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https://www.readbyqxmd.com/read/28419972/neprilysin-inhibitors-a-new-hope-to-halt-the-diabetic-cardiovascular-and-renal-complications
#1
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...
April 15, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28417439/clinical-pharmacokinetics-of-sacubitril-valsartan-lcz696-a-novel-angiotensin-receptor-neprilysin-inhibitor
#2
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
#3
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
#4
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
#5
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)...
April 5, 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
#6
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...
April 17, 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28338503/efficacy-and-safety-of-crystalline-valsartan-sacubitril-lcz696-compared-to-placebo-and-combinations-of-free-valsartan-and-sacubitril-in-patients-with-systolic-hypertension-the-ratio-study
#7
Joseph L Izzo, Dion H Zappe, Yan Jia, Kudsia Hafeez, Jack Zhang
We compared the systolic blood pressure-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 co-administered with placebo or increasing doses of free sacubitril (50, 100, 200, or 400 mg once daily) in order 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 systolic BP 150-179 mmHg)...
March 23, 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
#8
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...
March 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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
https://www.readbyqxmd.com/read/28030431/efficacy-and-safety-of-sacubitril-valsartan-lcz696-add-on-to-amlodipine-in-asian-patients-with-systolic-hypertension-uncontrolled-with-amlodipine-monotherapy
#15
Ji-Guang Wang, Kimihiko Yukisada, Antonio Sibulo, Kudsia Hafeez, Yan Jia, Jack Zhang
OBJECTIVE: The objective of this study is to evaluate the efficacy and safety of sacubitril/valsartan (LCZ696, an angiotensin receptor and neprilysin inhibitor) add-on to amlodipine compared with amlodipine monotherapy in Asian patients with systolic hypertension uncontrolled with amlodipine. METHODS: Patients with mean clinic SBP at least 145 mmHg and less than 180 mmHg after a 4-week treatment with amlodipine 5 mg/day were randomized to receive LCZ696/amlodipine (200/5 mg/day) or amlodipine 5 mg/day for 8 weeks...
April 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/28024961/efficacy-and-safety-of-sacubitril-valsartan-lcz696-in-japanese-patients-with-chronic-heart-failure-and-reduced-ejection-fraction-rationale-for-and-design-of-the-randomized-double-blind-parallel-hf-study
#16
Hiroyuki Tsutsui, Shinichi Momomura, Yoshihiko Saito, Hiroshi Ito, Kazuhiro Yamamoto, Tomomi Ohishi, Naoko Okino, Weinong Guo
BACKGROUND: The prognosis of heart failure patients with reduced ejection fraction (HFrEF) in Japan remains poor, although there is growing evidence for increasing use of evidence-based pharmacotherapies in Japanese real-world HF registries. Sacubitril/valsartan (LCZ696) is a first-in-class angiotensin receptor neprilysin inhibitor shown to reduce mortality and morbidity in the recently completed largest outcome trial in patients with HFrEF (PARADIGM-HF trial). The prospectively designed phase III PARALLEL-HF (Prospective comparison of ARNI with ACE inhibitor to determine the noveL beneficiaL trEatment vaLue in Japanese Heart Failure patients) study aims to assess the clinical efficacy and safety of LCZ696 in Japanese HFrEF patients, and show similar improvements in clinical outcomes as the PARADIGM-HF study enabling the registration of LCZ696 in Japan...
December 23, 2016: Journal of Cardiology
https://www.readbyqxmd.com/read/28004291/sacubitril-valsartan-lcz696-in-heart-failure
#17
Yasser Khder, Victor Shi, John J V McMurray, Martin P Lefkowitz
It has been known since the 1990s that long-term morbidity and mortality is improved in patients with heart failure with reduced ejection fraction (HFrEF) by treatments that target the renin-angiotensin-aldosterone system (RAAS). It has also long been thought that enhancement of the activity of natriuretic peptides (NPs) could potentially benefit patients with HFrEF, but multiple attempts to realize this benefit had failed over the years - until 2014, when a large, phase III, randomized, controlled clinical trial (PARADIGM-HF) was completed comparing sacubitril/valsartan with enalapril, a well-established treatment for HFrEF...
December 22, 2016: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/27974807/long-term-neprilysin-inhibition-implications-for-arnis
#18
REVIEW
Duncan J Campbell
Neprilysin has a major role in both the generation and degradation of bioactive peptides. LCZ696 (valsartan/sacubitril, Entresto), the first of the new ARNI (dual-acting angiotensin-receptor-neprilysin inhibitor) drug class, contains equimolar amounts of valsartan, an angiotensin-receptor blocker, and sacubitril, a prodrug for the neprilysin inhibitor LBQ657. LCZ696 reduced blood pressure more than valsartan alone in patients with hypertension. In the PARADIGM-HF study, LCZ696 was superior to the angiotensin-converting enzyme inhibitor enalapril for the treatment of heart failure with reduced ejection fraction, and LCZ696 was approved by the FDA for this purpose in 2015...
March 2017: Nature Reviews. Cardiology
https://www.readbyqxmd.com/read/27972095/cost-effectiveness-of-sacubitril-valsartan-formerly-lcz696-in-chronic-heart-failure-patients-with-reduced-ejection-fraction-an-analysis-for-switzerland
#19
Z Ademi, E Hancock, D Trueman, A Pfeil, R Haroun, C Deschaseaux, M Schwenkglenks
No abstract text is available yet for this article.
November 2016: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
https://www.readbyqxmd.com/read/27892684/angiotensin-receptor-neprilysin-inhibitor-lcz696-pharmacology-pharmacokinetics-and-clinical-development
#20
Yue Hua, Ian Wang, Bin Liu, Darren J Kelly, Christopher Reid, Danny Liew, Yingchun Zhou, Bing H Wang
Heart failure still has a significant disease burden with poor outcomes worldwide despite advances in therapy. The standard therapies have been focused on blockade of renin-angiotensin-aldosterone system with angiotensin-converting enzyme inhibitors, angiotensin receptor blockers and mineralocorticoid antagonists and the sympathetic nervous system with β-blockers. The natriuretic peptide system is a potential counter-regulatory system that promotes vasodilatation and natriuresis. Angiotensin receptor neprilysin inhibitors are a new class drug capable of blocking the renin-angiotensin-aldosterone system and enhancing the natriuretic peptide system to improve neurohormonal balance...
November 28, 2016: Future Cardiology
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