Montelukast disposition: No indication of transporter-mediated uptake in OATP2B1 and OATP1B1 expressing HEK293 cells

Pharmaceutics

Volumn 7, Issue 4, 2015, Pages 554-564

  Brännström, Marie ^a   Nordell, P ^a   Bonn, Britta ^a   Davis, Andrew M ^a   Palmgren, Anna Pia ^a   Hilgendorf, Constanze ^a   Rubin, Katarina ^a   Grime, Ken ^a  

^a ASTRAZENECA R AND D   (Sweden)

Author keywords

Hepatic uptake; Montelukast; OATP1B1; OATP2B1; Transporters

Indexed keywords

MONTELUKAST; ORGANIC ANION TRANSPORTER B; SOLUTE CARRIER ORGANIC ANION TRANSPORTER 1B1; SOLUTE CARRIER ORGANIC ANION TRANSPORTER 1B3;

ARTICLE; CONTROLLED STUDY; DRUG DISPOSITION; DRUG TRANSPORT; DRUG UPTAKE; HEK293 CELL LINE; HUMAN; HUMAN CELL; PH; PROTEIN EXPRESSION; PROTEIN FUNCTION;

EID: 84949804180     PISSN: None     EISSN: 19994923     Source Type: Journal    
DOI: 10.3390/pharmaceutics7040554     Document Type: Article

References (25)

