Peringatan Keamanan

The most common adverse reactions (?5%) are hypotension, hyperkalemia, cough, dizziness, and renal failure.

Sacubitril

DB09292

small molecule approved

Deskripsi

Sacubitril is a prodrug neprilysin inhibitor used in combination with valsartan to reduce the risk of cardiovascular events in patients with chronic heart failure (NYHA Class II-IV) and reduced ejection fraction. It was approved by the FDA after being given the status of priority review for on July 7, 2015.

Sacubitril's active metabolite, LBQ657 inhibits neprilysin, a neutral endopeptidase that would typically cleave natiuretic peptides such as atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), and c-type natriuretic peptide (CNP). ANP and BNP are released under atrial and ventricle stress, which activate downstream receptors leading to vasodilation, natriuresis and diuresis. Under normal conditions, neprilysin breaks down other vasodilating peptides and also vasoconstrictors such as angiotensin I and II, endothelin-1 and peptide amyloid beta-protein. Inhibition of neprilysin therefore leads to reduced breakdown and increased concentration of endogenous natriuretic peptides in addition to increased levels of vasoconstricting hormones such as angiotensin II.

Struktur Molekul 2D

Berat 411.498
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of sacubitril is 1.1 to 3.6 hours, and the half life of it's metabolite LBQ657 is 9.9 to 11.1 hours.
Volume Distribusi 103 L
Klirens (Clearance) -

Absorpsi

Peak plasma concentrations of sacubitril and it's metabolite, LBQ657 are reached in 0.5 hours and 2 hours respectively. Food does not clinically affect the systemic exposure of sacubitril or LBQ657. The oral bioavailability of sacubitril is >60%. It should be noted that the valsartan found in this combination is more bioavailable than other market available valsartan.

Metabolisme

Sacubitril is metabolized to LBQ657 by esterases. A low concentration (<10%) of a hydroxyl metabolite has been identified in plasma.

Rute Eliminasi

52% to 68% of sacubitril (primarily as the active metabolite LBQ657) is excreted in urine. 37% to 48% of sacubitril (primarily as LBQ657) is excreted in feces

