Linked Life Data

19705341

Source:http://linkedlifedata.com/resource/pubmed/id/19705341

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
9
pubmed:dateCreated
2009-8-25
pubmed:abstractText
Anacetrapib, under development by Merck & Co Inc, is an inhibitor of the cholesterol ester transfer protein (CETP) for the treatment of atherosclerosis. By reversibly increasing the affinity of CETP for lipoprotein particles, anacetrapib inhibits CETP-mediated cholesterol exchange, resulting in elevated HDL-cholesterol levels and reductions in LDL-cholesterol levels. In phase I and II clinical trials, anacetrapib was well tolerated and, unlike the now discontinued CETP inhibitor torcetrapib, did not affect blood pressure and aldosterone levels. The impact of anacetrapib on lipoprotein parameters was superior to that of the CETP inhibitors torcetrapib and dalcetrapib. However, while anacetrapib displays promising anti-arteriosclerotic properties, the long-term safety and tolerability of the agent remains to be evaluated. Moreover, the concept that inhibiting CETP is atheroprotective is yet to be proven. The future of CETP inhibitors has also been affected by the failure of torcetrapib, which increased mortality in a phase III trial. Results from an ongoing phase III trial of anacetrapib will determine the likely future development of not only anacetrapib, but of the pharmacological class of CETP inhibitors.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
2040-3429
pubmed:author
pubmed:issnType
Electronic
pubmed:volume
10
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
980-7
pubmed:meshHeading
pubmed-meshheading:19705341-Animals, pubmed-meshheading:19705341-Area Under Curve, pubmed-meshheading:19705341-Atherosclerosis, pubmed-meshheading:19705341-Cholesterol, HDL, pubmed-meshheading:19705341-Cholesterol, LDL, pubmed-meshheading:19705341-Cholesterol Ester Transfer Proteins, pubmed-meshheading:19705341-Clinical Trials as Topic, pubmed-meshheading:19705341-Cross-Over Studies, pubmed-meshheading:19705341-Dose-Response Relationship, Drug, pubmed-meshheading:19705341-Double-Blind Method, pubmed-meshheading:19705341-Humans, pubmed-meshheading:19705341-Inhibitory Concentration 50, pubmed-meshheading:19705341-Molecular Structure, pubmed-meshheading:19705341-Oxazolidinones, pubmed-meshheading:19705341-Randomized Controlled Trials as Topic, pubmed-meshheading:19705341-Structure-Activity Relationship
pubmed:year
2009
pubmed:articleTitle
Anacetrapib, a cholesterol ester transfer protein (CETP) inhibitor for the treatment of atherosclerosis.
pubmed:affiliation
INSERM, Centre de Recherche-Unite Mixte de Recherche 866, Faculté de Médecine, Université de Bourgogne, 21079 Dijon, France. david.masson@chu-dijon.fr
pubmed:publicationType
Journal Article, Review