Archives of Pharmacal Research

, Volume 25, Issue 2, pp 111–136

Prodrug and antedrug: Two diametrical approaches in designing safer drugs

  • Henry J. Lee
  • John S. Cooperwood
  • Zhengqing You
  • Dong-Hoon Ko
Research Articles Review

DOI: 10.1007/BF02976552

Cite this article as:
Lee, H.J., Cooperwood, J.S., You, Z. et al. Arch Pharm Res (2002) 25: 111. doi:10.1007/BF02976552

Abstract

The prodrug and antedrug concepts, which were developed to overcome the physical and pharmacological shortcomings of various therapeutic classes of agents, employ diametrically different metabolic transformations. The prodrug undergoes a predictable metabolic activation prior to exhibiting its pharmacological effects in a target tissue while the antedrug undergoes metabolic deactivation in the systemic circulation upon leaving a target tissue. An increased therapeutic index is the aspiration for both approaches in designing as well as evaluation criteria. The recent research endeavors of prodrugs include the gene-directed and antibodydirected enzymatic activation of a molecule in a targeted tissue, organ specific delivery, improved bioavailabilities of nucleosides and cellular penetration of nucleotides. As for antedrugs, emphasis in research has been based upon the design and synthesis of systemically inactive molecule by incorporating a metabolically labile functional group into an active molecule.

Key words

ProdrugAntedrugPro-AntedrugAnti-inflammationAsthmaGene-directed enzyme/prodrugAntibody-directed enzyme/prodrugNucleoside prodrugNucleotide prodrug

Copyright information

© The Pharmaceutical Society of Korea 2002

Authors and Affiliations

  • Henry J. Lee
    • 1
  • John S. Cooperwood
    • 1
  • Zhengqing You
    • 1
  • Dong-Hoon Ko
    • 1
  1. 1.College of Pharmacy and Pharmaceutical SciencesFlorida A&M UniversityTallahasseeUSA
  2. 2.College of Pharmacy and Pharmaceutical SciencesFlorida A&M UniversityTallahasseeUSA