High throughput ADME screening: practical considerations, impact on the portfolio and enabler of in silico ADME models.

abstract：BACKGROUND:Acute Kidney Injury (AKI) is a sudden decrease in kidney function. In the early period, the highest percentage of AKI occurs among newborns hospitalized in the neonatal intensive care units, especially premature neonates. The prognosis of AKI depends on the type and severity of the cause of an injury, the ac...

journal_title：Current drug metabolism

authors： Kamianowska M,Szczepański M,Wasilewska A

更新日期：2019-01-01 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：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：: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：: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：: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：:The in vivo hepatic clearance of tanshinone IIA in the rat was predicted using microsome, cytosol and S9 fractions combined with two different cofactor systems, NADPH-regenerating and UDPGA system. Two different models, the well stirred model and the parallel-tube model, were used in predicting the in vivo clearance i...

journal_title：Current drug metabolism

authors： Li P,Wang GJ,Li J,Zhang Q,Liu X,Khlentzos A,Roberts MS

更新日期：2008-01-01 00:00:00

abstract：BACKGROUND:Interleukin-28B (IL28B) locus on a human chromosomal region mapped to 19q13 execute immune defense against viruses. During Hepatitis C Virus (HCV) infection the IL28B has a promising role in deciding the consequence of infection for spontaneous clearance of viruses or causing chronic liver infection. Treatme...

journal_title：Current drug metabolism

authors： Asthana M,Sahu SK,Kumar A,Mohanty S,Chakrabarti S,Das P,Chattopadhya NR,Chatterjee K,Singh SP,Rajasubramaniam S,Choudhuri T

更新日期：2018-01-01 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

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：BACKGROUND:Glioblastoma multiforme, one of the most aggressive brain tumors, has a very poor clinical outcome. Despite the introduction of the alkylating reagent temozolomide (TMZ) to surgery and radiotherapy, the survival of patients could only be modestly increased up to less than 15 months. Therefore, innovative tre...

journal_title：Current drug metabolism

authors： Shevtsov M,Multhoff G

更新日期：2016-01-01 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：: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 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：: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：:Graphene possesses a wide range of potential biomedical applications because of the unique physical and chemical properties. However, the side effects of grapheme and its derivatives on a number of biological models even on human body are still not very clear. Therefore, to properly assess the potential risk of graphe...

journal_title：Current drug metabolism

authors： Xu C,Wang J,Xu Y,Shang G,Wang R,Lin Y

更新日期：2013-10-01 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：:Maternal antenatal therapy with glucocorticoids (GC) is routinely used to prevent lung immaturity. The potential harmful effects on other organs, including in particular the central nervous system (CNS), are still controversial. In the present review we aimed to investigate: i) the beneficial and detrimental effects o...

journal_title：Current drug metabolism

authors： Gazzolo D,Serpero LD,Frigiola A,Abella R,Dro Giamberti A,Li Volti G,Michetti F

更新日期：2013-02-01 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: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：: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：: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：:Chronic heart failure (CHF) is now recognized as a multisystem disorder with increased sympathetic tone, hormonal derangements, an anabolic/catabolic imbalance, endothelial dysfunction, and systemic low-grade inflammation affecting various organ systems. Pro-inflammatory cytokines appear to play important roles in tha...

journal_title：Current drug metabolism

authors： Sandek A,Anker SD,von Haehling S

更新日期：2009-01-01 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：:There are several clinically useful endoperoxides, mainly artemisinin derivatives available in market for the treatment of malaria. These are highly potent drugs, with fastest parasite reduction ratio, broadest parasite stage specificity and effectiveness against all species of plasmodium in human. Endoperoxides are c...

journal_title：Current drug metabolism

authors： Gautam A,Ahmed T,Batra V,Paliwal J

更新日期：2009-03-01 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 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: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：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