Cytochrome P450-activated prodrugs

Future Med Chem. 2013 Feb;5(2):213-28. doi: 10.4155/fmc.12.197.


A prodrug is a compound that has negligible, or lower, activity against a specified pharmacological target than one of its major metabolites. Prodrugs can be used to improve drug delivery or pharmacokinetics, to decrease toxicity, or to target the drug to specific cells or tissues. Ester and phosphate hydrolysis are widely used in prodrug design because of their simplicity, but such approaches are relatively ineffective for targeting drugs to specific sites. The activation of prodrugs by the cytochrome P450 system provides a highly versatile approach to prodrug design that is particularly adaptable for targeting drug activation to the liver, to tumors or to hypoxic tissues.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / metabolism
  • Cytochrome P-450 Enzyme System / metabolism*
  • Drug Delivery Systems* / methods
  • Humans
  • Prodrugs / administration & dosage
  • Prodrugs / chemistry*
  • Prodrugs / metabolism*


  • Antineoplastic Agents
  • Prodrugs
  • Cytochrome P-450 Enzyme System