Over the years, various technological advancements, such as antibody engineering for site-specific conjugation and enhanced pharmacokinetic and pharmacodynamic properties, have paved the way for antibody drug conjugates (ADCs) to be recognized as potent therapies targeting a wide range of indications, including solid tumors and hematological malignancies. ADCs are engineered therapeutics comprised of monoclonal antibodies attached to potent cytotoxic payloads through chemical linkers. In fact, the FDA has approved 11 ADCs, namely ado-trastuzumab emtansine (Kadcyla®), brentuximab vedotin (Adcetris®), inotuzumab ozogamicin (Besponsa®), gemtuzumab ozogamicin (Mylotarg®), moxetumomab pasudotox (Lumoxiti®), polatuzumab vedotin-piiq (Polivy®), enfortumab vedotin (Padcev®), sacituzumab govitecan (Trodelvy®), trastuzumab deruxtecan (Enhertu®), belantamab mafodotin-blmf (Blenrep®), and loncastuximab tesirine-lpyl (Zynlonta™) till date. The success of these therapeutics can be attributed to their high tumor selectivity and cell-killing potential of monoclonal antibodies, while limiting off target toxicities. These advantages have made ADCs a new frontier of chemotherapy, thus, bringing about a paradigm shift in the treatment protocol of different types of cancer.