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The ABCG2 transporter and its relations with the pharmacokinetics, drug interaction and lipid-lowering effects of statins

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Pages 49-62 | Published online: 23 Nov 2010

Keep up to date with the latest research on this topic with citation updates for this article.

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Najmeh Ahangari, Mohammad Doosti, Majid Ghayour Mobarhan, Amirhossein Sahebkar, Gordon A. Ferns & Alireza Pasdar. (2020) Personalised medicine in hypercholesterolaemia: the role of pharmacogenetics in statin therapy. Annals of Medicine 52:8, pages 462-470.
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Xue-Feng Lu, Yang Zhou, Kai-Shun Bi & Xiao-Hui Chen. (2016) Mixed effects of OATP1B1, BCRP and NTCP polymorphisms on the population pharmacokinetics of pravastatin in healthy volunteers. Xenobiotica 46:9, pages 841-849.
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Ioannis Koutsounas, Stamatios Theocharis, Ioanna Delladetsima, Efstratios Patsouris & Constantinos Giaginis. (2015) Farnesoid x receptor in human metabolism and disease: the interplay between gene polymorphisms, clinical phenotypes and disease susceptibility. Expert Opinion on Drug Metabolism & Toxicology 11:4, pages 523-532.
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Miao Hu & Brian Tomlinson. (2014) Evaluation of the pharmacokinetics and drug interactions of the two recently developed statins, rosuvastatin and pitavastatin. Expert Opinion on Drug Metabolism & Toxicology 10:1, pages 51-65.
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Miao Hu & Brian Tomlinson. (2013) Lipid-lowing pharmacogenomics in Chinese patients. Expert Review of Cardiovascular Therapy 11:8, pages 985-997.
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Rebecca Schnepf & Oliver Zolk. (2013) Effect of the ATP-binding cassette transporter ABCG2 on pharmacokinetics: experimental findings and clinical implications. Expert Opinion on Drug Metabolism & Toxicology 9:3, pages 287-306.
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Cesare R. Sirtori, Giuliana Mombelli, Michela Triolo & Reijo Laaksonen. (2012) Clinical response to statins: Mechanism(s) of variable activity and adverse effects. Annals of Medicine 44:5, pages 419-432.
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Gopal Krishna, Lei Ma, Pratapa Prasad, Allen Moton, Monika Martinho & Edward O'Mara. (2012) Effect of posaconazole on the pharmacokinetics of simvastatin and midazolam in healthy volunteers. Expert Opinion on Drug Metabolism & Toxicology 8:1, pages 1-10.
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Miao Hu, G Neil Thomas & Brian Tomlinson. (2011) Lipid disorders in Chinese populations. Clinical Lipidology 6:5, pages 549-562.
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Articles from other publishers (31)

Edward Zheng, Paulina Madura, Jakub Grandos, Marlena Broncel, Agnieszka Pawlos, Ewelina Woźniak & Paulina Gorzelak-Pabiś. (2024) When the same treatment has different response: The role of pharmacogenomics in statin therapy. Biomedicine & Pharmacotherapy 170, pages 115966.
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Marcos Ortiz-Uriarte, Jeanlouis Betancourt-Gaztambide, Alexandra Perez & Youssef M. Roman. (2023) Urate-Lowering Therapy Use among US Adults with Gout and the Relationship between Patients’ Gout Treatment Status and Associated Comorbidities. Rheumato 3:1, pages 74-85.
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Ola AlAzzeh & Youssef M Roman. (2023) The frequency of rs2231142 in ABCG2 among Native Hawaiian and Pacific Islander subgroups: implications for personalized rosuvastatin dosing . Pharmacogenomics 24:3, pages 173-182.
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Khalifa Alrajeh & Youssef M. Roman. (2023) The frequency of rs2231142 in ABCG2  among Asian subgroups: implications for personalized rosuvastatin dosing . Pharmacogenomics 24:1, pages 15-26.
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Ruijie D. Teo & D. Peter Tieleman. (2021) Modulation of Phospholipid Bilayer Properties by Simvastatin. The Journal of Physical Chemistry B 125:30, pages 8406-8418.
