Article: ABCB1 c.2677G>T/c.3435C>T diplotype increases the early-phase oral absorption of losartan.
Archives of pharmacal research
2020 Volume 43, Issue 11, Page(s) 1187–1196
Abstract: ... gene. ABCB1 c.2677G>T and c.3435C>T variants are known to be associated with reduced expression and ... of losartan. Thirty-eight healthy Korean volunteers with different ABCB1 diplotypes [c.2677G> T and c.3435C>T ... the concentrations of both samples were determined by HPLC method. Significant differences were observed in C ...
Abstract | Losartan has been shown to be a substrate of the drug-efflux transporter MDR1, encoded by the ABCB1 gene. ABCB1 c.2677G>T and c.3435C>T variants are known to be associated with reduced expression and function of P-glycoprotein (P-gp). We investigated the effects of ABCB1 diplotype on the pharmacokinetics of losartan. Thirty-eight healthy Korean volunteers with different ABCB1 diplotypes [c.2677G> T and c.3435C>T; carriers of GG/CC (n = 13), GT/CT (n = 12) and TT/TT (n = 13) diplotype] were recruited and administered a single 50 mg oral dose of losartan potassium. Losartan and its active metabolite E-3174 samples in plasma and urine were collected up to 10 and 8 h after drug administration, respectively, and the concentrations of both samples were determined by HPLC method. Significant differences were observed in C |
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MeSH term(s) | ATP Binding Cassette Transporter, Subfamily B/genetics ; ATP Binding Cassette Transporter, Subfamily B/metabolism ; Administration, Oral ; Adult ; Angiotensin II Type 1 Receptor Blockers/administration & dosage ; Angiotensin II Type 1 Receptor Blockers/pharmacokinetics ; Chromatography, High Pressure Liquid ; Gastrointestinal Absorption ; Genotype ; Humans ; Losartan/administration & dosage ; Losartan/pharmacokinetics ; Pharmacogenetics ; Pharmacogenomic Variants ; Republic of Korea ; Young Adult |
Chemical Substances | ABCB1 protein, human ; ATP Binding Cassette Transporter, Subfamily B ; Angiotensin II Type 1 Receptor Blockers ; Losartan (JMS50MPO89) |
Language | English |
Publishing date | 2020-11-29 |
Publishing country | Korea (South) |
Document type | Comparative Study ; Journal Article |
ZDB-ID | 447623-2 |
ISSN | 1976-3786 ; 0253-6269 |
ISSN (online) | 1976-3786 |
ISSN | 0253-6269 |
DOI | 10.1007/s12272-020-01294-3 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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