darapladib

Ligand id: 6696

Name: darapladib

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 6
Hydrogen bond donors 1
Rotatable bonds 15
Topological polar surface area 81.19
Molecular weight 667.27
XLogP 10.29
No. Lipinski's rules broken 2

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
This compound was being assessed in a Phase 3 clinical trial (NCT01067339) as a treatment for atherosclerosis, but it failed to meet clinical primary end points [4,6] and GSK has discontinued further development. Phase 2 trial results were published by Mohler et al. in 2008 [2].
Mechanism Of Action and Pharmacodynamic Effects
PLA2-G7 produced by macrophages in atherosclerotic plaques is implicated in the production of pro-inflammatory mediators that promote lesional inflammation and plaque growth and instability [5,8]. Selective PLA2-G7 inhibitors are thought to stabilise arterial plaques [3].