Page last updated: 2024-11-11

sacubitril

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Cross-References

ID SourceID
PubMed CID9811834
CHEMBL ID3137301
CHEBI ID134714
SCHEMBL ID2707112

Synonyms (47)

Synonym
CHEBI:134714
sacubitril
D10225
sacubitril (jan/usan/inn)
ahu 377
ahu377
sacubitril [usan:inn]
149709-62-6
17erj0mkgi ,
unii-17erj0mkgi
ahu-377
CHEMBL3137301
sacubitril [jan]
sacubitril [mi]
entresto component sacubitril
sacubitril [who-dd]
sacubitril [usan]
sacubitril [orange book]
sacubitril [inn]
sacubitril component of entresto
HY-15407
gtpl7857
neparvis
4-[[(2s,4r)-5-ethoxy-4-methyl-5-oxo-1-(4-phenylphenyl)pentan-2-yl]amino]-4-oxobutanoic acid
SCHEMBL2707112
mfcd00920862
PYNXFZCZUAOOQC-UTKZUKDTSA-N
(2r,4s)-5-biphenyl-4-yl-4-(3-carboxypropionylamino)-2-methylpentanoic acid ethyl ester
(2r,4s)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester
AM85599
alpha-ethyl (alphar,gammas)-gamma-<(3-carboxy-1-oxopropyl)amino>-alpha-methyl<1,1'-biphenyl>-4-pentanoate
4-(((2s,4r)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoic acid
AC-28899
DTXSID20164370
DB09292
[1,1'-biphenyl]-4-pentanoic acid, -[(3-carboxy-1-oxopropyl)amino]-alpha-methyl-, alpha-ethyl ester, (alphar,s)-
AKOS027321509
J-008612
3-{[(2s,4r)-5-ethoxy-4-methyl-5-oxo-1-(4-phenylphenyl)pentan-2-yl]carbamoyl}propanoic acid
4-(((2s,4r)-1-([1,1-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoic acid
AS-16703
Q17811448
NCGC00387800-02
[1,1'-biphenyl]-4-pentanoic acid, gamma-[(3-carboxy-1-oxopropyl)amino]-alpha-methyl-, alpha-ethyl ester, (alphar,gammas)-
3-{[(2s,4r)-1-{[1,1'-biphenyl]-4-yl}-5-ethoxy-4-methyl-5-oxopentan-2-yl]carbamoyl}propanoic acid
EN300-303419
4-(((2s,4r)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoicacid

Research Excerpts

Overview

Sacubitril/valsartan is a first-in-class Angiotensin Receptor-Neprilysin inhibitor (ARNi) to be approved for the treatment of heart failure with reduced ejection fraction (HFrEF) It is used to counteract the neuro-hormonal changes and reverse cardiac remodeling.

