Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 48, 2018 - Issue 3
966
Views
22
CrossRef citations to date
0
Altmetric
Xenobiotic Transporters

Transport properties of valsartan, sacubitril and its active metabolite (LBQ657) as determinants of disposition

, , , , , , & show all
Pages 300-313 | Received 17 Jan 2017, Accepted 10 Feb 2017, Published online: 10 Mar 2017

References

  • Ayalasomayajula S, Han Y, Langenickel T, et al. (2016a). In vitro and clinical evaluation of OATP-mediated drug interaction potential of sacubitril/valsartan (LCZ696). J Clin Pharm Ther 41:424–31
  • Ayalasomayajula S, Langenickel T, Jordaan P, et al. (2016b). Effect of renal function on the pharmacokinetics of LCZ696 (sacubitril/valsartan), an angiotensin receptor neprilysin inhibitor. Eur J Clin Pharmacol 72:1065–73
  • Bednarczyk D, Boiselle C. (2016). Organic anion transporting polypeptide (OATP)-mediated transport of coproporphyrins I and III. Xenobiotica 46:457–66
  • Brookman LJ, Rolan PE, Benjamin IS, et al. (1997). Pharmacokinetics of valsartan in patients with liver disease. Clin Pharmacol Ther 62:272–8
  • Byrne JA, Strautnieks SS, Miel-Vergani G, et al. (2002). The human bile salt export pump: Characterization of substrate specificity and identification of inhibitors. Gastroenterology 123:1649–58
  • Challa VR, Babu PR, Challa SR, et al. (2012). Pharmacokinetic interaction study between quercetin and valsartan in rats and in vitro models. Drug Dev Ind Pharm 39:865–72
  • Colombo F, Poirier H, Rioux N, et al. (2013). A membrane vesicle-based assay to enable prediction of human biliary excretion. Xenobiotica 43:915–19
  • Colussi DM, Parisot C, Rossolino ML, et al. (1997). Protein binding in plasma of valsartan, a new angiotensin II receptor antagonist. J Clin Pharmacol 37:214–21
  • Duan P, Li S, Ai N, et al. (2012). Potent inhibitors of human organic anion transporters 1 and 3 from clinical drug libraries: discovery and molecular characterization. Mol Pharm 9:3340–6
  • Entresto™ Prescribing Information. Highlights of Prescribing information. US FDA, 2015. Available from: https://www.pharma.us.novartis.com/sites/www.pharma.us.novartis.com/files/entresto.pdf (last accessed 12 Jan 2016)
  • Flarakos J, Du Y, Bedman T, et al. (2016). Disposition and metabolism of [(14)C] sacubitril/valsartan (formerly LCZ696) an angiotensin receptor neprilysin inhibitor, in healthy subjects. Xenobiotica 46:986–1000
  • Gan L, Jiang X, Mendonza A, et al. (2016). Pharmacokinetic drug-drug interaction assessment of LCZ696 (an angiotensin receptor neprilysin inhibitor) with omeprazole, metformin or levonorgestrel-ethinyl estradiol in healthy subjects. Clin Pharmacol Drug Dev 5:27–39
  • Groves CE, Evans K, Dantzler WH, et al. (1994). Peritubular organic cation transport in isolated rabbit proximal tubules. Am J Physiol 266:F450–8
  • Haugen DA, Suttue JW. (1974). Purification and properties of rat liver microsomal esterases. J Biol Chem 249:2717–22
  • Hirano M, Maeda K, Shitara Y, Sugiyama Y. (2004). Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther 311:139–46
  • Hirano M, Maeda K, Shitara Y, Sugiyama Y. (2006). Drug-drug interaction between pitavastatin and various drugs via OATP1B1. Drug Metab Dispos 34:1229–36
  • Hooiveld GJ, Heegsma J, van Montfoort JE, et al. (2002). Stereoselective transport of hydrophilic quaternary drugs by human MDR1 and rat Mdr1b P-glycoproteins. Br J Pharmacol 135:1685–94
  • Hosey CM, Chan R, Benet LZ. (2016). BDDCS predictions, self-correcting aspects of BDDCS assignments, BDDCS assignment corrections, and classification for more than 175 additional drugs. AAPS J 18:251–60
  • Hsiao HL, Langenickel TH, Greeley M, et al. (2015). Pharmacokinetic drug-drug interaction assessment between LCZ696, an angiotensin receptor neprilysin inhibitor, and hydrochlorothiazide, amlodipine, or carvedilol. Clin Pharmacol Drug Dev 4:407–17
  • Hunter J, Jepson M, Tsuruo T, et al. (1993). Functional expression of P-glycoprotein in apical membranes of human intestinal Caco-2 cells. Kinetics of vinblastine secretion and interaction with modulators. J Biol Chem 268:14991–7
  • Imai T, Imoto M, Sakamoto H, Hashimoto M. (2005). Identification of esterases expressed in Caco-2 cells and effects of their hydrolyzing activity in predicting human intestinal absorption. Drug Metab Dispos 33:1185–90
  • Ingraham L, Li M, Renfro JL, et al. (2014). A plasma concentration of α-ketoglutarate influences the kinetic interaction of ligands with organic anion transporter 1. Mol Pharmacol 86:86–95