1. Paggiaro, P.; Bacci, E. Montelukast in asthma: A review of its efficacy and place in therapy. Ther. Adv. Chronic Dis. 2011, 2, 47-58.
2. Lima, J.J. Treatment heterogeneity in asthma: Genetics of response to leukotriene modifiers. Mol. Diagn. Ther. 2007, 11, 97-104.
3. Cheng, H.; Leff, J.A.; Amin, R.; Gertz, B.J.; De Smet, M.; Noonan, N.; Rogers, J.D.; Malbecq, W.; Meisner, D.; Somers, G. Pharmacokinetics, bioavailability, and safety of montelukast sodium (MK-0476) in healthy males and females. Pharm. Res. 1996, 13, 445-448.
4. Zhao, J.J.; Rogers, J.D.; Holland, S.D.; Larson, P.; Amin, R.D.; Haesen, R.; Freeman, A.; Seiberling, M.; Merz, M.; Cheng, H. Pharmacokinetics and bioavailability of montelukast sodium (MK-0476) in healthy young and elderly volunteers. Biopharm. Drug Dispos. 1997, 18, 769-777.
5. Mougey, E.B.; Feng, H.; Castro, M.; Irvin, C.G.; Lima, J.J. Absorption of montelukast is transporter mediated: A common variant of OATP2B1 is associated with reduced plasma concentrations and poor response. Pharmacogenet. Genomics 2009, 19, 129-138.
6. Giacomini, K.M.; Huang, S.-M.; Tweedie, D.J.; Benet, L.Z.; Brouwer, K.L.R.; Chu, X.; Dahlin, A.; Evers, R.; Fischer, V.; Hillgren, K.M., et al. for The International Transporter Consortium Membrane transporters in drug development. Nat. Rev. DrugDiscov. 1996, 9, 215-236.
7. Chu, X.; Philip, G.; Evers, R. et al. (2009): Absorption of montelukast is transporter mediated: A common variant of OATP2B1 is associated with reduced plasma concentrations and poor response. Pharmacogenet. Genomics 2012, 22, 319-324.
8. Karlgren, M.; Vildhede, A.; Norinder, U.; Wisniewski, J.R.; Kimoto, E.; Lai, Y.; Haglund, U.; Artursson, P. Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): Influence of protein expression on drug-drug interactions. J. Med. Chem. 2012, 55, 4740-4763.
9. Sharma, P.; Holmes, V.; Elsby, R.; Lambert, C.; Surry, D. Validation of cell-based OATP1B1 assays to assess drug transport and the potential for drug-drug interaction to support regulatory submissions. Xenobiotica 2010, 40, 24-37.
10. European Medicines Agency. Guideline on the Investigation of Drug Interactions; European Medicines Agency: London, UK, 2012; p. 21. Available online: http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2012/07/WC500129606.pdf (accessed on 2 December 2015).
11. Nordell, P.; Svanberg, P.; Bird, J.; Grime, K. Predicting metabolic clearance for drugs that are actively transported into hepatocytes: Incubational binding as a consequence of in vitro hepatocyte concentration is a key factor. Drug Metab. Dispos. 2013, 41, 836-843.
12. Holm, S. A simple sequentially rejective multiple test procedure. Scand. J. Statist. 1979, 6, 65-70.
13. Okumo, A.; DiMaso, M.; Löbenberg, R. Dynamic dissolution testing to establish in vitro/in vivo correlations for montelukast sodium, a poorly soluble drug. Pharm. Res. 2008, 25, 2778-2785.
14. Annaert, P.; Ye, Z.W.; Stieger, B.; Augustijns, P. Interaction of HIV protease inhibitors with OATP1B1, 1B3, and 2B1. Xenobiotica 2010, 40, 163-176.
15. Pizzagalli, F.; Varga, Z.; Huber, R.D.; Folkers, G.; Meier, P.J.; St-Pierre, M.V. Identification of steroid sulfate transport processes in the human mammary gland. J. Clin. Endocrinol. Metab. 2003, 88, 3902-3912.
16. Tamai, I.; Nozawa, T.; Koshida, M.; Nezu, J.-I.; Sai, Y.; Tsuji, A. Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C. Pharm. Res. 2001, 18, 1262-1269.
17. Varma, M.V.; Rotter, C.J.; Chupka, J.; Whalen, K.M.; Duignan, D.B.; Feng, B.; Litchfield, J.; Goosen, T.C.; El-Kattan, A.F. pH-Sensitive interaction of HMG-CoA reductase inhibitors (statins) with organic anion transporting polypeptide 2B1. Mol. Pharm. 2011, 8, 1303-1313.
18. Kataoka, M.; Yano, K.; Hamatsu, Y.; Masaoka, Y.; Sakuma, S.; Yamashita, S. Assessment of absorption potential of poorly water-soluble drugs by using the dissolution/permeation system. Eur. J. Pharm. Biopharm. 2013, 85, 1317-1324.
19. Kim, K.-A.; Lee, H.-M.; Joo, H.-J.; Park, I.-B.; Park, J.-Y. Effects of polymorphisms of the SLC02B1 gene on the pharmacokinetics of montelukast in humans. J. Clin. Pharmacol. 2013, 53, 1186-1193.
20. Letschert, K.; Faulstich, H.; Kelle, D.; Keppler, D. Molecular characterization and inhibition of amanitin uptake into human hepatocytes. Toxicol. Sci. 2006, 91, 140-149.
21. Tamraz, B.; Fukushima, H.; Wolfe, A.R.; Kaspera, R.; Totah, R.A.; Floyd, J.S.; Ma, B.; Chu, C.; Marciante, K.D.; Heckbert, S.R., et al. OATP1B1-related drug-drug and drug-gene interactions as potential risk factors for cerivastatin-induced rhabdomyolysis. Pharmacogenet. Genomics 2013, 23, 355-364.
22. Soars, M.G.; Grime, K.; Sproston, J.L.; Webborn, P.J.H.; Riley, R.J. Use of hepatocytes to assess the contribution of hepatic uptake to clearance in vivo. Drug Metab. Dispos. 2007, 35, 859-865.
23. Soars, M.G.; Barton, P.; Ismair, M.; Jupp, R.; Riley, R.J. The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery. Drug Metab. Dispos. 2012, 40, 1641-1648.
24. Grime, K.; Barton, P.; McGinnity, D. Application of In Silico, In Vitro and Preclinical Pharmacokinetic Data for the Effective and Efficient Prediction of Human Pharmacokinetics. Mol. Pharm. 2013, 10, 1191-1206.
25. Gardiner, P.; Paine, S.W. The impact of hepatic uptake on the pharmacokinetics of organic anions. DrugMetab. Dispos. 2011, 39, 1930-1938.