PharmGKB very important pharmacogene: SLCO1B1

Pharmacogenetics and Genomics

Volumn 20, Issue 3, 2010, Pages 211-216

  Oshiro, Connie ^a   Mangravite, Lara ^c   Klein, Teri ^a   Altman, Russ ^a,b  

^a STANFORD UNIVERSITY   (United States)

^b STANFORD UNIVERSITY MEDICAL CENTER   (United States)

^c CHILDREN S HOSPITAL OAKLAND RESEARCH INSTITUTE   (United States)

Author keywords

OATP2; Organic anion transporter; Pharmacogenomics; Pharmacokinetics; SLCO1B1; Statins

Indexed keywords

7 ETHYL 10 HYDROXYCAMPTOTHECIN; ATORVASTATIN; ATRASENTAN; BOSENTAN; CASPOFUNGIN; CERIVASTATIN; ENALAPRILAT; ENZYME INHIBITOR; ESTRADIOL 17 GLUCURONIDE; ESTRONE SULFATE; LEUKOTRIENE C4; LEUKOTRIENE E4; LIOTHYRONINE; MEVINOLIN; OLMESARTAN; ORGANIC ANION TRANSPORTER 2; PENICILLIN G; PITAVASTATIN; PRASTERONE SULFATE; PRAVASTATIN; PROSTAGLANDIN E2; REPAGLINIDE; ROSUVASTATIN; TAUROCHOLIC ACID; TEMOCAPRIL; THROMBOXANE B2; THYROXINE; TROGLITAZONE; UNINDEXED DRUG; VALSARTAN;

DRUG ACTIVITY; ENZYME INHIBITION; ENZYME SUBSTRATE; HUMAN; NONHUMAN; PHARMACOGENETICS; PRIORITY JOURNAL; REVIEW;

ALLELES; AMINO ACID SEQUENCE; DATABASES, GENETIC; EXONS; GENE FREQUENCY; GENETIC VARIATION; HUMANS; INHIBITORY CONCENTRATION 50; KINETICS; KNOWLEDGE BASES; LIGANDS; MOLECULAR SEQUENCE DATA; ORGANIC ANION TRANSPORTERS; PHARMACEUTICAL PREPARATIONS; PHARMACOGENETICS; POLYMORPHISM, SINGLE NUCLEOTIDE; PROTEIN TRANSPORT; SEQUENCE HOMOLOGY, AMINO ACID; SUBSTRATE SPECIFICITY;

EID: 76749146910     PISSN: 17446872     EISSN: 17446880     Source Type: Journal    
DOI: 10.1097/FPC.0b013e328333b99c     Document Type: Review

References (70)