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Nada Božina, Lana Ganoci, Livija Simičević, Katarina Gvozdanović, Iva Klarica Domjanović, Margareta Fistrek Prlić, Tena Križ, Ana Borić Bilušić, Mario Laganović & Tamara Božina. (2021) Drug-drug-gene interactions as mediators of adverse drug reactions to diclofenac and statins: a case report and literature review. Archives of Industrial Hygiene and Toxicology 72:2, pages 114-128.
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Qingyang Xiao, Yitian Zhou & Volker M Lauschke. (2020) Impact of variants in ATP-binding cassette transporters on breast cancer treatment. Pharmacogenomics 21:18, pages 1299-1310.
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Qingyang Xiao, Yitian Zhou & Volker M. Lauschke. (2020) Ethnogeographic and inter-individual variability of human ABC transporters. Human Genetics 139:5, pages 623-646.
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David A. Rhodes, Hung-Chang Chen, James C. Williamson, Alfred Hill, Jack Yuan, Sam Smith, Harriet Rhodes, John Trowsdale, Paul J. Lehner, Thomas Herrmann & Matthias Eberl. (2018) Regulation of Human γδ T Cells by BTN3A1 Protein Stability and ATP-Binding Cassette Transporters. Frontiers in Immunology 9.
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Soo Hyeon BaeWan-Su ParkSeunghoon HanGab-jin ParkJongtae LeeTaegon HongSangil JeonDong-Seok Yim. (2018) Physiologically-based pharmacokinetic predictions of intestinal BCRP-mediated drug interactions of rosuvastatin in Koreans. The Korean Journal of Physiology & Pharmacology 22:3, pages 321.
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Alison E. Fohner, Deanna J. Brackman, Kathleen M. Giacomini, Russ B. Altman & Teri E. Klein. (2017) PharmGKB summary. Pharmacogenetics and Genomics 27:11, pages 420-427.
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Soo Hyeon Bae, Wan-Su Park, Seunghoon Han, Gab-jin Park, Jongtae Lee, Taegon Hong, Sangil Jeon & Dong-Seok Yim. (2017) Retracted: Physiologically based pharmacokinetic predictions of intestinal BCRP-mediated effect of telmisartan on the pharmacokinetics of rosuvastatin in humans. Biopharmaceutics & Drug Disposition 38:5, pages 363-363.
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Elena Arrigoni, Marzia Del Re, Leonardo Fidilio, Stefano Fogli, Romano Danesi & Antonello Di Paolo. (2017) Pharmacogenetic Foundations of Therapeutic Efficacy and Adverse Events of Statins. International Journal of Molecular Sciences 18:1, pages 104.
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Pedro Caetano-Pinto, Jitske Jansen, Yehuda G. Assaraf & Rosalinde Masereeuw. (2017) The importance of breast cancer resistance protein to the kidneys excretory function and chemotherapeutic resistance. Drug Resistance Updates 30, pages 15-27.
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Yufeng Wu, Ruirui Si, Sen Yang, Suhua Xia, Zelai He, Lili Wang, Zhen He, Qiming Wang & Hong Tang. (2016) Depression induces poor prognosis associates with the down-regulation brain derived neurotrophic factor of serum in advanced small cell lung cancer. Oncotarget 7:52, pages 85975-85986.
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Miao Hu, Hon-Kit Lee, Kenneth K. W. To, Benny S. P. Fok, Siu-Kwan Wo, Chung-Shun Ho, Chun-Kwok Wong, Zhong Zuo, Thomas Y. K. Chan, Juliana C. N. Chan & Brian Tomlinson. (2016) Telmisartan increases systemic exposure to rosuvastatin after single and multiple doses, and in vitro studies show telmisartan inhibits ABCG2-mediated transport of rosuvastatin. European Journal of Clinical Pharmacology 72:12, pages 1471-1478.
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Mei Liu, Xiu-Jun Wu, Gui-Lian Zhao, Ti Zhang, Shan-Sen Xu, Ya-Xin Sun, Feng Qiu & Li-Mei Zhao. (2016) Effects of Polymorphisms in NR1H4, NR1I2, SLCO1B1, and ABCG2 on the Pharmacokinetics of Rosuvastatin in Healthy Chinese Volunteers. Journal of Cardiovascular Pharmacology 68:5, pages 383-390.
