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|Molar mass||637.51 g·mol−1|
|Except where noted otherwise, data are given for materials in their standard state (at 25 °C (77 °F), 100 kPa)|
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At the 16th International Symposium on Drugs Affecting Lipid Metabolism (New York, Oct 4-7, 2007), Merck reported on a Phase IIb study. The eight week study reported dosage correlated reduction in LDL-C and increases in HDL-C levels with no corresponding increases in blood pressure in any cohort. The increase in HDL was particularly significant, averaging 44 percent, 86 percent, 139 percent and 133 percent at doses of 10 mg, 40 mg, 150 mg and 300 mg.
Phase III trial (DEFINE)
Merck started a Phase III trial to assess the drug's effects on LDL, HDL, clinically measurable cardiovascular events, and safety; It was code-named DEFINE (Determining the Efficacy and Tolerability of CETP Inhibition with Anacetrapib), and was described as a medium sized safety and efficacy trial.
Early results from the DEFINE trial were presented on November 17 at AHA2010, a meeting of the American Heart Association. At 100 mg dosage, LDL decreased by 36%, lipoprotein(a) decreased by 36.4%, while HDL increased by 138%. Systolic blood pressure showed no increase, and there was no association with increased CVD death or events. The results were later updated to 39.8% of LDL decrease.
Cardiologist Steve Nissen described DEFINE as a medium-sized safety trial intended to find out "whether anacetrapib would show the same increase in adverse cardiovascular events that was seen with torcetrapib." Fortunately, anacetrapib did not. In his opinion the DEFINE study was too small to show a clear benefit, but the trends in the major adverse cardiovascular events were going in the right direction.
A two year follow up is due to complete by December 2012.
Phase III trial (REVEAL)
The REVEAL (Randomized EValuation of the Effects of Anacetrapib Through Lipid-modification) will assess whether there is clinical benefit associated with anacetrapib. REVEAL recruited 30,000 participants for a randomized, double-blinded, placebo-controlled trial.
The study will compare patients with a history of vascular disease (such as heart disease, cerebrovascular disease, and peripheral vascular disease) on 100 mg of anacetrapib daily to those on placebo, to determine if the addition of anacetrapib reduces the risk of major coronary events (such as heart attack, death from heart disease, or requiring a coronary revascularization.) Data will be collected through 2017.
A concern raised in October 2013 is related to the time that the drug remains in people's body after they stop taking it. The report shows that even after 4 years the levels of the medicine were still detectable. 
Other CETP inhibitors:
- Torcetrapib was developed by Pfizer until December 2006 but caused unacceptable increases in blood pressure and had net cardiovascular detriment.
- Dalcetrapib was developed by Hoffmann–La Roche until May 2012. It did not raise blood pressure and did raise HDL, but it showed no clinically meaningful efficacy.
- Evacetrapib is under development by Eli Lilly & Company.
- "Statement on a nonproprietary name adopted by the USAN Council: Anacetrapib". American Medical Association. 2007. Retrieved 2008-01-19.
- Gutstein DE, Krishna R, Johns D, et al. (2012). "Anacetrapib, a Novel CETP Inhibitor: Pursuing a New Approach to Cardiovascular Risk Reduction". Clinical Pharmacology & Therapeutics 91 (1): 109–122. doi:10.1038/clpt.2011.271.
- "MK0859 Dose-Ranging Study". clinicaltrials.gov.
- Bloomfield D, Carlson GL, Sapre A et al. (October 2009). "Efficacy and safety of the cholesteryl ester transfer protein inhibitor anacetrapib as monotherapy and co-administered with atorvastatin in dyslipidemic patients". Am. Heart J. 157 (2): 352–360. doi:10.1016/j.ahj.2008.09.022. PMID 19185645.
- "Phase III Study to Assess the Tolerability and Efficacy of Anacetrapib in Patients With Coronary Heart Disease (CHD) or CHD Risk-Equivalent Disease (DEFINE)". ClinicalTrials.gov. U.S. NIH.
- Cannon CP, Dansky HM, Davidson M, et al. (October 2009). "Design of the DEFINE trial: determining the Efficacy and tolerability of CETP Inhibition with AnacEtrapib". Am. Heart J. 158 (4): 513–519.e3. doi:10.1016/j.ahj.2009.07.028. PMID 19781408.
- Cannon, Christopher, S. Shah et al (November 17, 2010). "Safety of Anacetrapib in Patients with or at High Risk for Coronary Heart Disease". The New England Journal of Medicine 363 (25): 2406. doi:10.1056/NEJMoa1009744.
- Antonio M Gotto Jr, Jennifer E Moon (August 2012). "Safety of Inhibition of Cholesteryl Ester Transfer Protein With AnacetrapibThe DEFINE Study". Expert Rev Cardiovasc Ther.
- O'Riordan, Michael (November 17, 2010). "DEFINE: Large effects on LDL and HDL cholesterol with CETP inhibitor anacetrapib". theheart.org.
- "HPS3/TIMI55 – REVEAL trial of Anacetrapib in high-risk vascular patients recruits the target of 30,000 participants". University of Oxford Clinical Trial Service Unit & Epidemiological Studies Unit. September 2, 2013.
- National Institute of Health (January 30, 2012). "REVEAL: Randomized EValuation of the Effects of Anacetrapib Through Lipid-modification". clinicaltrials.gov.
- Matthew Herper (October 22, 2013). "Merck heart drug runs into a new worry". Forbes.com.