The emergence of potent and selective peptide leukotriene receptor antagonists.
Leukotriene (LT) C4, LTD4 and LTE4 collectively comprise the constituents of slow reacting substance of anaphylaxis. Based on their well-documented physiology, and a substantial body of circumstantial evidence, it has been hypothesized that they may be etiologic in allergic diseases, including asthma. Using various chemical approaches, a variety of chemically distinct, highly potent and selective LT antagonists have been disclosed including SKF 104,353, ICI 198,615, L 660,711 and WY 48,252. All are, or will soon, enter clinical trials for asthma. These compounds should provide a viable test for the hypothesis that LTs are etiologic in asthma. The complexity of the disease suggests that clinical expectations for these compounds, or any single entity, should be moderate.
Krell
R D
RD
Department of Pharmacology, ICI Pharmaceuticals Group, Division of ICI Americas Inc., Wilmington, DE 19897.
D000818:Animals; D001249:Asthma / Q000188:drug therapy / Q000503:physiopathology; D006801:Humans; D015289:Leukotrienes / Q000502:physiology*; D010455:Peptides / Q000494:pharmacology*; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors*; D018077:Receptors, Leukotriene
D015289:Leukotrienes; D010455:Peptides; D011971:Receptors, Immunologic; D018077:Receptors, Leukotriene