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- Title
PI-33.
- Authors
Kim, H.; Go, M.; Jung, H.; Yeo, C.; Shon, J.; Liu, K.; Shin, J.
- Abstract
Objectives: The disposition of lamivudine, a substrate of BCRP, was evaluated in relation to three BCRP genetic variations' Gln141Lys, Val12Met and Gln126Stop, that cause the altered transport activity in vitro.Method: A single oral dose of 100mg lamivudine was given to 22 Korean healthy male subjects whose BCRP genotypes were predetermined: 7 subjects with wild-type, 6 with Lys141/Lys141, 4 with Gln126/Stop126 and 5 with Met12/Met12, respectively. The plasma and urine of lamivudine were collected up to 24hours and pharmacokinetic parameters were estimated using WinNonlin®.Result: (See Table).Conclusion: In subjects with BCRP variant of Lys141/Lys141, pharmacokinetic parameter such as AUC and Cl varies up to 4 folds. In the other subjects, the variability were relatively small. There was no significant association between genotype and phenotype of BCRP in the disposition of lamivudine. It would be worth contribution of other several transporters (OCT, OAT, MRP) for lamivudine. Further studies are remained to evaluate the clinical relevance of these genetic variants of BCRP.Clinical Pharmacology & Therapeutics (2005) 79, P16–P16; doi: 10.1016/j.clpt.2005.12.054
- Subjects
ANTIRETROVIRAL agents; CHEMICAL inhibitors; GENETIC polymorphisms; GENETIC research; PHARMACOKINETICS; DRUG metabolism; PHARMACOLOGY; THERAPEUTICS
- Publication
Clinical Pharmacology & Therapeutics, 2006, Vol 79, Issue 2, pP16
- ISSN
0009-9236
- Publication type
Article
- DOI
10.1016/j.clpt.2005.12.054