Bibliography
- Maton A, Hopkins RLJ, McLaughlin CW, et al. Human biology and health. 1993. Englewood Cliffs, New Jersey, USA:Prentice Hall
- Available from: http://www.mercksource.com/pp/us/cns/cns_merckmanual_frameset.jsp
- Available from: http://www.pharmaceutical-business-review.com/article_feature.asp?guid = 8EBD782E-1098-4E37-8AB3-6CE5BAFAD5E7
- Steinwachs RM, Collins-nakai RL, Cohn LH, et al. The future of cardiology utilization and cost of care. J Am Coll Cardiol 2000;35:1092-9
- Bruckert E. New lipid-modifying therapies. Expert Opin Investig Drugs 2003;12:325-35
- Wang M, Briggs MR. HDL: the metabolism, function, and therapeutic importance. Chem Rev 2004;104:119-37
- Jacobson TA. Combination lipid-altering therapy: an emerging treatment paradigm for the 21st century. Curr Atheroscler Rep 2001;3:373-82
- Mack WJ, Selzer RH, Hodis HN, et al. One-year reduction and longitudinal analysis of carotid intima-media thickness associated with colestipol/niacin therapy. Stroke 1993;24:1779-83
- Nikkila EA, Viikinkoski P, Valle M, Frick MH. Prevention of progression of coronary atherosclerosis by treatment of hyperlipidaemia: a seven year prospective angiographic study. Br Med J 1984;289:220-3
- Pritzker LB. Do lipid lowering drugs reduce the risk of coronary heart disease? Crit Rev Clin Lab Sci 1998;35:603-21
- Carlson LA. Nicotinic acid: the broad-spectrum lipid drug. A 50th anniversary review. J Intern Med 2005;258:94-114
- Knopp RH. Drug treatment of lipid disorders. N Engl J Med 1999;341:498-511
- Offermanns S. The nicotinic acid receptor GPR109A (HM74A or PUMA-G) as a new therapeutic target. Trends Pharmacol Sci 2006;27:384-90
- McKenney JM, Proctor JD, Harris S, Chinchili VM. A comparison of the efficacy and toxic effects of sustained vs. immediate-release niacin in hypercholesterolemic patients. J Am Med Assoc 1994;271:672-7
- Cheng K, Wu T, Wu KK, et al. Antagonism of the prostaglandin D2 receptor 1 suppresses nicotinic acid-induced vasodilationin mice and humans. Proc Natl Acd Sci USA 2006;103:6682-7
- Paolini JF, Mitchel YB, Reyes R, et al. Effects of laropiprant on nicotinic acid-induced flushing in patients with dyslipidemia. Am J Cardiol 2008;101:625-30
- Schaub A, Futterer A, Pfeffer K. PUMA-G, an IFN-γ-inducible gene in macrophages is a novel member of the seven transmembrane spanning receptor superfamily. Eur J Immunol 2001;31:3714-25
- Lorenzen A, Stannek C, Lang H, et al. Characterization of a G-protein coupled receptor for nicotinic acid. Mol Pharmacol 2001;59;349-57
- Lorenzen A, Stannek C, Burmeister A, et al. G-protein coupled receptor for nicotinic acid in mouse macrophages. Biochem Pharmacol 2002;64:645-8
- Wise A, Foord SM, Fraser NJ, et al. Molecular identification of high and low affinity receptors for nicotinic acid. J Biol Chem 2003;278:9869-74
- Tunaru S, Kero J, Schaub A, et al. PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect. Nat Med 2003;9:352-5
- Arena Pharmaceuticals, Inc. Endogenous and non-endogenous versions of human G-protein-coupled receptors. US20030166148; 2003
- Benyó Z, Gille A, Kero J, et al. GPR109A (PUMA-G/HM74A) mediates nicotinic acid-induced flushing. J Clin Invest 2005;115:3634-40
- Semple G, Boatman PD, Richman JG. Recent progress in the discovery of niacin receptor agonists. Curr Opin Drug Discov Dev 2007;10:452-9
- Boatman PD, Richman JG, Semple G. Nicotinic acid receptor agonists. J Med Chem 2008;51:7653-62
- Tunaru S, Lättig J, Kero J, et al. Characterization of determinants of ligand binding to the nicotinic acid receptor (HM74A/PUMA-G). Mol Pharmacol 2005;68:1271-80
- Deng Q, Frie JL, Marley DM, et al. Molecular modeling aided design of nicotinic acid receptor GPR109A agonists. Bioorg Med Chem Lett 2008;18:4963-7
- SmithKline Beecham Corp. Chemical compounds. WO2005016867; 2005
- SmithKline Beecham Corp. 2-Substituted benzoic acid derivatives as HM74A agonists. WO2005016870; 2005
- SmithKline Beecham Corp. Anthranilic acid derivatives active at the HM74A receptor. WO2006085111; 2006
- SmithKline Beecham Corp. Anthranilic acid derivatives as HM74A receptor agonists. WO2006085112; 2006
- SmithKline Beecham Corp. Anthranilic acid derivatives and their use in treatment of diseases of lipid metabolism, in particular dyslipidaemia. WO2006085108; 2006
- SmithKline Beecham Corp. Chemical compounds. WO2006085113; 2006
- SmithKline Beecham Corp. Novel compounds. WO2005077950; 2005
- SmithKline Beecham Corp. Xanthine derivatives with HM74A receptor activity. WO2006045564; 2006
- SmithKline Beecham Corp. Xanthine derivatives with HM74A receptor activity. WO2006045565; 2006
- SmithKline Beecham Corp. Xanthine derivatives as selective HM74A agonists. WO2007017261; 2007
