anacetrapib
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Introduction
Experimental agent. Drug in phase 1 trials.
Indications
- dyslipidemia, hypercholesterolemia
- anacetrapib may reduce risk of cardiovascular events in patients with atherosclerosis on intensive atorvastatin therapy[3]
Dosage
Mechanism of action
- inhibition of cholesteryl ester transfer protein (CETP)
- increases HDL 130% (300 mg)
- decrease LDL 40% (300 mg)
- no change in blood pressure
Clinical trials
- mean LDL cholesterol decrease from 81 to 45 mg/dL vs 82 to 77 mg/dL with placebo
- mean HDL cholesterol increase from 41 to 101 mg/dL vs 40 to 46 mg/dL with placebo
- no benefit in terms of cardiovascular events or mortality within trial window of 18 months
Notes
- Merck announced it will not seek regulatory approval for anacetrapib after disappointing trial results[4]
More general terms
References
- ↑ Krishna R et al, Effect of the cholesteryl ester transfer protein inhibitor, anacetrapib, on lipoproteins in patients with dyslipidaemia and on 24-h ambulatory blood pressure in healthy individuals: Two double-blind, randomised placebo-controlled phast I studies. Lancet 2007, 370:1907 PMID: https://www.ncbi.nlm.nih.gov/pubmed/18068514
- ↑ Physician' First Watch, Nov 18, 2010 Massachusetts Medical Society http://www.jwatch.org
Cannon CP et al Safety of Anacetrapib in Patients with or at High Risk for Coronary Heart Disease N Engl J Med November 17, 2010 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/21082868 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1009744 - ↑ 3.0 3.1 The HPS3/TIMI55-REVEAL Collaborative Group. Effects of anacetrapib in patients with atherosclerotic vascular disease. N Engl J Med 2017 Aug 29; <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/28847206 <Internet> http://www.nejm.org/doi/10.1056/NEJMoa1706444
- ↑ 4.0 4.1 Wendling P Merck Abandons Plans to Pursue Anacetrapib Medscape - Oct 12, 2017. https://www.medscape.com/viewarticle/886953