Investigational Drug Details
| Drug ID: | D252 |
| Drug Name: | Eprosartan |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00876 |
| DrugBank Description: | Eprosartan is an angiotensin II receptor antagonist used to treat hypertension. It performs 2 actions on the renin angiotensin system. By preventing the binding of angiotensin II to AT1, vascular smooth muscle relaxes and vasodilation occurs. By inhibiting norepinephrine production, blood pressure is further reduced. |
| PubChem ID: | 5281037 |
| CasNo: | 133040-01-4 |
| Repositioning for NAFLD: | Yes |
| SMILES: | CCCCC1=NC=C(\C=C(/CC2=CC=CS2)C(O)=O)N1CC1=CC=C(C=C1)C(O)=O |
| Structure: |
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| InChiKey: | OROAFUQRIXKEMV-LDADJPATSA-N |
| Molecular Weight: | 424.513 |
| DrugBank Targets: | Type-1 angiotensin II receptor |
| DrugBank MoA: | Eprosartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT<sub>1</sub> receptor found in many tissues (e.g., vascular smooth muscle, adrenal gland). There is also an AT<sub>2</sub> receptor found in many tissues but it is not known to be associated with cardiovascular homeostasis. Eprosartan does not exhibit any partial agonist activity at the AT<sub>1</sub> receptor. Its affinity for the AT<sub>1</sub> receptor is 1,000 times greater than for the AT<sub>2</sub> receptor. In vitro binding studies indicate that eprosartan is a reversible, competitive inhibitor of the AT<sub>1</sub> receptor. Eprosartan has also been shown to bind to AT<sub>1</sub> receptors both presynaptically and synaptically. Its action on presynaptic AT<sub>1</sub> receptors results in the inhibition of sympathetically stimulated noradrenaline release. Unlike ACE inhibitors, eprosartan and other ARBs do not interfere with response to bradykinins and substance P, which allows for the absence of adverse effects that are present in ACE inhibitors (eg. dry cough). |
| DrugBank Pharmacology: | Angiotensin II, the principal pressor agent of the renin-angiotensin system, is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme [kininase II]. It is responsible for effects such as vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Eprosartan selectively blocks the binding of angiotensin II to the AT<sub>1</sub> receptor, which in turn leads to multiple effects including vasodilation, a reduction in the secretion of vasopressin, and reduction in the production and secretion of aldosterone. The resulting effect is a decrease in blood pressure. |
| DrugBank Indication: | For the management of hypertension alone or in combination with other classes of antihypertensive agents. Also used as a first-line agent in the treatment of diabetic nephropathy, as well as a second-line agent in the treatment of congestive heart failure (only in those intolerant of ACE inhibitors). |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L1037 | NCT01929109 | PHASE1 | COMPLETED | YES | 2013-08 | 2018-10-29 | Details |
| L4841 | NCT00286455 | PHASE3 | COMPLETED | YES | 2006-02 | 2012-02-03 | Details |
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