Drug targeting via retrometabolic approaches

Nicholas Bodor, Peter Buchwald

Research output: Contribution to journalReview articlepeer-review

63 Scopus citations


Retrometabolic approaches incorporate targeting and metabolic considerations into the drug design process and represent a novel, systematic methodology for the design of safe, localized compounds. Two major design concepts aimed to increase the therapeutic index of drugs were developed. Chemical delivery systems allow targeting of active biological molecules to specific target sites or organs, based on predictable enzymatic activation. Soft drug approaches are used to design new drugs by building in the molecule, in addition to the activity, the most desired way in which the molecule is to be deactivated and detoxified subsequent to exerting its biological effects. Many examples are provided; related computer programs are also briefly discussed.

Original languageEnglish (US)
Pages (from-to)1-27
Number of pages27
JournalPharmacology and Therapeutics
Issue number1-3
StatePublished - Nov 1997
Externally publishedYes


  • Brain targeting
  • Eye targeting
  • Molecular packaging
  • Peptide delivery
  • Soft β-blockers
  • Soft anticholinergics

ASJC Scopus subject areas

  • Pharmacology


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