Lorcaserin for the treatment of obesity

Drugs of Today

Volumn 46, Issue 12, 2010, Pages 901-910

  Redman, Leanne M ^a   Ravussin, E ^a  

^a PENNINGTON BIOMEDICAL RESEARCH CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

(3 CHLOROPHENYL)PIPERAZINE; ALPHA INTERMEDIN; C REACTIVE PROTEIN; CHOLESTEROL; DEXFENFLURAMINE; FENFLURAMINE; FIBRINOGEN; FLUOXETINE; HEMOGLOBIN A1C; HIGH DENSITY LIPOPROTEIN; LORCASERIN; LOW DENSITY LIPOPROTEIN; MELANOCORTIN 4 RECEPTOR; PHENTERMINE; PROOPIOMELANOCORTIN; SEROTONIN 2C AGONIST; SIBUTRAMINE; TETRAHYDROLIPSTATIN; TRIACYLGLYCEROL;

ABSENCE OF SIDE EFFECTS; ARTHRALGIA; BASAL GANGLION; BLOOD PRESSURE; BODY MASS; CARDIOVASCULAR SYMPTOM; CENTRAL NERVOUS SYSTEM DISEASE; CHOLESTEROL BLOOD LEVEL; CHOROID PLEXUS; CLINICAL ASSESSMENT; DIARRHEA; DIASTOLIC BLOOD PRESSURE; DIZZINESS; DOSAGE SCHEDULE COMPARISON; DRUG CLEARANCE; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG INDUCED HEADACHE; DRUG MEGADOSE; DRUG TARGETING; ECHOCARDIOGRAPHY; ENERGY EXPENDITURE; FOOD INTAKE; HEART RATE; HIPPOCAMPUS; HUMAN; HYPOTHALAMUS; INFLUENZA; INSULIN SENSITIVITY; KNOCKOUT MOUSE; LIFESTYLE MODIFICATION; LIPID DIET; LIPOPROTEIN BLOOD LEVEL; LUNG ARTERY PRESSURE; META ANALYSIS (TOPIC); MULTICENTER STUDY (TOPIC); NAUSEA; NONHUMAN; OBESITY; OUTCOME ASSESSMENT; PHASE 3 CLINICAL TRIAL (TOPIC); PREFRONTAL CORTEX; PRODUCT RECALL; PROTEIN BLOOD LEVEL; PROTEIN EXPRESSION; RANDOMIZED CONTROLLED TRIAL (TOPIC); REVIEW; RHINOPHARYNGITIS; SATIETY; SIDE EFFECT; SINGLE DRUG DOSE; SINUSITIS; STROKE; SYSTOLIC BLOOD PRESSURE; THERMOGENESIS; TREATMENT DURATION; TRIACYLGLYCEROL BLOOD LEVEL; URINARY TRACT INFECTION; VALVULAR HEART DISEASE; VERTIGO; VOMITING; WAIST CIRCUMFERENCE; WEIGHT CONTROL; WEIGHT REDUCTION;

BENZAZEPINES; CLINICAL TRIALS AS TOPIC; HUMANS; OBESITY; SEROTONIN 5-HT2 RECEPTOR AGONISTS;

EID: 79955908067     PISSN: 16993993     EISSN: 16994019     Source Type: Journal    
DOI: 10.1358/dot.2010.46.12.1556433     Document Type: Review

References (52)