1. Gui C, Hagenbuch B. Amino acid residues in transmembrane domain 10 of organic anion transporting polypeptide 1B3 are critical for cholecystokinin octapeptide transport. Biochemistry 2008; 47:9090-9097.
2. Niemi M. Role of OATP transporters in the disposition of drugs. Pharmacogenomics 2007; 8:787-802.
3. Hagenbuch B, Meier PJ. The superfamily of organic anion transporting polypeptides. Biochim Biophys Acta 2003; 1609:1-18.
4. Hagenbuch B, Meier PJ. Organic anion transporting polypeptides of the OATP/ SLC21 family: phylogenetic classification as OATP/ SLCO superfamily, new nomenclature and molecular/functional properties. Pflugers Arch 2004; 447:653-665.
5. Konig J, Cui Y, Nies AT, Keppler D. A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane. Am J Physiol Gastrointest Liver Physiol 2000; 278:G156-G164.
6. Hsiang B, Zhu Y, Wang Z, Wu Y, Sasseville V, Yang WP, Kirchgessner TG. A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. J Biol Chem 1999; 274:37161-37168.
7. Shimizu M, Fuse K, Okudaira K, Nishigaki R, Maeda K, Kusuhara H, Sugiyama Y. Contribution of OATP (organic anion-transporting polypeptide) family transporters to the hepatic uptake of fexofenadine in humans. Drug Metab Dispos 2005; 33:1477-1481.
8. Erdman AR, Mangravite LM, Urban TJ, Lagpacan LL, Castro RA, de la Cruz M, et al. The human organic anion transporter 3 (OAT3; SLC22A8): genetic variation and functional genomics. Am J Physiol Renal Physiol 2006; 290:F905-F912.
9. Mangravite LM, Krauss RM. Pharmacogenomics of statin response. Curr Opin Lipidol 2007; 18:409-414.
10. Abe T, Kakyo M, Tokui T, Nakagomi R, Nishio T, Nakai D, et al. Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1. J Biol Chem 1999; 274:17159-17163.
11. Tirona RG, Leake BF, Merino G, Kim RB. Polymorphisms in OATP-C: identification of multiple allelic variants associated with altered transport activity among European-and African-Americans. J Biol Chem 2001; 276:35669-35675.
12. Tamai I, Nezu J, Uchino H, Sai Y, Oku A, Shimane M, Tsuji A. Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun 2000; 273:251-260.
13. Gui C, Miao Y, Thompson L, Wahlgren B, Mock M, Stieger B, Hagenbuch B. Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3. Eur J Pharmacol 2008; 584:57-65.
14. Kameyama Y, Yamashita K, Kobayashi K, Hosokawa M, Chiba K. Functional characterization of SLCO1B1 (OATP-C) variants, SLCO1B1*5, SLCO1B1*15 and SLCO1B1*15+ C1007G, by using transient expression systems of HeLa and HEK293 cells. Pharmacogenet Genomics 2005; 15:513-522.
15. Nakai D, Nakagomi R, Furuta Y, Tokui T, Abe T, Ikeda T, Nishimura K. Human liver-specific organic anion transporter, LST-1, mediates uptake of pravastatin by human hepatocytes. J Pharmacol Exp Ther 2001; 97:861-867.
16. Chen C, Mireles RJ, Campbell SD, Lin J, Mills JB, Xu JJ, Smolarek TA. Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1. Drug Metab Dispos 2005; 33:537-546.
17. Hirano M, Maeda K, Shitara Y, Sugiyama Y. Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther 2004; 311:139-146.
18. Hirano M, Maeda K, Shitara Y, Sugiyama Y. Drug-drug interaction between pitavastatin and various drugs via OATP1B1. Drug Metab Dispos 2006; 34:1229-1236.
19. Ho RH, Tirona RG, Leake BF, Glaeser H, Lee W, Lemke CJ, et al. Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology 2006; 130:1793-1806.
