The role of organic ion transporters in drug disposition: an update.

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：: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：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：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

abstract：:Thiopurines such as azathioprine, 6-mercaptopurine and 6-thioguanine are antimetabolites that have been used for several decades in the treatment of several diseases including inflammatory bowel diseases. Additional anti-inflammatory properties of these thiopurines have been discovered in recent years. Thiopurine meta...

journal_title：Current drug metabolism

authors： Van Asseldonk DP,de Boer NK,Peters GJ,Veldkamp AI,Mulder CJ,Van Bodegraven AA

更新日期：2009-11-01 00:00:00

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：:Diabetes is associated with an increase risk for cardiovascular disease (CVD). Recently, macrovascular complications of diabetes have been shown to start before the development of diabetes. Indeed, several clinical studies have confirmed the increased risk of CVD in patients with impaired glucose tolerance (IGT). Sinc...

journal_title：Current drug metabolism

authors： Yamagishi S,Matsui T,Ueda S,Fukami K,Okuda S

更新日期：2009-02-01 00:00:00

abstract：BACKGROUND:ET-26 hydrochloride is a novel intravenous anesthetic, approved for clinical trials, that produces a desirable sedative-hypnotic effect with stable myocardial performance and mild adrenocortical suppression in rats and beagle dogs. The objective of this study was to assess the absorption, distribution, metab...

journal_title：Current drug metabolism

authors： Zhang YJ,Deng C,Yang J,Gong D,Kang Y,Liu J,Zhang W

更新日期：2019-01-01 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：: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：:Understanding the mechanism of action of organophosphates (OP)/nerve agents -- irreversible acetylcholinesterase (AChE, EC 3.1.1.7) inhibition at the cholinergic synapses followed by metabolic dysbalance of the organism -- two therapeutic principles for antidotal treatment are derived. The main drugs are anticholinerg...

journal_title：Current drug metabolism

authors： Bajgar J,Kuca K,Jun D,Bartosova L,Fusek J

更新日期：2007-12-01 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：:Superparamagnetic iron oxide nanoparticles (SPIONs) have attracted a lot of interest due to their widespread diagnostic and therapeutic applications in neuro-oncology. Functinalization of the particles surface with targeting molecules that recognize tumor receptors might be exploited for the specific brain tumor targe...

journal_title：Current drug metabolism

authors： Shevtsov MA

更新日期：2016-06-15 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 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 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：: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：: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：: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：: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：:In recent years several arylpiperazine derivatives have reached the stage of clinical application, mainly for the treatment of depression, psychosis or anxiety. Examples are the pyrimidinylpiperazine buspirone, the chlorophenylpiperazine derivatives nefazodone and trazodone, the dichlorophenylpiperazine aripiprazole a...

journal_title：Current drug metabolism

authors： Caccia S

更新日期：2007-08-01 00:00:00

abstract：BACKGROUND:The administration of multiple drugs for the treatment of diseases is an integral aspect of modern medicine. Though its purpose is to create the intended therapeutic effect, the unintended consequences of drug interactions can cause severe side effects and subsequent economic losses. Likewise, herbal extract...

journal_title：Current drug metabolism

authors： Goon CP,Wang LZ,Wong FC,Thuya WL,Ho PC,Goh BC

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND:The red-crowned crane (Grus japonensis) is one of the most vulnerable bird species in the world. Mycotoxins are toxic secondary metabolites produced by fungi and considered naturally unavoidable contaminants in animal feed. Our recent survey indicated that the mycotoxins had the potential to contaminate redc...

journal_title：Current drug metabolism

authors： Liu D,Wu Q,Liu H,Lu C,Gu C,Kuca K,Wu W

更新日期：2020-01-01 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：: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：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：OBJECTIVES:Induction or inhibition of cytochrome P450 (CYP) enzyme activities, enzymes that activate or detoxify xenobiotics, is one mechanism by which vegetables may alter cancer risk. As the effect of food on CYP enzyme activities have not been studied in the Jordanian population, we examined the effect of supplement...

journal_title：Current drug metabolism

authors： Hakooz N,Hamdan I

更新日期：2007-01-01 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: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:Despite recent therapeutic advances, osteoarthritis continues to be a challenging health problem, especially in the elderly population. Opioids, which are potent analgesics, have shown an extraordinary ability to reduce intense pain in many osteoarthritic clinical trials; however, there is an increased need ...

journal_title：Current drug metabolism

authors： Alhaj-Suliman SO,Milavetz G,Salem AK

更新日期：2020-01-01 00:00:00