Soft drug design: General principles and recent applications

Nicholas Bodor, Peter Buchwald

Research output: Contribution to journalReview articlepeer-review

196 Scopus citations


Soft drug design represents a new approach aimed to design safer drugs with an increased therapeutic index by integrating metabolism considerations into the drug design process. Soft drugs are new therapeutic agents that undergo predictable metabolism to inactive metabolites after exerting their therapeutic effect. Hence, they are obtained by building into the molecule, in addition to the activity, the most desired way in which the molecule is to be deactivated and detoxified. In an attempt to systematize and summarize the related work done in a number of laboratories, including ours, the present review presents an overview of the general soft drug design principles and provides a variety of specific examples to illustrate the concepts. A number of already marketed drugs, such as esmolol, remifentanil, or loteprednol etabonate, resulted from the successful application of such design principles. Many other promising drug candidates are currently under investigation in a variety of fields including possible soft antimicrobials, anticholinergics, corticosteroids, β-blockers, analgetics, ACE inhibitors, antiarrhythmics, and others. Whenever possible, pharmacokinetic and pharmacodynamic properties are briefly summarized and compared to those of other compounds used in the same field.

Original languageEnglish (US)
Pages (from-to)58-101
Number of pages44
JournalMedicinal Research Reviews
Issue number1
StatePublished - Jan 14 2000
Externally publishedYes


  • Ester hydrolysis
  • Loteprednol etabonate
  • Metabolism
  • Soft β-blockers
  • Soft drugs

ASJC Scopus subject areas

  • Organic Chemistry
  • Pharmacology
  • Medicine(all)


Dive into the research topics of 'Soft drug design: General principles and recent applications'. Together they form a unique fingerprint.

Cite this