Decreasing systemic toxicity via transdermal delivery of anticancer drugs.

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：: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：: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：:Hepatotoxicity related to antidepressive pharmacotherapy is a major safety concern, particularly considering that severe forms of hepatic failure with fatal outcome have been reported. Severe hepatotoxic adverse drug reactions were also reported for agomelatine (AGM), an antidepressive agent, which was approved for th...

journal_title：Current drug metabolism

authors： Gahr M,Kratzer W,Fuchs M,Connemann BJ

更新日期：2014-01-01 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：: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：:Ophthalmic drugs are delivered to ocular tissues predominantly via relatively simple formulations, such as topically dosed water-soluble drug solutions and water-insoluble drug suspensions in ointments. An ideal topical drug delivery system should possess certain desirable properties, such as good corneal and conjunct...

journal_title：Current drug metabolism

authors： Bu HZ,Gukasyan HJ,Goulet L,Lou XJ,Xiang C,Koudriakova T

更新日期：2007-02-01 00:00:00

abstract：:This review introduces the Noscapine, which is being used as an antitussive drug for a long time has been recently discovered as a novel tubulin-binding, anti-angiogenic anticancer drug that causes cell cycle arrest and induces apoptosis in cancer cells both in vitro as well as in vivo. Noscapine is a multifunctional ...

journal_title：Current drug metabolism

authors： Singh H,Singh P,Kumari K,Chandra A,Dass SK,Chandra R

更新日期：2013-03-01 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：:5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) belongs to a group of naturally-occurring psychoactive indolealkylamine drugs. It acts as a nonselective serotonin (5-HT) agonist and causes many physiological and behavioral changes. 5-MeO-DMT is O-demethylated by polymorphic cytochrome P450 2D6 (CYP2D6) to an active metab...

journal_title：Current drug metabolism

authors： Shen HW,Jiang XL,Winter JC,Yu AM

更新日期：2010-10-01 00:00:00

abstract：:Since conventional therapeutic approaches in cancer are highly invasive they hardly prolong patient survival for more than few months. Having the ability to stimulate both cellular and humoural immune responses, immunisation with naked plasmid DNA encoding tumour-associated antigens or tumour-specific antigens has rec...

journal_title：Current drug metabolism

authors： Chiarella P,Fazio VM,Signori E

更新日期：2013-03-01 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：: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：: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:Increasing incidences of type 2 diabetes make it necessary to have a better understanding of the risk factors for its prediction. Taking a note of resilience in risk factors, dynamics of the emerging factors other than traditional ones are showing a great interest in recent years which imprints a significant...

journal_title：Current drug metabolism

authors： Yadav D,Cho KH

更新日期：2018-01-01 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：: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：: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：: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：: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：: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：: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：: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：: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：: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：BACKGROUND:In recent times, herbals or phytomedicines have become very popular due to their global acceptance as a complementary and alternative remedy. While modern drugs are commercially available only after laboratory validations, clinical trials, as well as approval from drug regulatory authorities, majority of the...

journal_title：Current drug metabolism

authors： Parvez MK,Rishi V

更新日期：2019-01-01 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：BACKGROUND:Drug-induced cholestasis is a risk factor in the progression of drug candidates, and poses a serious health hazard if not detected before going into a human. Intrahepatic accumulation of Bile Acids (BAs) represents a characteristic phenomenon associated with drug-induced cholestasis. METHODS:This review wil...

journal_title：Current drug metabolism

authors： Chatterjee S,Annaert P

更新日期：2018-01-01 00:00:00

abstract：:Arylamine N-acetyltransferases (NAT) are xenobiotic-metabolizing enzymes responsible for the acetylation of many aromatic arylamine and heterocyclic amines, thereby playing an important role in both detoxification and activation of numerous drugs and carcinogens. Two closely related isoforms (NAT1 and NAT2) have been ...

journal_title：Current drug metabolism

authors： Rodrigues-Lima F,Dairou J,Dupret JM

更新日期：2008-07-01 00:00:00

abstract：:The present study was designed to investigate the hepatic disposition of the prodrug AM365 and the generated antiviral guanosine analogue, AM188 in the isolated perfused rat liver (IPL). The livers of rats (n=12) were isolated and perfused with Krebs-Henseleit pH 7.4 buffer to which AM365 was added as a bolus to achie...

journal_title：Current drug metabolism

authors： Wang J,Nation RL,Evans AM,Cox S,Shackleford D

更新日期：2005-10-01 00:00:00