Erratum to: Clinical Pharmacokinetics of Sacubitril/Valsartan (LCZ696): A Novel Angiotensin Receptor-Neprilysin Inhibitor

Clinical Pharmacokinetics
Surya AyalasomayajulaGangadhar Sunkara

Abstract

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, ~1.9-fold for sacubitrilat, and ~1.7-fold for valsartan in healthy subjects. Following multiple twice-daily administration, steady-state maximum plasma concentration was reached within 3 days, showing no accumulation for sacubitril and valsartan, while ~1.6-fold accumulation for sacubitrilat. Sacubitril is eliminated predominantly as sacubitrilat through the kidney; valsartan is eliminated mainly by biliary route. Drug-drug interactions of sacubitril/valsartan were evaluated with medications commonly used in patients with heart failure including furosemide, warfarin, digoxin, carvedilol, levonorgestrel/ethinyl estradiol combination, amlodipine, omeprazole, hydrochlorothiazide, intravenous nitrates, metfor...Continue Reading

References

May 1, 1976·Clinical Pharmacology and Therapeutics·B BeermannA Rosén
Nov 30, 1992·Biochemical and Biophysical Research Communications·I A de Lannoy, M Silverman
Jun 27, 1991·The New England Journal of Medicine·J Hirsh
Aug 1, 1991·The New England Journal of Medicine·E Braunwald
May 1, 1990·Clinical Pharmacokinetics·L L Ponto, R D Schoenwald
Jun 1, 1983·Drugs·M J Serlin, A M Breckenridge
Jan 1, 1983·European Journal of Clinical Pharmacology·C NiemeyerE Mutschler
Jan 1, 1997·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·F WaldmeierM De Gasparo
Mar 1, 1997·Journal of Clinical Pharmacology·D M ColussiG Y Lefèvre
Jan 1, 1997·European Journal of Clinical Pharmacology·G FleschP Lloyd
Jan 1, 1997·European Journal of Clinical Pharmacology·M BindschedlerG Preiswerk
Oct 23, 1997·Clinical Pharmacology and Therapeutics·L J BrookmanF Mullins
Jun 2, 2001·The New England Journal of Medicine·M PackerUNKNOWN Carvedilol Prospective Randomized Cumulative Survival Study Group
May 15, 2002·Progress in Cardiovascular Diseases·Eric J Eichhorn, Mihai Gheorghiade
Oct 23, 2002·Circulation·Milton PackerUNKNOWN Carvedilol Prospective Randomized Cumulative Survival (COPERNICUS) Study Group
Nov 1, 2002·Journal of Cardiovascular Pharmacology·Pratapa P PrasadJames McLeod
Jan 24, 2003·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·Robert P MyersSamuel S Lee
Oct 12, 2004·Genomics·Sharon MarshHoward L McLeod
Nov 19, 2005·Proceedings of the National Academy of Sciences of the United States of America·Adam M HawkridgeDavid C Muddiman
Apr 21, 2006·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Wakaba YamashiroYuichi Sugiyama
May 5, 2006·Fundamental & Clinical Pharmacology·Iouri BachmakovMartin F Fromm
Jun 1, 2006·Circulation·Mihai GheorghiadeWilson S Colucci
Dec 21, 2006·Clinical Pharmacology and Therapeutics·Pertti J NeuvonenJanne T Backman
Jan 27, 2007·Clinical Pharmacokinetics·Hongjian ZhangA David Rodrigues
Dec 25, 2007·Journal of the American College of Cardiology·Lori B Daniels, Alan S Maisel
Jan 25, 2008·American Journal of Physiology. Renal Physiology·Volker VallonSanjay K Nigam
Feb 5, 2008·Pharmacogenomics·Mikko Niemi
Jul 23, 2008·International Journal of Clinical Practice·N ChungT Fujita
Aug 6, 2008·European Journal of Clinical Pharmacology·Shaojun Shi, Ulrich Klotz
May 7, 2009·Expert Opinion on Drug Metabolism & Toxicology·Jürgen KindlaJörg König
Sep 30, 2009·British Journal of Pharmacology·A Kalliokoski, M Niemi
Oct 8, 2009·Circulation. Heart Failure·Eric E NiederkoflerUte Schellenberger
Jul 9, 2010·Clinical Pharmacokinetics·Ryuichi Ogawa, Hirotoshi Echizen
Nov 16, 2010·The New England Journal of Medicine·Faiez ZannadUNKNOWN EMPHASIS-HF Study Group
Jan 14, 2011·Hypertension Research : Official Journal of the Japanese Society of Hypertension·Ji-Guang WangUNKNOWN Asian Pacific Heart Association
Jun 30, 2011·European Heart Journal·UNKNOWN European Association for Cardiovascular Prevention & RehabilitationUNKNOWN ESC Committee for Practice Guidelines (CPG) 2008-2010 and 2010-2012 Committees
Mar 20, 2012·Heart Failure Reviews·John G F ClelandRenjith Antony
Jun 8, 2012·European Journal of Clinical Pharmacology·Yuki SuzakiKyoichi Ohashi
Jan 4, 2013·Diabetes/metabolism Research and Reviews·Ji-Guang Wang, Yan Li

❮ Previous
Next ❯

Citations


❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.