Early drug safety evaluation: biomarkers, signatures, and fingerprints.

abstract：:The efficacy of drugs has to be demonstrated following the principal approach of statistical evaluation in controlled clinical trials. This scientifically and internationally accepted numerical approach has developed over the years to its importance, in contrast to the more pharmacologically attempt to extrapolate hum...

journal_title：Drug metabolism reviews

authors： Hildebrandt AG

更新日期：2004-10-01 00:00:00

abstract：:The cannabinoid receptor 1 (CB1) is a G protein-coupled receptor (GPCR) that is located primarily in the central nervous system. CB1 is a therapeutic target which may impact pathways to mediate pain, neurodegenerative disorders, hunger, and drug-seeking behavior. Despite these benefits, development of orthosteric ther...

journal_title：Drug metabolism reviews

authors： Dopart R,Lu D,Lichtman AH,Kendall DA

更新日期：2018-02-01 00:00:00

abstract：:Human CYP1A2 is one of the major CYPs in human liver and metabolizes a number of clinical drugs (e.g., clozapine, tacrine, tizanidine, and theophylline; n > 110), a number of procarcinogens (e.g., benzo[a]pyrene and aromatic amines), and several important endogenous compounds (e.g., steroids). CYP1A2 is subject to rev...

journal_title：Drug metabolism reviews

authors： Zhou SF,Wang B,Yang LP,Liu JP

更新日期：2010-05-01 00:00:00

abstract：:The mitochondrial amidoxime-reducing component (mARC) is a recently discovered molybdenum-containing enzyme in mammalians. Upon reconstitution with the electron transport proteins, cytochrome b(5) and its reductase, this molybdenum enzyme is capable of reducing N-hydroxylated compounds. It was named mARC because the N...

journal_title：Drug metabolism reviews

authors： Havemeyer A,Lang J,Clement B

更新日期：2011-11-01 00:00:00

abstract：:Herbert Remmer was a pioneer in the study of the phenomenon of enzyme induction. He was also a leading figure, if not the foremost, in the development of the discipline of toxicology in Germany during his tenure as Professor of Toxicology at the University of Tübingen. Included here are some brief thoughts about where...

journal_title：Drug metabolism reviews

authors： Guengerich FP

更新日期：2004-10-01 00:00:00

abstract：:Nano-hydroxyapatite (nano-HA) is a material with multiple uses due to its biocompatibility and its resemblance to the nonorganic bone structure. It is used in various dental domains such as implantology, surgery, periodontology, esthetics and prevention. The aim of this study is to provide a wide understanding of nano...

journal_title：Drug metabolism reviews

authors： Bordea IR,Candrea S,Alexescu GT,Bran S,Băciuț M,Băciuț G,Lucaciu O,Dinu CM,Todea DA

更新日期：2020-05-01 00:00:00

abstract：:For patients undergoing cardiopulmonary bypass (CPB) during cardiac surgery, there are well-documented changes in the pharmacokinetics (PK) of commonly administered drugs. Although multiple factors potentially underpin these changes, there has been scant research attention on the impact of CPB to alter the activities ...

journal_title：Drug metabolism reviews

authors： Adiraju SKS,Shekar K,Fraser JF,Smith MT,Ghassabian S

更新日期：2018-05-01 00:00:00

abstract：:Ronald Estabrook made his initial impact studying cytochrome P450 by demonstrating the oxidative metabolism function of this unique class of enzymes, which had an unusual spectral peak at 450 nm when reduced and in the presence of carbon monoxide. Utilizing a photochemical action spectrum, he demonstrated that a cytoc...

journal_title：Drug metabolism reviews

authors： Sheets JJ

更新日期：2007-01-01 00:00:00

abstract：:Cytochrome P450 2D6 (CYP2D6) is a polymorphic enzyme responsible for metabolizing approximately 25% of all drugs. CYP2D6 is highly expressed in the brain and plays a role as the major CYP in the metabolism of numerous brain-penetrant drugs, including antipsychotics and antidepressants. CYP2D6 activity and inhibition h...

journal_title：Drug metabolism reviews

authors： Ford KA,Ryslik G,Sodhi J,Halladay J,Diaz D,Dambach D,Masuda M

更新日期：2015-08-01 00:00:00

abstract：:S-carboxymethyl-L-cysteine, the side-chain carboxymethyl derivative of the sulfur-containing amino acid, cysteine, has been known and available for almost 80 years. During this time, it has been put to a variety of uses, but it is within the field of respiratory medicine that, presently, it has found a clinical niche....

journal_title：Drug metabolism reviews

authors： Mitchell SC,Steventon GB

更新日期：2012-05-01 00:00:00

abstract：:The physiological and biochemical measurements that can be performed noninvasively in humans with modern imaging techniques offer great promise for defining the precise state of a patient's disease and its response to therapy. In general, there are two critical points in drug development when PET measurements are like...

