A minireview of the current status of potential weight loss approaches that …

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- Addressing the Unmet Medical Need for Safe and Effective Weight Loss Therapies

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Table 1. Antiobesity therapeutics in development: appetite suppression via central nervous system action

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Table 2. Antiobesity therapeutics in development: gastrointestinal tract-signaling peptides, digestive enzyme targets

Pharmacological target Company Compound Development status -Glucosidase inhibitor, inhibits carbohydrate digestion and absorption Bayer/Pfizer (licensee, U.S.)/Sanofi-Synthelabo (licensee, European Union)/Sanwa Kagaku Kenkyusho (licensee, Japan) Miglitol Marketed for type 2 diabetes as Diastabol, Glyset, Miglibay, Plumarol Phase II for obesity in patients with type 2 diabetes Synthetic human amylin analog that acts as a gut-signaling peptide, prevents the abnormal rise in glucagon after meals, slows the rate of gastric emptying, and reduces postprandial glucose peaks Amylin Pharma Pramlintide/Symlin Preregistration for type 1 and type 2 diabetes Phase II for obesity indication Glucagon-like peptide peptide mimetic of GLP-17–36 amide, a peptide produced by the intestine, that stimulates insulin secretion in response to an increase in blood glucose, slows gastric emptying, and provides a satiety signal to the central nervous system Amylin Pharma/Lilly (licensee) Exenatide (AC2993) Phase III for type 2 diabetes Preclinical for obesity Exenatide-LAR (AC2993LAR) Phase II NovoNordisk Liraglutide (NN2211) Phase II for type 2 diabetes Preclinical for obesity indication Biomeasure, Ipsen/Roche (licensee) BIM 51077 Phase II for type 2 diabetes Zealand Pharma/Aventis (licensee) AVE0010 Phase II for type 2 diabetes ConjuChem CJC-1131 Phase II for type 2 diabetes Human Genome Sciences Albugon Preclinical Theratechnologies TH0318 Preclinical Genzyme GLP-1 gene therapy Research Pancreatic lipase inhibitor, inhibits fat digestion and absorption Alizyme/Takeda (licensee for Japan) ATL962 Phase II CCK-A agonist, provides a satiety signal to the central nervous system GSK 181771 Phase II Sanofi-Synthelabo SR146131 Phase I SR125180 Phase I Undisclosed target, decreases gastric emptying, provides a satiety signal to the central nervous system Aventis Pharma HMR1426 Phase II HMR1954 Phase I Dipeptidyl peptidase IV inhibitor, prevents the inactivation of GLP-1, prolonging its action Novartis NVP LAF237 Phase III for type 2 diabetes Merck MK431 Phase II for type 2 diabetes Tanabe/GSK (licensee) T6666/815541A, 825964, 823093 Phase I for type 2 diabetes BMS BMS 477119 Phase I for type 2 diabetes Several including Ferring/J&J (licensee), Kyowa Haako, Sanofi-Synthelabo, PPD/Syrrx, Graffinity Pharma Preclinical PYY3–36 receptor agonist, PYY3–36 is a naturally occurring intestinal peptide that provides a satiety signal to central nervous system Nastech PYY3–36 (intranasal) Phase I Curis/Amylin Pharma (licensee) AC162352 Preclinical Dual acting pancreatic lipase inhibitor and fat binding polymer, inhibits fat digestion and absorption without oil leakage Genzyme/Peptimmune (licensee) GT389-255 Phase I Ghrelin antagonist, inhibits the action of ghrelin, a natural peptide hormone produced by the stomach that increases appetite Zenteris Preclinical

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Table 3. Antiobesity therapeutics in development: metabolic regulators

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