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). They include:
- 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.
- NCBI Bookshelf provides free book resources on this topic.
- PubMed provides review articles from the past five years (limit to free review articles or to systematic reviews)
- The TRIP database provides clinical publications about evidence-based medicine.
- ↑ 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.