Darapladib

Darapladib

Systematic (IUPAC) name
N-(2-diethylaminoethyl)-2-[2-[(4-fluorophenyl)methylsulfanyl]-4-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamide
Clinical data
Pregnancy cat.	?
Legal status	?
Identifiers
CAS number	356057-34-6^Y
ATC code	None
PubChem	CID 9939609
UNII	UI1U1MYH09^Y
Chemical data
Formula	C₃₆H₃₈F₄N₄O₂S
Mol. mass	666.77 g/mol
SMILES	eMolecules & PubChem
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Darapladib is a drug used to inhibit lipoprotein-associated phospholipase A2 (lp-PLA2).

As of March 2008^[update], it is being studied as a possible add-on treatment for atherosclerosis.^[1]^[2]^[3]^[4]

References

^ Serruys, PW; et al. (2008). "Effects of the direct lipoprotein-associated phospholipase A(2) inhibitor darapladib on human coronary atherosclerotic plaque". Circulation 118 (11): 1172–1182. doi:10.1161/CIRCULATIONAHA.108.771899. PMID 18765397.
^ Mohler, ER 3rd; et al. (Apr 2008). "The effect of darapladib on plasma lipoprotein-associated phospholipase A2 activity and cardiovascular biomarkers in patients with stable coronary heart disease or coronary heart disease risk equivalent: the results of a multicenter, randomized, double-blind, placebo-controlled study". Journal of the American College of Cardiology 51 (17): 1632–41. doi:10.1016/j.jacc.2007.11.079. PMID 18436114.
^ Mohler, ER 3rd; et al (2008). "Treating Residual Cardiovascular RiskWill Lipoprotein-Associated Phospholipase A2 Inhibition Live Up to Its Promise?". J Am Coll Cardiol 51 (17): 1642–1644. doi:10.1016/j.jacc.2008.02.025. PMID 18436115.
^ Wilensky, RL; et al (2008). "Inhibition of lipoprotein-associated phospholipase A2 reduces complex coronary atherosclerotic plaque development". Nat Med 14 (1015–1016): 1059–66. doi:10.1038/nm.1870. PMC 2885134. PMID 18806801. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2885134.