Literature DB >> 21589947

Lorcaserin for the treatment of obesity.

L M Redman1, E Ravussin.   

Abstract

Obesity is a worldwide epidemic and there is an urgent need for the development of effective pharmacological therapies that target the metabolic and behavioral factors of body weight regulation. Serotonin (5-HT) has been implicated as a critical factor in the short-term (meal-by-meal) regulation of food intake and pharmaceutical companies have invested millions of dollars to discover and develop drug targets for the serotonergic pathway. Lorcaserin is a novel selective agonist of the 5-HT(2C) receptor for weight loss therapy. Preclinical and clinical studies indicate lorcaserin is well tolerated and not associated with cardiac valvulopathy or pulmonary hypertension suggesting that lorcaserin is a selective 5-HT(2C) receptor agonist and has little or no activation of the 5-HT(2B) and 5-HT(2A) receptors, respectively. Lorcaserin acts to alter energy balance through a reduction in energy intake and without an increase in energy expenditure and achieved the U.S. Food and Drug Administration guidelines for weight loss efficacy. It remains to be determined whether or not lorcaserin will be approved for the long-term management of obesity. Copyright 2010 Prous Science, S.A.U. or its licensors. All rights reserved.

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Year:  2010        PMID: 21589947      PMCID: PMC3773535          DOI: 10.1358/dot.2010.46.12.1556433

Source DB:  PubMed          Journal:  Drugs Today (Barc)        ISSN: 1699-3993            Impact factor:   2.245


  50 in total

1.  Pharmacotherapy for obesity: a quantitative analysis of four decades of published randomized clinical trials.

Authors:  C K Haddock; W S C Poston; P L Dill; J P Foreyt; M Ericsson
Journal:  Int J Obes Relat Metab Disord       Date:  2002-02

2.  Evidence that hypophagia induced by d-fenfluramine and d-norfenfluramine in the rat is mediated by 5-HT2C receptors.

Authors:  S P Vickers; C T Dourish; G A Kennett
Journal:  Neuropharmacology       Date:  2001-08       Impact factor: 5.250

3.  Possible role of valvular serotonin 5-HT(2B) receptors in the cardiopathy associated with fenfluramine.

Authors:  L W Fitzgerald; T C Burn; B S Brown; J P Patterson; M H Corjay; P A Valentine; J H Sun; J R Link; I Abbaszade; J M Hollis; B L Largent; P R Hartig; G F Hollis; P C Meunier; A J Robichaud; D W Robertson
Journal:  Mol Pharmacol       Date:  2000-01       Impact factor: 4.436

4.  The effect of sibutramine on energy expenditure and appetite during chronic treatment without dietary restriction.

Authors:  D L Hansen; S Toubro; M J Stock; I A Macdonald; A Astrup
Journal:  Int J Obes Relat Metab Disord       Date:  1999-10

5.  Lorcaserin (APD356), a selective 5-HT(2C) agonist, reduces body weight in obese men and women.

Authors:  Steven R Smith; Warren A Prosser; David J Donahue; Michael E Morgan; Christen M Anderson; William R Shanahan
Journal:  Obesity (Silver Spring)       Date:  2008-12-04       Impact factor: 5.002

6.  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.

Authors:  Brian M Smith; Jeffrey M Smith; James H Tsai; Jeffrey A Schultz; Charles A Gilson; Scott A Estrada; Rita R Chen; Douglas M Park; Emily B Prieto; Charlemagne S Gallardo; Dipanjan Sengupta; Peter I Dosa; Jon A Covel; Albert Ren; Robert R Webb; Nigel R A Beeley; Michael Martin; Michael Morgan; Stephen Espitia; Hazel R Saldana; Christina Bjenning; Kevin T Whelan; Andrew J Grottick; Frederique Menzaghi; William J Thomsen
Journal:  J Med Chem       Date:  2007-12-21       Impact factor: 7.446

7.  Serotonin 5-HT2C receptor agonist promotes hypophagia via downstream activation of melanocortin 4 receptors.

Authors:  Daniel D Lam; Magdalena J Przydzial; Simon H Ridley; Giles S H Yeo; Justin J Rochford; Stephen O'Rahilly; Lora K Heisler
Journal:  Endocrinology       Date:  2007-11-26       Impact factor: 4.736

8.  Estimating the changes in energy flux that characterize the rise in obesity prevalence.

Authors:  Boyd A Swinburn; Gary Sacks; Sing Kai Lo; Klaas R Westerterp; Elaine C Rush; Michael Rosenbaum; Amy Luke; Dale A Schoeller; James P DeLany; Nancy F Butte; Eric Ravussin
Journal:  Am J Clin Nutr       Date:  2009-04-15       Impact factor: 7.045

Review 9.  Pharmacological targeting of the serotonergic system for the treatment of obesity.

Authors:  Alastair S Garfield; Lora K Heisler
Journal:  J Physiol       Date:  2008-11-24       Impact factor: 5.182

10.  Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization.

Authors:  William J Thomsen; Andrew J Grottick; Frederique Menzaghi; Hazel Reyes-Saldana; Stephen Espitia; Diane Yuskin; Kevin Whelan; Michael Martin; Michael Morgan; Weichao Chen; Hussien Al-Shamma; Brian Smith; Derek Chalmers; Dominic Behan
Journal:  J Pharmacol Exp Ther       Date:  2008-02-05       Impact factor: 4.030

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  5 in total

1.  Targeting hyperglycaemia with anti-obesity drugs: time for a paradigm shift?

Authors:  Andrew J Krentz; Marcus Hompesch
Journal:  Drugs       Date:  2013-10       Impact factor: 9.546

2.  Lorcaserin: A novel antiobesity drug.

Authors:  Dick B S Brashier; A K Sharma; Navdeep Dahiya; S K Singh; Anjan Khadka
Journal:  J Pharmacol Pharmacother       Date:  2014-04

Review 3.  Pathobiological mechanisms underlying metabolic syndrome (MetS) in chronic obstructive pulmonary disease (COPD): clinical significance and therapeutic strategies.

Authors:  Stanley M H Chan; Stavros Selemidis; Steven Bozinovski; Ross Vlahos
Journal:  Pharmacol Ther       Date:  2019-02-26       Impact factor: 12.310

4.  Lorcaserin for prevention and remission of type 2 diabetes mellitus in people with overweight or obesity: protocol for a systematic review and meta-analysis.

Authors:  Hai Zeng; Meng Luo; Zunjiang Li; Junru Wen; Guoxin He; Yuelin Jin; Wenbin Fu; Peng Zhou
Journal:  BMJ Open       Date:  2019-07-27       Impact factor: 2.692

5.  Evidence for the Association of a Deleted Variant in the 5'-Flanking Region of the Chicken serotonin transporter (5-HTT) Gene with a Temporary Increase in Feed Intake and Growth Rate.

Authors:  Joergen B Kjaer; Loc Phi-van
Journal:  Animals (Basel)       Date:  2016-10-14       Impact factor: 2.752

  5 in total

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