Physiologically-Based Pharmacokinetic (PBPK) Modelling of Transporter Mediated Drug Absorption, Clearance and Drug-Drug Interactions.

abstract：:One of the major advances in the recent history of the treatment of HIV infections has been the development of different classes of effective antiretroviral drugs. In particular, the reverse transcriptase (RT) inhibitors still represent the majority of the clinically used anti-HIV drugs and constitute the main backbon...

journal_title：Current drug metabolism

authors： Locatelli GA,Cancio R,Spadari S,Maga G

更新日期：2004-08-01 00:00:00

abstract：:Several epidemiological studies throughout the years have suggested that polyphenols from fruits and vegetables promote health and reduce the risk of certain chronic and neurodegenerative diseases. Yet, it has been proved to be extremely difficult to quantitatively establish the benefit afforded by polyphenols, princi...

journal_title：Current drug metabolism

authors： Rubió L,Macià A,Motilva MJ

更新日期：2014-01-01 00:00:00

abstract：:The present review aims to give an overview of the cytochrome P450 8B (CYP8B) and cytochrome P450 4A (CYP4A) subfamilies in relation to biosynthesis of bile acids, in particular trihydroxy bile acids. Trihydroxy bile acids are basically required in most species and have an impact on cholesterol and lipid metabolism. T...

journal_title：Current drug metabolism

authors： Lundell K,Wikvall K

更新日期：2008-05-01 00:00:00

abstract：:Talin is an intracellular cytoskeletal protein and one of the major components of the focal adhesion complex. It mainly acts as an interlink between transmembrane integrin receptors and cytosolic F-actin. Apart from integrins and actin, it also interacts with various other proteins in the adhesion complex to regulate ...

journal_title：Current drug metabolism

authors： Malla RR,Vempati RK

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:In the last few years, the use of modified Carbon Nanomaterials (CNMs) for theranostics (therapeutic and diagnosis) applications is a new and rapidly growing area in pharmacy and medical fields. Owing to this, their specific physicochemical behaviors like high stability, drug loading, surface area to volume ...

journal_title：Current drug metabolism

authors： Gupta N,Rai DB,Jangid AK,Kulhari H

更新日期：2019-01-01 00:00:00

abstract：:The transcription factor networks that regulate basal and xenobiotic-modulated expression of the hepatic sulfotransferases affect the dynamics of xenobiotic detoxication, carcinogen bioactivation and metabolic homeostasis. Emerging evidence suggests that liver-enriched transcription factors, the aryl hydrocarbon (Ah) ...

journal_title：Current drug metabolism

authors： Runge-Morris M,Kocarek TA

更新日期：2005-08-01 00:00:00

abstract：BACKGROUND:Various transporters, including efflux transporters and uptake transporters, play an important role in the pharmacokinetics of drugs. Currently, studies suggest that several antibiotics also serve as substrates for transporters. In addition, these antibiotics are usually combined with other drugs to treat di...

journal_title：Current drug metabolism

authors： Hua WJ,Hua WX,Jian Z,Wei PH,Ni LY,Hua LY,Wen CD,Ying Z,Li C

更新日期：2016-01-01 00:00:00

abstract：:Decarboxylation, reduction and hydrolysis can yield active metabolites from the parent drug. Major therapeutic indications and metabolic routes of these drugs are reviewed. Changes in the logP values (determined and calculated) from the parent drug to the active metabolite show certain characteristics in comparison to...

journal_title：Current drug metabolism

authors： Hartyánszky I,Kalász H,Adeghate E,Gulyás Z,Hasan MY,Tekes K,Adem A,Sótonyi P

更新日期：2012-07-01 00:00:00

abstract：:Part I of this article published in the previous issue of Current Drug Metabolism discussed the substrate specificity, inhibitor selectivity and structure-activity relationship (SAR) of human CYP2C9. The features of CYP2C9 pharmacophore and SAR models have been elaborated. Part II of this article will address the homo...

journal_title：Current drug metabolism

authors： Mo SL,Zhou ZW,Yang LP,Wei MQ,Zhou SF

更新日期：2009-12-01 00:00:00

abstract：:This review provides a vista of the current opportunities and remaining challenges in the area of in vitro-in vivo extrapolation, with particular emphasis on drug binding terms in predictive models, which has been the source of much controversy. Although the importance of fu(inc) (fraction unbound in in vitro incubati...