20. Kalliokoski A, Neuvonen M, Neuvonen PJ, Niemi M. Different effects of SLCO1B1 polymorphism on the pharmacokinetics and pharmacodynamics of repaglinide and nateglinide. J Clin Pharmacol 2008; 48:311-321.
21. Niemi M, Backman JT, Kajosaari LI, Leathart JB, Neuvonen M, Daly AK, et al. Polymorphic organic anion transporting polypeptide 1B1 is a major determinant of repaglinide pharmacokinetics. Clin Pharmacol Ther 2005; 77:468-478.
22. Nozawa T, Minami H, Sugiura S, Tsuji A, Tamai I. Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms. Drug Metab Dispos 2005; 33:434-439.
23. Treiber A, Schneiter R, Hausler S, Stieger B. Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil. Drug Metab Dispos 2007; 35:1400-1407.
24. Katz DA, Carr R, Grimm DR, Xiong H, Holley-Shanks R, Mueller T, et al. Organic anion transporting polypeptide 1B1 activity classified by SLCO1B1 genotype influences atrasentan pharmacokinetics. Clin Pharmacol Ther 2006; 79:186-196.
25. Liu L, Cui Y, Chung AY, Shitara Y, Sugiyama Y, Keppler D, Pang KS. Vectorial transport of enalapril by Oatp1a1/Mrp2 and OATP1B1 and OATP1B3/MRP2 in rat and human livers. J Pharmacol Exp Ther 2006; 318:395-402.
26. Maeda K, Ieiri I, Yasuda K, Fujino A, Fujiwara H, Otsubo K, et al. Effects of organic anion transporting polypeptide 1B1 haplotype on pharmacokinetics of pravastatin, valsartan, and temocapril. Clin Pharmacol Ther 2006; 79:427-439.
27. Yamashiro W, Maeda K, Hirouchi M, Adachi Y, Hu Z, Sugiyama Y. 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 2006; 34:1247-1254.
28. Suwannakul S, Ieiri I, Kimura M, Kawabata K, Kusuhara H, Hirota T, et al. Pharmacokinetic interaction between pravastatin and olmesartan in relation to SLCO1B1 polymorphism. J Hum Genet 2008; 53:899-904.
29. Yamada A, Maeda K, Kamiyama E, Sugiyama D, Kondo T, Shiroyanagi Y, et al. Multiple human isoforms of drug transporters contribute to the hepatic and renal transport of olmesartan, a selective antagonist of the angiotensin II AT1-receptor. Drug Metab Dispos 2007; 35:2166-2176.
30. Sandhu P, Lee W, Xu X, Leake BF, Yamazaki M, Stone JA, et al. Hepatic uptake of the novel antifungal agent caspofungin. Drug Metab Dispos 2005; 33:676-682.
31. Nozawa T, Sugiura S, Nakajima M, Goto A, Yokoi T, Nezu J, et al. Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. Drug Metab Dispos 2004; 32:291-294.
32. Lu WJ, Tamai I, Nezu J, Lai ML, Huang JD. Organic anion transporting polypeptide-C mediates arsenic uptake in HEK-293 cells. J Biomed Sci 2006; 13:525-533.
33. Niemi M, Kivisto KT, Hofmann U, Schwab M, Eichelbaum M, Fromm MF. Fexofenadine pharmacokinetics are associated with a polymorphism of the SLCO1B1 gene (encoding OATP1B1). Br J Clin Pharmacol 2005; 59:602-604. (Pubitemid 40632253)
34. Cui Y, Konig J, Leier I, Buchholz U, Keppler D. Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J Biol Chem 2001; 276:9626-9630.
35. Wang P, Kim RB, Chowdhury JR, Wolkoff AW. The human organic anion transport protein SLC21A6 is not sufficient for bilirubin transport. J Biol Chem 2003; 278:20695-20699.
36. Wurtman RJ. The effects of light on man and other mammals. Annu Rev Physiol 1975; 37:467-483.
37. Migliorini MG, Galvan P, Sbrana G, Donzelli GP, Vecchi C. Bilirubin photoconversion induced by monochromatic laser radiation. Comparison between aerobic and anaerobic experiments in vitro. Biochem J 1988; 256:841-846.
38. Kivisto KT, Niemi M. Influence of drug transporter polymorphisms on pravastatin pharmacokinetics in humans. Pharm Res 2007; 24:239-247.
