Influence of hepatic and intestinal efflux transporters and their genetic variants on the pharmacokinetics and pharmacodynamics of raloxifene in osteoporosis treatment

Translational Research

Volumn 160, Issue 4, 2012, Pages 298-308

  Trdan Lušin, Tina ^a   Mrhar, Aleš ^a   Stieger, Bruno ^b   Kullak Ublick, Gerd A ^b   Marc, Janja ^a   Ostanek, Barbara ^a   Zavratnik, Andrej ^c   Kristl, Albin ^a   Berginc, Katja ^a   Delić, Katja ^a   Trontelj, Jurij ^a  

^a UNIVERSITY OF LJUBLJANA   (Slovenia)

^b UNIVERSITY HOSPITAL ZURICH   (Switzerland)

^c UNIVERSITY MEDICAL CENTRE LJUBLJANA   (Slovenia)

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE TRIPHOSPHATASE; BREAST CANCER RESISTANCE PROTEIN; DRUG METABOLITE; GLUCURONIDE; GLYCOPROTEIN P; MULTIDRUG RESISTANCE PROTEIN 1; MULTIDRUG RESISTANCE PROTEIN 2; MULTIDRUG RESISTANCE PROTEIN 3; RALOXIFENE; RALOXIFENE 4' BETA GLUCURONIDE; RALOXIFENE 6 BETA GLUCURONIDE; RALOXIFENE 6,4' DIGLUCURONIDE; UNCLASSIFIED DRUG;

ALLELE; ARTICLE; ARTIFICIAL MEMBRANE; BONE DENSITY; CELL STRAIN CACO 2; DRUG BLOOD LEVEL; DRUG DISPOSITION; DRUG PROTEIN BINDING; DRUG TRANSPORT; ENZYME ASSAY; FEMALE; GENETIC POLYMORPHISM; GENETIC VARIABILITY; HIP; HUMAN; IN VITRO STUDY; IN VIVO STUDY; MAJOR CLINICAL STUDY; MEMBRANE PERMEABILITY; MONOLAYER CULTURE; OSTEOPOROSIS; POSTMENOPAUSE; PRIORITY JOURNAL;

EID: 84866373717     PISSN: 19315244     EISSN: 18781810     Source Type: Journal    
DOI: 10.1016/j.trsl.2012.03.002     Document Type: Article

References (34)

