anti obesity agents


Summary: Agents that increase energy expenditure and weight loss by neural and chemical regulation. Beta-adrenergic agents and serotoninergic drugs have been experimentally used in patients with non-insulin dependent diabetes mellitus (NIDDM) to treat obesity.

Top Publications

  1. Chan T. Potential risks associated with the use of herbal anti-obesity products. Drug Saf. 2009;32:453-6 pubmed publisher
    ..They should warn their patients about the heterogeneous nature of these agents and the potential risks associated with their use. They should report suspected adverse reactions to their national spontaneous reporting system. ..
  2. Kim J, Kang S, Han S, Shim I. Comparison of the antiobesity effects of the protopanaxadiol- and protopanaxatriol-type saponins of red ginseng. Phytother Res. 2009;23:78-85 pubmed publisher
    ..The results suggest that the antiobesity activity of PD and PT type saponins may result from inhibiting energy gain, normalizing hypothalamic neuropeptides and serum biochemicals related to the control of obesity. ..
  3. Snitker S, Fujishima Y, Shen H, Ott S, Pi Sunyer X, Furuhata Y, et al. Effects of novel capsinoid treatment on fatness and energy metabolism in humans: possible pharmacogenetic implications. Am J Clin Nutr. 2009;89:45-50 pubmed publisher
    ..Capsinoid ingestion was associated with an increase in fat oxidation that was nearly significant. We identified 2 common genetic variants that may be predictors of therapeutic response. ..
  4. Pagotto U, Vanuzzo D, Vicennati V, Pasquali R. [Pharmacological therapy of obesity]. G Ital Cardiol (Rome). 2008;9:83S-93S pubmed
    ..9 kg/m2 with major obesity-related comorbidities such as hypertension, diabetes, dyslipidemia, obstructive sleep apnea, and metabolic syndrome. ..
  5. Bult M, van Dalen T, Muller A. Surgical treatment of obesity. Eur J Endocrinol. 2008;158:135-45 pubmed publisher
    ..Proposed criteria for bariatric surgery are given. Also, some attention is devoted to more basic insights that bariatric surgery has provided. Finally we deal with unsolved questions and future directions for research. ..
  6. Herling A, Kilp S, Elvert R, Haschke G, Kramer W. Increased energy expenditure contributes more to the body weight-reducing effect of rimonabant than reduced food intake in candy-fed wistar rats. Endocrinology. 2008;149:2557-66 pubmed publisher
    ..When the amount of endogenous fat stores declined, rimonabant-induced increased energy expenditure was maintained by a re-increase in food intake. ..
  7. García Peláez B, Vila R, Remesar X. The administration of oleoyl-estrone to lactating dams induces selective changes in the normal growth pattern of their pups. Horm Metab Res. 2007;39:582-8 pubmed
    ..Thus, treatment affects dams in a selective way that does not coincide with a simple food restriction model. ..
  8. Itoh M, Suganami T, Satoh N, Tanimoto Koyama K, Yuan X, Tanaka M, et al. Increased adiponectin secretion by highly purified eicosapentaenoic acid in rodent models of obesity and human obese subjects. Arterioscler Thromb Vasc Biol. 2007;27:1918-25 pubmed
    ..Because EPA has reduced the risk of major coronary events in a large-scale, prospective, randomized clinical trial, this study provides important insight into its therapeutic implication in obesity-related metabolic sequelae. ..
  9. Rucker D, Padwal R, Li S, Curioni C, Lau D. Long term pharmacotherapy for obesity and overweight: updated meta-analysis. BMJ. 2007;335:1194-9 pubmed
    ..Orlistat, sibutramine, and rimonabant modestly reduce weight, have differing effects on cardiovascular risk profiles, and have specific adverse effects. ..

More Information


  1. Madsen E, Rissanen A, Bruun J, Skogstrand K, Tonstad S, Hougaard D, et al. Weight loss larger than 10% is needed for general improvement of levels of circulating adiponectin and markers of inflammation in obese subjects: a 3-year weight loss study. Eur J Endocrinol. 2008;158:179-87 pubmed publisher
    ..Long-term weight loss (3 years) must exceed 10% to induce a combined significant improvement in these inflammatory markers. ..
