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LCZ696

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https://www.readbyqxmd.com/read/28623750/lcz696-improves-cardiac-function-via-alleviating-drp1-mediated-mitochondrial-dysfunction-in-mice-with-doxorubicin-induced-dilated-cardiomyopathy
#1
Yan Xia, Zhangwei Chen, Ao Chen, Mingqiang Fu, Zhen Dong, Kai Hu, Xiangdong Yang, Yunzeng Zou, Aijun Sun, Juying Qian, Junbo Ge
AIMS: LCZ696, a novel angiotensin receptor neprilysin inhibitor, is effective in treating heart failure patients. Doxorubicin (DOX) is an effective antitumor medication but the cardiotoxicity limited its clinical use. In this study, we aimed to determine the effect of LCZ696 on DOX-induced cardiomyopathy in mice and in vitro and to explore related mechanisms focusing on fission protein dynamin-related protein 1 (Drp1). METHODS AND RESULTS: In human study, we found that myocardial fission protein Drp1 expression and its ser 616 phosphorylation were significantly increased in dilated cardiomyopathy (DCM) patients...
June 14, 2017: Journal of Molecular and Cellular Cardiology
https://www.readbyqxmd.com/read/28614052/safety-of-the-neprilysin-renin-angiotensin-system-inhibitor-lcz696
#2
REVIEW
Bo Li, Yunhe Zhao, Bo Yin, Mengfei Helian, Xinmei Wang, Feng Chen, Hongxia Zhang, Hui Sun, Bin Meng, Fengshuang An
OBJECTIVES: The combined neprilysin/rennin-angiotensin system inhibitor sacubitril/valsartan (LCZ696) has shown its superiority over ACEI/ARB therapy. In view of the existing concern of its adverse effects, we aimed to provide evidence of the safety of the new drug. RESULTS: A total of 6 randomized trials with 11,821 subjects were included in this analysis. No significant differences were found in any adverse effects between LCZ696 and ACEI/ARB or placebo groups...
May 31, 2017: Oncotarget
https://www.readbyqxmd.com/read/28599060/evaluation-of-pharmacokinetic-and-pharmacodynamic-drug-drug-interaction-of-sacubitril-valsartan-lcz696-and-sildenafil-in-patients-with-mild-to-moderate-hypertension
#3
Hsiu-Ling Hsiao, Thomas H Langenickel, Jesika Petruck, Kiran Kode, Surya Ayalasomayajula, Uwe Schuehly, Michael Greeley, Parasar Pal, Wei Zhou, Margaret F Prescott, Gangadhar Sunkara, Iris Rajman
Sacubitril/valsartan (LCZ696) is indicated for the treatment of patients with heart failure and reduced ejection fraction (HFrEF). Since patients with HFrEF may receive sacubitril/valsartan and sildenafil, both increasing cGMP, the present study evaluated the pharmacokinetic and pharmacodynamic drug interaction potential between sacubitril/valsartan and sildenafil. In this open-label, 3-period, single sequence study, patients with mild-to-moderate hypertension (153.8±8.2 mm Hg mean SBP) received a single dose of sildenafil 50 mg, sacubitril/valsartan 400 mg once daily for 5 days, and sacubitril/valsartan and sildenafil co-administration...
June 9, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28569442/first-derivative-emission-spectrofluorimetric-method-for-the-determination-of-lcz696-a-newly-approved-fda-supramolecular-complex-of-valsartan-and-sacubitril-in-tablets
#4
Marwa A A Ragab, Shereen M Galal, Mohamed A Korany, Aya R Ahmed
LCZ696 (sacubitril/valsartan, Entresto™) is a therapy lately approved by United States Food and Drug Administration (US FDA) as a heart failure therapy. It is claimed to decrease the mortality rate and hospitalization for patients with chronic heart failure. This study is considered as the first report to investigate the fluorimetric behavior of sacubitril in addition to pursuing all the different conditions that may affect its fluorescence. Various conditions were studied, for example studying the effects of organized media, solvents and pH, which may affect the fluorescence behavior of sacubitril...
June 1, 2017: Luminescence: the Journal of Biological and Chemical Luminescence
https://www.readbyqxmd.com/read/28527109/erratum-to-clinical-pharmacokinetics-of-sacubitril-valsartan-lcz696-a-novel-angiotensin-receptor-neprilysin-inhibitor
#5
Surya Ayalasomayajula, Thomas Langenickel, Parasar Pal, Sreedevi Boggarapu, Gangadhar Sunkara
Sacubitril/valsartan (LCZ696) is indicated for the treatment of heart failure with reduced ejection fraction. Absorption of sacubitril/valsartan and conversion of sacubitril (prodrug) to sacubitrilat (neprilysin inhibitor) was rapid with maximum plasma concentrations of sacubitril, sacubitrilat, and valsartan (angiotensin receptor blocker) reaching within 0.5, 1.5-2.0, and 2.0-3.0 h, respectively. With a twofold increase in dose, an increase in the area under the plasma concentration-time curve was proportional for sacubitril, ~1...
