Genetic variations of the ABC transporter gene ABCB11 encoding the human bile salt export pump (BSEP) in a Japanese population.

abstract：:The hepatic uptake transporter organic anion transporting polypeptide (OATP) 1B1 is inhibited by some uremic toxins; however, direct inhibition can only partially explain the delayed systemic elimination of substrate drugs in renal failure patients. This study aimed to examine the long-lasting inhibition of OATP1B1 by...

journal_title：Drug metabolism and pharmacokinetics

authors： Masuo Y,Fujita KI,Mishiro K,Seba N,Kogi T,Okumura H,Matsumoto N,Kunishima M,Kato Y

更新日期：2020-12-01 00:00:00

abstract：:The drug interaction between new quinolone antibiotics (NQs) and polyvalent metal cation products, leading to a significant decrease in the absorption of NQ, is considered to be attributable to the formation of poorly absorbable chelate and physicochemical adsorption of NQs to cation products. To clarify the mechanism...

journal_title：Drug metabolism and pharmacokinetics

authors： Imaoka A,Hattori M,Akiyoshi T,Ohtani H

更新日期：2014-01-01 00:00:00

abstract：:The work described in this study aimed to express CYP2C8 wild-type and mutant proteins in bacterial expression system and to use the expressed proteins to investigate the structural and functional consequences of a reported allele CYP2C8(*)4 (carrying Ile264Met substitution) on protein activity. Ile264 was replaced by...

journal_title：Drug metabolism and pharmacokinetics

authors： Singh R,Ting JG,Pan Y,Teh LK,Ismail R,Ong CE

更新日期：2008-01-01 00:00:00

abstract：:Genetic polymorphisms in xenobiotic transporters have recently been clarified to be associated with change in drug distribution and disposition. To expand on recent identification of direct interaction and functional regulation of several transporters by a PDZ (PSD95, Dlg and ZO1) domain containing protein PDZK1, the ...

journal_title：Drug metabolism and pharmacokinetics

authors： Sugiura T,Kato Y,Kubo Y,Tsuji A

更新日期：2006-10-01 00:00:00

abstract：:In this study, we aimed to understand the gap in coverage of pharmacogenomic (PGx) biomarkers between Japan and the US. PGx biomarkers (1) in the Clinical Pharmacogenetics Implementation Consortium (CPIC) guidelines; (2) that are CPIC level A or B; or (3) have US Food and Drug Administration (FDA)-approved drug labels...

journal_title：Drug metabolism and pharmacokinetics

authors： Hikino K,Fukunaga K,Mushiroda T

更新日期：2018-12-01 00:00:00

abstract：:Most of cytochrome P450 (CYP) expressions are regulated by nuclear receptors. The regulation pathways of transcription are activated by binding of the ligand to the receptor. Many combination of CYPs and nuclear receptors in transcriptional regulation have been reported. However, we have reported that the combination ...

journal_title：Drug metabolism and pharmacokinetics

authors： Terashima J,Jimma Y,Jimma K,Hakata S,Yachi M,Habano W,Ozawa S

更新日期：2018-08-01 00:00:00

abstract：:The objective of this work was to develop a population pharmacokinetic model to assess the influence of subject covariates on the pharmacokinetics of valsartan in children. Data were collected from a single dose study in 26 hypertensive children ages 1 to 16 years. Subjects received 2 mg/kg valsartan suspension up to ...

journal_title：Drug metabolism and pharmacokinetics

authors： Habtemariam B,Sallas W,Sunkara G,Kern S,Jarugula V,Pillai G

更新日期：2009-01-01 00:00:00

abstract：:The participation of cytochrome P-450 (CYP) isoforms in the metabolism of selegiline was investigated. Experiments using recombinant CYP isoforms expressed in human lymphoblastoid cells showed CYP2B6 to be the major CYP isoform involved with the metabolism of selegiline. CYP1A2 and CYP3A4 also contributed to the metab...

