The use of lorcaserin in the management of obesity: A critical appraisal

Drug Design, Development and Therapy

Volumn , Issue 5, 2011, Pages 1-7

  Bai, Bo ^a   Wang, Yu ^a  

^a UNIVERSITY OF HONG KONG   (Hong Kong)

Author keywords

5 hydroxytryptamine receptor agonist; Anti obesity drug; Clinical trial; Obesity

Indexed keywords

CHOLESTEROL; HIGH DENSITY LIPOPROTEIN CHOLESTEROL; LORCASERIN; LOW DENSITY LIPOPROTEIN CHOLESTEROL; PLACEBO; SEROTONIN 2A RECEPTOR; SEROTONIN 2B RECEPTOR; SEROTONIN 2C RECEPTOR; SEROTONIN AGONIST; SEROTONIN RECEPTOR; TRIACYLGLYCEROL;

BACKACHE; BLOOD PRESSURE; BODY MASS; CALORIC RESTRICTION; CARDIOVASCULAR RISK; CHOLESTEROL BLOOD LEVEL; DEPRESSION; DIETARY INTAKE; DIZZINESS; DRUG ABSORPTION; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG METABOLISM; DRUG RECEPTOR BINDING; DRUG SAFETY; EXERCISE; HEADACHE; HEART RATE; HUMAN; HYPOGLYCEMIA; LUNG ARTERY PRESSURE; METABOLIC PARAMETERS; NAUSEA; NEPHROLITHIASIS; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; OBESITY; PATIENT COMPLIANCE; PATIENT SATISFACTION; PNEUMONIA; QUALITY OF LIFE; RECOMMENDED DRUG DOSE; REVIEW; RHINOPHARYNGITIS; RISK FACTOR; SEIZURE; SIDE EFFECT; TIME TO MAXIMUM PLASMA CONCENTRATION; UPPER RESPIRATORY TRACT INFECTION; VALVULAR HEART DISEASE; WAIST CIRCUMFERENCE; WEIGHT REDUCTION;

EID: 79952960760     PISSN: 11778881     EISSN: None     Source Type: Journal    
DOI: 10.2147/DDDT.S11945     Document Type: Review

References (48)