journal_title：Current drug metabolism

authors： Grime K,Riley RJ

更新日期：2006-04-01 00:00:00

abstract：:Cytochromes P450 of the liver are involved in maintenance of lipid homeostasis (cholesterol, vitamin D, oxysterol and bile acid metabolism) and in detoxification processes of endogenous compounds (i. e. bile acids) and xenochemicals (drugs). This review describes the roles of various CYPs in production of cholesterol ...

journal_title：Current drug metabolism

authors： Hafner M,Rezen T,Rozman D

更新日期：2011-02-01 00:00:00

abstract：:For the pharmaceutical industry, one of the challenges in evaluating the risk of future compound attrition at the discovery stage is the successful prediction of the major routes of clearance in humans. For compounds cleared by metabolism, such information will help to avoid the development of compounds that will exhi...

journal_title：Current drug metabolism

authors： Williams JA,Hurst SI,Bauman J,Jones BC,Hyland R,Gibbs JP,Obach RS,Ball SE

更新日期：2003-12-01 00:00:00

abstract：:Phenolic compounds are commonly found in natural sources like plant-based foods and beverages. These compounds have received much attention due to their unique biological properties. Polyphenols possess a significant binding affinity for serum albumins which are known to be principal extracellular proteins with a high...

journal_title：Current drug metabolism

authors： Jaldappagari S,Balakrishnan S,Hegde AH,Teradal NL,Narayan PS

更新日期：2013-05-01 00:00:00

abstract：:Bioavailability of orally administered drugs can be influenced by a number of factors including release from the formulation, dissolution, stability in the gastrointestinal (GI) environment, permeability through the gut wall and first-pass gut wall and hepatic metabolism. Although there are various enzymes in the gut ...

journal_title：Current drug metabolism

authors： Darwich AS,Neuhoff S,Jamei M,Rostami-Hodjegan A

更新日期：2010-11-01 00:00:00

abstract：:This paper reviews the empirical methods of quantitative microdialysis that have been used to interpret the results obtained from pharmacokinetic studies. The concept of extraction efficiency or recovery and the properties of recovery in vivo (variation with flow rate, time dependency and influence of the mode of admi...

journal_title：Current drug metabolism

authors： Cano-Cebrián MJ,Zornoza T,Polache A,Granero L

更新日期：2005-04-01 00:00:00

abstract：:The biochemical activities of plant flavonoids and stilbenoids point to many health-related applications, hampered however by a low bioavailability associated with rapid metabolic modification. A possible approach to overcome this obstacle is the development of prodrugs. In this review we provide some background infor...

journal_title：Current drug metabolism

authors： Biasutto L,Zoratti M

更新日期：2014-01-01 00:00:00

abstract：:During the lifetime, our cells encounter many challenges to their own existence. The survival of organisms and cells depends on the interplay within a complex, yet precisely orchestrated network of proteins. Since the discovery of the Rel/NF-kappaB family of transcription factors, the research has never come to a stop...

journal_title：Current drug metabolism

authors： Zineldeen DH,Uranishi H,Okamoto T

更新日期：2010-03-01 00:00:00

abstract：:A number of studies have appeared recently on the underlying mechanisms of liposome-cell interactions under in vitro conditions, in which isolated cell populations or cell lines were used. However, our knowledge of how liposomes interact with cells and the parameters that influence this in vivo is limited. We will sum...

journal_title：Current drug metabolism

authors： Ishida T,Harashima H,Kiwada H

更新日期：2001-12-01 00:00:00

abstract：:L-Carnitine has important roles in intermediary metabolism and patients with end-stage renal disease who are undergoing hemodialysis may develop a secondary L-carnitine deficiency. The extent of accumulation of the metabolites trimethylamine and trimethylamine-N-oxide when L-carnitine is administered orally has not be...

journal_title：Current drug metabolism

authors： Bain MA,Faull R,Milne RW,Evans AM

更新日期：2006-10-01 00:00:00

abstract：:Gender differences in drug concentrations, drug response and toxicity have been attributed to various distinct yet interrelated physiological and molecular mechanisms. Drug transporters and metabolising enzymes play an important role in the xenobiotic cascade and are important regulators of drug disposition at the mol...

