxic chemotherapy with that of targeted therapy to deliver highly potent cytotoxic agents to cancer cells that express a pre-defined cell surface target. In 2020, trastuzumab deruxtecan became the first FDA-approved ADC for the treatment of non-small cell lung cancer (NSCLC). Since then, two other ADCs have been granted an FDA Breakthrough Therapy Designation in this setting: patritumab deruxtecan and telisotuzumab vedotin. So far none of these ADCs received EMA-approval for the treatment of lung cancer yet. Nonetheless, several early-phase trials are assessing various novel ADCs in patients with advanced lung cancer and have demonstrated promising efficacy. This review provides an overview of the structure and relevant clinical data of ADCs currently under investigation for the treatment of advanced lung cancer.