Recent advances in retrometabolic drug design (RMDD) and development

Nicholas Bodor, P. Buchwald

Research output: Contribution to journalReview articlepeer-review

12 Scopus citations


As a general review for the 7th Retrometabolism-Based Drug Design and Targeting Conference, recent developments within this field are briefly reviewed with various illustrative examples from different therapeutic areas. Retrometabolic drug design incorporates two major systematic approaches: the design of soft drugs and of chemical delivery systems (CDS). Both aim to design new, safe drugs with an improved therapeutic index by integrating structure-activity and structure-metabolism relationships; however, they achieve it by different means: whereas soft drugs 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.

Original languageEnglish (US)
Pages (from-to)395-403
Number of pages9
Issue number6
StatePublished - Jun 1 2010

ASJC Scopus subject areas

  • Pharmaceutical Science


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