Liver-based in vitro technologies for drug biotransformation studies - a review.

abstract：:Recent advances in the biological and analytical sciences have led to unprecedented interest in the discovery and quantitation of endogenous molecules that serve as indicators of drug safety, mechanism of action, efficacy, and disease state progression. By allowing for improved decision-making, these indicators, refer...

journal_title：Current drug metabolism

authors： Ackermann BL,Hale JE,Duffin KL

更新日期：2006-06-01 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：: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：:The occurrence of idiosyncratic adverse drug reactions during late clinical trials or after a drug has been released can lead to a severe restriction in its use and even in its withdrawal. Metabolic activation of relatively inert functional groups to reactive electrophilic intermediates is considered to be an obligato...

journal_title：Current drug metabolism

authors： Kalgutkar AS,Gardner I,Obach RS,Shaffer CL,Callegari E,Henne KR,Mutlib AE,Dalvie DK,Lee JS,Nakai Y,O'Donnell JP,Boer J,Harriman SP

更新日期：2005-06-01 00:00:00

abstract：BACKGROUND:Gold nanoparticles have been exploited for nanobiotechnology applications for the last two decades. New insights of the nanomaterials as promising agent for cancer diagnosis and therapy have just started to emerge. Due to the size- and shape-dependent optical, electrical and thermal properties, gold nanopart...

journal_title：Current drug metabolism

authors： Ning L,Zhu B,Gao T

更新日期：2017-01-01 00:00:00

abstract：:Recently, it was found that mutations in the binding cavity of drug-metabolizing Cytochrome P450 BM3 mutants can result in major changes in regioselectivity in testosterone (TES) hydroxylation. In the current work, we report the intrinsic reactivity of TES' C-H bonds and our attempts to rationalize experimentally obse...

journal_title：Current drug metabolism

authors： de Beer SB,van Bergen LA,Keijzer K,Rea V,Venkataraman H,Guerra CF,Bickelhaupt FM,Vermeulen NP,Commandeur JN,Geerke DP

更新日期：2012-02-01 00:00:00

abstract：:Fluoropyrimidines and oxaliplatin continued to be the mainstay of therapeutic regimens in the treatment of colorectal cancer (CRC). For this reason, pharmacokinetic and metabolism of these drugs were analyzed and the identification of accurate and validated predictive, prognostic and toxicity markers became necessary ...

journal_title：Current drug metabolism

authors： Gnoni A,Russo A,Silvestris N,Maiello E,Vacca A,Marech I,Numico G,Paradiso A,Lorusso V,Azzariti A

更新日期：2011-12-01 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：:Transplantation has become an established and successful therapy. Rejections and infections are the principal immune-related complications in the post-transplant course. A reliable and early diagnosis is necessary to prevent graft failure and patient morbidity. Despite the immunologic nature of these complications the...

journal_title：Current drug metabolism

authors： Grebe SO,Mueller TF

更新日期：2002-04-01 00:00:00

abstract：:Photodynamic therapy (PDT) combines photosensitizer, visible light and oxygen, which has the characteristics of high selectivity, minimal invasiveness, low side effect, and allowing repetitive application. The photophysics and mechanisms leading to cell death mediated by PDT have been studied extensively, and PDT has ...

journal_title：Current drug metabolism

authors： Li WT

更新日期：2009-10-01 00:00:00

abstract：BACKGROUND:Bioequivalence studies are a vital part of drug development. The average bioequivalence approach is the standard method of assessment to conclude whether the generic product is bioequivalent to the innovator product. Of late, debates are on whether the average bioequivalence approach adequately addresses dru...

journal_title：Current drug metabolism

authors： Micheal F,Sayana M,Prasad R,Motilal BM

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:Nobel laureate Sir James Black's molecule, propranolol, still has broad potential in cardiovascular diseases, infantile haemangiomas and anxiety. A comprehensive and systematic review of the literature for the summarization of pharmacokinetic parameters would be effective to explore the new safe uses of prop...

journal_title：Current drug metabolism

authors： Kalam MN,Rasool MF,Rehman AU,Ahmed N

更新日期：2020-01-01 00:00:00

abstract：:The nature and level of systemic exposure to the active herbal constituents will profoundly affect their effects at action sites, which is fundamental in understanding their roles in the overall beneficial effects of a herbal medicine. The objective of this study is to gain a full picture of the systemic exposure to v...

journal_title：Current drug metabolism

authors： Li L,Zhao Y,Du F,Yang J,Xu F,Niu W,Ren Y,Li C

更新日期：2012-06-01 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：:We report here a comprehensive evaluation of the effects of culture duration on the gene expression of P450 isoforms, uptake transporters and efflux transporters in human hepatocyte cultured in the absence and presence of the prototypical proinflammatory cytokine, interleukin-6 (IL-6). Primary collagen-matrigel sandwi...

journal_title：Current drug metabolism

authors： Yang Q,Doshi U,Li N,Li AP

更新日期：2012-09-01 00:00:00

abstract：:Infection with the human immunodeficiency virus type 1 (HIV) results in a chronic infection that progressively cripples the host immune defenses. HIV infection is associated with increased tryptophan (trp) catabolism by the cytokine-inducible enzyme indoleamine 2,3-dioxygenase (IDO). IDO has powerful immune suppressiv...

