Investigational Drug Details
| Drug ID: | D334 |
| Drug Name: | Tolbutamide |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB01124 |
| DrugBank Description: | Tolbutamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It is structurally similar to acetohexamide, chlorpropamide and tolazamide and belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Tolbutamide appears to be metabolized in the liver. Tolbutamide and its metabolites are excreted in urine (75-85%) and feces. |
| PubChem ID: | 5505 |
| CasNo: | 64-77-7 |
| Repositioning for NAFLD: | Yes |
| SMILES: | CCCCNC(=O)NS(=O)(=O)C1=CC=C(C)C=C1 |
| Structure: |
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| InChiKey: | JLRGJRBPOGGCBT-UHFFFAOYSA-N |
| Molecular Weight: | 270.348 |
| DrugBank Targets: | ATP-binding cassette sub-family C member 8; ATP-sensitive inward rectifier potassium channel 1 |
| DrugBank MoA: | Sulfonylureas lower blood glucose in patients with NIDDM by directly stimulating the acute release of insulin from functioning beta cells of pancreatic islet tissue by an unknown process that involves a sulfonylurea receptor (receptor 1) on the beta cell. Sulfonylureas inhibit the ATP-potassium channels on the beta cell membrane and potassium efflux, which results in depolarization and calcium influx, calcium-calmodulin binding, kinase activation, and release of insulin-containing granules by exocytosis, an effect similar to that of glucose. |
| DrugBank Pharmacology: | Tolbutamide, a first-generation sulfonylurea antidiabetic agent, is used with diet to lower blood glucose levels in patients with diabetes mellitus type II. Tolbutamide is twice as potent as the related second-generation agent glipizide. Tolbutamide lowers blood sugar by stimulating the pancreas to secrete insulin and helping the body use insulin efficiently. The pancreas must be able to produce insulin for this drug to work. |
| DrugBank Indication: | For treatment of NIDDM (non-insulin-dependent diabetes mellitus) in conjunction with diet and exercise. |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted |
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| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
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| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A00002 | 10199785 | J Clin Endocrinol Metab | Heritability of pancreatic beta-cell function among nondiabetic members of Caucasian familial type 2 diabetic kindreds. | Details |
| A00083 | 16885549 | N Engl J Med | Activating mutations in the ABCC8 gene in neonatal diabetes mellitus. | Details |
| A00185 | 32634120 | JCI Insight | The value of genotypic and imaging information to predict functional and structural outcomes in ADPKD. | Details |