Darapladib.

Abstract

IMPORTANCE OF THE FIELD:

Atherosclerosis is an inflammatory-immune mediated disease process. Plaque rupture is responsible for the clinical events of ischemic death, myocardial infarction, acute coronary syndromes and ischemic strokes. Lipoprotein-associated phospholipase A(2) (Lp-PLA(2)) seems to play a major role in the development of such high-risk lesions, in both the coronary and carotid arteries. Darapladib is a selective inhibitor of Lp-PLA(2).

AREAS COVERED IN THIS REVIEW:

An overview of darapladib by reviewing the studies (1990 - 2009) that have provided the rationale for the development of darapladib; and a discussion of its potential merit as a new therapeutic drug to target high-risk atherosclerosis.

WHAT THE READER WILL GAIN:

The reader should gain an understanding of the importance of inflammation during atherogenesis as well as of the biology of Lp-PLA(2) and its proatherogenic role. Additional insights will be gained into the role of selective inhibitors of Lp-PLA(2) as new therapeutic agents.

TAKE HOME MESSAGE:

Darapladib is a selective inhibitor of Lp-PLA(2) and represents a new class of therapeutic agents that target inflammation to treat high-risk atherosclerosis.

• Authors: Quang T Bui, Robert L Wilensky
• Journal: Expert opinion on investigational drugs (Expert Opin Investig Drugs) Vol. 19 Issue 1 Pg. 161-8 (Jan 2010) ISSN: 1744-7658 [Electronic] England
• PMID: 20001561 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Anti-Inflammatory Agents, Non-Steroidal
• Benzaldehydes
• Oximes
• 1-Alkyl-2-acetylglycerophosphocholine Esterase
• darapladib

Topics

• 1-Alkyl-2-acetylglycerophosphocholine Esterase (antagonists & inhibitors)
• Anti-Inflammatory Agents, Non-Steroidal (administration & dosage, adverse effects, pharmacology, therapeutic use)
• Atherosclerosis (drug therapy, enzymology)
• Benzaldehydes (administration & dosage, adverse effects, pharmacology, therapeutic use)
• Clinical Trials as Topic
• Drug Discovery
• Humans
• Molecular Structure
• Oximes (administration & dosage, adverse effects, pharmacology, therapeutic use)