Valproic acid transport in the choriocarcinoma placenta cell line JEG-3 proceeds independently of the proton-dependent transporters MCT1 and MCT4.

abstract：:Polymorphic human flavin-containing monooxygenase (FMO) 3 is an important drug-metabolizing enzyme for nitrogen- or sulfur-containing compounds. Cynomolgus macaques, a non-human primate species widely used in drug metabolism studies, have corresponding FMO3 molecular and enzymatic similarities to humans; however, gene...

journal_title：Drug metabolism and pharmacokinetics

authors： Uno Y,Shimizu M,Yoda H,Origuchi Y,Yamazaki H

更新日期：2019-02-01 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：:New SRM (selected reaction monitoring) data dependent exclusion (MS)(n) measurement makes it possible to obtain MS(3) fragmentation data for all MS(2) fragments, useful for structural determination of drug metabolites using ESI ion trap. MS(2) fragments are produced by cleavage of all protonated molecules at the lone ...

journal_title：Drug metabolism and pharmacokinetics

authors： Tozuka Z,Kaneko H,Shiraga T,Beppu M,Niwa T,Kawamura A,Kagayama A

更新日期：2003-01-01 00:00:00

abstract：:Chemotherapy-induced neutropenia is one of the major adverse events which results in the reduction of chemotherapy. Doxorubicin is a substrate of the adenosine triphosphate-binding cassette subfamily B member 1 (ABCB1) transporter; reportedly, ABCB1 polymorphisms influence doxorubicin pharmacokinetics. We evaluated th...

journal_title：Drug metabolism and pharmacokinetics

authors： Ikeda M,Tsuji D,Yamamoto K,Kim YI,Daimon T,Iwabe Y,Hatori M,Makuta R,Hayashi H,Inoue K,Nakamichi H,Shiokawa M,Itoh K

更新日期：2015-04-01 00:00:00

abstract：:The injectable form of oxycodone contains hydrocotarnine that is supposed to potentiate the analgesic effect of oxycodone with unknown mechanism(s). In this study, the effects of hydrocotarnine on the cytochrome P450 (CYP) and P-glycoprotein (P-gp) were investigated. Hydrocotarnine did not induce a significant change ...

journal_title：Drug metabolism and pharmacokinetics

authors： Ito K,Kubota Y,Toda T,Suto S,Ikarashi N,Sugiyama K

更新日期：2009-01-01 00:00:00

abstract：:Repeated pretreatment with the antimalarial drug artemisinin (QHS) could lead to reduced exposure to the parent drug, which is mainly mediated by auto-induction of CYP2B6 activity. CYP2B6 is most sensitive to the inductive effect of constitutive androstane receptor (CAR), which can be activated by QHS. CYP2B6 polymorp...

journal_title：Drug metabolism and pharmacokinetics

authors： Zang M,Zhao L,Zhu F,Li X,Yang A,Xing J

更新日期：2015-02-01 00:00:00

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：:Resistance to antiemetic treatment with 5-hydroxytryptamine 3 receptor antagonists is a problem, with 20-30% of patients showing unsatisfactory responses. Efflux transport by P-glycoprotein, encoded by the ATP-binding cassette ABCB1 gene in the blood-brain barrier, has been the suggested resistance mechanism. We evalu...

journal_title：Drug metabolism and pharmacokinetics

authors： Tsuji D,Kim YI,Nakamichi H,Daimon T,Suwa K,Iwabe Y,Hayashi H,Inoue K,Yoshida M,Itoh K

更新日期：2013-01-01 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：:OCTN1/SLC22A4 is expressed on apical membranes of small intestine, and is involved in gastrointestinal absorption of its substrates, including the food-derived antioxidant ergothioneine (ERGO). ERGO concentration in circulating blood of patients with inflammatory bowel disease (Crohn's disease) is lower than that in h...

journal_title：Drug metabolism and pharmacokinetics

authors： Shimizu T,Masuo Y,Takahashi S,Nakamichi N,Kato Y

更新日期：2015-06-01 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：:After intravenous bolus administration of aprindine (AP) to conscious guinea pigs, the semilogarithmic plasma concentration versus time curve was linear at a dose of 2 mg/kg, but convex at doses of 5 and 10 mg/kg. AP concentrations immediately after administration (C(p0)) were almost identical, irrespective of the dos...