May 19, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28492561/-sacubitril-valsartan-a-new-and-effective-treatment-for-heart-failure-with-reduced-ejection-fraction
#6
Michele Senni, Bruno Trimarco, Michele Emdin, Luciano De Biase
Despite significant therapeutic advances, patients with chronic heart failure and reduced ejection fraction (HFrEF) remain at high risk for heart failure progression and death. The PARADIGM-HF study, the largest outcome trial in HFrEF, has shown improved cardiovascular outcomes with sacubitril/valsartan (Entresto®, Novartis), previously known as LCZ696, compared with angiotensin-converting enzyme (ACE) inhibitor therapy, possibly leading us to a new era for heart failure treatment. Sacubitril/valsartan represents a first-in-class drug acting through inhibition of angiotensin receptor and neprilysin, thus modulating the renin-angiotensin-aldosterone system and vasoactive substances such as natriuretic peptides...
January 2017: Giornale Italiano di Cardiologia
https://www.readbyqxmd.com/read/28419972/neprilysin-inhibitors-a-new-hope-to-halt-the-diabetic-cardiovascular-and-renal-complications
#7
REVIEW
Vajir Malek, Anil Bhanudas Gaikwad
Diabetes is an enormous and ever-growing calamity and a global public health threat of the 21st century. Besides insulin and oral hypoglycaemic drugs, blockage of the renin-angiotensin system (RAS) denotes a key pharmacotherapy for the management of cardiovascular (CVD) and chronic kidney diseases (CKD), which are the leading causes of disability and death among diabetic patients. Neprilysin (NEP) inhibition, auxiliary to RAS blockage increases the bioavailability of natriuretic peptides and benefits the cardio-renal system...
June 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28417439/clinical-pharmacokinetics-of-sacubitril-valsartan-lcz696-a-novel-angiotensin-receptor-neprilysin-inhibitor
#8
REVIEW
Surya Ayalasomayajula, Thomas Langenickel, Parasar Pal, Sreedevi Boggarapu, Gangadhar Sunkara
Sacubitril/valsartan (LCZ696) is indicated for the treatment of heart failure with reduced ejection fraction. Absorption of sacubitril/valsartan and conversion of sacubitril (prodrug) to sacubitrilat (neprilysin inhibitor) was rapid with maximum plasma concentrations of sacubitril, sacubitrilat, and valsartan (angiotensin receptor blocker) reaching within 0.5, 1.5-2.0, and 2.0-3.0 h, respectively. With a two-fold increase in dose, an increase in the area under the plasma concentration-time curve was proportional for sacubitril, ~1...
April 17, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28413968/hypertension-and-heart-failure-with-preserved-ejection-fraction-connecting-the-dots
#9
Costas Tsioufis, Georgios Georgiopoulos, Dimitrios Oikonomou, Costas Thomopoulos, Niki Katsiki, Alexandros Kasiakogias, Christina Chrysochoou, Dimitrios Konstantinidis, Theodoros Kalos, Dimitrios Tousoulis
Heart failure (HF) with preserved ejection fraction (EF) (HFpEF) accounts for approximately 50% of HF cases and its prevalence relative to HF with reduced EF is rising. Hypertension (HT) is the most common co-morbidity in HFpEF patients and it is implicated in both the pathogenesis and the prognosis of the disease. Therefore, HT is a modifiable risk factor of high yield in HFpEF. We reviewed the literature for epidemiologic data supporting the co-aggregation of the two entities as well as patho-physiologic mechanisms linking HT to HFpEF...
April 14, 2017: Current Vascular Pharmacology
https://www.readbyqxmd.com/read/28398362/-the-relationship-between-natriuretic-peptides-and-neprilysin-pathways-the-clinical-simplification-against-the-complexity-of-biological-systems
#10
Giuseppe Di Tano, Aldo Clerico
A large body of evidence supports the use of natriuretic peptides (brain natriuretic peptide [BNP] and N-terminal proBNP [NT-proBNP]) for the evaluation and management of patients with heart failure over time. Elevated values reflect an enhanced counterregulatory response to hemodynamic stress and are indicative of heart failure severity, thus predicting prognosis. The clinical relevance and result interpretation of natriuretic peptides for monitoring therapy are still debated, and our understanding of their complex nature is still far from being complete...