ExcerptReferenceRelevance
"Sacubitril/valsartan is a foundation of the pharmacological armamentarium in HFrEF to counteract the neuro-hormonal changes and reverse cardiac remodeling, together with beta-blockers, SGLT2i and mineralocorticoid receptor antagonists. "( Evaluating sacubitril/valsartan as a treatment option for heart failure with reduced ejection fraction and preserved ejection fraction.
De Ponti, F; Diemberger, I; Poluzzi, E; Potena, L; Raschi, E; Sabatino, M, 2022
)
2.55
"Sacubitril/valsartan is an angiotensin receptor/neprilysin inhibitor that the Food and Drug Administration has indicated to reduce the risk of cardiovascular hospitalization and death in patients with left ventricular ejection fraction below normal and with no specified ejection-fraction cut-off. "( Sacubitril/Valsartan Off-Label Uses for Heart Failure.
Colvin, BM; Guglin, M; Kido, K; Szymanski, TW, 2022
)
3.61
"Sacubitril/valsartan is a neprilysin-inhibitor/angiotensin II receptor blocker used for the treatment of heart failure. "( Acute effects on glucose tolerance by neprilysin inhibition in patients with type 2 diabetes.
Bojsen-Møller, KN; Deacon, CF; Gluud, LL; Goetze, JP; Gustafsson, F; Hansen, LH; Holst, JJ; Kjeldsen, S; Madsbad, S; Martinussen, C; Møller, A; Plomgaard, P; Rashu, EB; Richter, MM; Wewer Albrechtsen, NJ, 2022
)
2.16
"Sacubitril/valsartan is an important advancement in the treatment of HFrEF. "( Our Experience With Sacubitril/Valsartan in Chronic Heart Failure Management - HFrEF in the Ambulatory Setting.
Jatić, Z; Kulić, M; Naser, N, 2022
)
2.49
"Sacubitril/valsartan is a first-in-class Angiotensin Receptor-Neprilysin inhibitor (ARNi) to be approved for the treatment of heart failure with reduced ejection fraction (HFrEF). "( Activation of GLP-1 receptor signalling by sacubitril/valsartan: Implications for patients with poor glycaemic control.
Barron, A; Mahtani, K; Patel, B; Wang, B, 2022
)
2.43
"Sacubitril/valsartan is a commonly used medicine for treating heart failure (HF) patients, but the treatment effects significantly vary. "( Association between the NEP rs701109 polymorphism and the clinical efficacy and safety of sacubitril/valsartan in Chinese patients with heart failure.
Chen, R; Cheng, Y; Deng, P; Gao, LC; Li, CX; Li, FJ; Li, HL; Li, L; Long, HZ; Luo, HY; Peng, XY; Xu, SG; Zhou, ZW, 2023
)
2.57
"Sacubitril/valsartan is a mainstay of the treatment of heart failure with reduced ejection fraction (HFrEF); however, its effects on exercise performance yielded conflicting results. "( Effects of sacubitril/valsartan on exercise capacity: a prognostic improvement that starts during uptitration.
Agostoni, P; Capovilla, T; De Martino, F; Dell'Aversana, S; Esposito, I; Filardi, PP; Galotta, A; Magrì, D; Mantegazza, V; Mapelli, M; Mattavelli, I; Nepitella, AA; Paolillo, R; Paolillo, S; Salvioni, E; Tamborini, G; Vignati, C, 2023
)
2.74
"Sacubitril/valsartan is an integral part of value-based care providing high-value, cost-effective care, and bolstering the economic wellbeing of patient care."( Using Sacubitril/Valsartan to Decrease Health care Costs in Population Health Patients.
Bernhardt, R; Chapa, J; Damera, N; George, B; Lee, E; Rao, RA; Reese, L; Shah, C, 2023
)
2.11
"Sacubitril/valsartan is a medication recognized for its efficacy, and this consensus seeks to synthesize the available information regarding its use for the benefit of patients."( Consensus document on the use of sacubitril/valsartan in patients with heart failure: Consejo Interamericano de Falla Cardiaca e Hipertensión Pulmonar (CIFACAH) of the Inter-American Society of Cardiology (IASC).
Alarco, W; Figueroa, Y; Gómez-Mesa, JE; Magaña, A; Pow-Chon, F; Quesada, D; Ramos, CE; Rodríguez-García, D; Rossel, V; Saldarriaga, C; Speranza, M; Ventura-Umanzor, JR, 2023
)
1.91

Effects

Sacubitril/valsartan has been approved for the management of heart failure (HF) with reduced ejection fraction in adults. It has been demonstrated to reduce blood pressure in hypertensive patients, but the best dose remains unclear.

ExcerptReferenceRelevance
"Sacubitril valsartan has a protective effect on the vascular endothelial function of patients with hypertension and CHF."( The Difference between Sacubitril Valsartan and Valsartan on Vascular Endothelial Function, APN, MMP-9, and BNP Levels in Patients with Hypertension and Chronic Heart Failure.
Du, H; Jiang, N; Li, X; Zhao, W, 2022
)
1.75
"Sacubitril-valsartan has been shown to have superior effects over angiotensin-converting enzyme inhibitors and angiotensin receptor blockers in patients with heart failure (HF). "( Sacubitril/Valsartan for heart failure: A protocol for systematic review and meta-analysis.
Dai, W; Huang, X; Luo, J, 2022
)
3.61
"Sacubitril/valsartan has been approved for the treatment of heart failure (HF) patients with reduced ejection fraction; since then, it gradually became a new star drug in the therapy of HF. "( Emerging trends in sacubitril/valsartan research: A bibliometric analysis of the years 1995-2021.
Chen, D; Lai, P; Liao, YL; Ling, JY; Tian, KJ; Xie, MJ; Xue, JH; Ye, JH; Zhong, WT; Zhong, YM, 2022
)
2.49
"Sacubitril/valsartan has been demonstrated to reduce blood pressure in hypertensive patients, but the best dose remains unclear. "( Network meta-analysis of sacubitril/valsartan for the treatment of essential hypertension.
Huang, H; Li, M; Zhang, Y; Zhao, X, 2023
)
2.66
"Sacubitril/valsartan has been approved for the management of heart failure (HF) with reduced ejection fraction in adults. "( Baseline Characteristics of Pediatric Patients With Heart Failure Due to Systemic Left Ventricular Systolic Dysfunction in the PANORAMA-HF Trial.
Bonnet, D; Burch, M; Garito, T; Kantor, PF; Kocun, M; Shaddy, R; Solar-Yohay, S; Zhang, S, 2023
)
2.35
"Sacubitril/valsartan has been shown to decrease readmissions for patients with heart failure (HF) and decrease health care costs."( Using Sacubitril/Valsartan to Decrease Health care Costs in Population Health Patients.
Bernhardt, R; Chapa, J; Damera, N; George, B; Lee, E; Rao, RA; Reese, L; Shah, C, 2023
)
2.11