journal_title：Current drug metabolism

authors： Boasso A,Shearer GM

更新日期：2007-04-01 00:00:00

abstract：:The pharmacological effects of a drug are highly dependent on the absorption, metabolism, elimination, and distribution of the drug. In the past few years it has become apparent that transport proteins play a major role in regulating the distribution, elimination and metabolism of some drugs. As a consequence of our n...

journal_title：Current drug metabolism

authors： Hochman JH,Yamazaki M,Ohe T,Lin JH

更新日期：2002-06-01 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：:Vasopressin (AVP) and its receptors play a pivotal role in maintaining body homeostasis under physiological and pathophysiological conditions. As a consequence, the vasopressin system has emerged as an important target for both diagnostic and therapeutic applications in a number of medical conditions. Stoichiometric g...

journal_title：Current drug metabolism

authors： Szczepanska-Sadowska E,Zera T,Sosnowski P,Cudnoch-Jedrzejewska A,Puszko A,Misicka A

更新日期：2017-01-01 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：:Membrane transporters play an important role in intestinal absorption, distribution and clearance of drugs. Additionally transporters along with enzymes regulate tissue exposures (e.g. liver, kidney and brain), which are important for safety and efficacy considerations. Early identification of transporters involved gu...

journal_title：Current drug metabolism

authors： Taskar KS,Harada I,Alluri RV

更新日期：2021-01-01 00:00:00

abstract：:We present a review of recent investigations of anticancer drug bexarotene in this article. As one of the novel synthetic analogs of retinoids, bexarotene selectively binds to and activates the retinoid X receptor (RXRs) subfamilies, exerting a prophylactic and therapeutic effect on a large series of tumors in vitro a...

journal_title：Current drug metabolism

authors： Qi L,Guo Y,Zhang P,Cao X,Luan Y

更新日期：2016-01-01 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：BACKGROUND:Nanoparticles (NPs) are being used extensively owing to their increased surface area, targeted delivery and enhanced retention. NPs have the potential to be used in many disease conditions. Despite widespread use, their toxicity and clinical safety still remain a major concern. OBJECTIVE:The purpose of this...

journal_title：Current drug metabolism

authors： Malaviya P,Shukal D,Vasavada AR

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND:Despite major advances in transplant medicine, antibody-mediated rejection (AMR) continues to have severe clinical implications and adversely affect graft survival. Therefore, the search for alternative drugs to treat AMR is widely pursued. The first-in-class proteasome inhibitor bortezomib (BZ) is a selecti...

journal_title：Current drug metabolism

authors： Requiao-Moura LR,de Sandes-Freitas TV,Marcelo-Gomes G,Rangel EB

更新日期：2017-01-01 00:00:00

abstract：:Oral administration remains the most preferred route for the treatment of many diseases due to its convenience and adaptability. However, the presystemic metabolism may be an important barrier that prevents lipophilic drugs from achieving their pharmacological effects following oral delivery. Nano-based drug delivery ...

journal_title：Current drug metabolism

authors： Zhang Z,Gao F,Jiang S,Ma L,Li Y

更新日期：2012-10-01 00:00:00

abstract：BACKGROUND:Overactive bladder syndrome is a broadly occurring urological disorder with a distressing impact on the quality of life. The commonly used antimuscarinic drugs show poor patient compliance because of unsatisfactory potency, tolerability and high occurrence of adverse effects such as dry mouth, blurred vision...

journal_title：Current drug metabolism

authors： Mandpe P,Prabhakar B,Shende P

更新日期：2020-01-01 00:00:00

abstract：:Evaluation and optimization of drug metabolism and pharmacokinetic data plays an important role in drug discovery and development and several reliable in vitro ADME models are available. Recently higher throughput in vitro ADME screening facilities have been established in order to be able to evaluate an appreciable f...

journal_title：Current drug metabolism

authors： Hop CE,Cole MJ,Davidson RE,Duignan DB,Federico J,Janiszewski JS,Jenkins K,Krueger S,Lebowitz R,Liston TE,Mitchell W,Snyder M,Steyn SJ,Soglia JR,Taylor C,Troutman MD,Umland J,West M,Whalen KM,Zelesky V,Zhao SX

更新日期：2008-11-01 00:00:00

abstract：BACKGROUND:Methotrexate (MTX) is a folate analogue with high therapeutic efficiency in the treatment of cancers and autoimmune diseases. The efficacy and toxicity of MTX may be altered by genetic polymorphisms in genes involved in MTX metabolic pathway. Personalized pharmacotherapy based on gene polymorphisms enables a...

journal_title：Current drug metabolism

authors： Cao M,Guo M,Wu DQ,Meng L

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND:Wound healing is a composite and vital process in which devitalized tissue layers and cellular structures repair themselves. Bronchiolitis is generally prompted by respiratory syncytial virus or human metapneumovirus; this condition is an acute inflammatory injury of bronchioles. Heart problems that develop ...

journal_title：Current drug metabolism

authors： AlMatar M,Batool T,Makky EA

更新日期：2016-01-01 00:00:00