ABSTRACT: Among the non-communicable diseases (NCDs) cancer is a major global health burden with low survival rate. According to WHO’s Globocan-2018 report, the developing countries of Africa and Asia are contributing more to 7 million new cases and 6 million figures of death due to non-availability of targeted and affordable treatment. The selective targeting of biological targets in cancerous cells or tissue is a crucial criterion for successful treatment of cancer. The continuous findings in the area anticancer therapeutic development have been provided variety of potential targets such as receptors, proteins, enzymes, nucleic acids etc. which are present in cancer cells. Here, we provided detail on different biological targets and their biological role in cancer. Additionally, some clinically used as well as novel molecular agent acting on these anticancer targets have been included along with updation. This paper will be helpful in the target specific design and development of novel anticancer therapeutics.