Actions

ExcerptReferenceRelevance
"Sacubitril valsartan can increase serum APN levels, reduce MMP-9 and BNP levels, and have good clinical effects."( The Difference between Sacubitril Valsartan and Valsartan on Vascular Endothelial Function, APN, MMP-9, and BNP Levels in Patients with Hypertension and Chronic Heart Failure.
Du, H; Jiang, N; Li, X; Zhao, W, 2022
)
1.75

Treatment

Treatment with sacubitril/valsartan was effective and provided superior BP reduction. A higher proportion of patients achieving target BP goals than treatment with olmesartan in Japanese patients with mild to moderate essential hypertension.

ExcerptReferenceRelevance
"Sacubitril/valsartan treatment was well tolerated and did not affect ultrafiltration during HD treatment. "( Low dose sacubitril/valsartan is effective and safe in hemodialysis patient with decompensated heart failure and hypotension: A case report.
Chen, X; Feng, Y; Li, W; Liu, H, 2022
)
2.58
"Sacubitril-valsartan treatment, which lowered NT-proBNP levels and improved cardiac function, was more effective in HFpEF patients with acute decompensated heart failure than enalapril."( The Relationship between Angiotensin-Neprilysin Treatment, Echocardiographic Parameters, and NT-proBNP Levels in HFpEF Patients with Acute Decompensated Heart Failure.
Xu, Z; Yang, S; Zhang, X, 2022
)
2.16
"Treatment with sacubitril/valsartan was effective and provided superior BP reduction, with a higher proportion of patients achieving target BP goals than treatment with olmesartan in Japanese patients with mild to moderate essential hypertension."( Efficacy of sacubitril/valsartan versus olmesartan in Japanese patients with essential hypertension: a randomized, double-blind, multicenter study.
Gotou, H; Kario, K; Rakugi, H; Sasajima, T; Yamaguchi, M; Zhang, J, 2022
)
1.44
"Treatment of sacubitril/valsartan showed significantly higher KCCQ-CSS compared to the control (WMD=0.975, 95% CI: 0.885, 1.064, p<0.001; I2=94.8%, pheterogeneity<0.001). "( Effect on the Quality of Life of Patients with Heart Failure and Reduced/Preserved Ejection Fraction Using Sacubitril/Valsartan.
Huang, Y; Li, X; Li, Y; Liu, Z; Wu, X, 2023
)
1.49
"The treatment with sacubitril/valsartan in patients suffering from chronic heart failure with reduced ejection fraction increases left ventricular ejection fraction and decreases the risk of sudden cardiac death. "( Comparison of the prognosis and outcome of heart failure with reduced ejection fraction patients treated with sacubitril/valsartan according to age.
Abumayyaleh, M; Akin, I; Aweimer, A; Borggrefe, M; El-Battrawy, I; Kummer, M; Kuschyk, J; Mügge, A; Pilsinger, C; Sattler, K, 2021
)
1.16
"Treatment with sacubitril/valsartan in patients with systolic dysfunction is associated with an improvement in LVEF in a real world scenario. "( Remodelling is inversely proportional to left ventricular dimensions in a real-life population of patients with chronic heart failure after therapy with sacubitril/valsartan.
Brunetti, ND; Correale, M; Di Biase, M; Diella, C; Ferraretti, A; Iacoviello, M; Mallardi, A; Mazzeo, P; Merolla, G; Romano, V; Tricarico, L, 2022
)
1.27

Toxicity

Sacubitril/valsartan was found to inhibit ventricular remodeling after AMI, improve cardiac function, and reduce the incidence of adverse cardiovascular events after myocardial infarction. Hypotension is the most common adverse event compared with ACEI/ARB.

