PMID- 22970904
OWN - NLM
STAT- MEDLINE
DCOM- 20130129
LR  - 20220330
IS  - 1744-7666 (Electronic)
IS  - 1465-6566 (Linking)
VI  - 13
IP  - 15
DP  - 2012 Oct
TI  - Icatibant , the bradykinin B2 receptor antagonist with target to the 
      interconnected kinin systems.
PG  - 2233-47
LID - 10.1517/14656566.2012.723692 [doi]
AB  - INTRODUCTION: HOE-140/ Icatibant is a selective, competitive antagonist to 
      bradykinin (BK) against its binding to the kinin B2 receptor. Substitution of 
      five non-proteogeneic amino acid analogues makes icatibant resistant to 
      degradation by metalloproteases of kinin catabolism. Icatibant has clinical 
      applications in inflammatory and vascular leakage conditions caused by an acute 
      (non-controlled) production of kinins and their accumulation at the endothelium 
      B2 receptor. The clinical manifestation of vascular leakage, called angioedema 
      (AE), is characterized by edematous attacks of subcutaneous and submucosal 
      tissues, which can cause painful intestinal consequences, and life-threatening 
      complications if affecting the larynx. Icatibant is registered for the treatment 
      of acute attacks of the hereditary BK-mediated AE, i.e., AE due to C1 inhibitor 
      deficiency. AREAS COVERED: This review discusses emerging knowledge on the kinin 
      system: kinin pharmacological properties, biochemical characteristics of the 
      contact phase and kinin catabolism proteases. It underlines the responsibility of 
      the kinins in AE initiation and the potency of icatibant to inhibit AE formation 
      by kinin-receptor interactions. EXPERT OPINION: Icatibant antagonist properties 
      protect BK-mediated AE patients against severe attacks, and could be developed 
      for use in inflammatory conditions. More studies are required to confirm whether 
      or not prolonged and frequent applications of icatibant could result in the 
      impairment of the cardioprotective effect of BK.
FAU - Charignon, Delphine
AU  - Charignon D
AD  - Universite Joseph Fourier Grenoble 1, GREPI/AGIM CNRS-UJF FRE 3405 and Centre de 
      Reference des Angioedemes CREAK, CHU Grenoble POBox 217, F-38043 Grenoble, 
      France.
FAU - Spath, Peter
AU  - Spath P
FAU - Martin, Ludovic
AU  - Martin L
FAU - Drouet, Christian
AU  - Drouet C
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
DEP - 20120913
PL  - England
TA  - Expert Opin Pharmacother
JT  - Expert opinion on pharmacotherapy
JID - 100897346
RN  - 0 (Anti-Inflammatory Agents, Non-Steroidal)
RN  - 0 (Bradykinin B2 Receptor Antagonists)
RN  - 0 (Kinins)
RN  - 7PG89G35Q7 (icatibant)
RN  - S8TIM42R2W (Bradykinin)
SB  - IM
MH  - Angioedema/*drug therapy/metabolism
MH  - Animals
MH  - Anti-Inflammatory Agents, Non-Steroidal/pharmacology/*therapeutic use
MH  - Bradykinin/*analogs & derivatives/pharmacology/therapeutic use
MH  - *Bradykinin B2 Receptor Antagonists
MH  - Humans
MH  - Kinins/metabolism
EDAT- 2012/09/14 06:00
MHDA- 2013/01/30 06:00
CRDT- 2012/09/14 06:00
PHST- 2012/09/14 06:00 [entrez]
PHST- 2012/09/14 06:00 [pubmed]
PHST- 2013/01/30 06:00 [medline]
AID - 10.1517/14656566.2012.723692 [doi]
PST - ppublish
SO  - Expert Opin Pharmacother. 2012 Oct;13(15):2233-47. doi: 
      10.1517/14656566.2012.723692. Epub 2012 Sep 13.