Genetic variations in the MCT1 (SLC16A1) gene in the Chinese population of Singapore.

abstract：:To characterize the renal handling of CS-023 (RO4908463), a novel parenteral carbapenem antibiotic, and meropenem in humans, we examined their affinities as substrates to human renal transporters. In vitro studies on the uptake of [14C]CS-023 and [14C]meropenem were conducted using HEK293 cells expressing human organi...

journal_title：Drug metabolism and pharmacokinetics

authors： Shibayama T,Sugiyama D,Kamiyama E,Tokui T,Hirota T,Ikeda T

更新日期：2007-02-25 00:00:00

abstract：:In drug discovery, the cerebrospinal fluid (CSF) drug concentration (CCSF) has been used as a surrogate for the interstitial fluid (ISF) concentration (CISF). However, the CCSF-to-CISF gradient suggested for P-glycoprotein (P-gp) substrates in rodents causes uncertainty in CISF estimations and subsequent pharmacokinet...

journal_title：Drug metabolism and pharmacokinetics

authors： Nagaya Y,Nozaki Y,Takenaka O,Watari R,Kusano K,Yoshimura T,Kusuhara H

更新日期：2016-02-01 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：:Protein kinases are potential drug targets for the treatment of a variety of diseases, including cancer. In particular, specific tyrosine kinase inhibitors are rapidly being developed as new drugs for the inhibition of malignant cell growth and metastasis formation. Most of these newly developed tyrosine kinase inhibi...

journal_title：Drug metabolism and pharmacokinetics

authors： Saito H,An R,Hirano H,Ishikawa T

更新日期：2010-01-01 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：:Polymorphic distributions of pharmacogenes among some ethnicities are under-represented in current pharmacogenetic research. Particularly, there is a paucity of pharmacogenetic information in the Sherpa population in Tibet. We used the Sequenom MassARRAY single nucleotide polymorphism (SNP) genotyping technology to de...

journal_title：Drug metabolism and pharmacokinetics

authors： Wang L,Ren Y,Shi X,Yuan D,Liu K,Geng T,Li G,Kang L,Jin TB

更新日期：2016-02-01 00:00:00

abstract：SUMMARY:The diagnosis of cardiac ischemia remains a challenge in contemporary emergency medicine. A blood-borne biomarker is an attractive alternative to cardiac imaging or stress testing as it would be cheaper and logistically faster to obtain. A number of candidate biomarkers have been proposed for the detection of c...

journal_title：Drug metabolism and pharmacokinetics

authors： Gaze DC

更新日期：2009-01-01 00:00:00

abstract：:1. Assay methods to detect drug interaction in toxicological samples were established by determining cytochrome P450 content and its activity in liver samples. The O-dealkylation reaction of 7-alkoxycoumarin was indicated to reflect changes in the molecular forms of P450s, and the enzyme induction or inhibition in the...

journal_title：Drug metabolism and pharmacokinetics

authors： Matsubara T

更新日期：2002-01-01 00:00:00

abstract：:The current EMA drug interaction guideline was published in 2012. This guideline gives important recommendations on the information required to elucidate the interaction potential of an investigational drug, both as effects of the investigational drug on the PK of other drugs and effects of other medicinal products on...

journal_title：Drug metabolism and pharmacokinetics

authors： Cole S,Kerwash E,Andersson A

更新日期：2020-02-01 00:00:00

abstract：:Pregnane X receptor (PXR) is a ligand-activated nuclear factor that upregulates the expression of proteins involved in the detoxification and clearance of xenobiotics, primarily cytochrome P450 3A4 (CYP3A4). Structure-activity relationship (SAR) analysis of PXR agonists is useful for avoiding unwanted pharmacokinetics...

journal_title：Drug metabolism and pharmacokinetics

authors： Yoshida S,Yamashita F,Itoh T,Hashida M

更新日期：2012-01-01 00:00:00

abstract：:Twenty genetic variations, including seven novel ones, were found in the human SLC22A1 gene, which encodes organic cation transporter 1, from 116 Japanese individuals. The novel variations were as follows: -94C>A in the 5'-untranslated region (A of the translation start codon is numbered +1 in the cDNA sequence; MPJ6_...