February 2017: Giornale Italiano di Cardiologia
https://www.readbyqxmd.com/read/28378286/resetting-the-neurohormonal-balance-in-heart-failure-hf-the-relevance-of-the-natriuretic-peptide-np-system-to-the-clinical-management-of-patients-with-hf
#11
REVIEW
Speranza Rubattu, Filippos Triposkiadis
The natriuretic peptide (NP) system, which includes atrial natriuretic peptide, B-type natriuretic peptide, and C-type natriuretic peptide, has an important role in cardiovascular homeostasis, promoting a number of physiological effects including diuresis, vasodilation, and inhibition of the renin-angiotensin-aldosterone system. Heart failure (HF) is associated with defects in NP processing and synthesis, and there is a strong relationship between NP levels and disease state. NPs are useful biomarkers in HF, and their use in diagnosis and evaluation of prognosis is well established, particularly in patients with HF with reduced ejection fraction (HFrEF)...
May 2017: Heart Failure Reviews
https://www.readbyqxmd.com/read/28375036/new-developments-in-the-pharmacotherapeutic-management-of-heart-failure-in-elderly-patients-concerns-and-considerations
#12
Elles M Screever, Wouter C Meijers, Dirk J van Veldhuisen, Rudolf A de Boer
Heart failure (HF) remains a major public health problem worldwide, affecting approximately 23 million patients, and is predominantly a disease of the elderly population. Elderly patients mostly suffer from HF with preserved ejection fraction (HFpEF), which often presents with multiple co-morbidities and they require multiple medical treatments. This, together with the heterogeneous phenotype of HFpEF, makes it a difficult syndrome to diagnose and treat. Areas covered: Although HF is most abundant in the elderly, this group is still underrepresented in clinical trials, which results in the lack of evidence-based medical regimens...
May 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28338503/efficacy-and-safety-of-crystalline-valsartan-sacubitril-lcz696-compared-with-placebo-and-combinations-of-free-valsartan-and-sacubitril-in-patients-with-systolic-hypertension-the-ratio-study
#13
Joseph L Izzo, Dion H Zappe, Yan Jia, Kudsia Hafeez, Jack Zhang
We compared the systolic blood pressure (SBP)-lowering efficacy and safety of crystalline valsartan/sacubitril (LCZ696, an angiotensin receptor blocker-neprilysin inhibitor) 400 mg daily against valsartan (320 mg once daily) alone or coadministered with placebo or increasing doses of free sacubitril (50, 100, 200, or 400 mg once daily) to identify the optimal antihypertensive combination dose. This multicenter, double-blinded, 7-arm parallel-group study recruited patients with mild-to-moderate systolic hypertension (office SBP 150-179 mm Hg)...
June 2017: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/28315356/the-effect-of-angiotensin-receptor-neprilysin-inhibitor-sacubitril-valsartan-on-central-nervous-system-amyloid-%C3%AE-concentrations-and-clearance-in-the-cynomolgus-monkey
#14
Heidi A Schoenfeld, Tim West, Philip B Verghese, Mary Holubasch, Neeta Shenoy, David Kagan, Chiara Buono, Wei Zhou, Marc DeCristofaro, Julie Douville, Geoffrey G Goodrich, Keith Mansfield, Chandra Saravanan, Frederic Cumin, Randy L Webb, Randall J Bateman
Sacubitril/valsartan (LCZ696) is the first angiotensin receptor neprilysin inhibitor approved to reduce cardiovascular mortality and hospitalization in patients with heart failure with reduced ejection fraction. As neprilysin (NEP) is one of several enzymes known to degrade amyloid-β (Aβ), there is a theoretical risk of Aβ accumulation following long-term NEP inhibition. The primary objective of this study was to evaluate the potential effects of sacubitril/valsartan on central nervous system clearance of Aβ isoforms in cynomolgus monkeys using the sensitive Stable Isotope Labeling Kinetics (SILK™)-Aβ methodology...
May 15, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28281384/transport-properties-of-valsartan-sacubitril-and-its-active-metabolite-lbq657-as-determinants-of-disposition
#15
Imad Hanna, Natalya Alexander, Matthew H Crouthamel, John Davis, Adrienne Natrillo, Phi Tran, Arpine Vapurcuyan, Bing Zhu
1. The potential for drug-drug interactions of LCZ696 (a novel, crystalline complex comprising sacubitril and valsartan) was investigated in vitro. 2. Sacubitril was shown to be a highly permeable P-glycoprotein (P-gp) substrate and was hydrolyzed to the active anionic metabolite LBQ657 by human carboxylesterase 1 (CES1b and 1c). The multidrug resistance-associated protein 2 (MRP2) was shown to be capable of LBQ657 and valsartan transport that contributes to the elimination of either compound. 3. LBQ657 and valsartan were transported by OAT1, OAT3, OATP1B1 and OATP1B3, whereas no OAT- or OATP-mediated sacubitril transport was observed...