- SmithKline Beecham Corp. Xanthine derivatives as selective HM74A agonists. WO2007017262; 2007
- SmithKline Beecham Corp. Xanthine derivatives as selective HM74A agonists. WO2007017265; 2007
- Pipeline summary of GSK. Available from: www.gsk.com
- Merck & Co., Inc. Niacin receptor agonists, compositions containing such compounds and methods of treatment. WO2006052555; 2006
- Merck & Co., Inc. Niacin receptor agonists, compositions containing such compounds and methods of treatment. WO2006057922; 2006
- Shen HC, Ding F, Taggart A, et al. Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor. J Med Chem 2007;50:6303-6
- Merck & Co., Inc. Niacin receptor agonists, compositions containing such compounds and methods of treatment. WO2007035478; 2007
- Shen HC, Szymonifka M, Deng Q, et al. Discovery of orally bioavailable and novel urea agonists for the high affinity niacin receptor GPR109A. Bioorg Med Chem Lett 2007;17:6723-8
- Merck & Co., Inc. Niacin receptor agonists, compositions containing such compounds and methods of treatment. WO2007027532; 2007
- Merck & Co., Inc. Niacin receptor agonists, compositions containing such compounds and methods of treatment. WO2007120575; 2007
- Merck & Co., Inc. Niacin receptor agonists, compositions containing such compounds and methods of treatment. WO2007002557; 2007
- Merck & Co., Inc. Niacin receptor agonists, compositions containing such compounds and methods of treatment. US20060293364; 2006
- Merck & Co., Inc. Niacin receptor agonists, compositions containing such compounds and methods of treatment. WO2007092364; 2007
- Raghavan S, Tria GS, Shen HC, et al. Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists. Bioorg Med Chem Lett 2008;18:3163-7
- Merck & Co., Inc. Niacin receptor agonists, compositions containing such compounds and methods of treatment. WO2008051403; 2008
- Merck & Co., Inc. Niacin receptor agonists, compositions containing such compounds and methods of treatment. WO2007075749; 2007
- Arena Pharmaceuticals, Inc. 5-Substituted-2H-pyrazole-3-carboxylic acid derivatives as agonists for the nicotinic acid receptor RUP25 for the treatment of dyslipidemia and related diseases. WO2005011677; 2005
- van Herk T, Brussee J, van den Nieuwendijk AM, et al. Pyrazole derivatives as partial agonists for the nicotinic acid receptor. J Med Chem 2003;46:3945-51
- Skinner PJ, Cherrier MC, Webb PJ, et al. Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a. Bioorg Med Chem Lett 2007;17:5620-23
- Arena Pharmaceuticals, Inc. and Merck & Co., Inc. and Merck & Co., Inc. Tetrazole derivatives and methods of treatment of metabolic-related disorders thereof. WO2005044816; 2005
- Semple G, Skinner PJ, Gharbaoui T, et al. 3-(1H-Tetrazol-5-yl)-1,4,5,6-tetrahydro cycopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice. J Med Chem 2008;51:5101-8
- Lai E, Waters MG, Tata JR, et al. Effect of a niacin receptor partial agonist, MK-0354, on plasma free fatty acids, lipids, and cutaneous flushing in humans. J Clin Lipidol 2008;2:375-83
- Merck & Co., Inc. Niacin receptor agonists, compositions containing such compounds and methods of treatment. WO2006113150; 2006
- Arena Pharmaceuticals, Inc. 5-Substituted 2H-pyrazole-3-carboxylic acid derivatives as agonists for the nicotinic acid receptor RUP25 for the treatment of dyslipidemia and related diseases. WO2005011677; 2005
- Arena Pharmaceuticals, Inc. Tetrazole derivatives and methods of treatment of metabolic-related disorders thereof. WO2005044816; 2005
- Arena Pharmaceuticals, Inc. Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof. WO2006069242; 2006
- Schering Co. Heterocylces as nicotinic acid receptor agonists for treatment of dyslipidemia. WO2006124490; 2006
- Schering Co. Nitrogen-containing heterocyclic compounds and methods of use thereof. US2008019978; 2008
- Hoffmann-La Roche, Inc. Novel anthranilic acid derivatives. WO20060281810; 2006
- Hoffmann-La Roche, Inc. Novel thiophene derivatives which are HM74A agonists. 20070072873; 2007
- Hoffmann-La Roche, Inc. Novel aza-pyridopyrimidinone derivatives. US20080234277; 2008
- Hoffmann-La Roche, Inc. Novel pyridopyprimidinone derivatives which are HM74A agonists. US20070275987; 2007
- Incyte Corp. Disubstituted thienyl compounds and their use as pharmaceuticals. WO2007015744; 2007
- Lima LM, Barreiro EJ. Bioisosterism: a useful strategy for molecular modification and drug design. Curr Med Chem 2005;12:23-49
- Incyte Corp. Purinone derivatives as HM74A agonists. WO2007150025; 2007
- Incyte Corp. Purinone derivatives as HM74A agonists. WO2007150026; 2007
- Incyte corporation presentation at JP Morgan Healthcare Conference (January 8, 2008)
- Study ID NCT00698789. Available from: www.clincaltrials.gov