Preclinical Toxicology of Antimetabolite Drugs Used in Cancer Therapy – Literary Review

Abstract

This paper discusses the preclinical toxicology of some of the most commonly used antimetabolite drugs in cancer therapies, from their history up to their current use. The classes of antimetabolite drugs included in this discussion are purine antagonists, pyrimidine antagonists, folic acid antagonists, thymidylate synthase (TS) inhibitors, and phosphoribosylglycinamide formyltransferase (GARFT) inhibitors. These classes of drugs were designed to disrupt the synthesis of DNA, halt the cell cycle, and prevent the further growth of tumours. Purine antagonists used in cancer therapy include mercaptopurine, fludarabine, cladribine, clofarabine, nelarabine, and thioguanine. Their action is to compete with their respective purine analogues for incorporation into DNA synthesis.