Investigational Drug Details
Drug ID: | D377 |
Drug Name: | Cilazapril |
Synonyms: | |
Type: | small molecule |
DrugBank ID: | DB01340 |
DrugBank Description: | Cilazapril is an ACE inhibtor class drug used in the treatment of hypertension and heart failure. It belongs to the angiotensin-converting enzyme inhibitors (ACE inhibitors) class of drugs. It is a prodrug that is hydrolyzed after absorption to its main metabolite cilazaprilat. It is branded as Inhibace in Canada and other countries, Vascace and Dynorm in a number of European countries, among many other names. None of these varieties are available in the United States. |
PubChem ID: | 56330 |
CasNo: | 88768-40-5 |
Repositioning for NAFLD: | Yes |
SMILES: | CCOC(=O)[C@H](CCC1=CC=CC=C1)N[C@H]1CCCN2CCC[C@H](N2C1=O)C(O)=O |
Structure: |
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InChiKey: | HHHKFGXWKKUNCY-FHWLQOOXSA-N |
Molecular Weight: | 417.4986 |
DrugBank Targets: | Angiotensin-converting enzyme |
DrugBank MoA: | Cilazapril is a pyridazine ACE inhibitor. It competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. As angiotensin II is a vasoconstrictor and a negative feedback mediator for renin activity, lower angiotensin II levels results in a decrease in blood pressure, an increase in renin activity, and stimulation of baroreceptor reflex mechanisms. Kininase II, an enzyme which degrades the vasodilator bradykinin, is identical to ACE and may also be inhibited. |
DrugBank Pharmacology: | Cilazapril inhibits the production angiotensin II. By doing so, it decreases sodium and water reabsorption (via aldosterone) and it decreases vasoconstriction. The combined effect of this is a decrease in vascular resistance, and therefore, blood pressure. The absolute bioavailability of cilazaprilat after oral administration of cilazapril is 57% based on urinary recovery data. (The absolute bioavailability of cilazaprilat after oral administration of cilazaprilat is 19%.) Ingestion of food immediately before the administration of cilazapril reduces the average peak plasma concentration of cilazaprilat by 29%, delays the peak by one hour and reduces the bioavailability of cilazaprilat by 14%. These pharmacokinetic changes have little influence on plasma ACE inhibition. |
DrugBank Indication: | Cilazapril is an ACE inhibtor class drug used in the treatment of hypertension and heart failure. |
Targets: | |
Therapeutic Category: | |
Clinical Trial Progress: | |
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