  • Ishiguro N, Maeda K, Kishimoto W, et al. (2006). Predominant contribution of OATP1B3 to the hepatic uptake of telmisartan, an angiotensin II receptor antagonist, in humans. Drug Metab Dispos 34:1109–15
  • Kobalava Z, Kotovskaya Y, Averkov O, et al. (2016). Pharmacodynamic and pharmacokinetic profiles of sacubitril/valsartan (LCZ696) in patients with heart failure and reduced ejection fraction. Cardiovasc Ther. 34:191–8
  • König J, Cui Y, Nies AT, Keppler D. (2000). Localization and genomic organization of a new hepatocellular organic anion transporting polypeptide J Biol Chem 275:23161–8
  • Liu H, Goldenberg A, Chen Y, et al. (2016). Molecular properties of drugs interacting with SLC22 transporters OAT1, OAT3, OCT1, and OCT2: a machine-learning approach. J Pharmacol Exp Ther 359:215–29
  • Ma J, Maliepaard M, Nooter K, et al. (1998). Reduced cellular accumulation of topotecan: a novel mechanism of resistance in a human ovarian cancer cell line. Br J Cancer 77:1645–52
  • Maeda K, Ieiri I, Yasuda K, et al. (2006). Effects of organic anion transporting polypeptide 1B1 haplotype on pharmacokinetics of pravastatin, valsartan, and temocapril. Clin Pharmacol Ther 79:427–39
  • Matsushima S, Maeda K, Ishiguro N, et al. (2008). Investigation of the inhibitory effects of various drugs on the hepatic uptake of fexofenadine in humans. Drug Metab Dispos 36:663–9
  • McMurray J, Packer M, Desai A, et al. (2014). Angiotensin-neprilysin inhibition versus enalapril in heart failure. N Engl J Med 371:993–1004
  • Peterson M, Mooseker M. (1992). Characterization of the enterocyte-like brush border cytoskeleton of the C2BBe clones of the human intestinal cell line, Caco-2. J Cell Sci 102:581–600
  • Prasad B, Johnson K, Billington S, et al. (2016). Abundance of drug transporters in the human kidney cortex as quantified by quantitative targeted proteomics. Drug Metab Dispos 44:1920–4
  • Pratt J, Venkatraman N, Brinker A, et al. (2012). Use of zinc finger nuclease technology to knock out efflux transporters in C2BBe1 cells. Curr Protoc Toxicol 52:23.2.1–22
  • Sato M, Iwanaga T, Mamada H, et al. (2008). Involvement of uric acid transporters in alteration of serum uric acid level by angiotensin II receptor blockers. Pharm Res 25:639–46
  • Shi J, Wang X, Nguyen J, et al. (2016). Sacubitril is selectively activated by carboxylesterase 1 (CES1) in the liver and the activation is affected by CES1 genetic variation. Drug Metab Dispos 44:554–9
  • Shimizu M, Fuse K, Okudaira K, et al. (2005). Contribution of OATP (organic anion-transporting polypeptide) family transporters to the hepatic uptake of fexofenadine in humans. Drug Metab Dispos 33:1477–81
  • Tsutsui H, Momomura S, Saito Y, et al. (2016). 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. J Cardiol S0914-5087:30309-4
  • United States Food and Drug Administration. (2012). FDA Draft DDI Guidance 2012. Available from: http://www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation/guidances/ucm292362.pdf
  • Yamada A, Maeda K, Ishiguro N, et al. (2011). The impact of pharmacogenetics of metabolic enzymes and transporters on the pharmacokinetics of telmisartan in healthy volunteers. Pharmacogenet Genomics 21:523–30
  • Yamashiro W, Maeda K, Hirouchi M, et al. (2006). Involvement of transporters in the hepatic uptake and biliary excretion of valsartan, a selective antagonist of the angiotensin II AT1-receptor, in humans. Drug Metab Dispos 34:1247–54
  • Waldmeier F, Flesch G, Müller P, et al. (1997). Pharmacokinetics, disposition and biotransformation of [14C]-radiolabelled valsartan in healthy male volunteers after a single oral dose. Xenobiotica 27:59–71
  • Watanabe T, Kusuhara H, Watanabe T, et al. (2011). Prediction of the overall renal tubular secretion and hepatic clearance of anionic drugs and a renal drug-drug interaction involving organic anion transporter 3 in humans by in vitro uptake experiments. Drug Metab Dispos 39:1031–8
  • Wienkers L, Heath T. (2005). Predicting in vivo drug interactions from in vitro drug discovery data. Nat Rev Drug Discov 4:825–33
  • Wongwanakul R, Vardhanabhuti N, Siripong P, Jianmongkol S. (2013). Effects of rhinacanthin-C on function and expression of drug efflux transporters in Caco-2 cells. Fitoterapia 89:80–5
  • Wu CY, Benet LZ. (2005). Predicting drug disposition via application of BCS: Transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm Res 22:11–23
  • Xia C, Yang J, Gan L. (2005). Breast cancer resistance protein in pharmacokinetics and drug-drug interactions. Expert Opin Drug Metab Toxicol 1:595–611

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.