ABSTRACT: Cancer is one of the deadliest diseases and poses a risk to people all over the world. Surgery, chemo, and radiation therapy have been the only options available until today to combat this major problem. Chemotherapeutic drugs have been used for treatment for more than 50 years. Unfortunately, these drugs have inherent cytotoxicities and tumor cells have started inducing resistance against these drugs. Other common techniques such as surgery and radiotherapy have their own drawbacks. Therefore, such techniques are incompetent tools to alleviate the disease efficiently without any adverse effects. This scenario has inspired researchers to develop alternative techniques with enhanced therapeutic effects and minimal side effects. Such techniques include targeted therapy, liposomal therapy, hormonal therapy, and immunotherapy, etc. However, these therapies are expensive and not effective enough. Furthermore, researchers have conjugated therapeutic agents or drugs with different molecules, delivery vectors, and/or imaging modalities to combat such problems and enhance the therapeutic effect. This conjugation technique has led to the development of bioconjugation therapy, in which at least one molecule is of biological origin. These bioconjugates are the new therapeutic strategies, having prospective synergistic antitumor effects and have potency to overcome the complications being produced by chemo drugs. Herein, we provide an overview of various bioconjugates developed so far, as well as their classification, characteristics, and targeting approach for cancer. Additionally, the most popular nanostructures based on their organic or inorganic origin (metallic, magnetic, polymeric nanoparticles, dendrimers, and silica nanoparticles) characterized as nanocarriers are also discussed. Moreover, we hope that this review will provide inspiration for researchers to develop better bioconjugates as therapeutic agents.