journal_title：Drug metabolism and pharmacokinetics

authors： Kamada T,Chow T,Hiroi T,Imaoka S,Morimoto K,Ohde H,Funae Y

更新日期：2002-01-01 00:00:00

abstract：:Analysis of mRNAs from liver biopsy samples of patients with chronic hepatitis C revealed that the levels of nuclear receptor expression were correlated with those of drug-metabolizing enzymes and transporters in relation to the development of fibrosis. Overall, the median mRNA level was largely dependent on fibrosis ...

journal_title：Drug metabolism and pharmacokinetics

authors： Hanada K,Nakai K,Tanaka H,Suzuki F,Kumada H,Ohno Y,Ozawa S,Ogata H

更新日期：2012-01-01 00:00:00

abstract：:A population pharmacokinetic substudy design of a new chemical entity was evaluated based on the bias in parameter estimates and the power of detecting a specific subpopulation showing different clearance using a clinical trial simulation approach. The effect of analysis algorithms on type I error was also assessed. T...

journal_title：Drug metabolism and pharmacokinetics

authors： Nakade S,Nishibori A,Okamoto H,Higuchi S

更新日期：2004-10-01 00:00:00

abstract：:It is now widely appreciated that drug metabolites, in addition to the parent drugs themselves, can mediate the serious adverse effects exhibited by some new therapeutic agents, and as a result, there has been heightened interest in the field of drug metabolism from researchers in academia, the pharmaceutical industry...

journal_title：Drug metabolism and pharmacokinetics

authors： Baillie TA,Rettie AE

更新日期：2011-01-01 00:00:00

abstract：:Since porphyrins are regarded as endogenous substrates for the ATP-binding cassette (ABC) transporter ABCG2, it is hypothesized that functional impairment owing to genetic polymorphisms or inhibition of ABCG2 by drugs may result in a disruption of cellular porphyrin homeostasis. In the present study, we expressed ABCG...

journal_title：Drug metabolism and pharmacokinetics

authors： Tamura A,Onishi Y,An R,Koshiba S,Wakabayashi K,Hoshijima K,Priebe W,Yoshida T,Kometani S,Matsubara T,Mikuriya K,Ishikawa T

更新日期：2007-12-01 00:00:00

abstract：:We discovered a novel single nucleotide polymorphism (SNP) at position 325 (G325A) in exon 5 of the multidrug-resistance 1 (MDR1) gene in a study of 37 healthy Japanese subjects. Details are as follows. SNP, 020614Honda001; GENE NAME, human P-glycoprotein (MDR1); ACCESSION NUMBER, M29427; LENGTH, 25 bases; 5'-ATGAATCT...

journal_title：Drug metabolism and pharmacokinetics

authors： Honda T,Dan Y,Koyabu N,Ieiri I,Otsubo K,Higuchi S,Ohtani H,Sawada Y

更新日期：2002-01-01 00:00:00

abstract：:Accumulating evidences have shown that diabetes is often accompanied with depression, thus it is possible that oral antidiabetic agent glyburide and antidepressive agent paroxetine are co-administered in diabetic patients. The aim of this study was to assess interactions between glyburide and paroxetine in rats. Effec...

journal_title：Drug metabolism and pharmacokinetics

authors： Jiang S,Zhao W,Chen Y,Zhong Z,Zhang M,Li F,Xu P,Zhao K,Li Y,Liu L,Liu X

更新日期：2015-06-01 00:00:00

abstract：:Thirty-nine genetic variations, including thirty novel ones, were found in the human SLC29A1 gene, which encodes equilibrative nucleoside transporter 1, from 256 Japanese cancer patients administered gemcitabine. The found novel variations included -8,166G>A, -81,10A>G, -7,947G>A, -7,789T>C, -5,595G>A, -3,803_-3,783de...

journal_title：Drug metabolism and pharmacokinetics

authors： Kim SR,Saito Y,Maekawa K,Sugiyama E,Kaniwa N,Ueno H,Okusaka T,Morizane C,Yamamoto N,Ikeda M,Yoshida T,Minami H,Furuse J,Ishii H,Saijo N,Kamatani N,Ozawa S,Sawada J

