Anticancer drug, any drug that is effective in the treatment of malignant, or cancerous, disease. There are several major classes of anticancer drugs; these include alkylating agents, antimetabolites, natural products, and hormones. In addition, there are a number of drugs that do not fall within those classes but that demonstrate anticancer activity and thus are used in the treatment of malignant disease. The term chemotherapy frequently is equated with the use of anticancer drugs, although it more accurately refers to the use of chemical compounds to treat disease generally.
Conventional cytotoxic agents — Appropriate dosing for cytotoxic anticancer agents has been largely determined from prospective and retrospective studies in which the goal was to maximize efficacy and minimize toxicity. The starting dose for conventional cytotoxic agents in phase I studies has generally been based on animal studies, where doses are usually escalated until the LD10 is reached (the dose that results in lethality in 10 percent of the treated animals). By convention, in human phase I studies, the first dose employed has been one-tenth of the LD10.
Based on the theory and intuitive belief that larger patients have a larger volume of distribution and a higher metabolizing capacity, it has been assumed that they require more drug to induce the same effects. In an attempt to minimize interindividual variation, dosing for most anticancer agents has generally been normalized using mg of drug per m2 of body surface area (BSA), which is calculated using a patient's height and weight.