This review article is focused on the drug delivery platforms and cancer treatment systems recently developed based on molybdenum disulfide (MoS₂) nanosheets. Two-dimensional MoS₂ can be used as a therapeutic nanoparticle and tissue engineering scaffold for tumor healing. Structure, different synthesis methods, unique properties, and surface modification approaches of MoS₂ as a newly emerging carrier for a wide range of drugs were comprehensively discussed. Numerous examples of drug delivery systems based on these carriers were introduced, and their key characteristics and highlights were compared in tables. Striking features in the two-dimensional nanostructure state like the high degree of anisotropy, mechanical strength, biocompatibility, large surface area, availability of surface modification methods for enhanced functionality, distinctive band gap structure, high absorbance in the near-infrared region, and remarkable magnetic attributes render MoS₂ an ideal and attractive candidate to develop multifunctional platforms for combined chemotherapy and photothermal therapy as well as biosensing and bioimaging applications. These properties have piqued the interest of many researchers and led them to study the versatile biomedical applications of these materials, particularly drug delivery and photothermal therapy. Finally, the opportunities, remaining challenges, and future prospects ahead in this area were mapped out.