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Antimetabolites are drugs that inhibit the formation and/or utilization of crucial metabolites. The term 'antimetabolite' is usually used to refer to cytotoxic agents that interfere with DNA and RNA synthesis via inhibiting crucial enzymes involved in the formation of nucleic acids (namely thymidine and purines).[1] They include:[1]

  • Purine/pyrimidine antagonists which 'look like' purines and pyrimidines and hence competitively inhibit the enzymes purines/pyrimidines require in order to be synthesized and incorporated into DNA/RNA. Examples include azathioprine, cladribine, clofarabine, mercaptopurine, tioguanine, etc.
  • Antifolates like aminopterin, methotrexate, pemetrexed and raltitrexed that inhibit tetrahydrofolate synthesis from dihydrofolate, a folate metabolite.
  • Miscellaneous enzyme inhibitors like hydroxycarbamide and mycophenolates.

External linksEdit

Reference listEdit

  1. 1.0 1.1 Brunton, LL; Chabner, BA; Knollmann, BC, ed. (2010). "Chapter 61. Cytotoxic Agents". Goodman & Gilman's Pharmacological Basis of Therapeutics (12th ed.). New York, USA: McGraw-Hill Professional. ISBN 978-0-07-162442-8. 

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