Metabolism and disposition of the antiviral nucleoside analogue AM365 in the isolated perfused rat liver.

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：:Cytochrome P450s (P450 or CYPs) comprise a superfamily of enzymes that catalyze the oxidation of a wide variety of xenobiotic chemicals. Although most of P450 inhibitors decrease the metabolic activities mediated by the corresponding P450 forms, unexpected phenomena, which are called as activation or heterotropic coop...

journal_title：Current drug metabolism

authors： Niwa T,Murayama N,Yamazaki H

更新日期：2008-06-01 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：:The aim of the present study was to develop and improve methods for phenotyping of CYP2E1, an important enzyme in the biotransformation of many industrial chemicals, therapeutic drugs and endogenous substances. The possibility to measure CYP2E1 activity in lymphocytes by using p-nitrophenol as a substrate and CYP2E1 p...

journal_title：Current drug metabolism

authors： Ernstgård L,Johanson G,Karlsson AS,Warholm M

更新日期：2007-06-01 00:00:00

abstract：BACKGROUND:It is well known that ethanol can cause significant morbidity and mortality, and much of the related toxic effects can be explained by its metabolic profile. OBJECTIVE:This work performs a complete review of the metabolism of ethanol focusing on both major and minor metabolites. METHOD:An exhaustive litera...

journal_title：Current drug metabolism

authors： Dinis-Oliveira RJ

更新日期：2016-01-01 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 M2 proton channel is translated by the M gene segment of influenza viruses, and has been adopted as an attractive target for influenza A viruses, on which a series of adamantane-based drugs act. However, recently epidemic influenza viruses have had strong resistant effects against the adamantane-based drugs. In th...

journal_title：Current drug metabolism

authors： Yu Y,Li X,Hao P,Wang JF,Chou KC

更新日期：2014-01-01 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：: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

abstract：:Ageing is characterized by a progressive decline in the functional reserve of multiple organs and systems, which can influence drug disposition. In addition, comorbidity and polypharmacy are highly prevalent in the elderly. As ageing is associated with some reduction in first-pass metabolism, bioavailability of a few ...

journal_title：Current drug metabolism

authors： Shi S,Klotz U

更新日期：2011-09-01 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：:Advances in high-throughput technologies to measure genome-scale changes of genes, proteins, and other biomolecular components ('omics') in complex biological systems have dramatically revolutionized biomedical research. However, the benefits of utilizing omics information in drug development have not yet been fully r...

journal_title：Current drug metabolism

authors： Fang H,Wang K,Zhang J

更新日期：2008-12-01 00:00:00

abstract：:Early understanding of the metabolic pathway and potential interaction of new drug candidates with other drugs is one of the goals of preclinical studies in the drug discovery process. Although other body organs are involved in drug biotransformation, the liver is the predominant organ of metabolism for a wide range o...

journal_title：Current drug metabolism

authors： Fasinu P,Bouic PJ,Rosenkranz B

更新日期：2012-02-01 00:00:00

abstract：BACKGROUND:Clinical studies during pregnancy are rare due to ethical and practical limitations. Giving pregnant females the same dosing regimen used in adult males or nonpregnant females is inappropriate. Pregnancy physiologically-based pharmacokinetic modeling is a powerful tool that can be used to refine pharmacother...

journal_title：Current drug metabolism

authors： Alsmadi MM,Idkaidek N

更新日期：2018-01-01 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：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：: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：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：:Transporters for organic anions and organic cations in kidney, liver, intestine, brain, and placenta play essential roles in drug disposition. The cloning and characterization of these transporters have significantly advanced our understanding of the molecular and cellular mechanisms of the drug disposition process. T...

journal_title：Current drug metabolism

authors： You G

更新日期：2004-02-01 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：: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：: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：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：BACKGROUND:The metabolic/biotransformation pathways of atypical antipsychotics (aripiprazole, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, and ziprasidone) have been characterized and reviewed. However, comparisons of excretory pathways remain unexplored. OBJECTIVE:To analyze the excretio...

journal_title：Current drug metabolism

authors： Sheehan JJ,Sliwa JK,Amatniek JC,Grinspan A,Canuso CM

更新日期：2010-07-01 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：: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：:Human genome sequencing highlights the involvement of genetic variation towards differential risk of human diseases, presence of different phenotypes, and response to pharmacological elements. This brings the field of personalized medicine to forefront in the era of modern health care. Numerous recent approaches have ...

journal_title：Current drug metabolism

authors： Prakash S,Agrawal S

更新日期：2016-01-01 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：:Knowledge regarding cytochrome P450 (P450) is crucial to the fields of drug therapy and drug development, as well as in our understanding of the mechanisms underlying the metabolic activation of potentially toxic and carcinogenic compounds. Escherichia coli is the most extensively utilized host in the production of re...

journal_title：Current drug metabolism

authors： Yun CH,Yim SK,Kim DH,Ahn T

更新日期：2006-05-01 00:00:00

abstract：BACKGROUND:The prolonged circulation time of nanoparticles in the blood is a prerequisite to realize a controlled and targeted (passive or active targeting) release of the encapsulated gene/drug at the desired site of action. The most popular method to mask or camouflage nanoparticles is the adsorbed, grafted or conjug...

journal_title：Current drug metabolism

authors： Hu J,Sheng Y,Shi J,Yu B,Yu Z,Liao G

更新日期：2018-01-01 00:00:00