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

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Eicosanoids

Part of the book series: NATO ASI Series ((NSSA,volume 283))

Abstract

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).

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  1. Cardiovascular and Arteriosclerosis Research, Bayer AG, Aprather Weg 18a, D-42096, Wuppertal, Germany

    R. Müller-Peddinghaus & R. Kast

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  1. Institute of Pharmacological Sciences, University of Milan, Milan, Italy

    Gian Carlo Folco

  2. Karolinska Institute, Stockholm, Sweden

    Bengt Samuelsson

  3. Hôpital Lariboisére, Paris, France

    Jacques Maclouf

  4. University of Verona Medical School, Verona, Italy

    G. P. Velo

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Müller-Peddinghaus, R., Kast, R. (1996). Leukotriene Synthesis (FLAP) Inhibition: Biochemistry and Pharmacology of Bay X 1005. In: Folco, G.C., Samuelsson, B., Maclouf, J., Velo, G.P. (eds) Eicosanoids. NATO ASI Series, vol 283. Springer, Boston, MA. https://doi.org/10.1007/978-1-4899-0200-9_18

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