39. Corsini A, Bellosta S, Baetta R, Fumagalli R, Paoletti R, Bernini F. New insights into the pharmacodynamic and pharmacokinetic properties of statins. Pharmacol Ther 1999; 84:413-428.
40. Link E, Parish S, Armitage J, Bowman L, Heath S, Matsuda F, et al. SLCO1B1 variants and statin-induced myopathy-a genomewide study. N Engl J Med 2008; 359:789-799.
41. Bachmakov I, Glaeser H, Fromm MF, Konig J. Interaction of oral anti-diabetic drugs with hepatic uptake transporters: focus on organic anion transporting polypeptides and organic cation transporter 1. Diabetes 2008; 57:1463-1469.
42. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, Fattinger K. Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology 2002; 36:164-172.
43. Nozawa T, Nakajima M, Tamai I, Noda K, Nezu J, Sai Y, et al. Genetic polymorphisms of human organic anion transporters OATP-C (SLC21A6) and OATP-B (SLC21A9): allele frequencies in the Japanese population and functional analysis. J Pharmacol Exp Ther 2002; 302:804-813.
44. Van der Deure WM, Friesema EC, de Jong FJ, de Rijke YB, de Jong FH, Uitterlinden AG, et al. Organic anion transporter 1B1: an important factor in hepatic thyroid hormone and estrogen transport and metabolism. Endocrinology 2008; 149:4695-4701.
45. Iwai M, Suzuki H, Ieiri I, Otsubo K, Sugiyama Y. Functional analysis of single nucleotide polymorphisms of hepatic organic anion transporter OATP1B1 (OATP-C). Pharmacogenetics 2004; 14:749-757.
46. Nishizato Y, Ieiri I, Suzuki H, Kimura M, Kawabata K, Hirota T, et al. Polymorphisms of OATP-C (SLC21A6) and OAT3 (SLC22A8) genes: consequences for pravastatin pharmacokinetics. Clin Pharmacol Ther 2003; 73:554-565. (Pubitemid 37249126)
47. Niemi M, Schaeffeler E, Lang T, Fromm MF, Neuvonen M, Kyrklund C, et al. High plasma pravastatin concentrations are associated with single nucleotide polymorphisms and haplotypes of organic anion transporting polypeptide-C (OATP-C, SLCO1B1). Pharmacogenetics 2004; 14:429-440.
48. Ho RH, Choi L, Lee W, Mayo G, Schwarz UI, Tirona RG, et al. Effect of drug transporter genotypes on pravastatin disposition in European-and African-American participants. Pharmacogenet Genomics 2007; 17:647-656.
49. Mwinyi J, Johne A, Bauer S, Roots I, Gerloff T. Evidence for inverse effects of OATP-C (SLC21A6) 5 and 1b haplotypes on pravastatin kinetics. Clin Pharmacol Ther 2004; 75:415-421.
50. Pasanen MK, Fredrikson H, Neuvonen PJ, Niemi M. Different effects of SLCO1B1 polymorphism on the pharmacokinetics of atorvastatin and rosuvastatin. Clin Pharmacol Ther 2007; 82:726-733.
51. Thompson JF, Man M, Johnson KJ, Wood LS, Lira ME, Lloyd DB, et al. An association study of 43 SNPs in 16 candidate genes with atorvastatin response. Pharmacogenomics J 2005; 5:352-358.
52. Takane H, Miyata M, Burioka N, Shigemasa C, Shimizu E, Otsubo K, Ieiri I. Pharmacogenetic determinants of variability in lipid-lowering response to pravastatin therapy. J Hum Genet 2006; 51:822-826.
53. Igel M, Arnold KA, Niemi M, Hofmann U, Schwab M, Lutjohann D, et al. Impact of the SLCO1B1 polymorphism on the pharmacokinetics and lipid-lowering efficacy of multiple-dose pravastatin. Clin Pharmacol Ther 2006; 79:419-426.
54. Tachibana-Iimori R,Tabara Y, Kusuhara H, Kohara K, Kawamoto R, Nakura J, et al. Effect of genetic polymorphism of OATP-C (SLCO1B1) on lipid-lowering response to HMG-CoA reductase inhibitors. Drug Metab Pharmacokinet 2004; 19:375-380.