1. Ogden, C.L., Yanovski, S.Z., Carroll, M.D., Flegal, K.M. The epidemiology of obesity. Gastroenterology 2007, 132(6): 2087-102.
2. Flegal, K.M., Carroll, M.D., Ogden, C.L., Curtin, L.R. Prevalence and trends in obesity among US adults, 1999-2008. JAMA 2010, 303(3): 235-41.
3. Swinburn, B.A., Sacks, G., Lo, S.K. et al. Estimating the changes in energy flux that characterize the rise in obesity prevalence. Am J Clin Nutr 2009, 89(6): 1723-8.
4. Finkelstein, E.A., Trogdon, J.G., Cohen, J.W., Dietz, W. Annual medical spending attributable to obesity: Payer-and service-specific estimates. Health Aff (Millwood) 2009, 28(5): W822-31.
5. Blundell, J.E. Is there a role for serotonin (5-hydroxytryptamine) in feeding? Int J Obes 1977, 1(1): 15-42.
6. Tecott, L.H., Sun, L.M., Akana, S.F. et al. Eating disorder and epilepsy in mice lacking 5-HT2c serotonin receptors. Nature 1995, 374(6522): 542-6.
7. Roth, B.L., Willins, D.L., Kristiansen, K., Kroeze, W.K. 5-Hydroxytryptamine2-family receptors (5-hydroxytryptamine2A, 5-hydroxytryptamine2B, 5-hydroxytryptamine2C): Where structure meets function. Pharmacol Ther 1998, 79(3): 231-57. (Pubitemid 28393877)
8. Kaumann, A.J., Levy, F.O. 5-Hydroxytryptamine receptors in the human cardiovascular system. Pharmacol Ther 2006, 111(3): 674-706. (Pubitemid 44118434)
9. 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): 2209-18. (Pubitemid 35434865)
10. Roth, B.L. Drugs and valvular heart disease. N Engl J Med 2007, 356(1): 6-9.
11. Fan, W., Boston, B.A., Kesterson, R.A., Hruby, V.J., Cone, R.D. Role of melanocortinergic neurons in feeding and the agouti obesity syndrome. Nature 1997, 385(6612): 165-8. (Pubitemid 27034218)
12. Lam, D.D., Przydzial, M.J., Ridley, S.H., Yeo, G.S., Rochford, J.J., O'Rahilly, S., Heisler, L.K. Serotonin 5-HT2C receptor agonist promotes hypophagia via downstream activation of melanocortin 4 receptors. Endocrinology 2008, 149(3): 1323-8. (Pubitemid 351397929)
13. Smith, B.M., Smith, J.M., Tsai, J.H. 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): 305-13.
14. Heal, D.J., Aspley, S., Prow, M.R., Jackson, H.C., Martin, K.F., Cheetham, S.C. Sibutramine: A novel anti-obesity drug. A review of the pharmacological evidence to differentiate it from d-amphetamine and d-fenfluramine. Int J Obes Relat Metab Disord 1998, 22(Suppl. 1): S18-28.
15. Hansen, D.L., Toubro, S., Stock, M.J., Macdonald, I.A., Astrup, A. Thermogenic effects of sibutramine in humans. Am J Clin Nutr 1998, 68(6): 1180-6. (Pubitemid 28550946)
16. Hansen, D.L., Toubro, S., Stock, M.J., Macdonald, I.A., Astrup, A. The effect of sibutramine on energy expenditure and appetite during chronic treatment without dietary restriction. Int J Obes Relat Metab Disord 1999, 23(10): 1016-24. (Pubitemid 29476203)
17. Barkeling, B., Elfhag, K., Rooth, P., Rössner, S. Short-term effects of sibutramine (Reductil) on appetite and eating behaviour and the long-term therapeutic outcome. Int J Obes Relat Metab Disord 2003, 27(6): 693-700. (Pubitemid 36712953)
18. Rolls, B.J., Shide, D.J., Thorwart, M.L., Ulbrecht, J.S. Sibutramine reduces food intake in non-dieting women with obesity. Obes Res 1998, 6(1): 1-11. (Pubitemid 128679638)
19. Padwal, R., Li, S.K., Lau, D.C. Long-term pharmacotherapy for obesity and overweight. Cochrane Database Syst Rev 2003(4): CD004094.