March 10, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28176630/novel-drugs-for-hypertension-and-heart-failure-struggling-for-a-place-under-the-sun
#16
Charles Faselis, Chrysoula Boutari, Michael Doumas, Konstantinos Imprialos, Konstantinos Stavropoulos, Peter Kokkinos
BACKGOUND: Current drug therapy for the management of arterial hypertension and heart failure has provided substantial benefits but has also some limitations. LCZ696, a dual inhibitor of angiotensin receptor blockers and neprilysin, and finerenone, a non-steroidal mineralocorticoid receptor antagonist, are two recently developed novel agents for the management of these conditions. METHODS: This review aims to present the pathophysiological basis for the use of these two novel drugs, critically discuss available clinical data, and provide future perspectives...
February 6, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28158398/systolic-blood-pressure-cardiovascular-outcomes-and-efficacy-and-safety-of-sacubitril-valsartan-lcz696-in-patients-with-chronic-heart-failure-and-reduced-ejection-fraction-results-from-paradigm-hf
#17
Michael Böhm, Robin Young, Pardeep S Jhund, Scott D Solomon, Jianjian Gong, Martin P Lefkowitz, Adel R Rizkala, Jean L Rouleau, Victor C Shi, Karl Swedberg, Michael R Zile, Milton Packer, John J V McMurray
Background: Compared to heart failure patients with higher systolic blood pressure (SBP), those with lower SBP have a worse prognosis. To make matters worse, the latter patients often do not receive treatment with life-saving therapies that might lower blood pressure further. We examined the association between SBP and outcomes in the Prospective Comparison of angiotensin receptor-neprilysin inhibitor (ARNI) with an angiotensin-converting enzyme (ACE) inhibitor to Determine Impact on Global Mortality and Morbidity in Heart Failure trial (PARADIGM-HF), as well as the effect of sacubitril/valsartan, compared with enalapril, according to baseline SBP...
April 14, 2017: European Heart Journal
https://www.readbyqxmd.com/read/28133468/changing-the-treatment-of-heart-failure-with-reduced-ejection-fraction-clinical-use-of-sacubitril-valsartan-combination
#18
REVIEW
Edgardo Kaplinsky
Despite significant therapeutic advances, patients with chronic heart failure (HF) remain at high risk of morbidity and mortality. Sacubitril valsartan (previously known as LCZ696) is a new oral agent approved for the treatment of symptomatic chronic heart failure in adults with reduced ejection fraction. It is described as the first in class angiotensin receptor neprilysin inhibitor (ARNI) since it incorporates the neprilysin inhibitor, sacubitril and the angiotensin II receptor antagonist, valsartan. Neprilysin is an endopeptidase that breaks down several vasoactive peptides including natriuretic peptides (NPs), bradykinin, endothelin and angiotensin II (Ang-II)...
November 2016: Journal of Geriatric Cardiology: JGC
https://www.readbyqxmd.com/read/28093466/effects-of-sacubitril-valsartan-versus-olmesartan-on-central-hemodynamics-in-the-elderly-with-systolic-hypertension-the-parameter-study
#19
Bryan Williams, John R Cockcroft, Kazuomi Kario, Dion H Zappe, Patrick C Brunel, Qian Wang, Weinong Guo
Effective treatment of systolic hypertension in elderly patients remains a major therapeutic challenge. A multicenter, double-blind, randomized controlled trial with sacubitril/valsartan (LCZ696), a first-in-class angiotensin receptor neprilysin inhibitor, was conducted to determine its effects versus olmesartan (angiotensin receptor blocker) on central aortic pressures, in elderly patients (aged ≥60 years) with systolic hypertension and pulse pressure >60 mm Hg, indicative of arterial stiffness. Patients (n=454; mean age, 67...
March 2017: Hypertension
https://www.readbyqxmd.com/read/28089685/evaluation-of-drug-drug-interaction-potential-between-sacubitril-valsartan-lcz696-and-statins-using-a-physiologically-based-pharmacokinetic-model
#20
Wen Lin, Tao Ji, Heidi Einolf, Surya Ayalasomayajula, Tsu-Han Lin, Imad Hanna, Tycho Heimbach, Christopher Breen, Venkateswar Jarugula, Handan He
Sacubitril/valsartan (LCZ696) has been approved for the treatment of heart failure. Sacubitril is an in vitro inhibitor of organic anion-transporting polypeptides (OATPs). In clinical studies, LCZ696 increased atorvastatin Cmax by 1.7-fold and area under the plasma concentration-time curve by 1.3-fold, but had little or no effect on simvastatin or simvastatin acid exposure. A physiologically based pharmacokinetics modeling approach was applied to explore the underlying mechanisms behind the statin-specific LCZ696 drug interaction observations...
January 13, 2017: Journal of Pharmaceutical Sciences
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