ExcerptReferenceRelevance
" Due to the limited literature on patient safety outcomes for recently approved CVD medications, this study investigated adverse drug reports (ADRs) reported in the FDA Adverse Event Reporting System (FAERS)."( A Pharmacovigilance Study of Adverse Drug Reactions Reported for Cardiovascular Disease Medications Approved Between 2012 and 2017 in the United States Food and Drug Administration Adverse Event Reporting System (FAERS) Database.
Boyce, RD; Gray, MP; Kane-Gill, SL; Patel, NM; Stottlemyer, BA, 2022
)
0.72
" Sacubitril/valsartan was well tolerated with fewer study drug discontinuations due to adverse events, although the sacubitril/valsartan group had a higher proportion of patients with hypotension."( Efficacy and Safety of Sacubitril/Valsartan in Japanese Patients With Chronic Heart Failure and Reduced Ejection Fraction - Results From the PARALLEL-HF Study.
Desai, AS; Guo, W; Iimori, T; Ito, H; Kitamura, T; Momomura, SI; Ohishi, T; Saito, Y; Sakata, Y; Tsutsui, H; Yamamoto, K, 2021
)
1.84
"In Japanese patients with HFrEF, there was no difference in reduction in the risk of CV death or HF hospitalization between sacubitril/valsartan and enalapril, and sacubitril/valsartan was safe and well tolerated."( Efficacy and Safety of Sacubitril/Valsartan in Japanese Patients With Chronic Heart Failure and Reduced Ejection Fraction - Results From the PARALLEL-HF Study.
Desai, AS; Guo, W; Iimori, T; Ito, H; Kitamura, T; Momomura, SI; Ohishi, T; Saito, Y; Sakata, Y; Tsutsui, H; Yamamoto, K, 2021
)
1.14
" This study explores the safety profile of sacubitril/valsartan by comparing adverse events in RCT and real-world use."( Five Years of Sacubitril/Valsartan-a Safety Analysis of Randomized Clinical Trials and Real-World Pharmacovigilance.
Brar, S; D'Albo, N; Dani, SS; Dey, A; Ganatra, S; Kim, YS; Shah, S, 2022
)
1.34
" WHO's VigiBase, FAERS, and EMA's EudraVigilance were mined to obtain spontaneously reported real-world adverse events."( Five Years of Sacubitril/Valsartan-a Safety Analysis of Randomized Clinical Trials and Real-World Pharmacovigilance.
Brar, S; D'Albo, N; Dani, SS; Dey, A; Ganatra, S; Kim, YS; Shah, S, 2022
)
1.08
" A total of 103,038 adverse events were registered in the spontaneous reporting systems."( Five Years of Sacubitril/Valsartan-a Safety Analysis of Randomized Clinical Trials and Real-World Pharmacovigilance.
Brar, S; D'Albo, N; Dani, SS; Dey, A; Ganatra, S; Kim, YS; Shah, S, 2022
)
1.08
"The aim of this study was to characterise clinical priority of adverse events with sacubitril/valsartan for targeting preventive measures."( Adverse events with sacubitril/valsartan in the real world: emerging signals to target preventive strategies from the FDA adverse event reporting system.
Antonazzo, IC; De Ponti, F; Diemberger, I; Gatti, M; Raschi, E, 2021
)
1.17
"We used the US Food and Drug Administration adverse event reporting system (worldwide pharmacovigilance database) to compare adverse events recording sacubitril/valsartan as suspect with other cardiovascular drugs."( Adverse events with sacubitril/valsartan in the real world: emerging signals to target preventive strategies from the FDA adverse event reporting system.
Antonazzo, IC; De Ponti, F; Diemberger, I; Gatti, M; Raschi, E, 2021
)
1.14
"Sacubitril/valsartan was recorded in 20,021 reports, with 178 adverse events associated with significant disproportionality: 71."( Adverse events with sacubitril/valsartan in the real world: emerging signals to target preventive strategies from the FDA adverse event reporting system.
Antonazzo, IC; De Ponti, F; Diemberger, I; Gatti, M; Raschi, E, 2021
)
2.39
"There were no deaths, serious adverse events, or discontinuations due to TEAEs, and there were no significant safety concerns associated with S086."( A randomized, double-blind, placebo-controlled, single, and multiple dose-escalation Phase I clinical trial to investigate the safety, pharmacokinetic, and pharmacodynamic profiles of oral S086, a novel angiotensin receptor-neprilysin inhibitor, in health
He, S; Hu, Y; Li, J; Li, X; Li, Y; Mai, J; Sun, J; Wu, M; Xu, W; Yan, J; Yang, L; Zhang, H, 2022
)
0.72
" Case reports from the United States Food and Drug Administration's Adverse Event Reporting System from 1991 to Q4/2020 were used."( Potential Safety Signals for Rhabdomyolysis Associated With High-Potency Statin Use With or Without Sacubitril/Valsartan.
Ryo, Y; Sunaga, T, 2022
)
0.94
" The total incidence of adverse cardiovascular events in the sacubitril/valsartan group was significantly lower than that in the control group {relative risk (RR) =0."( Therapeutic effects and safety of early use of sacubitril/valsartan after acute myocardial infarction: a systematic review and meta-analysis.
Chen, J; Chen, T; Shou, Y; Yan, K; Zhang, L; Zhao, H, 2022
)
1.22
"Sacubitril/valsartan was found to inhibit ventricular remodeling after AMI, improve cardiac function, and reduce the incidence of adverse cardiovascular events after myocardial infarction, the rehospitalization rate, and the mortality rate."( Therapeutic effects and safety of early use of sacubitril/valsartan after acute myocardial infarction: a systematic review and meta-analysis.