  2. Bray G, Greenway F. Pharmacological treatment of the overweight patient. Pharmacol Rev. 2007;59:151-84 pubmed
  3. Borges R, Ribeiro Filho F, Carvalho K, Zanella M. [Impact of weight loss on adipocytokines, C-reactive protein and insulin sensitivity in hypertensive women with central obesity]. Arq Bras Cardiol. 2007;89:409-14 pubmed
    ..The greatest improvements in insulin sensitivity experienced by the orlistat-treated patients could not be attributed to the use of this drug because of the higher number of insulin-resistant subjects in this group. ..
  4. Richelsen B, Tonstad S, Rossner S, Toubro S, Niskanen L, Madsbad S, et al. Effect of orlistat on weight regain and cardiovascular risk factors following a very-low-energy diet in abdominally obese patients: a 3-year randomized, placebo-controlled study. Diabetes Care. 2007;30:27-32 pubmed
    ..4 kg weight loss after VLED for up to 3 years in obese subjects. The combination of orlistat and lifestyle intervention was associated with a reduced occurrence of type 2 diabetes. ..
  5. Aronne L. Therapeutic options for modifying cardiometabolic risk factors. Am J Med. 2007;120:S26-34 pubmed
  6. Oben J, Enyegue D, Fomekong G, Soukontoua Y, Agbor G. The effect of Cissus quadrangularis (CQR-300) and a Cissus formulation (CORE) on obesity and obesity-induced oxidative stress. Lipids Health Dis. 2007;6:4 pubmed
  7. Christensen R, Kristensen P, Bartels E, Bliddal H, Astrup A. Efficacy and safety of the weight-loss drug rimonabant: a meta-analysis of randomised trials. Lancet. 2007;370:1706-13 pubmed
  8. Fong T, Guan X, Marsh D, Shen C, Stribling D, Rosko K, et al. Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents. J Pharmacol Exp Ther. 2007;321:1013-22 pubmed
    ..These studies demonstrated that MK-0364 is a highly potent and selective CB1R inverse agonist and that it is orally active in rodent models of obesity. ..
  9. Padwal R, Majumdar S. Drug treatments for obesity: orlistat, sibutramine, and rimonabant. Lancet. 2007;369:71-7 pubmed
    ..Only then can patients and their physicians be confident that the putative benefits of such drugs outweigh their risks and costs. ..
  10. Maynadier M, Basile I, Gary Bobo M. Adiponectin normalization: a clue to the anti-metabolic syndrome action of rimonabant. Drug Discov Today. 2009;14:192-7 pubmed publisher
  11. Velasquez Mieyer P, Neira C, Nieto R, Cowan P. Obesity and cardiometabolic syndrome in children. Ther Adv Cardiovasc Dis. 2007;1:61-81 pubmed publisher
    ..This review provides rationale for additional assessments to determine cardiometabolic risk in overweight youth and recommends treatment options. ..
  12. Sarwer D, von Sydow Green A, Vetter M, Wadden T. Behavior therapy for obesity: where are we now?. Curr Opin Endocrinol Diabetes Obes. 2009;16:347-52 pubmed publisher
    ..Recent studies also have suggested that the combination of lifestyle modification with long-term use of pharmacotherapy holds promise for maximizing initial weight losses and promoting long-term maintenance. ..
  13. Ohman M, Eitzman D. Targeting MCP-1 to reduce vascular complications of obesity. Recent Pat Cardiovasc Drug Discov. 2009;4:164-76 pubmed
    ..Since MCP-1 promotes atherosclerosis, inhibition of MCP-1 may be effective in reducing the vascular risk associated with obesity. ..
  14. Di Pierro F, Menghi A, Barreca A, Lucarelli M, Calandrelli A. Greenselect Phytosome as an adjunct to a low-calorie diet for treatment of obesity: a clinical trial. Altern Med Rev. 2009;14:154-60 pubmed
    ..Taking into consideration the high safety profile of the product and the total absence of adverse effects observed during and after the trial, MonCam appears to be a safe and effective tool for weight loss. ..
  15. Kim M, Kim H. Perilla leaf extract ameliorates obesity and dyslipidemia induced by high-fat diet. Phytother Res. 2009;23:1685-90 pubmed publisher
    ..These results suggest that the PLE supplement suppressed body weight gain and improved the blood lipid profiling, in part by down-regulating adipogenic transcription factor and other specific target genes...