Interaksi Obat

1014 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Sacubitril is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Sacubitril is combined with Levodopa.
Risperidone Sacubitril may increase the hypotensive activities of Risperidone.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Sacubitril.
Aripiprazole Aripiprazole may increase the hypotensive activities of Sacubitril.
Aripiprazole lauroxil Aripiprazole lauroxil may increase the hypotensive activities of Sacubitril.
Nicorandil Nicorandil may increase the hypotensive activities of Sacubitril.
Ramipril The risk or severity of angioedema can be increased when Ramipril is combined with Sacubitril.
Fosinopril The risk or severity of angioedema can be increased when Fosinopril is combined with Sacubitril.
Trandolapril The risk or severity of angioedema can be increased when Trandolapril is combined with Sacubitril.
Benazepril The risk or severity of angioedema can be increased when Benazepril is combined with Sacubitril.
Enalapril The risk or severity of angioedema can be increased when Enalapril is combined with Sacubitril.
Moexipril The risk or severity of angioedema can be increased when Moexipril is combined with Sacubitril.
Lisinopril The risk or severity of angioedema can be increased when Lisinopril is combined with Sacubitril.
Perindopril The risk or severity of angioedema can be increased when Perindopril is combined with Sacubitril.
Quinapril The risk or severity of angioedema can be increased when Quinapril is combined with Sacubitril.
Omapatrilat The risk or severity of angioedema can be increased when Omapatrilat is combined with Sacubitril.
Rescinnamine The risk or severity of angioedema can be increased when Rescinnamine is combined with Sacubitril.
Captopril The risk or severity of angioedema can be increased when Captopril is combined with Sacubitril.
Cilazapril The risk or severity of angioedema can be increased when Cilazapril is combined with Sacubitril.
Spirapril The risk or severity of angioedema can be increased when Spirapril is combined with Sacubitril.
Temocapril The risk or severity of angioedema can be increased when Temocapril is combined with Sacubitril.
Enalaprilat The risk or severity of angioedema can be increased when Enalaprilat is combined with Sacubitril.
Imidapril The risk or severity of angioedema can be increased when Imidapril is combined with Sacubitril.
Zofenopril The risk or severity of angioedema can be increased when Zofenopril is combined with Sacubitril.
Delapril The risk or severity of angioedema can be increased when Delapril is combined with Sacubitril.
Benazeprilat The risk or severity of angioedema can be increased when Benazeprilat is combined with Sacubitril.
Fosinoprilat The risk or severity of angioedema can be increased when Fosinoprilat is combined with Sacubitril.
Ramiprilat The risk or severity of angioedema can be increased when Ramiprilat is combined with Sacubitril.
Trandolaprilat The risk or severity of angioedema can be increased when Trandolaprilat is combined with Sacubitril.
Moexiprilat The risk or severity of angioedema can be increased when Moexiprilat is combined with Sacubitril.
Perindoprilat The risk or severity of angioedema can be increased when Perindoprilat is combined with Sacubitril.
Quinaprilat The risk or severity of angioedema can be increased when Quinaprilat is combined with Sacubitril.
Quinoline Yellow WS The risk or severity of angioedema can be increased when Sacubitril is combined with Quinoline Yellow WS.
Cilazaprilat The risk or severity of angioedema can be increased when Cilazaprilat is combined with Sacubitril.
Linezolid Linezolid may increase the orthostatic hypotensive activities of Sacubitril.
Furazolidone Furazolidone may increase the orthostatic hypotensive activities of Sacubitril.
Procaine Procaine may increase the orthostatic hypotensive activities of Sacubitril.
Tranylcypromine Tranylcypromine may increase the orthostatic hypotensive activities of Sacubitril.
Phenelzine Phenelzine may increase the orthostatic hypotensive activities of Sacubitril.
Minaprine Minaprine may increase the orthostatic hypotensive activities of Sacubitril.
Selegiline Selegiline may increase the orthostatic hypotensive activities of Sacubitril.
Procarbazine Procarbazine may increase the orthostatic hypotensive activities of Sacubitril.
Moclobemide Moclobemide may increase the orthostatic hypotensive activities of Sacubitril.
Isocarboxazid Isocarboxazid may increase the orthostatic hypotensive activities of Sacubitril.
Rasagiline Rasagiline may increase the orthostatic hypotensive activities of Sacubitril.
Pargyline Pargyline may increase the orthostatic hypotensive activities of Sacubitril.
Clorgiline Clorgiline may increase the orthostatic hypotensive activities of Sacubitril.
Iproniazid Iproniazid may increase the orthostatic hypotensive activities of Sacubitril.
Nialamide Nialamide may increase the orthostatic hypotensive activities of Sacubitril.
Safinamide Safinamide may increase the orthostatic hypotensive activities of Sacubitril.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Sacubitril.
Methylene blue Methylene blue may increase the orthostatic hypotensive activities of Sacubitril.
