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Association between pharmacokinetics of lenvatinib in healthy subjects and genetic polymorphisms of ABCB1 3435C>T and ABCB1 2677G>T/A.
- Source :
- Xenobiotica; Dec 021, Vol. 51 Issue 12, p1463-1469, 7p
- Publication Year :
- 2021
-
Abstract
- The aim of this study was to evaluate the impact of genetic polymorphisms in the pharmacokinetics of metabolism and transportation of lenvatinib in the Chinese population. Sixty-three healthy Chinese individuals were recruited and administered with a single dose of 4 mg lenvatinib. Allelic discriminations for 10 SNPs of CYP3A4 (20230 G>A(*1G)), CYP3A5 (6986 A>G(*3)), ABCB1 (1236 C>T, 2677 G>T/A, 3435 C>T), ABCG2 (421 C>A, 34 G>A), ABCC2 (-24 C>T, 1249 G>A, 3972 C>T) were performed. The concentrations of lenvatinib in the plasma were determined by UPLC-MS/MS. Under the fasting condition, individuals carrying of ABCB1 3435 C>T genotype presented lower C<subscript>max</subscript> (p < 0.01) and λz (p < 0.05), but higher t<subscript>1/2</subscript> (p < 0.05) than those carrying C/C and T/T genotypes. For ABCB1 2677 G>T/A variant, individuals with the G/T and A/G genotype showed higher AUC (p < 0.05) and t<subscript>1/2</subscript> (p < 0.01), but lower λz (p < 0.05) than those carrying G/G genotypes. Individuals with the A/T, A/A and T/T genotype had higher AUC, but no significant differences (p > 0.05) were observed. They also had higher t<subscript>1/2</subscript> (p < 0.01) and lower λz (p < 0.01) than those carrying G/G genotypes. Under the fed condition, no difference in any pharmacokinetic parameters were observed with any polymorphisms in the 10 fragments. Data in this paper had demonstrated that polymorphisms ABCB1 3435 C>T and ABCB1 2677 G>T/A were associated with the pharmacokinetic variability of lenvatinib. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 00498254
- Volume :
- 51
- Issue :
- 12
- Database :
- Complementary Index
- Journal :
- Xenobiotica
- Publication Type :
- Academic Journal
- Accession number :
- 155030043
- Full Text :
- https://doi.org/10.1080/00498254.2021.2023913