  16. An S, Han J, Kim M, Park J, Han J, Baek N, et al. Ethanolic extracts of Brassica campestris spp. rapa roots prevent high-fat diet-induced obesity via beta(3)-adrenergic regulation of white adipocyte lipolytic activity. J Med Food. 2010;13:406-14 pubmed publisher
    ..These results suggest that EBR may have potential as a safe and effective anti-obesity agent via the inhibition of adipocyte lipid accumulation and the stimulation of beta(3)-AR-dependent lipolysis. ..
  17. Tziomalos K, Dimitroula H, Katsiki N, Savopoulos C, Hatzitolios A. Effects of lifestyle measures, antiobesity agents, and bariatric surgery on serological markers of inflammation in obese patients. Mediators Inflamm. 2010;2010:364957 pubmed publisher
  18. Teta D. Weight loss in obese patients with chronic kidney disease: who and how?. J Ren Care. 2010;36 Suppl 1:163-71 pubmed publisher
    ..Bariatric surgery should be carried out by experienced surgeons due to the high risk of complications. For obese patients who are not considered transplant candidates the benefits of weight loss remain uncertain. ..
  19. Dahl C, Allen M, Urie P, Hopkins P. Valvular regurgitation and surgery associated with fenfluramine use: an analysis of 5743 individuals. BMC Med. 2008;6:34 pubmed publisher
    ..We performed an observational study of 5743 users of fenfluramines examined by echocardiography between July 1997 and February 2004 in a single large cardiology clinic...
  20. Yamada Y, Kato T, Ogino H, Ashina S, Kato K. Cetilistat (ATL-962), a novel pancreatic lipase inhibitor, ameliorates body weight gain and improves lipid profiles in rats. Horm Metab Res. 2008;40:539-43 pubmed publisher
    ..These results suggest that cetilistat ameliorates obesity and hyperlipidemia in DIO rats, a plausible animal model of the most common type of human obesity. ..
  21. August G, Caprio S, Fennoy I, Freemark M, Kaufman F, Lustig R, et al. Prevention and treatment of pediatric obesity: an endocrine society clinical practice guideline based on expert opinion. J Clin Endocrinol Metab. 2008;93:4576-99 pubmed publisher
  22. Jensen G. Drug-induced hyperphagia: what can we learn from psychiatric medications?. JPEN J Parenter Enteral Nutr. 2008;32:578-81 pubmed publisher
    ..Better understanding of the underlying mechanisms can guide useful interventions. Medication selection and dosing appear to be important strategies to minimize adverse weight gain. ..
  23. . Influence of body mass index on prescribing costs and potential cost savings of a weight management programme in primary care. J Health Serv Res Policy. 2008;13:158-66 pubmed publisher
  24. Beck E, Esser N, Paquot N, Scheen A. [Metabolically obese normal-weight individuals and metabolically healthy, but obese, subjects]. Rev Med Suisse. 2009;5:1644-6, 1648-9 pubmed
  25. Di Marco M, Marier J, Ducharme M, Morin I, Engel C, Gulbranson S, et al. Pharmacodynamic equivalence of two orlistat capsule formulations in healthy volunteers under fed conditions. Int J Clin Pharmacol Ther. 2008;46:319-26 pubmed
    ..Results from this study suggest that pharmacodynamics of the generic capsule formulation of orlistat were similar to the marketed capsule formulation based on FFE(24) values. ..
  26. Kim N, Choi S, Kim S, Moon P, Lim H, Choi I, et al. Green tea seed oil reduces weight gain in C57BL/6J mice and influences adipocyte differentiation by suppressing peroxisome proliferator-activated receptor-gamma. Pflugers Arch. 2008;457:293-302 pubmed publisher
    ..These results indicate that the anti-obesity effects of green tea seed oil might be, in part, through suppression of transcription factors related to adipocyte differentiation. ..
  27. Khan U, Collier M. Medical interventions in adolescent obesity. Adolesc Med State Art Rev. 2008;19:406-20, viii pubmed
    ..Pharmacologic agents should be used carefully as adjuncts, but long-term studies regarding their efficacy in sustaining weight loss are not available in adolescents. ..