更新日期：2006-06-01 00:00:00

abstract：:Troglitazone induced an idiosyncratic, hepatocellular injury-type hepatotoxicity in humans. Statistically, double null genotype of glutathione S-transferase isoforms, GSTT1 and GSTM1, was a risk factor, indicating a low activity of the susceptible patients in scavenging chemically reactive metabolites. CYP3A4 and CYP2...

journal_title：Drug metabolism and pharmacokinetics

authors： Ikeda T

更新日期：2011-01-01 00:00:00

abstract：:Cytochrome P450 2A6 (CYP2A6) is an enzyme involved in the metabolism of tobacco carcinogens, which are important risk factors in lung cancer. We and others have previously reported that CYP2A6*4, a whole-gene deletion polymorphism, is associated with lower risk of lung cancer than the wild-type allele. However, the ge...

journal_title：Drug metabolism and pharmacokinetics

authors： Hosono H,Kumondai M,Arai T,Sugimura H,Sasaki T,Hirasawa N,Hiratsuka M

更新日期：2015-08-01 00:00:00

abstract：:The pharmacokinetics of telmisartan are nonlinear within the clinical dose range. To identify the underlying mechanism of this nonlinearity, we conducted a PET study in healthy subjects using [11C]telmisartan. Eight healthy male subjects were enrolled in a 2-way crossover study. PET imaging was performed after intrave...

journal_title：Drug metabolism and pharmacokinetics

authors： Maeda K,Ohnishi A,Sasaki M,Ikari Y,Aita K,Watanabe Y,Kusuhara H,Sugiyama Y,Senda M

更新日期：2019-10-01 00:00:00

abstract：:  Human cytochrome P450 CYP2A6 and CYP2A13 catalyze nicotine metabolisms and mediate activation of tobacco-specific carcinogens including 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) and 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanol (NNAL). In this study, we found rhinacanthins A, B, and C isolated from Rhinac...

journal_title：Drug metabolism and pharmacokinetics

authors： Pouyfung P,Prasopthum A,Sarapusit S,Srisook E,Rongnoparut P

更新日期：2014-01-01 00:00:00

abstract：:The interaction between cytochrome P450s (CYP, P450) and UDP-glucuronosyltransferases (UGTs) was studied by co-immunoprecipitation. P450 isoform-selective antibody was used as a probe to co-precipitate UGTs with the P450s from solubilized rat liver microsomes. Antibodies toward CYP3A2, CYP2B2, CYP2C11/13 and CYP1A2 co...

journal_title：Drug metabolism and pharmacokinetics

authors： Ishii Y,Iwanaga M,Nishimura Y,Takeda S,Ikushiro S,Nagata K,Yamazoe Y,Mackenzie PI,Yamada H

更新日期：2007-10-01 00:00:00

abstract：:Hypoglycemia is one of the serious adverse effects induced by cibenzoline (CBZ), an antiarrhythmic agent. In order to clarify the pharmacodynamics of CBZ-induced hypoglycemia, CBZ was administered intravenously to conscious rats at a dose of 5, 10 or 20 mg/kg and serum samples were collected periodically to determine ...

journal_title：Drug metabolism and pharmacokinetics

authors： Takahashi Y,Ishiwata Y,Kojima Y,Yasuhara M

更新日期：2011-06-01 00:00:00

abstract：:The concentration and distribution of a drug or its metabolites in tissues are key factors for understanding drug efficacy or toxicity. Conventional pharmacokinetic studies show that the plasma concentration of a drug is often unrelated to the intra-tissue concentration. Moreover, it is difficult to predict the distri...

journal_title：Drug metabolism and pharmacokinetics

authors： Nishidate M,Hayashi M,Aikawa H,Tanaka K,Nakada N,Miura SI,Ryu S,Higashi T,Ikarashi Y,Fujiwara Y,Hamada A

更新日期：2019-08-01 00:00:00

abstract：:Tacrolimus is a widely used immunosuppressant after organ transplantation. The narrow therapeutic window and individual variability in tacrolimus pharmacokinetics make management of this agent a great challenge. This study was undertaken to determine the association of clinical markers, cytochrome P450, family 3, subf...

