Efficacy and Safety of a Novel Cholesteryl Ester Transfer Protein Inhibitor, JTT-705, in Humans. A Randomized Phase II Dose-Response Study

doi:10.1161/01.CIR.0000015857.31889.7B

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on April 15, 2002

Circulation. 2002
Published online before print April 15, 2002, doi: 10.1161/01.CIR.0000015857.31889.7B

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Submitted on December 13, 2001
Revised on February 28, 2002
Accepted on February 28, 2002

Efficacy and Safety of a Novel Cholesteryl Ester Transfer Protein Inhibitor, JTT-705, in Humans. A Randomized Phase II Dose-Response Study

Greetje J. de Grooth MD, Jan Albert Kuivenhoven PhD, Anton F.H. Stalenhoef MD, PhD, Jacqueline de Graaf MD, PhD, Aeilko H. Zwinderman PhD, Jan L. Posma MD, PhD, Arie van Tol PhD, and John J.P. Kastelein MD, PhD^*

From the Department of Vascular Medicine (G.J.d.G., J.A.K., J.J.P.K.) and Department of Statistics (A.H.Z.), Academic Medical Center, University of Amsterdam; Department of General Internal Medicine, University Medical Center (A.F.H.S., J.d.G.), Nijmegen; Department of Cardiology, Martini Hospital (J.L.P.), Groningen; and Cardiovascular Research Institute COEUR Biochemistry, Erasmus University (A.v.T.), Rotterdam, the Netherlands.

^* To whom correspondence should be addressed. E-mail: e.vandongen{at}amc.uva.nl.

Background—Cholesteryl ester transfer protein (CETP) mediates the transfer of neutral lipids between lipoproteins. High plasma levels of CETP are correlated with low HDL cholesterol levels, a strong risk factor for coronary artery disease. In earlier studies, JTT-705, a novel CETP inhibitor, was shown to increase plasma HDL cholesterol and to inhibit the progression of atherosclerosis in cholesterol-fed rabbits. This study describes the first results using this CETP inhibitor in humans.

Methods and Results—In a randomized, double-blind, and placebo-controlled trial, we evaluated the efficacy and safety of daily treatment with 300, 600, and 900 mg JTT-705 in 198 healthy subjects with mild hyperlipidemia. Treatment with 900 mg JTT-705 for 4 weeks led to a 37% decrease in CETP activity (P<0.0001), a 34% increase in HDL cholesterol (P<0.0001), and a 7% decrease in LDL cholesterol (P=0.017), whereas levels of triglycerides, phospholipid transfer protein, and lecithin-cholesterol acyltransferase were unaffected. In line with the increase of total HDL, a rise of HDL_2, HDL₃, and apolipoprotein A-I was also noted. JTT-705 showed no toxicity with regard to physical examination and routine laboratory tests.

Conclusions—We show that the use of the CETP inhibitor JTT-705 in humans is an effective means to raise HDL cholesterol levels with minor gastrointestinal side effects (P=0.06). Although these results hold promise, further studies are needed to investigate whether the observed increase in HDL cholesterol translates into a concomitant reduction in coronary artery disease risk.

Key words: cholesterol • lipoproteins • atherosclerosis • cardiovascular diseases

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				A. R. Tall, L. Yvan-Charvet, and N. Wang The Failure of Torcetrapib: Was it the Molecule or the Mechanism? Arterioscler. Thromb. Vasc. Biol., February 1, 2007; 27(2): 257 - 260. [Full Text] [PDF]

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				A. Kontush and M. J. Chapman Functionally Defective High-Density Lipoprotein: A New Therapeutic Target at the Crossroads of Dyslipidemia, Inflammation, and Atherosclerosis Pharmacol. Rev., September 1, 2006; 58(3): 342 - 374. [Abstract] [Full Text] [PDF]

				P. C.N. Rensen and L. M. Havekes Cholesteryl Ester Transfer Protein Inhibition: Effect on Reverse Cholesterol Transport? Arterioscler. Thromb. Vasc. Biol., April 1, 2006; 26(4): 681 - 684. [Full Text] [PDF]

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				H. Watanabe, S. Soderlund, A. Soro-Paavonen, A. Hiukka, E. Leinonen, C. Alagona, R. Salonen, T.-P. Tuomainen, C. Ehnholm, M. Jauhiainen, et al. Decreased High-Density Lipoprotein (HDL) Particle Size, Pre{beta}-, and Large HDL Subspecies Concentration in Finnish Low-HDL Families: Relationship With Intima-Media Thickness Arterioscler. Thromb. Vasc. Biol., April 1, 2006; 26(4): 897 - 902. [Abstract] [Full Text] [PDF]