  28. Del Mar Romero M, Fernández López J, Alemany M, Esteve M. Gene expression modulation of liver energy metabolism by oleoyl-oestrone in overweight rats. Biosci Rep. 2009;30:81-9 pubmed publisher
  29. Zhang G, Wujcik C. Overcoming ionization effects through chromatography: a case study for the ESI-LC-MS/MS quantitation of a hydrophobic therapeutic agent in human serum using a stable-label internal standard. J Chromatogr B Analyt Technol Biomed Life Sci. 2009;877:2003-10 pubmed publisher
    ..The successful validation of this method demonstrates the value of investigating minor chromatographic changes to remediate detrimental ionization effects without further altering extraction procedures. ..
  30. de Kloet A, Woods S. Minireview: Endocannabinoids and their receptors as targets for obesity therapy. Endocrinology. 2009;150:2531-6 pubmed publisher
    ..Although clinical trials with CB1 antagonists have yielded beneficial metabolic effects, concerns about negative affect have limited the therapeutic potential of the first class of CB1 antagonists available. ..
  31. Cannon C. Cardiovascular disease and modifiable cardiometabolic risk factors. Clin Cornerstone. 2008;9:24-38; discussion 39-41 pubmed
    ..The new agents have the potential to significantly improve several CVD risk factors with a single medication and may provide clinicians with several new strategies to reduce the long-term risk of CVD. ..
  32. Ahn J, Lee H, Kim S, Park J, Ha T. The anti-obesity effect of quercetin is mediated by the AMPK and MAPK signaling pathways. Biochem Biophys Res Commun. 2008;373:545-9 pubmed publisher
  33. Cook D. Adult obesity 2: treatment and management options for weight loss and maintenance. Nurs Times. 2009;105:24-6 pubmed
    ..This part outlines management options, including dietary change, physical activity, pharmacotherapy and surgery. The issue of how to maintain weight once lost is also examined. ..
  34. Martins F, Noso T, Porto V, Curiel A, Gambero A, Bastos D, et al. Maté tea inhibits in vitro pancreatic lipase activity and has hypolipidemic effect on high-fat diet-induced obese mice. Obesity (Silver Spring). 2010;18:42-7 pubmed publisher
    ..6 +/- 3.9 to 95.6 +/- 6.1 mg/g of tissue; P < 0.05). These results suggest that MT could be a potentially therapeutic alternative in the treatment of obesity caused by a HFD. ..
  35. Romero M, Vila R, Fernandez Lopez J, Esteve M, Alemany M. Influence of oleoyl-estrone treatment on circulating testosterone. Role of 17beta-hydroxysteroid dehydrogenase isoenzymes. J Physiol Pharmacol. 2009;60:181-90 pubmed
    ..In consequence, we can assume that OE effects on androgens, and the hypothalamic-pituitary-gonadal axis are limited to testicles. ..
  36. Ross R, Bradshaw A. The future of obesity reduction: beyond weight loss. Nat Rev Endocrinol. 2009;5:319-25 pubmed publisher
    ..Clinicians could encourage positive lifestyle changes in their patients by counseling them that obesity and its associated health risks can be reduced in response to an increase in physical activity with or without weight loss. ..
  37. Baxter J, Webb P. Thyroid hormone mimetics: potential applications in atherosclerosis, obesity and type 2 diabetes. Nat Rev Drug Discov. 2009;8:308-20 pubmed publisher
    ..Such drugs could serve as powerful new tools to address two of the largest medical problems in developed countries--atherosclerosis and obesity. ..
  38. Gagnon A, Landry A, Sorisky A. IKKbeta and the anti-adipogenic effect of platelet-derived growth factor in human abdominal subcutaneous preadipocytes. J Endocrinol. 2009;201:75-80 pubmed publisher
    ..Our data describe a novel PDGF response in human preadipocytes that involves the pro-inflammatory kinase IKKbeta and demonstrate that it is required for the inhibition of adipogenesis. ..
  39. Shakya N, Roy K, Saxena A. Substituted 1,2,3,4-tetrahydroquinolin-6-yloxypropanes as beta3-adrenergic receptor agonists: design, synthesis, biological evaluation and pharmacophore modeling. Bioorg Med Chem. 2009;17:830-47 pubmed publisher
    ..A putative pharmacophore model has been modeled considering the above four active molecules which distinguishes well between the active and inactive molecules. ..
  40. Yao Y, Li X, Zhao W, Zeng Y, Shen H, Xiang H, et al. Anti-obesity effect of an isoflavone fatty acid ester on obese mice induced by high fat diet and its potential mechanism. Lipids Health Dis. 2010;9:49 pubmed publisher
    ..In order to investigate the anti-obesity effect of compound 1a and its potential mechanism of influence in adipocyte differentiation, Obese male C57BL/6J mice induced by high-fat diet (HFD) and rat preadipocytes (3T3-L1 cell) were used...