1. S. Choudhuri, and C.D. Klaassen Structure, function, expression, genomic organization, and single nucleotide polymorphisms of human ABCB1 (MDR1), ABCC (MRP), and ABCG2 (BCRP) efflux transporters Int J Toxicol 25 2006 231 259
2. B. Stieger, and P.J. Meier Pharmacogenetics of drug transporters in the enterohepatic circulation Pharmacogenomics 12 2011 611 631
3. P.D. Delmas, N.H. Bjarnason, and B.H. Mitlak Effects of raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal women N Engl J Med 337 1997 1641 1647
4. C.C. Johnston Jr., N.H. Bjarnason, and F.J. Cohen Long-term effects of raloxifene on bone mineral density, bone turnover, and serum lipid levels in early postmenopausal women: three-year data from 2 double-blind, randomized, placebo-controlled trials Arch Intern Med 160 2000 3444 3450
5. B. Ettinger, D.M. Black, and B.H. Mitlak Reduction of vertebral fracture risk in postmenopausal women with osteoporosis treated with raloxifene: results from a 3-year randomized clinical trial. Multiple Outcomes of Raloxifene Evaluation (MORE) Investigators JAMA 282 1999 637 645
6. E.S. Siris, S.T. Harris, and R. Eastell Skeletal effects of raloxifene after 8 years: results from the continuing outcomes relevant to Evista (CORE) study J Bone Miner Res 20 2005 1514 1524
7. D. Hochner-Celnikier Pharmacokinetics of raloxifene and its clinical application Eur J Obstet Gynecol Reprod Biol 85 1999 23 29
8. E.J. Jeong, Y. Liu, H. Lin, and M. Hu Species- and disposition model-dependent metabolism of raloxifene in gut and liver: role of UGT1A10 Drug Metab Dispos 33 2005 785 794
9. US Food and Drug Administration. NDA-020-815. Rockville, MD; 1999. Available at: http://www.fda.gov/cder/foi/nda/99/20815S3-Evista.htm. Accessed February 10, 2009.
10. J.A. Dodge, C.W. Lugar, and S. Cho Evaluation of the major metabolites of raloxifene as modulators of tissue selectivity J Steroid Biochem Mol Biol 61 1997 97 106
11. J.H. Chang, C.J. Kochansky, and M. Shou The role of P-glycoprotein in the bioactivation of raloxifene Drug Metab Dispos 34 2006 2073 2078
12. E.J. Jeong, H. Lin, and M. Hu Disposition mechanisms of raloxifene in the human intestinal Caco-2 model J Pharmacol Exp Ther 310 2004 376 385
13. S. Hoffmeyer, O. Burk, and O. von Richter Functional polymorphisms of the human multidrug-resistance gene: multiple sequence variations and correlation of one allele with P-glycoprotein expression and activity in vivo Proc Natl Acad Sci U S A 97 2000 3473 3478
14. S.J. Hemauer, T.N. Nanovskaya, S.Z. Abdel-Rahman, S.L. Patrikeeva, G.D. Hankins, and M.S. Ahmed Modulation of human placental P-glycoprotein expression and activity by MDR1 gene polymorphisms Biochem Pharmacol 79 2010 921 925
15. C.J. Foote, W. Greer, and B.A. Kiberd MDR1 C3435T polymorphisms correlate with cyclosporine levels in de novo renal recipients Transplant Proc 38 2006 2847 2849
16. S. Basic, S. Hajnsek, and N. Bozina The influence of C3435T polymorphism of ABCB1 gene on penetration of phenobarbital across the blood-brain barrier in patients with generalized epilepsy Seizure 17 2008 524 530
17. A. Saitoh, K.K. Singh, and C.A. Powell An MDR1-3435 variant is associated with higher plasma nelfinavir levels and more rapid virologic response in HIV-1 infected children AIDS 19 2005 371 380
18. M. Naesens, D.R. Kuypers, K. Verbeke, and Y. Vanrenterghem Multidrug resistance protein 2 genetic polymorphisms influence mycophenolic acid exposure in renal allograft recipients Transplantation 82 2006 1074 1084
19. S. Laechelt, E. Turrini, A. Ruehmkorf, W. Siegmund, I. Cascorbi, and S. Haenisch Impact of ABCC2 haplotypes on transcriptional and posttranscriptional gene regulation and function Pharmacogenomics J 11 2011 25 34
20. B. Briggs, P.J. Baker, and M.D. Belvo Microbial process for preparation of glucuronides of raloxifene J Ind Microbiol Biotechnol 23 1999 194 197
21. T. Trdan, R. Roskar, J. Trontelj, M. Ravnikar, and A. Mrhar Determination of raloxifene and its glucuronides in human urine by liquid chromatography-tandem mass spectrometry assay J Chromatogr B Analyt Technol Biomed Life Sci 879 2011 2323 2331
22. K. Berginc, S. Zakelj, and A. Kristl In vitro interactions between aged garlic extract and drugs used for the treatment of cardiovascular and diabetic patients Eur J Nutr 49 2010 373 384
23. J. Noe, B. Stieger, and P.J. Meier Functional expression of the canalicular bile salt export pump of human liver Gastroenterology 123 2002 1659 1666
24. D.R. de Waart, C.C. Paulusma, C. Kunne, and R.P. Oude Elferink Multidrug resistance associated protein 2 mediates transport of prostaglandin E2 Liver Int 26 2006 362 368
25. T. Gerloff, B. Stieger, and B. Hagenbuch The sister of P-glycoprotein represents the canalicular bile salt export pump of mammalian liver J Biol Chem 273 1998 10046 10050
26. J. Trontelj, M. Bogataj, J. Marc, and A. Mrhar Development and validation of a liquid chromatography-tandem mass spectrometry assay for determination of raloxifene and its metabolites in human plasma J Chromatogr B Analyt Technol Biomed Life Sci 855 2007 220 227
27. H. Schmidt-Gayk, E. Spanuth, and J. Kotting Performance evaluation of automated assays for beta-CrossLaps, N-MID-Osteocalcin and intact parathyroid hormone (BIOROSE Multicenter Study) Clin Chem Lab Med 42 2004 90 95
28. A. Dahan, and G.L. Amidon Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting Am J Physiol Gastrointest Liver Physiol 297 2009 G371 G377
29. A.K. Luders, R. Saborowski, and U. Bickmeyer Inhibition of multidrug/xenobiotic resistance transporter by MK571 improves dye (Fura 2) accumulation in crustacean tissues from lobster, shrimp, and isopod Comp Biochem Physiol C Toxicol Pharmacol 150 2009 368 371
30. C. Hegedus, G. Szakacs, and L. Homolya Ins and outs of the ABCG2 multidrug transporter: an update on in vitro functional assays Adv Drug Deliv Rev 61 2009 47 56
31. E. Jeannesson, L. Albertini, and G. Siest Determination of ABCB1 polymorphisms and haplotypes frequencies in a French population Fundam Clin Pharmacol 21 2007 411 418
32. J.E. Keskitalo, O. Zolk, M.F. Fromm, K.J. Kurkinen, P.J. Neuvonen, and M. Niemi ABCG2 polymorphism markedly affects the pharmacokinetics of atorvastatin and rosuvastatin Clin Pharmacol Ther 86 2009 197 203
33. B.J. Aungst, N.H. Nguyen, J.P. Bulgarelli, and K. Oates-Lenz The influence of donor and reservoir additives on Caco-2 permeability and secretory transport of HIV protease inhibitors and other lipophilic compounds Pharm Res 17 2000 1175 1180
34. F. Faassen, J. Kelder, J. Lenders, R. Onderwater, and H. Vromans Physicochemical properties and transport of steroids across Caco-2 cells Pharm Res 20 2003 177 186