CHEMICALS SUMMARY PAGE

Trifluridine:

Summary Information

Classification Chemicals / Complex Chemical Agents / Type:

(This chemicals section is currently predominantly used in Wildpro to link different data types and demonstrate inter-relationships. It does not contain detailed information on the chemical itself.)

Alternative Names
  • 5-trifluoromethyl-2-deoxyuridine. (B135.49.w49)
  • 5-trifluoromethyl-2'-deoxyuridine. (B553.44.w44)
Notes
  • Thymidine analogue, active against DNA viruses (herpesviruses, poxviruses). (B553.44.w44)
  • Active against HSV-1, VZV and some other herpesviruses. (J549.30.w1)
  • This drug is phosphorylated intracellularly to form BVDU 5'-triphosphate.(J549.30.w1)
    • Both the first and second phosphorylation steps are catalysed by viral-encoded proteins (HSV-1 TK, VZV TK), therefore t he drug is specific for these viruses. (J549.30.w1)
  • Inhibits DNA synthesis. (B135.49.w49)
    • BVDU 5'-triphosphate can act as a competitive inhibitor, with respect to the normal substrate of dTTP, of viral DNA polymerase. Alternatively it acts as an alternative substrate, is incorporated into viral DNA and causes reduced DNA integrity and functioning. (J549.30.w1)
  • Inside the host cell it is phosphorylated then incorporated into DNA during synthesis. (B553.44.w44)
    • DNA containing trifluridine is thought to be more susceptible to breakage, and if transcribed results in faulty proteins. (B553.44.w44)
  • Compared with Idoxuridine, higher activity and has a higher affinity for viral rather than mammalian DNA. (B553.44.w44)
  • Not suitable for systemic use due to toxicity. (B553.44.w44)
    • Side effects include leucopaenia, hepatotoxocoity and GIT toxicity. (B553.44.w44)

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