Investigational Drug Details
| Drug ID: | D332 |
| Drug Name: | Diazoxide |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB01119 |
| DrugBank Description: | A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group. |
| PubChem ID: | 3019 |
| CasNo: | 364-98-7 |
| Repositioning for NAFLD: | Yes |
| SMILES: | CC1=NS(=O)(=O)C2=C(N1)C=CC(Cl)=C2 |
| Structure: |
|
| InChiKey: | GDLBFKVLRPITMI-UHFFFAOYSA-N |
| Molecular Weight: | 230.671 |
| DrugBank Targets: | ATP-sensitive inward rectifier potassium channel 11; NA |
| DrugBank MoA: | As a diuretic, diazoxide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like diazoxide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of diazoxide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle. As a antihypoglycemic, diazoxide inhibits insulin release from the pancreas, probably by opening potassium channels in the beta cell membrane. |
| DrugBank Pharmacology: | Diazoxide is a potassium channel activator. Its mechanism of action revolves around enhancing cell membrane permeability to potassium ions. This action consequently elicits the relaxation of local smooth muscles. This switches off voltage-gated calcium ion channels which inhibits the generation of an action potential. |
| DrugBank Indication: | Used parentally to treat hypertensive emergencies. Also used to treat hypoglycemia secondary to insulinoma. |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L4966 | NCT03987802 | COMPLETED | NO | 2021-01-20 | 2024-09-23 | Details | |
| L5076 | NCT02875821 | PHASE4 | COMPLETED | NO | 2016-04-26 | 2017-06-23 | Details |
| L6241 | NCT02942056 | PHASE2 | WITHDRAWN | NO | 2017-01 | 2019-08-06 | Details |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 | |
|---|---|---|---|---|
| A00113 | 18596924 | J Clin Invest | Clinical characteristics and biochemical mechanisms of congenital hyperinsulinism associated with dominant KATP channel mutations. | Details |
| A00139 | 21536946 | Diabetes | Diazoxide-unresponsive congenital hyperinsulinism in children with dominant mutations of the β-cell sulfonylurea receptor SUR1. | Details |
| A00143 | 23275527 | J Clin Endocrinol Metab | Genotype and phenotype correlations in 417 children with congenital hyperinsulinism. | Details |
| A00155 | 25741167 | World J Gastroenterol | Hepatic phenotypes of HNF1B gene mutations: a case of neonatal cholestasis requiring portoenterostomy and literature review. | Details |
| A00159 | 26340261 | Am J Nephrol | Hypomagnesemia as First Clinical Manifestation of ADTKD-HNF1B: A Case Series and Literature Review. | Details |