Cancer is one of the leading causes of death in developed countries, responsible for about 25% of all deaths. On a yearly basis, 0.5% of the population is diagnosed with cancer. Treatment options include surgery, radiotherapy, and systemic therapies such as chemotherapy, endocrine therapy, and targeted agents. Conventional chemotherapeutical agents act by creating toxic effects on all dividing cells. The toxic by-products of some chemotherapeutic drugs are deposited mainly in the liver producing hepatotoxicity, leading to many side-effects like loss of appetite, nausea, vomiting, diarrhea, abdominal cramps and constipation, anemia, fatigue, hyperthermia, loss of hair, etc. In this review update, the benefits and problems of chemotherapy have been highlighted and the mechanisms involved in cancer formation, groups of chemotherapeutic agents, as well as method of chemotherapeutic administration, have been discussed