Retrometabolic drug design: Principles and recent developments

Nicholas Bodor, Peter Buchwald

Research output: Contribution to journalArticlepeer-review

16 Scopus citations


Retrometabolic drug design incorporates two major systematic approaches: the design of soft drugs (SDs) and of chemical delivery systems (CDSs). Both aim to design new, safe drugs with an improved therapeutic index by integrating structure-activity and -metabolism relationships; however, they achieve it by different means: whereas SDs are new, active therapeutic agents that undergo predictable metabolism to inactive metabolites after exerting their desired therapeutic effect, CDSs are biologically inert molecules that provide enhanced and targeted delivery of an active drug to a particular organ or site through a designed sequential metabolism that involves several steps. General principles and recent developments are briefly reviewed with various illustrative examples from different therapeutic areas with special focus on soft corticosteroids and on brain targeting.

Original languageEnglish (US)
Pages (from-to)1669-1682
Number of pages14
JournalPure and Applied Chemistry
Issue number8
StatePublished - Aug 2008


  • Brain targeting
  • Drug design
  • Hydrolysis
  • Metabolism
  • Oxime

ASJC Scopus subject areas

  • Chemical Engineering(all)
  • Chemistry(all)


Dive into the research topics of 'Retrometabolic drug design: Principles and recent developments'. Together they form a unique fingerprint.

Cite this