Lack of a primary physicochemical determinant in the direct transport of drugs to the brain after nasal administration in rats: potential involvement of transporters in the pathway.

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：:We performed a caffeine (N-3-methyl-13C) breath test (CafeBT) to determine whether it can be employed to identify caffeine metabolism-associated single nucleotide polymorphisms. The study included 130 healthy adults (mean age: 21.9 years). Saliva was collected using an Oragene®•DNA saliva collection kit. Breath sample...

journal_title：Drug metabolism and pharmacokinetics

authors： Ishii M,Ishii Y,Nakayama T,Takahashi Y,Asai S

更新日期：2020-06-01 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：: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：: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：: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：:Decitabine (DAC), a DNA methylation inhibitor, is transported into cancer cells mainly via equilibrative nucleoside transporter 1 (ENT1) and subsequently phosphorylated by deoxycytidine kinase (dCK). We previously reported that apparent DAC uptake into cells may be described using a simple compartment model with clear...

journal_title：Drug metabolism and pharmacokinetics

authors： Ueda K,Nakamura T,Tanaka S,Hosokawa M,Iwakawa S,Ogawara KI

更新日期：2020-02-01 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：: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：: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：: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：: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：: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 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：: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：: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：: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：: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：: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：: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：:Nevirapine (NVP) is widely used as a non-nucleoside reverse transcriptase inhibitor of HIV-1, however, it is associated with severe skin and liver injury. The mechanisms of these adverse reactions are not yet clear, but the metabolic activation of NVP is thought to be related to the injury process. Until now, several ...

journal_title：Drug metabolism and pharmacokinetics

authors： Tateishi Y,Ohe T,Yasuda D,Takahashi K,Nakamura S,Kazuki Y,Mashino T

更新日期：2020-04-01 00:00:00

abstract：:DDI could be caused by the inhibition of OATP-mediated hepatic uptakes. The aim of this study is to set the risk criteria for the compounds that would cause DDI via OATP inhibition at the drug discovery stage. The IC50 values of OATP inhibitors for human OATP-mediated atorvastatin uptake were evaluated in the expressi...

journal_title：Drug metabolism and pharmacokinetics

authors： Nakakariya M,Goto A,Amano N

更新日期：2016-10-01 00:00:00

abstract：:UDP-glucuronosyltransferases (UGTs) are drug-metabolizing enzymes essential for the metabolism of endogenous substrates and xenobiotics. The cynomolgus macaque is a nonhuman primate species widely used in drug metabolism studies. The molecular characteristics of UGTs have been extensively investigated in humans, but t...

journal_title：Drug metabolism and pharmacokinetics

authors： Uno Y,Yamazaki H

更新日期：2020-08-01 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 vivo percutaneous absorption of emedastine difumarate was investigated in rats and compared with rat skin in vitro. Since emedastine entering the systemic circulation is mostly excreted in bile, we first came up with the method of collecting bile with a minimal skin incision. In vivo skin permeation of the drug was...

journal_title：Drug metabolism and pharmacokinetics

authors： Harada S,Yamashita F,Hashida M

更新日期：2005-10-01 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：:This study aimed to evaluate the relationship between the concentrations of plasma fentanyl and serum 4β-hydroxycholesterol based on CYP3A5 genotype and gender in cancer patients. Thirty-three Japanese cancer patients treated with transdermal fentanyl were enrolled. The concentrations of plasma fentanyl and norfentany...

journal_title：Drug metabolism and pharmacokinetics

authors： Ishida T,Naito T,Sato H,Kawakami J

更新日期：2016-06-01 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：: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：: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