1. Haslam DW, James WP. Obesity. Lancet. 2005;366(9492):1197-1209.
2. York DA, Rossner S, Caterson I, et al. Prevention Conference VII: Obesity, a worldwide epidemic related to heart disease and stroke: Group I: worldwide demographics of obesity. Circulation. 2004; 110(18):e463-e470.
3. De Onis M, Blossner M, Borghi E. Global prevalence and trends of overweight and obesity among preschool children. Am J Clin Nutr. 2010;92(5):1257-1264.
4. Kumanyika SK, Obarzanek E, Stettler N, et al. Population-based prevention of obesity: the need for comprehensive promotion of healthful eating, physical activity, and energy balance: a scientific statement from American Heart Association Council on Epidemiology and Prevention, Interdisciplinary Committee for Prevention (formerly the expert panel on population and prevention science). Circulation. 2008;118(4):428-464.
5. Danaei G, Ding EL, Mozaffarian D, et al. The preventable causes of death in the United States: comparative risk assessment of dietary, lifestyle, and metabolic risk factors. PLoS Med. 2009;6(4):e1000058.
6. Kremers S, Reubsaet A, Martens M, et al. Systematic prevention of overweight and obesity in adults: a qualitative and quantitative literature analysis. Obes Rev. 2010;11(5):371-379.
7. Riebe D, Blissmer B, Greene G, et al. Long-term maintenance of exercise and healthy eating behaviors in overweight adults. Prev Med. 2005;40(6):769-778.
8. Lindstrom J, Ilanne-Parikka P, Peltonen M, et al. Sustained reduction in the incidence of type 2 diabetes by lifestyle intervention: follow-up of the Finnish Diabetes Prevention Study. Lancet. 2006;368(9548): 1673-1679.
9. Wassertheil-Smoller S, Oberman A, Blaufox MD, Davis B, Langford H. The trial of antihypertensive interventions and management (TAIM) study. Final results with regard to blood pressure, cardiovascular risk, and quality of life. Am J Hypertens. 1992;5(1):37-44.
10. Lazo M, Solga SF, Horska A, et al. Effect of a 12-month intensive lifestyle intervention on hepatic steatosis in adults with type 2 diabetes. Diabetes Care. 2010;33(10):2156-2163.
11. Oza N, Eguchi Y, Mizuta T, et al. A pilot trial of body weight reduction for nonalcoholic fatty liver disease with a home-based lifestyle modification intervention delivered in collaboration with interdisciplinary medical staff. J Gastroenterol. 2009;44(12):1203-1208.
12. Flum DR, Salem L, Elrod JA, Dellinger EP, Cheadle A, Chan L. Early mortality among Medicare beneficiaries undergoing bariatric surgical procedures. JAMA. 2005;294(15):1903-1908.
13. Wolfe BM, Morton JM. Weighing in on bariatric surgery: procedure use, readmission rates, and mortality. JAMA. 2005;294(15):1960-1963.
14. National Institutes of Health, National Heart, Lung, and Blood Institute, in cooperation with the National Institute of Diabetes and Digestive and Kidney Diseases. Clinical guidelines on the identification, evaluation, and treatment of overweight and obesity in adults: the evidence report. Obes Res. 1998;6 Suppl 2:S51-S209.
15. Bray GA, Greenway FL. Pharmacological treatment of the overweight patient. Pharmacol Rev. 2007;59(2):151-184.
16. Rubio MA, Gargallo M, Millan AI, Moreno B. Drugs in the treatment of obesity: sibutramine, orlistat and rimonabant. Public Health Nutr. 2007;10(10A):1200-1205.
17. Coutinho W. The first decade of sibutramine and orlistat: a reappraisal of their expanding roles in the treatment of obesity and associated conditions. Arq Bras Endocrinol Metabol. 2009;53(2):262-270.
18. Thomsen WJ, Grottick AJ, Menzaghi F, et al. Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. J Pharmacol Exp Ther. 2008;325(2): 577-587.
19. Leibowitz SF, Weiss GF, Shor-Posner G. Hypothalamic serotonin: pharmacological, biochemical, and behavioral analyses of its feedingsuppressive action. Clin Neuropharmacol. 1988;11 Suppl 1:S51-S71.
20. Nelson DL, Gehlert DR. Central nervous system biogenic amine targets for control of appetite and energy expenditure. Endocrine. 2006;29(1): 49-60.
21. Bickerdike MJ. 5-HT2C receptor agonists as potential drugs for the treatment of obesity. Curr Top Med Chem. 2003;3(8):885-897.
22. Charney DS, Woods SW, Krystal JH, Heninger GR. Serotonin function and human anxiety disorders. Ann N Y Acad Sci. 1990;600:558-573.
23. Lucki I, Kreider MS, Simansky KJ. Reduction of feeding behavior by the serotonin uptake inhibitor sertraline. Psychopharmacology (Berl). 1988;96(3):289-295.