journal_title：Drug metabolism and pharmacokinetics

authors： Itoda M,Saito Y,Maekawa K,Hichiya H,Komamura K,Kamakura S,Kitakaze M,Tomoike H,Ueno K,Ozawa S,Sawada J

更新日期：2004-08-01 00:00:00

abstract：:Bioavailability and therapeutic outcome of treatment with HIV-protease inhibitors depends on intestinal and hepatic transporter-enzyme interplay. Liver transport of HIV protease inhibitors (saquinavir, darunavir) was assessed in the presence of aged garlic extract, because the HIV-infected often consume garlic supplem...

journal_title：Drug metabolism and pharmacokinetics

authors： Berginc K,Trontelj J,Kristl A

更新日期：2010-01-01 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：:The mRNA levels of human cytochrome P450 (CYP)2Cs and CYP3As in primary cultures of freshly isolated human hepatocytes were assessed after exposure to NO-1886 and rifampicin, a typical inducer of CYP3As. mRNA levels were analyzed by real-time RT-PCR using an ABI PRISM 7700 Sequence Detector system. Exposure to NO-1886...

journal_title：Drug metabolism and pharmacokinetics

authors： Morioka Y,Nishimura M,Imai T,Suzuki S,Harada M,Satoh T,Naito S

更新日期：2006-02-01 00:00:00

abstract：:The roots of Sophora flavescens (Sf) have been widely used as a herbal medicine for the treatment of diarrhea, gastrointestinal hemorrhage, and eczema. Cytochrome P450 (P450) forms including CYP1A2, CYP2B, CYP2E1, and CYP3A participate in the oxidative metabolism of theophylline, which is an important bronchodilation ...

journal_title：Drug metabolism and pharmacokinetics

authors： Ueng YF,Tsai CC,Lo WS,Yun CH

更新日期：2010-01-01 00:00:00

abstract：:UDP-glucuronosyltransferases (UGTs) are glycoproteins in endoplasmic reticulum membranes. UGT2B7 is an important UGT isoenzyme expressed in human liver and glucuronidates various endogenous and exogenous substances. Although this enzyme has three potential N-glycosylation sites (asparagine at positions 67, 68 and 315)...

journal_title：Drug metabolism and pharmacokinetics

authors： Nagaoka K,Hanioka N,Ikushiro S,Yamano S,Narimatsu S

更新日期：2012-01-01 00:00:00

abstract：:It has been reported that inhibition of the P-glycoprotein (P-gp) results in the improved absorption of P-gp substrate in the intestinal tract. In fact, the increased permeability of P-gp substrate across the intestinal epithelium was observed following inhibition of P-gp in in vitro experiments. To develop the formul...

journal_title：Drug metabolism and pharmacokinetics

authors： Iida A,Tomita M,Hayashi M

更新日期：2005-04-01 00:00:00

abstract：:Methyl gallate (MG) and pentagalloyl glucopyranose (PGG) are bioactive phenolic compounds that possess various pharmacological activities. However, the knowledge of hepatic metabolism of MG and PGG is limited. The purpose of this study was to investigate the in vitro glucuronidation of MG and PGG using liver microsome...

journal_title：Drug metabolism and pharmacokinetics

authors： Jiamboonsri P,Pithayanukul P,Bavovada R,Leanpolchareanchai J,Gao S,Hu M

更新日期：2016-08-01 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：: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：:The objectives of this study were to evaluate the relative contribution of the direct pathway in overall brain transport for 17 model drugs with different physicochemical properties after nasal administrations and to identify factors that govern the fraction of the dose transported to the brain via the direct pathway ...

journal_title：Drug metabolism and pharmacokinetics

authors： Lee KR,Maeng HJ,Chae JB,Chong S,Kim DD,Shim CK,Chung SJ

更新日期：2010-01-01 00:00:00

abstract：:Microdose (MD) clinical trials have been introduced to obtain human pharmacokinetic data early in drug development. Here we assessed the cost-effectiveness of microdose integrated drug development in a hypothetical model, as there was no such quantitative research that weighed the additional effectiveness against the ...