  41. Bischoff A. [Struggle about the best reducing diet, Fat gone by means of more fat?]. MMW Fortschr Med. 2004;146:4-6 pubmed
  42. de Castro J, Dias T, Chambel P, Carvalheiro M, Correia L, Guerreiro L, et al. A randomized double-blind study comparing the efficacy and safety of orlistat versus placebo in obese patients with mild to moderate hypercholesterolemia. Rev Port Cardiol. 2009;28:1361-74 pubmed
    ..Treatment with orlistat plus a reduced calorie diet for 6 months achieved significant reductions in weight, BMI and lipid parameters. ..
  43. Date H, Toyota A, Terauchi M, Sugimura M, Matsuo T, Mochiike C. [Rapid determination of medical components found in the health food for weight loss by liquid chromatography/tandem mass spectrometry (LC/MS/MS)]. Yakugaku Zasshi. 2008;128:811-7 pubmed
    ..3-114% and each coefficient of variation was 13.7% or less. It was confirmed that this method is applicable to the urgent analysis of health foods that have caused damage to health. ..
  44. Forrester M. Redotex ingestions reported to Texas poison centers. Hum Exp Toxicol. 2010;29:789-91 pubmed publisher
    ..8%, not followed but minimal clinical effects possible in 47.1%, and unable to follow but judged to be potentially toxic in 11.8%. Most Redotex calls to the Texas poison center system originated from counties bordering Mexico. ..
  45. Svacina S. [Treatment of an obese diabetic]. Vnitr Lek. 2010;56:1078-81 pubmed
    ..We thus have a sufficient range of options available for weight reduction in diabetic patients. ..
  46. Supuran C, Di Fiore A, De Simone G. Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008;13:383-92 pubmed
    ..The use of topiramate and zonisamide as lead molecules for the design of CA inhibitors targeting isozymes involved in lipogenesis could represent the beginning of a very promising new approach for the treatment of obesity. ..
  47. Ando M, Sekino E, Haga Y, Moriya M, Ito M, Ito J, et al. Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists. Bioorg Med Chem Lett. 2009;19:5186-90 pubmed publisher
    ..Successive optimization of the right-hand moiety led to the identification of a number of potent derivatives. ..
  48. Kelsall D. Editor's response. Can Fam Physician. 2008;54:850-1 pubmed
  49. Moya M. An update in prevention and treatment of pediatric obesity. World J Pediatr. 2008;4:173-85 pubmed publisher
    ..Treatment of obesity should never be postponed whatever the clinical care is. ..
  50. Kim J, Kim Y, Jeun J, Choi D, Shin C. L-Trp and L-Leu-OEt derivatives of the monascus pigment exert high anti-obesity effects on mice. Biosci Biotechnol Biochem. 2010;74:304-8 pubmed
    ..An in vivo test with mice showed the L-Trp derivative to have higher anti-obesity effects than the L-Leu-OEt derivative. ..
  51. Belcaro G, Cesarone M, Silvia E, Ledda A, Stuard S, G V, et al. Daily consumption of Reliv Glucaffect for 8 weeks significantly lowered blood glucose and body weight in 50 subjects. Phytother Res. 2009;23:1673-7 pubmed publisher
    ..3 kg (BMI 24.5 kg/m2) as compared to the control group. In conclusion, Glucaffect enabled subjects with metabolic syndrome to achieve healthy BMI and blood glucose levels. Glucaffect was well tolerated and no subject dropped out. ..
  52. Astrup A, Madsbad S, Breum L, Jensen T, Kroustrup J, Larsen T. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet. 2008;372:1906-1913 pubmed publisher
    ..0001). Our results suggest that tesofensine 0.5 mg might have the potential to produce a weight loss twice that of currently approved drugs. However, these findings of efficacy and safety need confirmation in phase III trials. ..
  53. Canals I, Carmona M, Amigó M, Barbera A, Bortolozzi A, Artigas F, et al. A functional leptin system is essential for sodium tungstate antiobesity action. Endocrinology. 2009;150:642-50 pubmed publisher
    ..In summary, the results indicate that the effectiveness of tungstate in reducing body weight gain is completely dependent on a functional leptin system...