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anacetrapib
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:
- 100 mg QD
- 10-300 mg PO QHS
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]
Interactions
drug adverse effects of anti-hyperlipidemic agents
General
cholesteryl ester transfer protein (CETP) inhibitor
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: 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
PMID: 21082868
http://www.nejm.org/doi/full/10.1056/NEJMoa1009744
- The HPS3/TIMI55-REVEAL Collaborative Group.
Effects of anacetrapib in patients with atherosclerotic vascular
disease.
N Engl J Med 2017 Aug 29;
PMID: 28847206
http://www.nejm.org/doi/10.1056/NEJMoa1706444
- Wendling P
Merck Abandons Plans to Pursue Anacetrapib
Medscape - Oct 12, 2017.
https://www.medscape.com/viewarticle/886953