journal_title：Drug metabolism and pharmacokinetics

authors： Shimizu M,Ohota T,Kishida M,Ogata H

更新日期：2002-01-01 00:00:00

abstract：:Pitavastatin undergoes little hepatic metabolism but it is a substrate for uptake and efflux transporters, particularly OATP1B1 (gene SLCO1B1). A previous study in 8 Japanese healthy subjects showed that co-administration with grapefruit juice (GFJ) resulted in a small increase in systemic exposure to pitavastatin. We...

journal_title：Drug metabolism and pharmacokinetics

authors： Hu M,Mak VW,Yin OQ,Chu TT,Tomlinson B

更新日期：2013-01-01 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：:CYP2D6 is involved in the biotransformation of a large number of drugs, including risperidone. This study was designed to detect CYP2D6 polymorphisms with a Luminex assay, including assessment the relationship of CYP2D6 polymorphisms and risperidone plasma concentration in autism spectrum disorder children (ASD) treat...

journal_title：Drug metabolism and pharmacokinetics

authors： Vanwong N,Ngamsamut N,Hongkaew Y,Nuntamool N,Puangpetch A,Chamnanphon M,Sinrachatanant A,Limsila P,Sukasem C

更新日期：2016-04-01 00:00:00

abstract：:Most cephalosporin antibiotics are excreted into urine via glomerular filtration and active tubular secretion by renal organic anion transporters. In this study, we investigated the interaction of cephalosporins with rat organic anion transporter rOAT1, mainly expressed at the basolateral membrane of the renal proxima...

journal_title：Drug metabolism and pharmacokinetics

authors： Uwai Y,Saito H,Inui K

更新日期：2002-01-01 00:00:00

abstract：:Pept2 knockout mice are an important tool to evaluate the evolving role and relevance of this proton-coupled oligopeptide transporter beyond drug disposition, where the transporter also modulates the pharmacodynamic and toxicodynamic effects of drug substrates. Our in vivo studies with glycylsarcosine in Pept2 knockou...

journal_title：Drug metabolism and pharmacokinetics

authors： Kamal MA,Keep RF,Smith DE

更新日期：2008-01-01 00:00:00

abstract：UNLABELLED:Better prediction of drug disposition prior to the clinical trial is critical for the efficient development of new drugs. The purpose of this study is to develop a novel multiple assessment methodology of hepatocellular drug disposition from drug uptake to efflux including biliary and basolateral excretion, ...

journal_title：Drug metabolism and pharmacokinetics

authors： Takahashi R,Ichikawa H,Kanda K

更新日期：2016-04-01 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：: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：: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：: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：: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：: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：: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：: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：:The bile salt export pump (BSEP) encoded by ABCB11 is located in the canalicular membrane of hepatocytes and mediates the secretion of numerous conjugated bile salts into the bile canaliculus. In this study, 28 ABCB11 exons (including non-coding exon 1) and their flanking introns were comprehensively screened for gene...

journal_title：Drug metabolism and pharmacokinetics

authors： Kim SR,Saito Y,Itoda M,Maekawa K,Kawamoto M,Kamatani N,Ozawa S,Sawada J

更新日期：2009-01-01 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：:Eight covalent tyrosine kinase inhibitors (TKIs) were investigated to determine the characteristics of their covalent binding to plasma proteins. The data revealed that their covalent binding to plasma proteins is of species difference. In addition to the reports on neratinib and pyrotinib, osimertinib, alflutinib, AS...

journal_title：Drug metabolism and pharmacokinetics

authors： Liu X,Feng D,Zheng M,Cui Y,Zhong D

更新日期：2020-10-01 00:00:00

abstract：:MCT1(SLC16A1) is the first member of the monocarboxylate transporter (MCT) and its family is involved in the transportation of metabolically important monocarboxylates such as lactate, pyruvate, acetate and ketone bodies. This study identifies genetic variations in SLC16A1 in the ethnic Chinese group of the Singaporea...

journal_title：Drug metabolism and pharmacokinetics

authors： Lean CB,Lee EJ

更新日期：2009-01-01 00:00:00