20. Wadden, T.A., Berkowitz, R.I., Womble, L.G. et al. Randomized trial of lifestyle modification and pharmacotherapy for obesity. N Engl J Med 2005, 353(20): 2111-20. (Pubitemid 41653103)
21. Kaplan, L.M. Pharmacologic therapies for obesity. Gastroenterol Clin North Am 2010, 39(1): 69-79.
22. James, W.P., Caterson, I.D., Coutinho, W. et al. Effect of sibutramine on cardiovascular outcomes in overweight and obese subjects. N Engl J Med 2010, 363(10): 905-17.
23. Garfield, A.S., Heister, L.K. Pharmacological targeting of the serotonergic system for the treatment of obesity. J Physiol 2009, 587(Pt. 1): 49-60.
24. Vickers, S.P., Clifton, P.G., Dourish, C.T., Tecott, L.H. Reduced satiating effect of d-fenfluramine in serotonin 5-HT2C receptor mutant mice. Psychopharmacology (Berl) 1999, 143(3): 309-14.
25. Vickers, S.P., Dourish, C.T., Kennett, G.A. Evidence that hypophagia induced by d-fenfluramine and d-norfenfluramine in the rat is mediated by 5-HT2C receptors. Neuropharmacology 2001, 41(2): 200-9. (Pubitemid 32728091)
26. Lucas, J.J., Yamamoto, A., Scearce-Levie, K., Saudou, F., Hen, R. Absence of fenfluramine-induced anorexia and reduced c-Fos induction in the hypothalamus and central amygdaloid complex of serotonin 1B receptor knock-out mice. J Neurosci 1998, 18(14): 5537-44. (Pubitemid 28311968)
27. Gibson, E.L., Kennedy, A.J., Curzon, G. d-Fenfluramine- and d-norfenfluramine-induced hypophagia: Differential mechanisms and involvement of postsynaptic 5-HT receptors. Eur J Pharmacol 1993, 242(1): 83-90. (Pubitemid 23279514)
28. Rogers, P.J., Blundell, J.E. Effect of anorexic drugs on food intake and the micro-structure of eating in human subjects. Psychopharmacology (Berl) 1979, 66(2): 159-65. (Pubitemid 10180146)
29. Blundell, J.E., Hill, A.J. On the mechanism of action of dexfenfluramine: Effect on alliesthesia and appetite motivation in lean and obese subjects. Clin Neuropharmacol 1988, 11(Suppl. 1): S121-34.
30. Goodall, E., Silverstone, T. Differential effect of d-fenfluramine and metergoline on food intake in human subjects. Appetite 1988, 11(3): 215-28. (Pubitemid 19078005)
31. Hill, A.J., Blundell, J.E. Sensitivity of the appetite control system in obese subjects to nutritional and serotoninergic challenges. Int J Obes 1990, 14(3): 219-33. (Pubitemid 20150407)
32. Wurtman, J., Wurtman, R., Mark, S., Tsay, R., Gilbert, W., Growdon, J. d-Fenfluramine selectively suppresses carbohydrate snacking by obese subjects. Int J Eat Disord 1985, 4(1): 89-99. (Pubitemid 15116356)
33. Haddock, C.K., Poston, W.S., Dill, P.L., Foreyt, J.P., Ericsson, M. Pharmacotherapy for obesity: A quantitative analysis of four decades of published randomized clinical trials. Int J Obes Relat Metab Disord 2002, 26(2): 262-73. (Pubitemid 34151206)
34. Guy-Grand, B., Apfelbaum, M., Crepaldi, G., Gries, A., Lefebvre, P., Turner, P. International trial of long-term dexfenfluramine in obesity. Lancet 1989, 2(8672): 1142-5. (Pubitemid 19267116)
35. Weintraub, M., Sundaresan, P.R., Schuster, B., Averbuch, M., Stein, E.C., Cox, C., Byrne, L. Long-term weight control study. IV (weeks 156 to 190). The second double-blind phase. Clin Pharmacol Ther 1992, 51(5): 608-14.
