23. Leukotrienes

  1. Kenji Izuhara MD, PhD2,
  2. Stephen T. Holgate MD, DSc, FMedSci3 and
  3. Marsha Wills-Karp PhD4
  1. Katsuhide Okunishi MD, PhD and
  2. Marc Peters-Golden MD

Published Online: 27 JUL 2011

DOI: 10.1002/9781444346688.ch23

Inflammation and Allergy Drug Design

Inflammation and Allergy Drug Design

How to Cite

Okunishi, K. and Peters-Golden, M. (2011) Leukotrienes, in Inflammation and Allergy Drug Design (eds K. Izuhara, S. T. Holgate and M. Wills-Karp), Wiley-Blackwell, Oxford, UK. doi: 10.1002/9781444346688.ch23

Editor Information

  1. 2

    Department of Biomolecular Sciences, Division of Medical Biochemistry, Saga Medical School, Nabeshima, Saga, Japan

  2. 3

    School of Medicine, Allergy and Inflammation Research, Southampton General Hospital, University Medicine, Southampton, UK

  3. 4

    Division of Immunology, Cincinnati Children's Medical Center, Cincinnati, OH, USA

Author Information

  1. Division of Pulmonary and Critical Care Medicine, Department of Internal Medicine, University of Michigan Health System, Ann Arbor, MI, USA

Publication History

  1. Published Online: 27 JUL 2011
  2. Published Print: 13 AUG 2011

ISBN Information

Print ISBN: 9781444330144

Online ISBN: 9781444346688



  • leukotrienes, potent lipid mediators - multiple aspects of asthma pathophysiology;
  • airway inflammation - central feature of asthma;
  • leukotriene biosynthesis, triggered by stimuli - as antigens, cytokines, immune complexes;
  • factors, influencing output - of leukotriene biosynthetic pathway;
  • leukotriene receptor expression - in cell types, actions of cysLTs and LTB4;
  • CysLT1, more being known - than any other cysLT receptor, on immune-competent cells and structural cells;
  • CysLT2, co-expressed with CysLT1 - in cell types, endothelium, eosinophils, mast cells and macrophages;
  • antileukotriene drugs - currently, three CysLT1 receptor antagonists;
  • optimizing antileukotriene therapy - targets within leukotriene pathway, new drug development;
  • LTRAs and Churg–Strauss syndrome – rare, life-threatening granulomatous and eosinophilic vasculitis


Leukotrienes (LTs) are lipid mediators that contribute to many aspects of asthma pathogenesis. As the LT pathway is relatively steroid-resistant, its blockade by alternative strategies is a desirable component of asthma management. Cysteinyl LT receptor 1 antagonists have been utilized worldwide for more than 10 years, and while their efficacy in asthma is well accepted, their limitations are also evident. In this chapter, we summarize the biologic effects of LTs in asthma, review recent advances in LT receptors, and consider possible new therapeutic targets in the LT pathway that offer the potential to achieve better control of asthma in the future.