Eicosanoids pp 195-204 | Cite as

Leukotriene Synthesis (FLAP) Inhibition: Biochemistry and Pharmacology of Bay X 1005

  • R. Müller-Peddinghaus
  • R. Kast
Part of the NATO ASI Series book series (NSSA, volume 283)


Leukotrienes have been recognized as mediators of inflammatory allergic diseases of the lung (22). Consequently, antileukotriene therapy appears to be nearly established as novel pharmacotherapy of allergic asthma (15, 31). Cysteinyl-leukotrienes (LTC4, LTD4, LTE4) appear to have considerable pathophysiological importance in allergie asthma, because functional lung parameters improve with antileukotriene therapy after LTD4 challenge, antigen provocation, cold air exposure, exercise-induced asthma, and even aspirin-induced asthma (22, 24, 46). Effective antileukotriene therapy comprises various LTD4 receptor antagonists (LTD4ra) and 5-lipoxygenase (5-LOX) inhibitors (15, 22). 5-LOX inhibitors can be differentiated into the direct 5-LOX inhibitors (LOI) and FLAP (Five Lipoxygenase Activating Protein) binding leukotriene synthesis inhibitors (LSI) (Figure 1).


LTB4 Receptor Human PMNL LTD4 Receptor Antagonist Antileukotriene Therapy Five Lipoxygenase Activate Protein 
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Copyright information

© Springer Science+Business Media New York 1996

Authors and Affiliations

  • R. Müller-Peddinghaus
    • 1
  • R. Kast
    • 1
  1. 1.Cardiovascular and Arteriosclerosis ResearchBayer AGWuppertalGermany

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