Corticosteroid design for the treatment of asthma: Structural insights and the therapeutic potential of soft corticosteroids

Nicholas Bodor, Peter Buchwald

Research output: Contribution to journalReview article

46 Scopus citations

Abstract

Inhaled and intranasal corticosteroids (ICSs) still are the most effective treatment available for allergic airway diseases and are likely to remain the cornerstone of managing persistent asthma/allergic rhinitis in the foreseeable future. Even if the therapeutic index of this class increased significantly with the introduction of newer corticosteroids, and even if new therapeutic potentials are beginning to emerge with our increasing understanding of the mechanisms of asthma, chronic obstructive pulmonary disease, and rhinitis, corticosteroid development still remains a very important field for drug designers. After a brief review of issues related to the structure-activity relationships of glucocorticoids and the main determinants of their receptor-binding affinity at the glucocorticoid receptor, the main focus of the present article will be on the development of soft corticosteroids, as they are particularly well suited to separate local activity from systemic side effects, which still is an important issue for ICSs. Design consideration required in the search for safe and effective soft drugs on one hand, and safe and effective ICSs on the other hand, will be briefly discussed and illustrated with a number of cases, in particular, with that of loteprednol etabonate and etiprednol dicloacetate, soft corticosteroids that are being developed for a full spectrum of therapeutic applications including asthma and allergic rhinitis.

Original languageEnglish (US)
Pages (from-to)3241-3260
Number of pages20
JournalCurrent pharmaceutical design
Volume12
Issue number25
DOIs
StatePublished - Sep 2006

Keywords

  • Glucocorticoid
  • Itrocinonide
  • Loteprednol etabonate
  • Prednisolone
  • Receptor-binding affinity;
  • Soft Corticosteroid Designs

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology, Toxicology and Pharmaceutics(all)

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