55. Neuvonen PJ, Backman JT, Niemi M. Pharmacokinetic comparison of the potential over-the-counter statins simvastatin, lovastatin, fluvastatin and pravastatin. Clin Pharmacokinet 2008; 47:463-474.
56. Zhang W, Chen BL, Ozdemir V, He YJ, Zhou G, Peng DD, et al. SLCO1B1 521T- C functional genetic polymorphism and lipid-lowering efficacy of multiple-dose pravastatin in Chinese coronary heart disease patients. Br J Clin Pharmacol 2007; 64:346-352.
57. Kalliokoski A, Backman JT, Kurkinen KJ, Neuvonen PJ, Niemi M. Effects of gemfibrozil and atorvastatin on the pharmacokinetics of repaglinide in relation to SLCO1B1 polymorphism. Clin Pharmacol Ther 2008; 84:488-496.
58. Kalliokoski A, Neuvonen M, Neuvonen PJ, Niemi M. The effect of SLCO1B1 polymorphism on repaglinide pharmacokinetics persists over a wide dose range. Br J Clin Pharmacol 2008; 66:818-825.
59. Innocenti F, Kroetz DL, Schuetz E, Dolan ME, Ramirez J, Relling M, et al. Comprehensive pharmacogenetic analysis of irinotecan neutropenia and pharmacokinetics. J Clin Oncol 2009; 27:2604-2614.
60. Han JY, Lim HS, Park YH, Lee SY, Lee JS. Integrated pharmacogenetic prediction of irinotecan pharmacokinetics and toxicity in patients with advanced non-small cell lung cancer. Lung Cancer 2009; 63:115-120.
61. Takane H, Kawamoto K, Sasaki T, Moriki K, Moriki K, Kitano H, et al. Life-threatening toxicities in a patient with UGT1A1*6/*28 and SLCO1B1*15/*15 genotypes after irinotecan-based chemotherapy. Cancer Chemother Pharmacol 2009; 63:1165-1169.
62. Xiang X, Jada SR, Li HH, Fan L, Tham LS, Wong CI, et al. Pharmacogenetics of SLCO1B1 gene and the impact of *1b and *15 haplotypes on irinotecan disposition in Asian cancer patients. Pharmacogenet Genomics 2006; 16:683-691.
63. Werner D, Werner U, Meybaum A, Schmidt B, Umbreen S, Grosch A, et al. Determinants of steady-state torasemide pharmaco-kinetics: impact of pharmacogenetic factors, gender and angiotensin II receptor blockers. Clin Pharmacokinet 2008; 47:323-332.
64. Hopkins PN, Wu LL, Hunt SC, James BC, Vincent GM, Williams RR. Higher serum bilirubin is associated with decreased risk for early familial coronary artery disease. Arterioscler Thromb Vasc Biol 1996; 16:250-255.
65. Zhang W, He YJ, Gan Z, Fan L, Li Q,Wang A, et al. OATP1B1 polymorphism is a major determinant of serum bilirubin level but not associated with rifampicin-mediated bilirubin elevation. Clin Exp Pharmacol Physiol 2007; 34:1240-1244.
66. Johnson AD, Kavousi M, Smith AV, Chen MH, Dehghan A, Aspelund T, et al. Genome-wide association meta-analysis for total serum bilirubin levels. Hum Mol Genet 2009; 18:2700-2710.
67. Mwinyi J, Kopke K, Schaefer M, Roots I, Gerloff T. Comparison of SLCO1B1 sequence variability among German, Turkish, and African populations. Eur J Clin Pharmacol 2008; 64:257-266.
68. Ho WF, Koo SH, Yee JY, Lee EJ. Genetic variations of the SLCO1B1 gene in the Chinese, Malay and Indian populations of Singapore. Drug Metab Pharmacokinet 2008; 23:476-482.
69. Couvert P, Giral P, Dejager S, Gu J, Huby T, Chapman MJ, et al. Association between a frequent allele of the gene encoding OATP1B1 and enhanced LDL-lowering response to fluvastatin therapy. Pharmacogenomics 2008; 9:1217-1227.
70. Pasanen MK, Backman JT, Neuvonen PJ, Niemi M. Frequencies of single nucleotide polymorphisms and haplotypes of organic anion transporting polypeptide 1B1 SLCO1B1 gene in a Finnish population. Eur J Clin Pharmacol 2006; 62:409-415.