24. Pascual J. Serotonin, serotonin receptors, serotonin receptor subtype agonists and pain. Pain. 1990;40(1):115-116.
25. Roth BL, Willins DL, Kristiansen K, Kroeze WK. 5-Hydroxytryptamine2- family receptors (5-hydroxytryptamine2A, 5-hydroxytryptamine2B, 5-hydroxytryptamine2C): where structure meets function. Pharmacol Ther. 1998;79(3):231-257.
26. Hoyer D, Clarke DE, Fozard JR, et al. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (serotonin). Pharmacol Rev. 1994;46(2):157-203.
27. Kaumann AJ, Levy FO. 5-hydroxytryptamine receptors in the human cardiovascular system. Pharmacol Ther. 2006;111(3):674-706.
28. Xu J, Jian B, Chu R, et al. Serotonin mechanisms in heart valve disease II: the 5-HT2 receptor and its signaling pathway in aortic valve interstitial cells. Am J Pathol. 2002;161(6):2209-2218.
29. Bos M, Jenck F, Martin JR, et al. Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder. J Med Chem. 1997;40(17):2762-2769.
30. Halford JC, Boyland EJ, Blundell JE, Kirkham TC, Harrold JA. Pharmacological management of appetite expression in obesity. Nat Rev Endocrinol. 2010;6(5):255-269.
31. 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(23):2836-2841.
32. 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(2):305-313.
33. Smith SR, Weissman NJ, Anderson CM, et al. Multicenter, placebocontrolled trial of lorcaserin for weight management. N Engl J Med. 2010;363(3):245-256.
34. Morgan M, Chen WC, Anderson C, Prosser W, Donahue D, Shanahan W. Pharmacokinetic properties, metabolism, and tolerability of lorcaserin in healthy volunteers. Annual Meeting of the Obesity Society; 2008 Oct 3-7; Phoenix, AZ, USA.
35. Chen WG, Xu J, Gwathney W, et al. Metabolism and disposition of lorcaserin, a novel selective serotonin 5-HT2c receptor agonist, in rats, mice, monkeys and humans. Drug Metab Rev. 2008;40:131.
36. Rodrigues AD, Roberts EM. The in vitro interaction of dexmedetomidine with human liver microsomal cytochrome P4502D6 (CYP2D6). Drug Metab Dispos. 1997;25(5):651-655.
37. Gueorguieva I, Jackson K, Wrighton SA, Sinha VP, Chien JY. Desipramine, substrate for CYP2D6 activity: population pharmacokinetic model and design elements of drug-drug interaction trials. Br J Clin Pharmacol. 2010;70(4):523-536.
38. Smith SR, Prosser WA, Donahue DJ, et al. Lorcaserin (APD356), a selective 5-HT2C agonist, reduces body weight in obese men and women. Obesity (Silver Spring). 2009;17(3):494-503.
39. Astrup A. Drug management of obesity - efficacy versus safety. N Engl J Med. 2010;363(3):288-290.
40. Viner RM, Hsia Y, Tomsic T, Wong IC. Efficacy and safety of antiobesity drugs in children and adolescents: systematic review and metaanalysis. Obes Rev. 2010;11(8):593-602.
41. Christensen R, Kristensen PK, Bartels EM, Bliddal H, Astrup A. Efficacy and safety of the weight-loss drug rimonabant: a meta-analysis of randomised trials. Lancet. 2007;370(9600):1706-1713.
42. Andersson C, Weeke P, Fosbol EL, et al. Acute effect of weight loss on levels of total bilirubin in obese, cardiovascular high-risk patients: an analysis from the lead-in period of the Sibutramine Cardiovascular Outcome trial. Metabolism. 2009;58(8):1109-1115.
43. Graham DJ, Green L. Further cases of valvular heart disease associated with fenfluramine-phentermine. N Engl J Med. 1997;337(9):635.
44. Rochefort GY, Lemaire MC, Eder V, et al. Dexfenfluramine does not worsen but moderates progression of chronic hypoxia-induced pulmonary hypertension. Eur J Pharmacol. 2006;550(1-3):149-154.
45. Souza R, Humbert M, Sztrymf B, et al. Pulmonary arterial hypertension associated with fenfluramine exposure: report of 109 cases. Eur Respir J. 2008;31(2):343-348.
46. Davidson MH, Hauptman J, DiGirolamo M, et al. Weight control and risk factor reduction in obese subjects treated for 2 years with orlistat - a randomized controlled trial. JAMA. 1999;281(3):235-242.
47. Pi-Sunyer Fx, Aronne LJ, Heshmati HM, Devin J, Rosenstock J; RIO-North America Study Group. Effect of rimonabant, a cannabinoid- 1 receptor blocker, on weight and cardiometabolic risk factors in overweight or obese patients: RIO-North America: a randomized controlled trial. JAMA. 2006;295(7):761-775.
48. Jones D. Novel pharmacotherapies for obesity poised to enter market. Nat Rev Drug Discov. 2009;8(11):833-834.