journal_title：Drug metabolism and pharmacokinetics

authors： Yamane N,Igarashi A,Kusama M,Maeda K,Ikeda T,Sugiyama Y

更新日期：2013-01-01 00:00:00

abstract：:A population pharmacokinetic (PK) model for meropenem in Japanese pediatric patients with various infectious diseases was developed based on 116 plasma concentrations from 50 pediatric patients. The population PK parameters developed in this analysis are useful for calculation of the percent time above minimum inhibit...

journal_title：Drug metabolism and pharmacokinetics

authors： Ohata Y,Tomita Y,Nakayama M,Kozuki T,Sunakawa K,Tanigawara Y

更新日期：2011-01-01 00:00:00

abstract：:Dihydrofolate reductase gene (DHFR) 19-bp deletion polymorphisms result in varied DHFR enzymatic activity affecting the risk for preterm delivery, spina bifida, and the efficacy of methotrexate (MTX). Ethnic differences in DHFR 19-bp polymorphisms may be responsible for the divergent findings in previous genetic studi...

journal_title：Drug metabolism and pharmacokinetics

authors： Hayashi H,Horino M,Morishita M,Tazoe Y,Tsuboi S,Matsuyama T,Kosuge K,Yamada H,Tsuji D,Inoue K,Itoh K

更新日期：2010-01-01 00:00:00

abstract：:Morphine is one of the strongest analgesics and is commonly used for the treatment of chronic pain. The pharmacokinetic properties of morphine are, in part, modulated by P-glycoprotein (P-gp). We previously reported that intestinal P-gp expression levels are influenced via the activation of inducible nitric oxide synt...

journal_title：Drug metabolism and pharmacokinetics

authors： Nawa A,Fujita-Hamabe W,Kishioka S,Tokuyama S

更新日期：2011-01-01 00:00:00

abstract：:Maleic acid (MA) was purposefully adulterated in an array of starch-based foods in Taiwan, inciting a food safety incident. Due to limited data on the pharmacokinetics and bioavailability of ingested MA, we studied pharmacokinetic (PK) parameters in serum and urine of Sprague Dawley rats. Three groups of male and fema...

journal_title：Drug metabolism and pharmacokinetics

authors： Wu C,Chen HC,Luo YS,Chiang SY,Wu KY

更新日期：2016-12-01 00:00:00

abstract：:In a clinical setting, changes in pharmacokinetics due to drug-drug interactions can often directly affect the therapeutic safety and efficacy of drugs. Recently, interest has been shown in drug-drug interactions in the intestine. It is now recognized that changes in the functions of drug transporters substantially in...

journal_title：Drug metabolism and pharmacokinetics

authors： Segawa M,Ogura J,Seki S,Itagaki S,Takahashi N,Kobayashi M,Hirano T,Yamaguchi H,Iseki K

更新日期：2013-01-01 00:00:00

abstract：:Genetic factors have a significant impact on the PK variability of EFV, much higher than other non-genetic factors, such as demography. In this work we have performed a comprehensive PG analysis of genes encoding the major metabolizing enzymes and transporters of EFV, establishing a clear relationship between the PK p...

journal_title：Drug metabolism and pharmacokinetics

authors： Sánchez-Martín A,Cabrera Figueroa S,Cruz R,Porras-Hurtado L,Calvo-Boyero F,Rasool M,Tormes Team.,Domínguez-Gil Hurlé A,Carracedo A

更新日期：2016-10-01 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：:In the present study, we identified three novel single nucleotide polymorphisms (SNPs), 147C>T in exon 2 (silent), 602G>C in exon 3 (Arg201Pro), and 1134C>T in exon 4 (silent), in the gene of bile acid CoA: amino acid N-acyltransferase (BAAT) by resequencing the entire coding region and the exon-intron junctions of 10...

journal_title：Drug metabolism and pharmacokinetics

authors： Tougou K,Fukuda T,Ito T,Yamazaki H,Fujio Y,Azuma J

更新日期：2007-04-01 00:00:00