Chen, J; Chen, T; Shou, Y; Yan, K; Zhang, L; Zhao, H, 2022
)
2.42
" It was also safe and well tolerated."( Low dose sacubitril/valsartan is effective and safe in hemodialysis patient with decompensated heart failure and hypotension: A case report.
Chen, X; Feng, Y; Li, W; Liu, H, 2022
)
1.14
" The potential risk factors for the discontinuation events caused by sac/val-related adverse events (AEs) were explored."( Effectiveness and safety of sacubitril/valsartan for patients with hypertension and heart failure in the real-world setting: A retrospective study in China.
Chen, C; Fan, L; Li, J; Li, X; Lv, Q; Tian, D; Zuo, C, 2022
)
1.02
"001), while there was no significant difference in the incidence of adverse events [odds ratio (OR) =1."( Efficacy and safety of sacubitril/valsartan in the treatment of middle-aged and elderly patients with hypertension: a systematic review and meta-analysis of randomized controlled trials.
Jin, JC; Li, BN; Liu, KK; Liu, S; Wu, HX, 2022
)
1.03
"Concomitant use of sacubitril/valsartan for at least 3 months did not alter the efficacy of vericiguat and was similarly safe and tolerated in both study arms."( Efficacy and safety of vericiguat in patients with heart failure with reduced ejection fraction treated with sacubitril/valsartan: insights from the VICTORIA trial.
Alemayehu, WG; Armstrong, PW; Butler, J; Edelmann, F; Ezekowitz, J; Hernandez, AF; Lam, CSP; McMullan, C; O'Connor, CM; Pieske, B; Ponikowski, P; Roessig, L; Senni, M; Sim, D; Voors, AA; Westerhout, CM, 2022
)
1.26
" No major adverse events occurred."( Safety and Efficacy of Sacubitril/Valsartan in Patients With a Failing Systemic Right Ventricle: A Prospective Single-Center Study.
Fusco, F; Grimaldi, N; Iannuzzi, A; Merola, A; Palma, M; Sarubbi, B; Scognamiglio, G, 2023
)
1.22
" The most frequently reported adverse event for sacubitril/valsartan is hypotension and the risk is higher than for ACEI/ARB."( Efficacy and Safety of Sacubitril/Valsartan Compared With ACEI/ARB on Health-Related Quality of Life in Heart Failure Patients: A Meta-Analysis.
Shaikh, AS; Xu, XD; Yang, HR; Zhou, BT, 2023
)
1.48
" Hypotension is the most common adverse event with sacubitril/valsartan compared with ACEI/ARB."( Efficacy and Safety of Sacubitril/Valsartan Compared With ACEI/ARB on Health-Related Quality of Life in Heart Failure Patients: A Meta-Analysis.
Shaikh, AS; Xu, XD; Yang, HR; Zhou, BT, 2023
)
1.47
"Low-dose sacubitril/valsartan might also be effective and safe in HF patients."( Efficacy and safety of low-dose sacubitril/valsartan in heart failure patients: A systematic review and meta-analysis.
Chen, WW; Dang, HQ; Gao, J; Jiang, J; Li, YM; Liu, YL; Zhang, XZ, 2023
)
1.61
" Key safety endpoints were the incidences of adverse events during hospitalization and during follow-up planned at 1 month, 3-6 months and 12-18 months after discharge."( Safety and feasibility of angiotensin receptor neprilysin inhibitor in real-world patients with acute decompensated heart failure.
Angelini, F; Coppini, L; Ferraro, I; Giordana, F; Musumeci, G; Rossini, R; Ruffino, E; Tizzani, E; Valente, E; Varbella, F, 2023
)
0.91
"In-hospital initiation of sacubitril/valsartan treatment in real-world ADHF patients may be a safe and feasible treatment option."( Safety and feasibility of angiotensin receptor neprilysin inhibitor in real-world patients with acute decompensated heart failure.
Angelini, F; Coppini, L; Ferraro, I; Giordana, F; Musumeci, G; Rossini, R; Ruffino, E; Tizzani, E; Valente, E; Varbella, F, 2023
)
1.21
"Sacubitril/Valsartan therapy in HFrEF patients is safe and moderately tolerated among the Pakistani population."( Safety and tolerability of Sacubitril/Valsartan in heart failure patient with reduced ejection fraction.
Ashraf, T; Balouch, IJ; Bashir, S; Bhatti, UH; Karim, M; Khan, MN; Moazzam, A; Naseeb, K; Rauf, R; Soomro, NA, 2023
)
2.65
" Safety assessments included all adverse events and serious adverse events."( Efficacy and safety of sacubitril/allisartan for the treatment of primary hypertension: a phase 2 randomized, double-blind study.
Chen, SX; Ge, Q; He, SY; Li, JF; Li, Y; Lu, XH; Wang, JG; Xu, WJ; Yan, J; Zhang, J; Zhang, W, 2023
)
1.22
"CIS-induced cardiotoxicity and L-NNA co-administered group showed significant increases in cardiac enzymes, toxic histopathological features, elevated heart weights, angiotensin II (Ang II), neprilysin, malondialdehyde (MDA), inflammatory mediators, blood pressure (BP) and caspase 3 expressions, but there are significant decreases in the antioxidant parameters, vascular endothelial growth factor (VEGF) and endothelial nitric oxide synthase (eNOS)."( Sacubitril/valsartan cardioprotective effect against cisplatin-induced cardiotoxicity via modulation of VEGF/eNOS and TLR4/TNFα/IL6 signalling pathways.
Ahmed Rifaai, R; Bayoumi, AMA; Mahmoud Refaie, MM; Shehata, S, 2023
)
2.35

