Peptidoleukotriene Antagonists State of the Art

Abstract

Peptidoleukotrienes (LTC₄, LTD₄, and LTE₄) have been proposed as important mediators of asthma. Twenty years of research in the field of peptidoleukotriene (pLT) antagonists have generated a number of biologically active compounds from different structural classes. Several drugs have been or are currently in clinical trials. The first generation peptidoleukotriene antagonists (e.g. FPL 55712) showed disappointing results in asthmatic patients, due to insufficient potency. However, new classes of highly potent antagonists (e.g. ICI 204219) are proving successfull in clinical trials in asthma patients. Thus, peptidoleukotriene antagonists may represent a new principle in asthma therapy. In this paper, the in vitro potency and clinical data of different classes of peptidoleukotriene antagonists are reviewed.