The drug methotrexate (right) is an antimetabolite that interferes with the metabolism of folic acid (left).

An antimetabolite is a chemical that inhibits the use of a metabolite, which is another chemical that is part of normal metabolism.[1] Such substances are often similar in structure to the metabolite that they interfere with, such as the antifolates that interfere with the use of folic acid. The presence of antimetabolites can have toxic effects on cells, such as halting cell growth and cell division, so these compounds are used as chemotherapy for cancer.[2]



Cancer treatment

Antimetabolites can be used in cancer treatment,[3] as they interfere with DNA production and therefore cell division and the growth of tumors. Because cancer cells spend more time dividing than other cells, inhibiting cell division harms tumor cells more than other cells.

Anti-metabolites masquerade as a purine (azathioprine, mercaptopurine) or a pyrimidine, chemicals that become the building-blocks of DNA. They prevent these substances becoming incorporated in to DNA during the S phase (of the cell cycle), stopping normal development and division.[4]

They also affect RNA synthesis. However, because thymidine is used in DNA but not in RNA (where uracil is used instead), inhibition of thymidine synthesis via thymidylate synthase selectively inhibits DNA synthesis over RNA synthesis.

Due to their efficiency, these drugs are the most widely used cytostatics.

In the ATC system, they are classified under L01B.


Antimetabolites may also be antibiotics, such as sulfanilamide drugs, which inhibit dihydrofolate synthesis in bacteria by competing with para-aminobenzoic acid.[5]


Main representatives of these drugs are:

See also


  1. ^ Smith, A. L. (1997). Oxford dictionary of biochemistry and molecular biology. Oxford [Oxfordshire]: Oxford University Press. pp. 43. ISBN 0-19-854768-4. 
  2. ^ Peters GJ, van der Wilt CL, van Moorsel CJ, Kroep JR, Bergman AM, Ackland SP (2000). "Basis for effective combination cancer chemotherapy with antimetabolites". Pharmacol. Ther. 87 (2–3): 227–53. doi:10.1016/S0163-7258(00)00086-3. PMID 11008002. 
  3. ^ MeSH Antineoplastic+Antimetabolites
  4. ^ Takimoto CH, Calvo E. "Principles of Oncologic Pharmacotherapy" in Pazdur R, Wagman LD, Camphausen KA, Hoskins WJ (Eds) Cancer Management: A Multidisciplinary Approach. 11 ed. 2008.
  5. ^ "The Organic Chemistry of Drug Design and Drug Action" (2nd edition), R. B. Silverman, 2004.

External links

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Look at other dictionaries:

  • antimétabolite — ● antimétabolite nom masculin Chimiothérapie anticancéreuse. ⇒ANTIMÉTABOLITE, subst. masc. MÉD. ,,Substance entravant le métabolisme. En particulier, médicament (...) s opposant à certaines réactions chimiques intracellulaires et par conséquent à …   Encyclopédie Universelle

  • Antimetabolite — sind chemische Verbindungen, die natürlichen Metaboliten in ihrer chemischen Struktur ähneln, aber dessen Stoffwechselweg hemmen (Inhibitor). Ergebnis ist eine Störung der normalen Enzymfunktion in einem Stoffwechselweg oder biologischen Prozess …   Deutsch Wikipedia

  • antimetabolite — [an΄tī mə tab′ə līt΄; an΄tēmə tab′ə līt΄, an΄timə tab′ə līt΄] n. a drug or biochemical that inhibits a metabolic process by competing with a similarly shaped metabolite for a particular enzyme …   English World dictionary

  • antimetabolite — /an tee meuh tab euh luyt , an tuy /, n. 1. Biochem. any substance that interferes with growth of an organism by competing with or substituting for an essential nutrient in an enzymatic process. adj. 2. Pharm. of or pertaining to certain… …   Universalium

  • Antimétabolite — Un antimétabolite est une substance chimique qui empêche l utilisation d un métabolite, qui est un autre produit chimique qui fait partie du métabolisme normal. Ces substances sont souvent similaires dans leur structure à celle du métabolite avec …   Wikipédia en Français

  • antimetabolite — antimetabolitas statusas T sritis chemija apibrėžtis Biologiškai aktyvus junginys, inhibuojantis metabolizmo fermentus. atitikmenys: angl. antimetabolite rus. антиметаболит …   Chemijos terminų aiškinamasis žodynas

  • antimetabolite — antimetabolitas statusas T sritis ekologija ir aplinkotyra apibrėžtis Gamtinis ar sintetinis biologiškai aktyvus junginys (pvz., metatreksatas, merkaptopurinas, gemcitabinas), pakeičiantis metabolitus biocheminėse reakcijose, trikdantis medžiagų… …   Ekologijos terminų aiškinamasis žodynas

  • antimetabolite — noun Date: 1945 a substance that replaces or inhibits an organism s utilization of a metabolite …   New Collegiate Dictionary

  • antimetabolite — n. [Gr. anti, against; metabole, change] Any compound that interferes with normal cellular metabolism …   Dictionary of invertebrate zoology

  • antimetabolite — (an tī mē tab o laīt) A compound that blocks metabolic pathway function by competitively inhibiting a key enzyme s use of a metabolite because it closely resembles the normal enzyme substrate …   Dictionary of microbiology

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