Pharmacokinetics

ExcerptReferenceRelevance
"This study evaluated the safety, pharmacokinetic (PK), and pharmacodynamic (PD) profiles of single ascending doses (SAD) and multiple ascending doses (MAD) of S086 in healthy Chinese volunteers."( A randomized, double-blind, placebo-controlled, single, and multiple dose-escalation Phase I clinical trial to investigate the safety, pharmacokinetic, and pharmacodynamic profiles of oral S086, a novel angiotensin receptor-neprilysin inhibitor, in health
He, S; Hu, Y; Li, J; Li, X; Li, Y; Mai, J; Sun, J; Wu, M; Xu, W; Yan, J; Yang, L; Zhang, H, 2022
)
0.72
" However, the pharmacokinetic (PK) and pharmacodynamic properties of SAC/VAL in HD patients with HF remain uncertain."( Pharmacokinetics and Pharmacodynamics of Sacubitril/Valsartan in Maintenance Hemodialysis Patients with Heart Failure.
Apaer, R; Che, H; Chen, J; Dou, X; Feng, Z; Fu, L; Fu, X; He, C; Huang, R; Ke, G; Kong, Y; Li, S; Li, X; Li, Z; Liang, X; Lin, T; Liu, S; Ma, J; Mei, L; Shi, W; Su, X; Tang, B; Tao, Y; Wang, X; Wang, Y; Wen, F; Xia, Y; Xiao, J; Xiong, Y; Xu, L; Xue, Z; Ye, Z; Zhang, H; Zhang, L, 2022
)
0.99

