Population pharmacokinetic analysis of micafungin in Japanese patients with fungal infections.

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：:Tralokinumab is a human monoclonal antibody in clinical development for asthma and atopic dermatitis that specifically neutralizes interleukin-13. This phase I, single-blind, randomized, placebo-controlled, single ascending-dose study assessed the safety, tolerability, pharmacokinetics (PK), and immunogenicity of subc...

journal_title：Drug metabolism and pharmacokinetics

authors： Baverel P,She D,Piper E,Ueda S,Yoshioka T,Faggioni R,Gevorkyan H

更新日期：2018-06-01 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：: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 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 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：: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：: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 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：:Human OATP2B1, a member of organic anion transporting polypeptide family, is expressed in several tissues, including small intestine and liver, and contributes to cellular uptake of endogenous compounds and various drugs. Altered expression of OATP2B1 affects pharmacokinetics of substrate drugs; however, limited infor...

journal_title：Drug metabolism and pharmacokinetics

authors： Liu W,Nakano M,Nakanishi T,Nakajima M,Tamai I

更新日期：2020-12-01 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：:This exploratory retrospective study examined the effects of polymorphisms in transporter genes related to irinotecan pharmacokinetics and those in genes related to irinotecan pharmacodynamics on the efficacy of first-line combination chemotherapy with irinotecan, 5-fluorouracil, and folinic acid (leucovorin) (FOLFIRI...

journal_title：Drug metabolism and pharmacokinetics

authors： Akiyama Y,Fujita K,Ishida H,Sunakawa Y,Yamashita K,Kawara K,Miwa K,Saji S,Sasaki Y

更新日期：2012-01-01 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：:The ATP-binding cassette transporter, ABCG2, which is expressed at high levels in the intestine and liver, functions as an efflux transporter for many drugs, including clinically used anticancer agents such as topotecan and the active metabolite of irinotecan (SN-38). In this study, to elucidate the linkage disequilib...

journal_title：Drug metabolism and pharmacokinetics

authors： Maekawa K,Itoda M,Sai K,Saito Y,Kaniwa N,Shirao K,Hamaguchi T,Kunitoh H,Yamamoto N,Tamura T,Minami H,Kubota K,Ohtsu A,Yoshida T,Saijo N,Kamatani N,Ozawa S,Sawada J

更新日期：2006-04-01 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：: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：:To investigate the transport function of the blood-brain barrier (BBB), we employed an in vitro model of the BBB, consisting of a co-culture of porcine brain capillary endothelial cells (BCECs) with rat astrocytes. Porcine BCECs were cultured on a filter insert with rat astrocytes on the underlying plastic well. Rat a...

journal_title：Drug metabolism and pharmacokinetics

authors： Kido Y,Tamai I,Nakanishi T,Kagami T,Hirosawa I,Sai Y,Tsuji A

更新日期：2002-01-01 00:00:00

abstract：:A novel method for the prediction of drug-drug interaction has been established based on the in vitro metabolic stability in the "serum incubation method" using cryopreserved human hepatocytes suspended in 100% human serum. As a novel approach, the inhibitory effect of inhibitors on the metabolism of substrates during...

journal_title：Drug metabolism and pharmacokinetics

authors： Shibata Y,Takahashi H,Chiba M,Ishii Y

更新日期：2008-01-01 00:00:00

abstract：:This study aimed to develop a drug metabolism prediction platform using knowledge-based prediction models. Site of Metabolism (SOM) prediction models for four cytochrome P450 (CYP) subtypes were developed along with uridine 5'-diphosphoglucuronosyltransferase (UGT) and sulfotransferase (SULT) substrate classification ...

journal_title：Drug metabolism and pharmacokinetics

authors： Hwang S,Shin HK,Shin SE,Seo M,Jeon HN,Yim DE,Kim DH,No KT

更新日期：2020-08-01 00:00:00

abstract：:Nifedipine is one of drugs that have been suggested to undergo significant first-pass metabolism by cytochrome P450 (CYP) 3A in the intestine, based mainly on pharmacokinetic analyses of in vivo observations. To further substantiate this suggestion, we examined the metabolic extraction of nifedipine from the rat small...

journal_title：Drug metabolism and pharmacokinetics

authors： Iwao T,Inoue K,Hayashi Y,Yuasa H,Watanabe J

更新日期：2002-01-01 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：: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：:Tuftsin, a natural phagocytosis-stimulating tetrapeptide, had aroused much interest in tumor immunotherapy, but the poor pharmacokinetics hampered its clinical developments, for that it was extremely susceptible to degradation by enzymolysis in vivo. T Peptide (TP) was a newly designed tuftsin derivative aimed to enha...

journal_title：Drug metabolism and pharmacokinetics

authors： Gu R,He Y,Han S,Yuan S,An Y,Meng Z,Zhu X,Gan H,Wu Z,Li J,Zheng Y,Zhang L,Gao L,Dou G

更新日期：2016-02-01 00:00:00

abstract：:Five novel single nucleotide polymorphisms (SNPs) were found in the EPHX1 gene from 96 Japanese epileptic patients. The detected SNPs were as follows: 1) SNP, MPJ6_EX1009; GENE NAME, EPHX1 ACCESSION NUMBER, NT_004525.12; LENGTH, 25 bases; 5'-CCTCACTTCAGTG/ACTGGGCTTTGCC-3'. 2) SNP, MPJ6_EX1013; GENE NAME, EPHX1; ACCESS...

journal_title：Drug metabolism and pharmacokinetics

authors： Shiseki K,Itoda M,Saito Y,Nakajima Y,Maekawa K,Kimura H,Goto Y,Saitoh O,Katoh M,Ohnuma T,Kawai M,Sugai K,Ohtsuki T,Suzuki C,Minami N,Ozawa S,Sawada J

更新日期：2003-01-01 00:00:00

abstract：:Cytochrome P450 (P450) constitutes a superfamily of enzymes which activate dioxygen and carry out monooxygenation reactions of large numbers of endogenous and xenobiotic compounds. Drug metabolism is a particularly important P450 function, and, therefore, elucidating the metabolic products and pathways of drugs is ess...

journal_title：Drug metabolism and pharmacokinetics

authors： Yasui H,Hayashi S,Sakurai H

更新日期：2005-02-01 00:00:00

abstract：:Standard incubation procedures for carrying out microsomal assays involve the use of less than 1% w/v organic solvents to minimize the potential inhibitory effects of organic solvents on metabolic activity. This presents a practical limitation for poorly soluble xenobiotics, which cannot be incubated at concentrations...

journal_title：Drug metabolism and pharmacokinetics

authors： Argikar UA,Liang G,Bushee JL,Hosagrahara VP,Lee W

更新日期：2011-01-01 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：:In this study, a simple in vitro method for detecting human P450 (CYP) quasi-irreversible and irreversible inhibitors was evaluated. For the method, cDNA-expressed CYPs were applied to microtiter plate assays, CYP inhibitors were co-incubated with fluorometric substrates, and IC(50) were continuously measured (without...

journal_title：Drug metabolism and pharmacokinetics

authors： Naritomi Y,Teramura Y,Terashita S,Kagayama A

更新日期：2004-02-01 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：: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