| 词条 | Sacubitril |
| 释义 |
| drug_name = | IUPAC_name = 4[(2S,4R)-1-(4-Biphenylyl)-5-ethoxy-4-methyl-5-oxo-2-pentanyl]amino4-oxobutanoic acid | image = Sacubitril skeletal.svg | alt = | caption = | tradename = | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | licence_EU = yes | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | onset = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|correct|CAS}} | CAS_number = 149709-62-6 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 17ERJ0MKGI | ATCvet = 149709-62-6 | ATC_prefix = C09 | ATC_suffix = DX04 | ATC_supplemental = (combination with valsartan) | PubChem = 9811834 | DrugBank = DB09292 | ChemSpiderID = 7987587 | KEGG = D10225 | synonyms = AHU-377 | C=24 | H=29 | N=1 | O=5 | molecular_weight = 411.49 g/mol | smiles = CCOC(=O)[C@H](C)C[C@@H](CC1=CC=C(C=C1)C2=CC=CC=C2)NC(=O)CCC(=O)O | StdInChI = 1S/C24H29NO5/c1-3-30-24(29)17(2)15-21(25-22(26)13-14-23(27)28)16-18-9-11-20(12-10-18)19-7-5-4-6-8-19/h4-12,17,21H,3,13-16H2,1-2H3,(H,25,26)(H,27,28)/t17-,21+/m1/s1 | StdInChIKey = PYNXFZCZUAOOQC-UTKZUKDTSA-N }} Sacubitril ({{IPAc-en|s|ə|ˈ|k|juː|b|ᵻ|t|r|ɪ|l}}; INN) is an antihypertensive drug used in combination with valsartan. The combination drug sacubitril/valsartan, known during trials as LCZ696 and marketed under the brand name Entresto, is a treatment for heart failure. It was approved under the FDA's priority review process for use in heart failure on July 7, 2015. Mechanism of actionSacubitril is a prodrug that is activated to sacubitrilat (LBQ657) by de-ethylation via esterases.[2] Sacubitrilat inhibits the enzyme neprilysin,[3] which is responsible for the degradation of atrial and brain natriuretic peptide, two blood pressure-lowering peptides that work mainly by reducing blood volume.[4] In addition, neprilysin degrades a variety of peptides including bradykinin,[1] an inflammatory mediator exerting potent vasodilatory action. {{clear left}}See also
References1. ^{{cite web | title = Entrez Gene: Membrane metallo-endopeptidase | url = https://www.ncbi.nlm.nih.gov/gene/4311 }} [2][3][4]2. ^1 {{Cite journal | last1 = Gu | first1 = J. | last2 = Noe | first2 = A. | last3 = Chandra | first3 = P. | last4 = Al-Fayoumi | first4 = S. | last5 = Ligueros-Saylan | first5 = M. | last6 = Sarangapani | first6 = R. | last7 = Maahs | first7 = S. | last8 = Ksander | first8 = G. | last9 = Rigel | first9 = D. F. | doi = 10.1177/0091270009343932 | last10 = Jeng | first10 = A. Y. | last11 = Lin | first11 = T. H. | last12 = Zheng | first12 = W. | last13 = Dole | first13 = W. P. | title = Pharmacokinetics and Pharmacodynamics of LCZ696, a Novel Dual-Acting Angiotensin Receptor-Neprilysin Inhibitor (ARNi) | journal = The Journal of Clinical Pharmacology | volume = 50 | issue = 4 | pages = 401–414 | year = 2009 | pmid = 19934029 | pmc = }} 3. ^1 {{Cite document|last1=Schubert-Zsilavecz|first1=M|last2=Wurglics|first2=M|title=Neue Arzneimittel 2010/2011.|language=German|postscript={{inconsistent citations}}}} 4. ^1 {{cite web|url=http://spo.escardio.org/eSlides/view.aspx?eevtid=46&fp=13|title=HFpEF in the Future: New Diagnostic Techniques and Treatments in the Pipeline|last=Solomon|first=SD|location=Boston|page=48|accessdate=2012-01-26}} }}{{Peptidergics}}{{cardiovascular-drug-stub}} 5 : Antihypertensive agents|Biphenyls|Carboxylic acid derivatives|Ethyl esters|Prodrugs |
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