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Sacubitril
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(Difference between revisions)
(New page: <StructureSection load='' size='340' side='right' caption='Caption for this structure' scene=''> Sacubitril is an antihypertensive drug used in combination with valsartan. The combination ...) |
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| - | <StructureSection load='' size='340' side='right' caption=' | + | <StructureSection load='' size='340' side='right' caption='Sacubitril' scene='10/1001143/Cv/1'> |
| - | Sacubitril 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. See also [https://en.wikipedia.org/wiki/Sacubitril Sacubitril]. | + | Sacubitril 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. See also [https://en.wikipedia.org/wiki/Sacubitril Sacubitril]. |
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| + | Sacubitril is a prodrug that is activated to sacubitrilat (LBQ657) by de-ethylation via esterases.<ref name="a2">Solomon SD. [https://esc365.escardio.org/home "HFpEF in the Future: New Diagnostic Techniques and Treatments in the Pipeline".] Boston. p. 48. Retrieved 2012-01-26</ref> Sacubitrilat inhibits the enzyme [[neprilysin]],<ref name="a3">PMID:19934029</ref> which is responsible for the degradation of atrial and brain natriuretic peptide, two blood pressure–lowering peptides that work mainly by reducing blood volume. | ||
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| + | <scene name='10/1001143/Overall/1'>NEPRILYSIN COMPLEXED WITH Sacubitrilat</scene> ([[5jmy]]). | ||
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| + | <scene name='10/1001143/Binding_site/1'>Sacubitrilat binding site</scene>. Water molecules are shown as red spheres. | ||
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| + | <scene name='10/1001143/Zn_coord/1'>Zn coordination site</scene>. | ||
</StructureSection> | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||
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References
- ↑ 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 DF, Jeng AY, Lin TH, Zheng W, Dole WP. Pharmacokinetics and pharmacodynamics of LCZ696, a novel dual-acting angiotensin receptor-neprilysin inhibitor (ARNi). J Clin Pharmacol. 2010 Apr;50(4):401-14. PMID:19934029 doi:10.1177/0091270009343932