36. Connolly, H.M., Crary, J.L., McGoon, M.D., Hensrud, D.D., Edwards, B.S., Edwards, W.D., Schaff, H.V. Valvular heart disease associated with fenfluramine-phentermine. N Engl J Med 1997, 337(9): 581-8. (Pubitemid 27360757)
37. Halford, J.C., Blundell, J.E. Metergoline antagonizes fluoxetine-induced suppression of food intake but not changes in the behavioural satiety sequence. Pharmacol Biochem Behav 1996, 54(4): 745-51. (Pubitemid 26258659)
38. Lee, M.D., Clifton, P.G. Partial reversal of fluoxetine anorexia by the 5-HT antagonist metergoline. Psychopharmacology (Berl) 1992, 107(2-3): 359-64.
39. McGuirk, J., Silverstone, T. The effect of the 5-HT re-uptake Inhibitor fluoxetine on food intake and body weight in healthy male subjects. Int J Obes 1990, 14(4): 361-72. (Pubitemid 20212177)
40. Pijl, H., Koppeschaar, H.P., Willekens, F.L., Op de Kamp, I., Veldhuis, H.D., Meinders, A.E. Effect of serotonin re-uptake inhibition by fluoxetine on body weight and spontaneous food choice in obesity. Int J Obes 1991, 15(3): 237-42.
41. Darga, L.L., Carroll-Michals, L., Botsford, S.J., Lucas, C.P. Fluoxetine's effect on weight loss in obese subjects. Am J Clin Nutr 1991, 54(2): 321-5. (Pubitemid 21898937)
42. Goldstein, D.J., Rampey, A.H. Jr., Enas, G.G., Potvin, J.H., Fludzinski, L.A., Levine, L.R. Fluoxetine: a randomized clinical trial in the treatment of obesity. Int J Obes Relat Metab Disord 1994, 18(3): 129-35. (Pubitemid 24087126)
43. Walsh, A.E., Smith, K.A., Oldman, A.D., Williams, C., Goodall, E.M., Cowen. P.J. m-Chlorophenylpiperazine decreases food intake in a test meal. Psychopharmacology (Berl) 1994, 116(1): 120-2.
44. Sargent, P.A., Sharpley, A.L., Williams, C., Goodall, E.M., Cowen. P.J. 5-HT2C receptor activation decreases appetite and body weight in obese subjects. Psychopharmacology (Berl) 1997, 133(3): 309-12. (Pubitemid 27445666)
45. Thomsen, W.J., Grottick, A.J., 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): 577-87.
46. Arena Pharmaceuticals reports successful phase Ia safety and clinical pharmacology trial results of novel anti-obesity compound [news release]. Arena Pharmaceuticals, July 14, 2004.
47. Smith, S.R., Prosser, W.A., Donahue, D.J., Morgan, M.E., Anderson, C.M., Shanahan, W.R.; APD356-004 Study Group. Lorcaserin (APD356), a selective 5-HT(2C) agonist, reduces body weight in obese men and women. Obesity (Silver Spring) 2009, 17(3): 494-503.
48. Arena Pharmaceuticals announces results of its phase Ib safety study for Its novel anti-obesity compound, [news release]. Arena Pharmaceuticals, November 3, 2004.
49. Smith, S.R., Weissman, N.J., Anderson, C.M. 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(3): 245-56.
50. Martin, C.K. Redman, L.M., Zhang, J., Sanchez, M., Anderson, C.M., Smith, S.R., Ravussin, E. Lorcaserin, a 5-HT2C receptor agonist, reduces body weight by decreasing energy intake without influencing energy expenditure. J Clin Endocrinol Metab 2010, Epub ahead of print.
51. Fitzgerald, L.W., Burn, T.C., Brown, B.S. et al. Possible role of valvular serotonin 5-HT2B receptors in the cardiopathy associated with fenfluramine. Mol Pharmacol 2000, 57(1): 75-81. (Pubitemid 30033262)
52. Rothman, R.B., Baumann, M.H. Serotonergic drugs and valvular heart disease. Expert Opin Drug Saf 2009, 8(3): 317-29.