				R. W. Clark, R. B. Ruggeri, D. Cunningham, and M. J. Bamberger Description of the torcetrapib series of cholesteryl ester transfer protein inhibitors, including mechanism of action J. Lipid Res., March 1, 2006; 47(3): 537 - 552. [Abstract] [Full Text] [PDF]

				D. Duffy and D. J. Rader Emerging Therapies Targeting High-Density Lipoprotein Metabolism and Reverse Cholesterol Transport Circulation, February 28, 2006; 113(8): 1140 - 1150. [Full Text] [PDF]

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				D. Masson, J.-P. Pais de Barros, Z. Zak, T. Gautier, N. Le Guern, M. Assem, J. W. Chisholm, J. R. Paterniti Jr., and L. Lagrost Human apoA-I expression in CETP transgenic rats leads to lower levels of apoC-I in HDL and to magnification of CETP-mediated lipoprotein changes J. Lipid Res., February 1, 2006; 47(2): 356 - 365. [Abstract] [Full Text] [PDF]

				R. Ohashi, H. Mu, X. Wang, Q. Yao, and C. Chen Reverse cholesterol transport and cholesterol efflux in atherosclerosis QJM, December 1, 2005; 98(12): 845 - 856. [Abstract] [Full Text] [PDF]

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				L. Dumont, T. Gautier, J.-P. P. de Barros, H. Laplanche, D. Blache, P. Ducoroy, J. Fruchart, J.-C. Fruchart, P. Gambert, D. Masson, et al. Molecular Mechanism of the Blockade of Plasma Cholesteryl Ester Transfer Protein by Its Physiological Inhibitor Apolipoprotein CI J. Biol. Chem., November 11, 2005; 280(45): 38108 - 38116. [Abstract] [Full Text] [PDF]

				R. J. Bisoendial, G. K. Hovingh, K. El Harchaoui, J. H.M. Levels, S. Tsimikas, K. Pu, A. E. Zwinderman, J. A. Kuivenhoven, J. J.P. Kastelein, and E. S.G. Stroes Consequences of Cholesteryl Ester Transfer Protein Inhibition in Patients With Familial Hypoalphalipoproteinemia Arterioscler. Thromb. Vasc. Biol., September 1, 2005; 25(9): e133 - e134. [Full Text] [PDF]

				G. K. Hovingh, B. A. Hutten, A. G. Holleboom, W. Petersen, P. Rol, A. Stalenhoef, A. H. Zwinderman, E. de Groot, J. J.P. Kastelein MD, and J. A. Kuivenhoven Compromised LCAT Function Is Associated With Increased Atherosclerosis Circulation, August 9, 2005; 112(6): 879 - 884. [Abstract] [Full Text] [PDF]

				G. F. Lewis and D. J. Rader New Insights Into the Regulation of HDL Metabolism and Reverse Cholesterol Transport Circ. Res., June 24, 2005; 96(12): 1221 - 1232. [Abstract] [Full Text] [PDF]

				G D Kolovou, K K Anagnostopoulou, and D V Cokkinos Pathophysiology of dyslipidaemia in the metabolic syndrome Postgrad. Med. J., June 1, 2005; 81(956): 358 - 366. [Abstract] [Full Text] [PDF]

				M. E. Brousseau, M. R. Diffenderfer, J. S. Millar, C. Nartsupha, B. F. Asztalos, F. K. Welty, M. L. Wolfe, M. Rudling, I. Bjorkhem, B. Angelin, et al. Effects of Cholesteryl Ester Transfer Protein Inhibition on High-Density Lipoprotein Subspecies, Apolipoprotein A-I Metabolism, and Fecal Sterol Excretion Arterioscler. Thromb. Vasc. Biol., May 1, 2005; 25(5): 1057 - 1064. [Abstract] [Full Text] [PDF]

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				J. W. Burgess, T. A-M. Neville, P. Rouillard, Z. Harder, D. S. Beanlands, and D. L. Sparks Phosphatidylinositol increases HDL-C levels in humans J. Lipid Res., February 1, 2005; 46(2): 350 - 355. [Abstract] [Full Text] [PDF]