Owing to the devastating impacts of cancer, scientists are working hard to create innovative delivery methods and new medications that target distinct pathways to deliver anticancer medicines to their intended targets without endangering healthy cells. The kind, location, and stage of cancer will all affect how well treatment works. Many approaches are employed in cancer therapy, such as hormone therapy, radiation, immunotherapy, chemotherapy, and surgery. Chemotherapy is widely acknowledged as the primary option for the complete elimination of cancer cells, but the cancer cells become resistant to the effects of chemotherapy and manage to evade them. Novel developments in the field of drug discovery utilizing protein engineering chemistry with computer simulations and natural products can be utilized to improve the basic understanding of various routes to treat various malignancies. It also aids in the comprehension of enzymes, their function, and the mechanisms underlying the therapy of various cancer kinds. There is a diversity of drugs that target interdisciplinary pathways to overcome cancer such as inhibitors of Topo II enzyme, intercalators of DNA, inhibitors of VEGFR-2, EGFR inhibitors, and dual EGFR/VEGFR-2 inhibitors.