The gut and intestinal bacteria in chronic heart failure.

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：: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: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：:With the recent advancement in nanoscience and nanotechnology, there is a growing demand for assessment of the toxicological effects of nano materials to humans and other biological systems. And a predictive toxicology approach that uses in vitro screening assays in conjunction with in vivo study results are widely em...

journal_title：Current drug metabolism

authors： Suma RN,Mohanan PV

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:Neuropsychiatric diseases primarily characterized by dementia stand third in the global list of diseases causing disability. The poor water solubility, erratic oral absorption, low bioavailability, poor intestinal absorption, and the impeding action of the blood-brain barrier (BBB) are the major factors limi...

journal_title：Current drug metabolism

authors： Rehman S,Nabi B,Pottoo FH,Baboota S,Ali J

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：: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：:The binding of drugs with serum proteins can affect the activity, distribution, rate of excretion, and toxicity of pharmaceutical agents in the body. One tool that can be used to quickly analyze and characterize these interactions is high-performance affinity chromatography (HPAC). This review shows how HPAC can be us...

journal_title：Current drug metabolism

authors： Hage DS,Anguizola J,Barnaby O,Jackson A,Yoo MJ,Papastavros E,Pfaunmiller E,Sobansky M,Tong Z

更新日期：2011-05-01 00:00:00

abstract：BACKGROUND:Painful peripheral neuropathy is a dose-limiting adverse effect of the antitumor drug oxaliplatin. The main symptoms of neuropathy: tactile allodynia and cold hyperalgesia, appear in more than 80% of patients on oxaliplatin therapy and are due to the overexpression of neuronal sodium channels (Navs) and neur...

journal_title：Current drug metabolism

authors： Furgała-Wojas A,Kowalska M,Nowaczyk A,Fijałkowski Ł,Sałat K

更新日期：2020-01-01 00:00:00

abstract：:It has long been suggested that some of the neuropharmacological, neurochemical and behavioural effects of ethanol are mediated by its first metabolite, acetaldehyde. In spite of the well documented psychoactivity of acetaldehyde, the precise role of this compound in alcohol abuse remains a matter of intense debate am...

journal_title：Current drug metabolism

authors： Hipólito L,Sánchez MJ,Polache A,Granero L

更新日期：2007-10-01 00:00:00

abstract：:With the advances in recombinant DNA biotechnology, molecular biology and immunology, the number of biotech drugs, including peptides, proteins and monoclonal antibodies, available for clinical use has dramatically increased in recent years. Although pharmacokinetic principles are equally applicable to the large molec...

journal_title：Current drug metabolism

authors： Lin JH

更新日期：2009-09-01 00:00:00

abstract：:The assessment of in vitro inhibition and induction of the cytochrome P450 enzymes of the liver is a critical part of the drug discovery and development process in order to ensure that two or more drugs can be safely coadministered without alterations in exposure. Early assessment of potential candidates using high th...

journal_title：Current drug metabolism

authors： Walsky RL,Boldt SE

更新日期：2008-11-01 00:00:00

abstract：BACKGROUND:The management of ischemic nephropathy due to atherosclerotic renal artery stenosis has become increasingly conservative in the modern era, with current guidelines recommending optimized medical therapy as the initial step. The doubts raised by the recently published trials of revascularization strategies ha...

journal_title：Current drug metabolism

authors： Rivoli L,Di Mario F,Coppolino G,Gigante A,Barbano B,Farrah TE,Rosato E,Fuiano G,Cianci R

更新日期：2016-01-01 00:00:00

abstract：:Currently the major research highlights of bioengineering and medical technology are directed towards development of improved diagnostic techniques to screen complex diseases. Screening requirements are to identify the cause of illnesses, monitor improvement or progression of the state of diseases such as cancer, card...

journal_title：Current drug metabolism

authors： Savaliya R,Shah D,Singh R,Kumar A,Shanker R,Dhawan A,Singh S

更新日期：2015-01-01 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：BACKGROUND:Mutation in the B RAF at V600E has been well implicated in the carcinogenesis that makes it as an attractive therapeutictarget. In the present study, we sought to identify the basis of V600E mutation at functional and structural grounds. The study also endeavors in identification of small molecule as a poten...

journal_title：Current drug metabolism

authors： Bandaru S,Sumithnath TG,Sharda S,Lakhotia S,Sharma A,Jain A,Hussain T,Nayarisseri A,Singh SK

更新日期：2017-07-21 00:00:00

abstract：:Pharmacokinetic studies conducted in patients with CRF demonstrate that the nonrenal clearance of multiple drugs is reduced. Although the mechanism by which this occurs is unclear, several studies have shown that CRF affects the metabolism of drugs by inhibiting key enzymatic systems in the liver, intestine and kidney...

journal_title：Current drug metabolism

authors： Pichette V,Leblond FA

更新日期：2003-04-01 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：:Work on human immortalized cell lines is not considered research on human subjects, but does involve biohazards. It has also been estimated that about 80% of human cell lines are the kind of cells that they are expected. Cells that are cultured directly from a subject are referred to as primary cells. Clonetics is the...

journal_title：Current drug metabolism

authors： Gomase VS,Tagore S,Changbhale SS,Kale KV

更新日期：2008-03-01 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：:Drug metabolite identification and metabolic characteristics analysis play a crucial role in new drug research and development, because they can lead to varied efficacy, severe adverse reactions, and even toxicity. Classical methodologies for metabolite identification have mainly been based on mass spectrometry (MS) c...

journal_title：Current drug metabolism

authors： Lu W,Xu Y,Zhao Y,Cen X

更新日期：2014-01-01 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：:Glucuronidation is responsible for the clearance of a diverse range of drug and chemicals whose topology confers properties that complicate in vitro-in vivo clearance correlations as compared to those possible for oxidative metabolism. The active site of the UGTs faces the inside of the luminal space of the endoplasmi...

journal_title：Current drug metabolism

authors： Lin JH,Wong BK

更新日期：2002-12-01 00:00:00

abstract：:Graphene and its modified nano-composites have gained much attention in recent times in cancer therapy as nanotheranostics due to low production cost, ease in synthesis and physicochemical properties (ultra-large surface area with planar structure and π-π conjugation with the unsaturated and aromatic drugs/biomolecule...

journal_title：Current drug metabolism

authors： Rahman M,Ahmad MZ,Ahmad J,Firdous J,Ahmad FJ,Mushtaq G,Kamal MA,Akhter S

更新日期：2015-01-01 00:00:00

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：: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：: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：:Brain, the centre of the nervous system and an integral part the body, is protected by two anatomical and physiological barriers- Blood-Brain Barrier (BBB) and Blood-Cerebrospinal Fluid Barrier (BCSFB). Blood-Brain Barrier is a very complex and highly organized multicellular structure that shields the brain from harmf...

journal_title：Current drug metabolism

authors： Sarkar A,Fatima I,Jamal QMS,Sayeed U,Khan MKA,Akhtar S,Kamal MA,Farooqui A,Siddiqui MH

更新日期：2017-01-01 00:00:00

abstract：:The pressing need for targeting, detecting, monitoring, and treating diseased cells concomitantly gives rise to multi-functional nanomedicines, especially those that can combine diagnostic and therapeutic abilities, which are referred to as nanotheranostics. Recently, nanotheranostics are of significant clinical inter...

journal_title：Current drug metabolism

authors： Han N,Yang YY,Wang S,Zheng S,Fan W

更新日期：2013-07-01 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