Compound-Compound Interactions

ExcerptReferenceRelevance
" The drugs potentiating them interact pharmacodynamically, resulting in adverse consequences."( An Overview of Clinically Imperative and Pharmacodynamically Significant Drug Interactions of Renin-Angiotensin-Aldosterone System (RAAS) Blockers.
Balasubramanian, R; Mohamed Pakkir Maideen, N; Muthusamy, S; Nallasamy, V, 2022
)
0.72
" To avoid adverse implications, prescribers and pharmacists must be aware of the drugs that interact with RAAS blockers."( An Overview of Clinically Imperative and Pharmacodynamically Significant Drug Interactions of Renin-Angiotensin-Aldosterone System (RAAS) Blockers.
Balasubramanian, R; Mohamed Pakkir Maideen, N; Muthusamy, S; Nallasamy, V, 2022
)
0.72
" Here, we have performed robust virtual screening combined with biased-force pulling molecular dynamic (MD) simulations to predict high-affinity GPR17 modulators followed by experimental validation."( Bias-force guided simulations combined with experimental validations towards GPR17 modulators identification.
Kandhavelu, M; Kari, S; Kidambi, S; Marimuthu, P; Murugesan, A; Razzokov, J; Selvaraj, C; Thiyagarajan, R, 2023
)
0.91
"This study aimed to evaluate the efficacy of nifedipine controlled-release tablets combined with sacubitril valsartan in diabetic nephropathy (DN) patients with hypertension."( Therapeutic improvements of nifedipine controlled-release tablets combined with sacubitril valsartan on patients with diabetic nephropathy complicated with hypertension.
Hu, L; Liu, G; Wei, Y, 2023
)
1.35

Dosage Studied

Early use or high dosage of sacubitril/valsartan medication is associated with an improvement in clinical outcome. The mean dosage of azilsartan was 30 ± 10 mg/day at baseline and that of Sacub itril/Valsartan after 3 months of treatment was 204 ±-64 mg per day.