journal_title：Current drug metabolism

authors： Bebawy M,Chetty M

更新日期：2009-05-01 00:00:00

abstract：:Accompanying with hot discussions on developing multi-target drugs for the therapy of multi-gene diseases, herbal medicines are receiving more and more attention worldwide in both academic and industrial fields. Pharmacokinetic and metabolic research is one of the important issues for intensive understanding of therap...

journal_title：Current drug metabolism

authors： Wu L,Hao H,Wang G

更新日期：2012-11-01 00:00:00

abstract：BACKGROUND:Thiopurine antimetabolites are important agents for the treatment of severe diseases, such as acute lymphoblastic leukemia and inflammatory bowel disease. Their pharmacological actions depend on biotransformation into active thioguanine-nucleotides; intracellular metabolism is mediated by enzymes of the salv...

journal_title：Current drug metabolism

authors： Pelin M,De Iudicibus S,Londero M,Spizzo R,Dei Rossi S,Martelossi S,Ventura A,Decorti G,Stocco G

更新日期：2016-01-01 00:00:00

abstract：: ...

journal_title：Current drug metabolism

authors： Wei JF

更新日期：2018-01-01 00:00:00

abstract：:Glucuronidation represents a major pathway which enhances the elimination of many lipophilic xenobiotics and endobiotics to more water-soluble compounds. The UDP-glucuronosyltransferase (UGT) family catalyzes the glucuronidation of the glycosyl group of a nucleotide sugar to an acceptor compound (aglycone) at a nucleo...

journal_title：Current drug metabolism

authors： King CD,Rios GR,Green MD,Tephly TR

更新日期：2000-09-01 00:00:00

abstract：:To understand the sophisticated dynamic behaviors of drug elution and permeation in the gastrointestinal tract (GIT), researchers have tried to reemerge it by employing various in vitro experimental models. However, official in vitro apparatuses routinely used for quality control purposes, employ simple, non-physiolog...

journal_title：Current drug metabolism

authors： Li Z,He X

更新日期：2015-01-01 00:00:00

abstract：:The Cytochrome P450 4A subfamily is one of eighteen subfamilies in the CYP4 family and presently consists of twenty individual forms in nine different mammalian species. The major substrates for CYP4A forms are fatty acids, but recent studies have shown other non-fatty acid substrates may be metabolized by specific CY...

journal_title：Current drug metabolism

authors： Okita RT,Okita JR

更新日期：2001-09-01 00:00:00

abstract：OBJECTIVE:Tyrosine kinase inhibitors (TKIs) are widely used drugs which have high availability in reducing the activity of BCR-ABL1 tyrosine kinase, therefore they play an indispensable role in the treatment of Chronic myeloid leukemia (CML). Imatinib, dasatinib and nilotinib have been proved to have absolute bioavaila...

journal_title：Current drug metabolism

authors： Wang R,Zhong C,Zhang C,Hua M,Ma D

更新日期：2017-01-01 00:00:00

abstract：:New chemical entities are routinely screened in vitro and in vivo for their ability to induce cytochrome P450s (CYP), other drug-metabolizing enzymes and possibly transporters in an attempt to more accurately predict clinical parameters such as drug-drug interactions and clearance in humans. Some of these potential th...

journal_title：Current drug metabolism

authors： Mankowski DC,Ekins S

更新日期：2003-10-01 00:00:00

abstract：:Modern biologics are biotechnology-derived pharmaceuticals. They are mostly used for diagnosis, prevention and treatment of serious and chronic diseases. Today, therapeutic biologics range from traditional biologics like blood and blood components, fractionated blood products, and antitoxins to modern biologics such a...

journal_title：Current drug metabolism

authors： Baumann A

更新日期：2006-01-01 00:00:00

abstract：:The combined treatment with anticonvulsant and antidepressant drugs is reported in both neurologic and psychiatric practice; it is, therefore, evident that the issue of managing such type of polytherapy is frequently encountered by clinicians. To review current literature on pharmacokinetic interactions between antico...

journal_title：Current drug metabolism

authors： Mula M

更新日期：2008-10-01 00:00:00