C5a receptor antagonists for the treatment of inflammation

Curr Opin Investig Drugs. 2004 May;5(5):505-10.


The anaphylatoxin C5a is a classic, potent inflammatory mediator, with biological activities that have been implicated in a variety of diseases. As a result of two decades of study, C5a receptor antagonists that prevent high-affinity binding of C5a to its receptor have been discovered, which show therapeutic effects in various inflammatory disease models. Moreover, the involvement of C5a in disease models has been demonstrated in various experiments using C5/C5a receptor-deficient mice and anti-C5/C5a antibodies. It is therefore anticipated that these antagonists will have potential as novel anti-inflammatory therapeutics.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology*
  • Anti-Inflammatory Agents / therapeutic use
  • Complement C5a / metabolism
  • Disease Models, Animal
  • Drug Design
  • Humans
  • Inflammation / drug therapy
  • Inflammation / metabolism
  • Receptor, Anaphylatoxin C5a / antagonists & inhibitors*
  • Receptor, Anaphylatoxin C5a / metabolism
  • Structure-Activity Relationship


  • Anti-Inflammatory Agents
  • Receptor, Anaphylatoxin C5a
  • Complement C5a