Repositioning Candidate Details
| Candidate ID: | R0372 |
| Source ID: | DB01275 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Hydralazine |
| Synonyms: | |
| Molecular Formula: | C8H8N4 |
| SMILES: | NNC1=NN=CC2=CC=CC=C12 |
| Structure: |
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| DrugBank Description: | Originally developed in the 1950s as a malaria treatment, hydralazine showed antihypertensive ability and was soon repurposed.[A186841] Hydralazine is a hydrazine derivative vasodilator used alone or as adjunct therapy in the treatment of hypertension and only as adjunct therapy in the treatment of heart failure.[A186820,L8782,L8785] Hydralazine is no longer a first line therapy for these indications since the development of newer antihypertensive medications.[T691] Hydralazine hydrochloride was FDA approved on 15 January 1953.[L8779] |
| CAS Number: | 86-54-4 |
| Molecular Weight: | 160.1759 |
| DrugBank Indication: | Hydralazine is indicated alone or adjunct to standard therapy to treat essential hypertension.[L8782] A combination product with isosorbide dinitrate is indicated as an adjunct therapy in the treatment of heart failure.[L8785] |
| DrugBank Pharmacology: | Hydralazine interferes with calcium transport to relax arteriolar smooth muscle and lower blood pressure.[L8782] Hydralazine has a short duration of action of 2-6h.[A186820] This drug has a wide therapeutic window, as patients can tolerate doses of up to 300mg.[L8782] Patients should be cautioned regarding the risk of developing systemic lupus erythematosus syndrome.[L8782] |
| DrugBank MoA: | Hydralazine may interfere with calcium transport in vascular smooth muscle by an unknown mechanism to relax arteriolar smooth muscle and lower blood pressure.[A186820,A13596] The interference with calcium transport may be by preventing influx of calcium into cells, preventing calcium release from intracellular compartments, directly acting on actin and myosin, or a combination of these actions.[A186829] This decrease in vascular resistance leads to increased heart rate, stroke volume, and cardiac output.[L8782] Hydralazine also competes with protocollagen prolyl hydroxylase (CPH) for free iron.[A13596] This competition inhibits CPH mediated hydroxylation of HIF-1α, preventing the degradation of HIF-1α.[A13596] Induction of HIF-1α and VEGF promote proliferation of endothelial cells and angiogenesis.[A13596] |
| Targets: | Membrane primary amine oxidase; Hypoxia-inducible factor 1-alpha; Prolyl 4-hydroxylase subunit alpha-1 |
| Inclusion Criteria: |
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