Pharmacokinetic and pharmacogenomic profiles of telmisartan after the oral microdose and therapeutic dose

Pharmacogenetics and Genomics

Volumn 21, Issue 8, 2011, Pages 495-505

  Ieiri, Ichiro ^a   Nishimura, Chisa ^a   Maeda, Kazuya ^c   Sasaki, Tomohiro ^a   Kimura, Miyuki ^b   Chiyoda, Takeshi ^d   Hirota, Tekeshi ^a   Irie, Shin ^b   Shimizu, Hitoshi ^e   Noguchi, Takanori ^f   Yoshida, Kenji ^e   Sugiyama, Yuichi ^c  

^a KYUSHU UNIVERSITY   (Japan)

^b Kyushu Clinical Pharmacology Research Clinic   (Japan)

^c UNIVERSITY OF TOKYO   (Japan)

^d Sumida Hospital   (Japan)

^e SEKISUI CHEMICAL CO LTD   (Japan)

^f TORAY RESEARCH CENTER INC   (Japan)

Author keywords

microdose; OATP1B3; pharmacogenomics; telmisartan; therapeutic dose; UGT1As

Indexed keywords

DRUG METABOLITE; GLUCURONIDE; GLUCURONOSYLTRANSFERASE 1A1; GLUCURONOSYLTRANSFERASE 1A3; TELMISARTAN;

ADULT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DNA FLANKING REGION; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG DOSE COMPARISON; DRUG ELIMINATION; DRUG EXPOSURE; DRUG HALF LIFE; DRUG MICRODOSE; EXON; GENETIC SCREENING; GENETIC VARIABILITY; GENOTYPE; HAPLOTYPE; HUMAN; HUMAN EXPERIMENT; INTRON; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; NUCLEOTIDE SEQUENCE; PHARMACOGENOMICS; PLASMA CONCENTRATION-TIME CURVE; PRIORITY JOURNAL; SINGLE NUCLEOTIDE POLYMORPHISM; TIME TO MAXIMUM PLASMA CONCENTRATION;

EID: 79960837480     PISSN: 17446872     EISSN: 17446880     Source Type: Journal    
DOI: 10.1097/FPC.0b013e3283489ce2     Document Type: Article

References (29)