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Cheynne McLean, Aze Wilson & Richard B. Kim. (2016) Impact of Transporter Polymorphisms on Drug Development: Is It Clinically Significant?. The Journal of Clinical Pharmacology 56, pages S40-S58.
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Yufeng Wu, Ruirui Si, Hong Tang, Zhen He, Hui Zhu, Lili Wang, Yingchao Fan, Suhua Xia, Zelai He & Qiming Wang. (2015) Cholesterol reduces the sensitivity to platinum-based chemotherapy via upregulating ABCG2 in lung adenocarcinoma. Biochemical and Biophysical Research Communications 457:4, pages 614-620.
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Mijeong Son, Yukyung Kim, Donghwan Lee, Hyerang Roh, Hankil Son, Jinju Guk, Seong Bok Jang, Su Youn Nam & Kyungsoo Park. (2014) Pharmacokinetic Interaction Between Rosuvastatin and Telmisartan in Healthy Korean Male Volunteers: A Randomized, Open-label, Two-period, Crossover, Multiple-dose Study. Clinical Therapeutics 36:8, pages 1147-1158.
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RH Rose, S Neuhoff, K Abduljalil, M Chetty, A Rostami‐Hodjegan & M Jamei. (2014) Application of a Physiologically Based Pharmacokinetic Model to Predict OATP1B1 ‐Related Variability in Pharmacodynamics of Rosuvastatin . CPT: Pharmacometrics & Systems Pharmacology 3:7, pages 1-9.
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Kenneth KW To, Miao Hu & Brian Tomlinson. (2014) Expression and activity of ABCG2, but not ABCB1 or OATP1B1, are associated with cholesterol levels: evidence from in vitro and in vivo experiments. Pharmacogenomics 15:8, pages 1091-1104.
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Yi-Lung Ding, Yu-Hsuan Shih, Fu-Yuan Tsai & Max K. Leong. (2014) In Silico Prediction of Inhibition of Promiscuous Breast Cancer Resistance Protein (BCRP/ABCG2). PLoS ONE 9:3, pages e90689.
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Hon-Kit Lee, Miao Hu, Sandra SH Lui, Chung-Shun Ho, Chun-Kwok Wong & Brian Tomlinson. (2013) Effects of polymorphisms in ABCG2 , SLCO1B1 , SLC10A1 and CYP2C9 / 19 on plasma concentrations of rosuvastatin and lipid response in Chinese patients . Pharmacogenomics 14:11, pages 1283-1294.
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Miao Hu & Brian Tomlinson. (2013) Pharmacogenomics of lipid-lowering therapies. Pharmacogenomics 14:8, pages 981-995.
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Lei Zhang, Gilbert J. Burckart, Lawrence J. Lesko & Shiew‐Mei Huang. 2013. Pharmacogenomics of Human Drug Transporters. Pharmacogenomics of Human Drug Transporters 39 71 .
Anne Sophie Grandvuinet, Henrik Tang Vestergaard, Nicolas Rapin & Bente Steffansen. (2012) Intestinal transporters for endogenic and pharmaceutical organic anions: the challenges of deriving in-vitro kinetic parameters for the prediction of clinically relevant drug–drug interactions. Journal of Pharmacy and Pharmacology 64:11, pages 1523-1548.
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Miao Hu, Sandra S.H. Lui, Lai-Shan Tam, Edmund K. Li & Brian Tomlinson. (2012) The farnesoid X receptor -1G>T polymorphism influences the lipid response to rosuvastatin. Journal of Lipid Research 53:7, pages 1384-1389.
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Miao Hu, Bernard M.Y. Cheung & Brian Tomlinson. (2012) Safety of statins: an update. Therapeutic Advances in Drug Safety 3:3, pages 133-144.
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K. L. MEALEY. (2011) ABCG2 transporter: therapeutic and physiologic implications in veterinary species. Journal of Veterinary Pharmacology and Therapeutics 35:2, pages 105-112.
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Bruno Stieger & Peter J Meier. (2011) Pharmacogenetics of drug transporters in the enterohepatic circulation. Pharmacogenomics 12:5, pages 611-631.
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