ExcerptRelevanceReference
" We conducted a systematic review of articles published between January 2014 and May 2019 that described dosing patterns and factors associated with non-use and sub-target dosing of HFrEF therapies in clinical practice."( Factors associated with non-use and sub-target dosing of medical therapy for heart failure with reduced ejection fraction.
Bernauer, M; Butler, J; Greene, SJ; Tan, X; Yang, M; Yeh, YC; Zaidi, O, 2022
)
0.72
" Our objective was to describe the sacubitril/valsartan initiation rate, associated characteristics, and 6-month follow-up dosing among veterans with HFrEF who are renin-angiotensin-aldosterone system inhibitor (RAASi) naïve."( Sacubitril/Valsartan Initiation Among Veterans Who Are Renin-Angiotensin-Aldosterone System Inhibitor Naïve With Heart Failure and Reduced Ejection Fraction.
Alba, PR; Bress, AP; Choi, ME; Cook, J; Dodson, JA; Fang, JC; He, T; Herrick, JS; King, JB; Levitan, EB; Mohanty, AF; Obi, EN; Patterson, OV; Russo, PA; Vardeny, O, 2021
)
2.34
" These issues have been linked to significant gaps in the usage and dosing of guideline-directed medical therapy with ARNI in patients with HFrEF."( Acute Tubular Necrosis Associated with Angiotensin Receptor-neprilysin Inhibitor.
Jang, HN; Kang, MG; Kim, MJ; Lee, JS; Song, HN, 2022
)
0.72
" During follow-up, 27% of patients increased their dosage to 49/50 mg twice daily, 68% of patients were taking 24/26 mg twice daily, and 5% of the patients were still taking 12/13 mg twice daily."( Sacubitril/Valsartan in the Treatment of Right Ventricular Dysfunction in Patients With Heart Failure With Reduced Ejection Fraction: A Real-world Study.
Fu, G; Lu, J; Shen, C; Xiong, C; Yang, Y, 2022
)
2.16
" Participants were initially instructed to take SV 50 mg twice daily, and the dosage was gradually increased up to 100 mg twice daily."( Effects of Sacubitril/Valsartan on resistant hypertension and myocardial work in hemodialysis patients.
Ding, XX; Liu, BC; Tang, HX; Wang, B; Wang, GH; Zhang, XL; Zheng, J, 2022
)
1.11
"This study aims to investigate the dosage pattern, efficacy, and safety of sacubitril/valsartan (Sac/Val) in Chinese heart failure with reduced ejection fraction (HFrEF) patients regarding real-world settings."( Efficacy and Dosage Pattern of Sacubitril/Valsartan in Chinese Heart Failure with Reduced Ejection Fraction Patients.
Cheang, I; Dai, C; Li, X; Liao, S; Lu, Q; Lu, X; Shi, S; Su, X; Wang, J; Xu, D; Yuan, F; Yuan, J; Zhang, M; Zhao, Y; Zhou, J; Zhu, X, 2022
)
1.24
"Spontaneously hypertensive rats (SHR) were pretreated by daily angiotensin receptor blocker (ARB; 30 mg/kg intraperitoneally), Sacubitril/Valsartan (ARNI; 60 mg/kg intraperitoneally) or the same dosage of physiological saline for 1 week."( The impact of Sacubitril/Valsartan on cardiac fibrosis early after myocardial infarction in hypertensive rats.
Chen, S; Kang, L; Liu, Y; Si, J; Xu, B; Zhong, C, 2022
)
1.29
" Up-titration was defined as an increase in dosage above 24/26 mg BID beyond 12 weeks after the initiation of sacubitril/valsartan."( Up-Titration of Sacubitril/Valsartan Among Patients With Heart Failure and Preserved Ejection Fraction.
Ijichi, T; Matsumura, K; Miho, M; Morimoto, J; Nakazawa, G; Takabayashi, K; Takase, T; Ueno, K; Ueno, M; Yagi, E,
)
0.69
" The mean dosage of azilsartan was 30 ± 10 mg/day at baseline and that of sacubitril/valsartan after 3 months of treatment was 204 ± 64 mg/day."( Efficacy and safety of sacubitril/valsartan after switching from azilsartan in hemodialysis patients with hypertension.
Fukushima, H; Horio, T; Ishimitsu, T; Iwashima, Y; Rai, T, 2023
)
1.45
" Sacubitril/valsartan was started at a dosage of 12/13 mg in 52 (43%) patients, 24/26 mg in 61 (50%) patients and 49/51 mg in 8 (7%) patients."( Safety and feasibility of angiotensin receptor neprilysin inhibitor in real-world patients with acute decompensated heart failure.
Angelini, F; Coppini, L; Ferraro, I; Giordana, F; Musumeci, G; Rossini, R; Ruffino, E; Tizzani, E; Valente, E; Varbella, F, 2023
)
1.82
" The purpose of this study was to investigate the efficacy of different initial timing and dosage of sacubitril/valsartan in AMI patients."( The initial timing and dosage pattern of sacubitril/valsartan in patients with acute myocardial infarction undergoing percutaneous coronary intervention.
Gu, J; Wang, CQ; Wang, Y; Zhang, JF, 2023
)
1.39
" After a median follow-up of 38 months, early use or high dosage of sacubitril/valsartan was associated with an improvement in primary endpoint as well as the incidence of new-onset HF."( The initial timing and dosage pattern of sacubitril/valsartan in patients with acute myocardial infarction undergoing percutaneous coronary intervention.
Gu, J; Wang, CQ; Wang, Y; Zhang, JF, 2023
)
1.41
"Early use or high dosage of sacubitril/valsartan medication is associated with an improvement in clinical outcome."( The initial timing and dosage pattern of sacubitril/valsartan in patients with acute myocardial infarction undergoing percutaneous coronary intervention.
Gu, J; Wang, CQ; Wang, Y; Zhang, JF, 2023
)
1.47
"5 mg/day and the mean dosage was increased to 84."( The efficacy and safety of sacubitril/valsartan in heart failure with reduced ejection fraction patients with hypotension.
Ako, J; Eda, Y; Fujita, T; Iida, Y; Ikeda, Y; Ishii, S; Koitabashi, T; Nabeta, T; Oikawa, J; Takigami, Y; Yazaki, M, 2023
)
1.21
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
biphenylsBenzenoid aromatic compounds containing two phenyl or substituted-phenyl groups which are joined together by a single bond.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID1542152Invivo inhibition of NEP in Sprague-Dawley rat assessed as increase in PANP level at 30 mg/kg, po measured after 15 mins2020ACS medicinal chemistry letters, Feb-13, Volume: 11, Issue:2
Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin Inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (339)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's339 (100.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 119.18

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index119.18 (24.57)
Research Supply Index5.96 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index215.59 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (119.18)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials38 (10.95%)5.53%
Reviews62 (17.87%)6.00%
Case Studies13 (3.75%)4.05%
Observational19 (5.48%)0.25%
Other215 (61.96%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]