Hydracarbazine Hydracarbazine may increase the orthostatic hypotensive activities of Sacubitril.
Pirlindole Pirlindole may increase the orthostatic hypotensive activities of Sacubitril.
Toloxatone Toloxatone may increase the orthostatic hypotensive activities of Sacubitril.
Benmoxin Benmoxin may increase the orthostatic hypotensive activities of Sacubitril.
Mebanazine Mebanazine may increase the orthostatic hypotensive activities of Sacubitril.
Octamoxin Octamoxin may increase the orthostatic hypotensive activities of Sacubitril.
Pheniprazine Pheniprazine may increase the orthostatic hypotensive activities of Sacubitril.
Phenoxypropazine Phenoxypropazine may increase the orthostatic hypotensive activities of Sacubitril.
Pivhydrazine Pivhydrazine may increase the orthostatic hypotensive activities of Sacubitril.
Safrazine Safrazine may increase the orthostatic hypotensive activities of Sacubitril.
Caroxazone Caroxazone may increase the orthostatic hypotensive activities of Sacubitril.
Harmaline Harmaline may increase the orthostatic hypotensive activities of Sacubitril.
Brofaromine Brofaromine may increase the orthostatic hypotensive activities of Sacubitril.
Butalbital Butalbital may increase the hypotensive activities of Sacubitril.
Pentobarbital Pentobarbital may increase the hypotensive activities of Sacubitril.
Secobarbital Secobarbital may increase the hypotensive activities of Sacubitril.
Methohexital Methohexital may increase the hypotensive activities of Sacubitril.
Thiopental Thiopental may increase the hypotensive activities of Sacubitril.
Primidone Primidone may increase the hypotensive activities of Sacubitril.
Methylphenobarbital Methylphenobarbital may increase the hypotensive activities of Sacubitril.
Thiamylal Thiamylal may increase the hypotensive activities of Sacubitril.
Phenobarbital Phenobarbital may increase the hypotensive activities of Sacubitril.
Amobarbital Amobarbital may increase the hypotensive activities of Sacubitril.
Hexobarbital Hexobarbital may increase the hypotensive activities of Sacubitril.
Barbital Barbital may increase the hypotensive activities of Sacubitril.
Barbexaclone Barbexaclone may increase the hypotensive activities of Sacubitril.
Butabarbital Butabarbital may increase the hypotensive activities of Sacubitril.
Ropinirole The risk or severity of adverse effects can be increased when Ropinirole is combined with Sacubitril.
Morphine The risk or severity of adverse effects can be increased when Morphine is combined with Sacubitril.
Bupivacaine The risk or severity of adverse effects can be increased when Bupivacaine is combined with Sacubitril.
Olanzapine The risk or severity of adverse effects can be increased when Olanzapine is combined with Sacubitril.
Nabilone The risk or severity of adverse effects can be increased when Nabilone is combined with Sacubitril.
Sotalol The risk or severity of adverse effects can be increased when Sotalol is combined with Sacubitril.
Thioridazine The risk or severity of adverse effects can be increased when Thioridazine is combined with Sacubitril.
Tizanidine The risk or severity of adverse effects can be increased when Tizanidine is combined with Sacubitril.
Sufentanil The risk or severity of adverse effects can be increased when Sufentanil is combined with Sacubitril.
Apomorphine The risk or severity of adverse effects can be increased when Apomorphine is combined with Sacubitril.
Isoflurane The risk or severity of adverse effects can be increased when Isoflurane is combined with Sacubitril.
Propofol The risk or severity of adverse effects can be increased when Propofol is combined with Sacubitril.
Isosorbide dinitrate The risk or severity of adverse effects can be increased when Isosorbide dinitrate is combined with Sacubitril.
Remifentanil The risk or severity of adverse effects can be increased when Remifentanil is combined with Sacubitril.
Levosimendan The risk or severity of adverse effects can be increased when Levosimendan is combined with Sacubitril.
Dipyridamole The risk or severity of adverse effects can be increased when Dipyridamole is combined with Sacubitril.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Sacubitril.
Iloprost The risk or severity of adverse effects can be increased when Iloprost is combined with Sacubitril.
Papaverine The risk or severity of adverse effects can be increased when Papaverine is combined with Sacubitril.
Amiodarone The risk or severity of adverse effects can be increased when Amiodarone is combined with Sacubitril.

Target Protein

Neprilysin MME

Referensi & Sumber

Artikel (PubMed)
  • PMID: 19934029
    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. doi: 10.1177/0091270009343932. Epub 2009 Nov 23.
  • PMID: 26466607
    Mills J, Vardeny O: The Role of Neprilysin Inhibitors in Cardiovascular Disease. Curr Heart Fail Rep. 2015 Dec;12(6):389-94. doi: 10.1007/s11897-015-0270-8.
  • PMID: 26406774
    King JB, Bress AP, Reese AD, Munger MA: Neprilysin Inhibition in Heart Failure with Reduced Ejection Fraction: A Clinical Review. Pharmacotherapy. 2015 Sep;35(9):823-37. doi: 10.1002/phar.1629.

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