Lorcaserin: a novel serotonin 2C agonist for the treatment of obesity

References

• Centers for Disease Control and Prevention. Overweight and obesity. Available at: http://www.cdc.gov/obesity/data/adult.html [Last accessed 15 September 2012]
   Google Scholar
• Centers for Disease Control and Prevention. Chronic disease prevention and health promotion. Available at: www.cdc.gov/chronicdisease/index.htm [Last accessed 15 September 2012]
   Google Scholar
• Olshansky SJ, Passaro DJ, Hershow RC, et al. A potential decline in life expectancy in the United States in the 21st century. N Engl J Med 2005;352:1138-45
   PubMed Web of Science ®Google Scholar
• Snow V, Barry P, Fitterman N, et al. Clinical Efficacy Assessment Subcommittee of the American College of Physicians. Pharmacologic and surgical management of obesity in primary care: a clinical practice guideline from the American College of Physicians. Ann Intern Med 2005;142:525-31
   PubMed Web of Science ®Google Scholar
• National Heart Lung and Blood Institute. Clinical Guidelines on the identification, evaluation, and treatment of overweight and obesity in adults. The evidence report. Available at: http://www.nhlbi.nih.gov/guidelines/obesity/ob_gdlns.pdf [Last accessed 15 September 2012]
   Google Scholar
• U.S. Food and Drug Administration (FDA). FDA approves Belviq to treat some overweight or obese adults [press announcement]. Available at: http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm309993.htm [Last accessed 15 September 2012]
   Google Scholar
• Leibowitz SF, Weiss GF, Shor-Posner G. Hypothalamic serotonin: pharmacological, biochemical, and behavioral analyses of its feeding-suppressive action. Clin Neuropharmacol 1988;11(Suppl I):S51-71
   PubMedGoogle Scholar
• Heisler LK, Cowley MA, Kishi T, et al. Central serotonin and pathways regulating energy homeostasis. Ann N Y Acad Sci 2003;994:169-74
   PubMed Web of Science ®Google Scholar
• Nelson DL, Gehlert DR. Central nervous system biogenic amine targets for control of appetite and energy expenditure. Endocrine 2006;29:49-60
   PubMed Web of Science ®Google Scholar
• Kaumann AJ, Levy FO. 5-hydroxytryptamine receptors in the human cardiovascular system. Pharmacol Ther 2006;111:674-706
   PubMed Web of Science ®Google Scholar
• Connolly HM, Crary JL, McGoon MD, et al. Valvular heart disease associated with fenfluramine–phentermine. N Engl J Med 1997;337:581-8
   PubMed Web of Science ®Google Scholar
• Rothman RB, Baumann MH, Savage JE, et al. Evidence for possible involvement of 5-HT (2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications. Circulation 2000;102:2836-41
   PubMed Web of Science ®Google Scholar
• Miller KJ. Serotonin 5-HT2C receptor agonists: potential for the treatment of obesity. Mol Interv 2005;5:282-91
   PubMed Web of Science ®Google Scholar
• Bayes HE. Lorcaserin and adiposopathy: 5-HT2c agonism as a treatment for ‘sick fat’ and metabolic disease. Expert Rev Cardiovasc Ther 2009;7:1429-45
   PubMedGoogle Scholar
• Smith BM, Smith JM, Tsai JH, et al. Discovery and structure–activity relationship of (1R)-8-Chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity. J Med Chem 2008;51:305-13
   PubMed Web of Science ®Google Scholar
• Thomsen WJ, Grottick AJ, Manzaghi F, et al. Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacologic characterization. J Pharmacol Exp Ther 2008;325:577-87
   PubMed Web of Science ®Google Scholar
• Martin CK, Redman LM, Zhang J, et al. Lorcaserin, a 5-HT2C receptor agonist, reduces body weight by decreasing energy intake without influencing energy expenditure. J Clin Endocrinol Metab 2010;96:837-45
   PubMed Web of Science ®Google Scholar
• Levin ED, Johnson JE, Slade S, et al. Lorcaserin, a 5-HT2C agonist, decreases nicotine self-administration in female rats. J Pharmacol Exp Ther 1022;338:890-6
   Google Scholar
• Higgins GA, Silenieks LB, Robmann A, et al. The 5-HT2C receptor agonist lorcaserin reduces nicotine self-administration, discrimination, and reinstatement: relationship to feeding behavior and impulse control. Neuropsychopharmacology 2012;37:1177-91
   PubMed Web of Science ®Google Scholar
• Sadeque AJM, Usmani KA, Palamar S, et al. Identification of human UDP-glucuronosyltransferases involved in N-carbamoyl glucuronidation of lorcaserin. Drug Metab Disp 2012;40:772-8
   PubMed Web of Science ®Google Scholar