journal_title：Drug metabolism and pharmacokinetics

authors： Chen D,Guo F,Shi J,Zhang C,Wang Z,Fan J,Peng Z

更新日期：2014-01-01 00:00:00

abstract：:The objectives of this study were to develop a population pharmacokinetic model of imidafenacin and to explore the factors that affect the pharmacokinetics of imidafenecin. A total of 2406 plasma samples were collected from 90 healthy volunteers and 457 patients with overactive bladder. We determined the plasma concen...

journal_title：Drug metabolism and pharmacokinetics

authors： Ohno T,Nakade S,Nakayama K,Kitagawa J,Miyabe H,Konomi T,Miyata Y

更新日期：2008-01-01 00:00:00

abstract：:Human carboxylesterase 1 (hCE-1, CES1A1, HU1) and carboxylesterase 2 (hCE-2, hiCE, HU3) are a serine esterase involved in both drug metabolism and activation. Although both hCE-1 and hCE-2 are present in several organs, the hydrolase activity of liver and small intestine is predominantly attributed to hCE-1 and hCE-2,...

journal_title：Drug metabolism and pharmacokinetics

authors： Imai T

更新日期：2006-06-01 00:00:00

abstract：:Altered expression of P-glycoprotein (P-gp), a drug efflux transporter expressed by brain capillary endothelial cells (BCECs), may contribute to the development of opioid analgesic tolerance, as demonstrated by cumulative evidence from research. However, the detailed mechanism by which chronic morphine treatment incre...

journal_title：Drug metabolism and pharmacokinetics

authors： Kobori T,Fujiwara S,Miyagi K,Harada S,Nakamoto K,Nakagawa T,Takahashi H,Narita M,Tokuyama S

更新日期：2014-01-01 00:00:00

abstract：:To evaluate the effect of protein binding of pilsicainide on its clearance and the contribution of protein binding to optimized pilsicainide therapy, clinical laboratory and pharmacokinetic data were studied in 160 Japanese inpatients (Study 1) and 18 Japanese inpatients (Study 2). To determine the relation between pr...

journal_title：Drug metabolism and pharmacokinetics

authors： Fukumoto K,Tanemura M,Tsuchishita Y,Kusumoto M,Matsumoto K,Kamakura S,Ueno K

更新日期：2005-06-01 00:00:00

abstract：:Fast disintegrating lansoprazole tablet (LFDT) has been developed as a multiple unit formulation and evaluated using human subjects as compared to the conventional lansoprazole (LPZ) capsule containing enteric coated granules. Twelve healthy male volunteers, who were confirmed as extensive metabolizers (EMs) based on ...

journal_title：Drug metabolism and pharmacokinetics

authors： Iwasaki K,Yoshikawa Y,Shibata N,Takada K,Sakurai Y,Takagi N,Irie S,Nakamura K

更新日期：2004-06-01 00:00:00

abstract：:The basement membrane at the blood-brain barrier (BBB) plays important roles in maintaining the structure and function of capillary vessels. The BBB is constructed from endothelial cells, astrocytes and pericytes, but their interactions in the formation or maintenance of basement membrane have not been established. Tr...

journal_title：Drug metabolism and pharmacokinetics

authors： Kose N,Asashima T,Muta M,Iizasa H,Sai Y,Terasaki T,Nakashima E

更新日期：2007-08-01 00:00:00

abstract：:Aldehyde oxidase contributes to drug metabolism and pharmacokinetics (PK), and a few clinical studies were discontinued because of aldehyde oxidase metabolism. Its AOX1, AOX3, AOX3L1, and AOX4 isoforms are expressed in mammals, and species differences in expression profiles reflect differences in drug metabolism and P...

journal_title：Drug metabolism and pharmacokinetics

authors： Sanoh S,Tayama Y,Sugihara K,Kitamura S,Ohta S

更新日期：2015-02-01 00:00:00