Sacubitril
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| Clinical data | |
|---|---|
| ATC code | C09DX04 (WHO) (combination with valsartan) |
| Identifiers | |
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| Synonyms | AHU-377; AHU377 |
| CAS Number | 149709-62-6 |
| PubChem (CID) | 9811834 |
| DrugBank | DB09292 |
| ChemSpider | 7987587 |
| KEGG | D10225 |
| Chemical and physical data | |
| Formula | C24H29NO5 |
| Molar mass | 411.49 g/mol |
| 3D model (Jmol) | Interactive image |
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| |
Sacubitril (/səˈkjuːbᵻtrɪl/;[1] INN developmental code name AHU-377) is an antihypertensive drug used in combination with valsartan. The combination drug valsartan/sacubitril, known during trials as LCZ696 and marketed under the brand name Entresto, is a treatment for heart failure.[2] It was approved under the FDA's priority review process for use in heart failure on July 7, 2015.
Mechanism of action
Sacubitril activation to sacubitrilat
Sacubitril is a prodrug that is activated to sacubitrilat (LBQ657) by de-ethylation via esterases.[3] Sacubitrilat inhibits the enzyme neprilysin,[4] which is responsible for the degradation of atrial and brain natriuretic peptide, two blood pressure-lowering peptides that work mainly by reducing blood volume.[5]
See also
References
- ↑ "sacubitril - Dictiome pronunciation database". Dictiome. Retrieved 19 April 2016.
- ↑ John J.V. McMurray, Milton Packer, Akshay S. Desai, et al. for the PARADIGM-HF Investigators and Committees (August 30, 2014). "Angiotensin–Neprilysin Inhibition versus Enalapril in Heart Failure". N Engl J Med. 371: 993–1004. doi:10.1056/NEJMoa1409077. PMID 25176015.
- ↑ Solomon, SD. "HFpEF in the Future: New Diagnostic Techniques and Treatments in the Pipeline". Boston. p. 48. Retrieved 2012-01-26.
- ↑ Gu, J.; Noe, A.; Chandra, P.; Al-Fayoumi, S.; Ligueros-Saylan, M.; Sarangapani, R.; Maahs, S.; Ksander, G.; Rigel, D. F.; Jeng, A. Y.; Lin, T. H.; Zheng, W.; Dole, W. P. (2009). "Pharmacokinetics and Pharmacodynamics of LCZ696, a Novel Dual-Acting Angiotensin Receptor-Neprilysin Inhibitor (ARNi)". The Journal of Clinical Pharmacology. 50 (4): 401–414. doi:10.1177/0091270009343932. PMID 19934029.
- ↑ Schubert-Zsilavecz, M; Wurglics, M. "Neue Arzneimittel 2010/2011." (in German)
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