• Eisai Inc. Belviq (lorcaserin) product information. Woodcliff Lake, NJ: Eisai Inc., 2012
   Google Scholar
• Morgan M, Chen W, Anderson C et al. Pharmacokinetic properties, metabolism and tolerability of lorcaserin in healthy volunteers. Paper presented at Annual Scientific Meeting of the Obesity Society. Phoenix, AZ, 2008 Oct 3–7
   Google Scholar
• Smith SR, Prosser WA, Donahue DJ, et al. Lorcaserin (APD356), a selective 5-HT2C agonist, reduces body weight in obese men and women. Obesity 2008;17:494-503
   PubMed Web of Science ®Google Scholar
• Smith SR, Weissman NJ, Anderson CM, et al. for the Behavioral Modification and Lorcaserin for Overweight and Obesity Management (BLOOM) Study Group. Multicenter, placebo-controlled trial of lorcaserin for weight management. N Engl J Med 2010;363:245-56
   PubMed Web of Science ®Google Scholar
• Fidler MC, Sanchez M, Raether B, et al. A one-year randomized trial of lorcaserin for weight loss in obese and overweight adults: the BLOSSOM trial. J Clin Endocrinol Metab 2011;96:3067-77
   PubMed Web of Science ®Google Scholar
• O’Neil PM, Smith SR, Weissman NJ, et al. Randomized placebo-controlled clinical trial of lorcaserin for weight loss in type 2 diabetes mellitus: the BLOOM-DM study. Obesity 2012;20:1426-36
   PubMed Web of Science ®Google Scholar
• Chan EW, He Y, Chui CSL et al. Efficacy and safety of lorcaserin in obese adults: a meta-analysis of 1-year randomized controlled trials (RCTs) and narrative review of short-term RCTs. Obes Rev 2013;14:383-92
   Google Scholar
• Martin CK, Redman Lm, Zhang J, et al. Lorcaserin, a 5-HT(2C) receptor agonist, reduces body weight by decreasing energy intake without influencing energy expenditure. J Clin Endocrinol Metab 2011;96:837-45
   PubMed Web of Science ®Google Scholar
• Food and Drug Administration Endocrinologic and Metabolic Drugs Advisory Committee. FDA briefing document: NDA 22529, Lorqess (lorcaserin hydrochloride) tablets. Available at: www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/Drugs/EndocrinologicandMetabolicDrugsAdvisoryCommittee/UCM225631.pdf [Last accessed 27 September 2012]
   Google Scholar
• Shram MJ, Schoedel KA, Bartlett C, et al. Evaluation of the abuse potential of lorcaserin, a serotonin 2C (5-HT2C) receptor agonist. Clin Pharmacol Ther 2011;89:683-92
   PubMed Web of Science ®Google Scholar
• Food and Drug Administration (FDA). Guidance for industry: developing products for weight management. Available at: http://www.fda.gov/downloads/Drugs/…/Guidances/ucm071612.pdf [Last accessed 27 October 2012]
   Google Scholar
• Kaplan LM. Pharmacologic therapies for obesity. Gastroenterol Clin North Am 2010;39:69-79
   PubMed Web of Science ®Google Scholar
• Centers for Disease Control and Prevention. Facts about physical activity. Available at: http://www.cdc.gov/physicalactivity/data/facts.html [Last accessed 28 October 2012]
   Google Scholar
• Torgerson JL, Hauptman J, Boldrin MN, et al. Xenical in the prevention of diabetes in obese subjects (XENDOS) study: a randomized study of orlistat as an adjunct to lifestyle changes for the prevention of type 2 diabetes in obese patients. Diabetes Care 2004;27:155-61
   PubMed Web of Science ®Google Scholar
• Hauptman J, Lucas C, Boldrin MN, et al. Orlistat in the long-term treatment of obesity in primary care settings. Arch Fam Med 2000;9:160-7
   PubMedGoogle Scholar
• Finer N, James WPT, Kopelman PG, et al. One-year treatment of obesity: a randomized, double-blind, placebo-controlled, multicenter study of orlistat, a gastrointestinal lipase inhibitor. Int J Obes 2000;24:306-13
   PubMed Web of Science ®Google Scholar
• Gadde KM, Allison DB, Ryan DH, et al. Effects of low-dose, controlled-release, phentermine plus topiramate combination on weight and associated comorbidities in overweight and obese adults (CONQUER): a randomized, placebo-controlled, phase 3 trial. Lancet 2011;377:1341-52
   PubMed Web of Science ®Google Scholar
• Garvey WT, Ryan DH, Look M, et al. Two-year sustained weight loss and metabolic benefits with controlled-release phentermine/topiramate in obese and overweight adults (SEQUEL): a randomized, placebo-controlled, phase 3 extension study. Am J Clin Nutr 2012;95:297-308
   PubMed Web of Science ®Google Scholar
• Available at: http://www.fda.gov/downloads/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/UCM312598.pdf [Last accessed 28 March 2013]
   Google Scholar