Investigational Drug Details
| Drug ID: | D333 |
| Drug Name: | Sibutramine |
| Synonyms: | Sibutramine |
| Type: | Chemical drug |
| DrugBank ID: | DB01105 |
| DrugBank Description: | Sibutramine (trade name Meridia in the USA, Reductil in Europe and other countries), usually as sibutramide hydrochloride monohydrate, is an orally administered agent for the treatment of obesity. It is a centrally acting stimulant chemically related to amphetamines thus it is classified as a Schedule IV controlled substance in the United States. In October 2010, Sibutramine was withdrawn from Canadian and U.S. markets due to concerns that the drug increases the risk of heart attack and stroke in patients with a history of heart disease. |
| PubChem ID: | 5210 |
| CasNo: | 106650-56-0 |
| Repositioning for NAFLD: | Yes |
| SMILES: | C(CC(C)C)(N(C)C)C1(CCC1)c1ccc(cc1)Cl |
| Structure: |
|
| InChiKey: | UNAANXDKBXWMLN-UHFFFAOYSA-N |
| Molecular Weight: | 279.855 |
| DrugBank Targets: | Sodium-dependent noradrenaline transporter inhibitor; Sodium-dependent serotonin transporter inhibitor; Sodium-dependent dopamine transporter inhibitor |
| DrugBank MoA: | Sibutramine produces its therapeutic effects by inhibition of norepinephrine (NE), serotonin (5-hydroxytryptamine, 5-HT), and to a lesser extent, dopamine reuptake at the neuronal synapse. By inhibiting the reuptake of these neurotransmitters, sibutramine promotes a sense of satiety and decrease in appetite, thereby reducing food intake. Data from animal studies also suggest that sibutramine may also increase energy expenditure through thermogenic effects in both the basal and fed states, but this has not been confirmed in humans. Sibutramine and its major pharmacologically active metabolites (M1 and M2) do not act via release of monoamines. |
| DrugBank Pharmacology: | Sibutramine is an orally administered agent for the treatment of obesity. Sibutramine exerts its pharmacological actions predominantly via its secondary (M1) and primary (M2) amine metabolites. The parent compound, sibutramine, is a potent inhibitor of serotonin and norepinephrine reuptake <i>in vivo</i>, but not <i>in vitro</i>. However, metabolites M1 and M2 inhibit the reuptake of these neurotransmitters both <i>in vitro</i> and <i>in vivo</i>. In human brain tissue, M1 and M2 also inhibit dopamine reuptake <i>in vitro</i>, but with ~3-fold lower potency than for the reuptake inhibition of serotonin or norepinephrine. Sibutramine, M1 and M2 exhibit no evidence of anticholinergic or antihistaminergic actions. In addition, receptor binding profiles show that sibutramine, M1 and M2 have low affinity for serotonin (5-HT<sub>1</sub>, 5-HT<sub>1A</sub>, 5-HT<sub>1B</sub>, 5-HT<sub>2A</sub>, 5-HT<sub>2C</sub>), norepinephrine (b, b1, b3, a1 and a2), dopamine (D1 and D2), benzodiazepine, and glutamate (NMDA) receptors. These compounds also lack monoamine oxidase inhibitory activity <i>in vitro</i> and <i>in vivo</i>. |
| DrugBank Indication: | For the treatment of obesity. |
| Targets: | -- |
| Therapeutic Category: | -- |
| Clinical Trial Progress: | Clinical trial on-going (IRCT201012275483N1) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0957 | IRCT201012275483N1 | Not applicable | Not Recruiting | No Results Available | 28/01/2011 | 22 February 2018 | Details |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
|---|
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A16464 | 28372259 | Biomed Pharmacother | Medicinal plants and phytochemicals with anti-obesogenic potentials: A review. | Details |
| A18313 | 27219496 | Endocr Pract | AMERICAN ASSOCIATION OF CLINICAL ENDOCRINOLOGISTS AND AMERICAN COLLEGE OF ENDOCRINOLOGY COMPREHENSIVE CLINICAL PRACTICE GUIDELINES FOR MEDICAL CARE OF PATIENTS WITH OBESITY. | Details |
| A26054 | 21160985 | World J Hepatol | Combination drug treatment in patients with non-alcoholic fatty liver disease. | Details |
| A26478 | 20415685 | Diabetes Obes Metab | The role of adiponectin in the pathogenesis and treatment of non-alcoholic fatty liver disease. | Details |
| A27087 | 19199918 | Curr Med Chem | Obesity: pathophysiology and clinical management. | Details |
| A28062 | 16540766 | J Clin Gastroenterol | Weight loss as a treatment for nonalcoholic fatty liver disease. | Details |
| A28283 | 15811215 | Curr Med Res Opin | A review of the metabolic effects of sibutramine. | Details |
| A37841 | 14502318 | Rom J Gastroenterol | The effects of sibutramine and orlistat on the ultrasonographic findings, insulin resistance and liver enzyme levels in obese patients with non-alcoholic steatohepatitis. | Details |
| A46864 | 12230315 | Semin Gastrointest Dis | Medical management of obesity. | Details |
| A52961 | 18773755 | G Ital Cardiol (Rome) | [Pharmacological therapy of obesity]. | Details |