1. Watanabe M, Inukai K, Sumita T, Ikebukuro K, Ito D, Kurihara S, et al. Effects of telmisartan on insulin resistance in Japanese type 2 diabetic patients. Intern Med 2010; 49:1843-1847.
2. Gillespie EL, White CM, Kardas M, Lindberg M, Coleman CI. The impact of ACE inhibitors or angiotensin II type 1 receptor blockers on the development of new-onset type 2 diabetes. Diabetes Care 2005; 28:2261-2266. (Pubitemid 41242483)
3. Stangier J, Su CA, Schöndorfer G, Roth W. Pharmacokinetics and safety of intravenous and oral telmisartan 20mg and 120 mg in subjects with hepatic impairment compared with healthy volunteers. J Clin Pharmacol 2000; 40:1355-1364.
4. Stangier J, Schmid J, Türck D, Switek H, Verhagen A, Peeters PA, et al. Absorption, metabolism, and excretion of intravenously and orally administered [14C]telmisartan in healthy volunteers. J Clin Pharmacol 2000; 40:1312-1322.
5. WienenW, Entzeroth M, Van Meel JCA, Stangier J, Busch U, Ebner T, et al. A review on telmisartan: a novel, long-acting angiotensin II-receptor antagonist. Cardiovasc Drug Rev 2000; 18:127-156. (Pubitemid 30637040)
6. Stangier J, Su CA, Roth W. Pharmacokinetics of orally and intravenously administered telmisartan in healthy young and elderly volunteers and in hypertensive patients. J Int Med Res 2000; 28:149-167. (Pubitemid 30648951)
7. König J, Cui Y, Nies AT, Keppler D. Localization and genomic organization of a new hepatocellular organic anion transporting polypeptide. J Biol Chem 2000; 275:23161-23168. (Pubitemid 30646210)
8. Ieiri I, Higuchi S, Sugiyama Y. Genetic polymorphisms of uptake (OATP1B1, 1B3) and efflux (MRP2, BCRP) transporters: implications for inter-individual differences in the pharmacokinetics and pharmacodynamics of statins and other clinically relevant drugs. Expert Opin Drug Metab Toxicol 2009; 5:703-729.
9. Ishiguro N, Maeda K, Kishimoto W, Saito A, Harada A, Ebner T, et al. Predominant contribution of OATP1B3 to the hepatic uptake of telmisartan, an angiotensin II receptor antagonist, in humans. Drug Metab Dispos 2006; 34:1109-1115.
10. Ishiguro N, Maeda K, Saito A, Kishimoto W, Matsushima S, Ebner T, et al. Establishment of a set of double transfectants coexpressing organic anion transporting polypeptide 1B3 and hepatic efflux transporters for the characterization of the hepatobiliary transport of telmisartan acylglucuronide. Drug Metab Dispos 2008; 36:796-805. (Pubitemid 351468387)
11. Smith NF, Marsh S, Scott-Horton TJ, Hamada A, Mielke S, Mross K, et al. Variants in the SLCO1B3 gene: interethnic distribution and association with paclitaxel pharmacokinetics. Clin Pharmacol Ther 2007; 81:76-82. (Pubitemid 46050869)
12. Kiyotani K, Mushiroda T, Kubo M, Zembutsu H, Sugiyama Y, Nakamura Y. Association of genetic polymorphisms in SLCO1B3 and ABCC2 with docetaxel-induced leukopenia. Cancer Sci 2008; 99:967-972. (Pubitemid 351997599)
13. Ebner T, RothW. In vitro glucuronidation of telmisartan, a novel angiotensin II receptor antagonist (abstract). J Hum Hypertens 1999; 113:S12.
14. Busch U, Ebner T, Heinzel G, Schmid J, Schmaus H. Special in vitro and in vivo investigations on the pharmacokinetics of telmisartan and its glucuronide (abstract). J Hum Hypertens 1999; 113:S11.
15. Chen Y, Chen S, Li X,Wang X, Zeng S. Genetic variants of human UGT1A3: functional characterization and frequency distribution in a Chinese Han population. Drug Metab Dispos 2006; 34:1462-1467. (Pubitemid 44285386)
16. Iwai M, Maruo Y, Ito M, Yamamoto K, Sato H, Takeuchi Y. Six novel UDPglucuronosyltransferase (UGT1A3) polymorphisms with varying activity. J Hum Genet 2004; 49:123-128. (Pubitemid 38506725)
17. Riedmaier S, Klein K, Hofmann U, Keskitalo JE, Neuvonen PJ, Schwab M, et al. UDP-glucuronosyltransferase (UGT) polymorphisms affect atorvastatin lactonization in vitro and in vivo. Clin Pharmacol Ther 2010; 87:65-73.
18. Committee for Medical Products for Human Use. Position paper on nonclinical safety studies to support clinical trials with a single microdose. EMEA, CPMP/SWP/2599/02/Rev. 1, 2004.
19. Combes RD, Berridge T, Connelly J, Eve MD, Garner RC, Toon S, et al. Early microdose drug studies in human volunteers can minimise animal testing: Proceedings of a workshop organised by Volunteers in Research and Testing. Eur J Pharm Sci 2003; 19:1-11. (Pubitemid 36506932)
20. Ministry of Health, Labour and Welfare. Guidance. Tokyo, Japan: Microdose Clinical Studies, Ministry of Health, Labour, and Welfare, Pharmaceutical and Medical Safety Bureau, 2008.
21. Lappin G, Shishikura Y, Jochemsen R, Weaver RJ, Gesson C, Houston B, et al. Pharmacokinetics of fexofenadine: evaluation of a microdose and assessment of absolute oral bioavailability. Eur J Pharm Sci 2010; 40:125-131.
22. Lappin G, Kuhnz W, Jochemsen R, Kneer J, Chaudhary A, Oosterhuis B, et al. Use of microdosing to predict pharmacokinetics at the therapeutic dose: experience with 5 drugs. Clin Pharmacol Ther 2006; 80:203-215. (Pubitemid 44313903)
23. Beal SL, Sheiner LB. NONMEM User's Guides. San Francisco, CA, NONMEM Project Group, University of California at San Francisco, San Francisco, CA, 1986.
24. Ide T, Sasaki T, Maeda K, Higuchi S, Sugiyama Y, Ieiri I. Quantitative population pharmacokinetic analysis of pravastatin using an enterohepatic circulation model combined with pharmacogenomic information on SLCO1B1 and ABCC2 polymorphisms. J Clin Pharmacol 2009; 49:1309-1317.
25. Purcell S, Neale B, Todd-Brown K, Thomas L, Ferreira MA, Bender D, et al. PLINK: A tool set for whole-genome association and population-based linkage analysis. Am J Hum Genet 2007; 81:559-575. (Pubitemid 47330214)
26. Broad Institute of MIT and Harvard. Haploview http://www.broad.mit.edu/ mpg/haploview.
27. Tsujimoto M, Hirata S, Dan Y, Ohtani H, Sawada Y. Polymorphisms and linkage disequilibrium of the OATP8 (OATP1B3) gene in Japanese subjects. Drug Metab Pharmacokinet 2006; 21:165-169.
28. Letschert K, Keppler D, König J. Mutations in the SLCO1B3 gene affecting the substrate specificity of the hepatocellular uptake transporter OATP1B3 (OATP8). Pharmacogenetics 2004; 14:441-452. (Pubitemid 38971234)
29. Caillier B, Lé pine J, Tojcic J, Mé nard V, Perusse L, Bé langer A, et al. A pharmacogenomics study of the human estrogen glucuronosyltransferase UGT1A3. Pharmacogenet Genom 2007; 17:481-495. (Pubitemid 46905215)