journal_title：Drug metabolism reviews

authors： Fischman AJ,Alpert NM,Babich JW,Rubin RH

更新日期：1997-11-01 00:00:00

abstract：:Bupropion is an atypical antidepressant of the aminoketone group, structurally related to cathinone, associated with a wide interindividual variability. An extensive pharmacokinetic and pharmacodynamic review of bupropion was performed, also focusing on chemical, pharmacological, toxicological, clinical and forensic a...

journal_title：Drug metabolism reviews

authors： Costa R,Oliveira NG,Dinis-Oliveira RJ

更新日期：2019-08-01 00:00:00

abstract：:Like any other drugs, antiallergic medications can be associated with large inter- and intraindividual variability in their disposition. The best-documented examples belong to the H1 antihistamines. Variable drugs are more likely to show unpredictable therapeutic response with both increased risks of side effects and ...

journal_title：Drug metabolism reviews

authors： Nicolas JM,Espie P,Molimard M

更新日期：2009-01-01 00:00:00

abstract：:Flavin-containing monooxygenases (FMOs) are important oxidative drug metabolizing enzymes. FMO3 is the primary human adult liver FMO enzyme, but is developmentally regulated. FMO3 promoter characterization using in vitro DNA binding assays with HepG2 cell and fetal and adult liver nuclear protein, as well as FMO3/repo...

journal_title：Drug metabolism reviews

authors： Klick DE,Hines RN

更新日期：2007-01-01 00:00:00

abstract：:Hyperbilirubinemia may accompany harmful effects such as jaundice, brain dysfunction, and pharmacokinetic alterations of drugs. Clinical drugs are the important causes of hyperbilirubinemia, especially for patients with certain pathologic conditions or with genetic variations. This article reviews hyperbilirubinemic p...

journal_title：Drug metabolism reviews

authors： Ah YM,Kim YM,Kim MJ,Choi YH,Park KH,Son IJ,Kim SG

更新日期：2008-01-01 00:00:00

abstract：:The CYP4 family of cytochrome P450 enzymes and the mammalian peroxidases covalently bind their heme groups. In the CYP4 enzymes this involves one, and in the peroxidases two, covalent ester links between heme methys and carboxylic acid side-chains. In addition, in myeloperoxidase, a methionine forms a sulfonium link t...

journal_title：Drug metabolism reviews

authors： Ortiz de Montellano PR

更新日期：2008-01-01 00:00:00

abstract：:Dehydroepiandrosterone has been thought to have physiological functions other than as an androgen precursor. The previous studies performed have demonstrated a number of biological effects in rodents, such as amelioration of disease in diabetic, chemical carcinogenesis, and obesity models. To date, activation of the p...

journal_title：Drug metabolism reviews

authors： Webb SJ,Geoghegan TE,Prough RA,Michael Miller KK

更新日期：2006-01-01 00:00:00

abstract：:At present, the methods and enzymology of the UDP-glucuronosyltransferases (UGTs) lag behind that of the cytochromes P450 (CYPs). About 15 human UGTs have been identified, and knowledge about their regulation, substrate selectivity, and tissue distribution has progressed recently. Alamethicin has been characterized as...

journal_title：Drug metabolism reviews

authors： Fisher MB,Paine MF,Strelevitz TJ,Wrighton SA

更新日期：2001-08-01 00:00:00

abstract：:An association between marijuana use and schizophrenia has been noted for decades, and the recent emergence of high-efficacy synthetic cannabinoids (SCBs) as drugs of abuse has lead to a growing number of clinical reports of persistent psychotic effects in users of these substances. The mechanisms underlying SCB-elici...

journal_title：Drug metabolism reviews

authors： Fantegrossi WE,Wilson CD,Berquist MD

更新日期：2018-02-01 00:00:00

abstract：:Synthetic cannabinoids (SC), originally developed as research tools, are now highly abused novel psychoactive substances. We present a comprehensive systematic review covering in vivo and in vitro animal and human pharmacokinetics and analytical methods for identifying SC and their metabolites in biological matrices. ...

journal_title：Drug metabolism reviews

authors： Castaneto MS,Wohlfarth A,Desrosiers NA,Hartman RL,Gorelick DA,Huestis MA

更新日期：2015-05-01 00:00:00

abstract：:Human cytochrome P450 (CYP) 3A subfamily members (mainly CYP3A4 and CYP3A5) mediate the metabolism of approximately half all marketed drugs and thus play a critical role in the drug metabolism. A huge number of studies on CYP3A-mediated drug metabolism in humans have demonstrated that CYP3A activity exhibits marked et...

journal_title：Drug metabolism reviews

authors： Liu YT,Hao HP,Liu CX,Wang GJ,Xie HG

更新日期：2007-01-01 00:00:00

abstract：:In this paper, we evaluate methodologies and null mouse models used to study drug transporter function in vitro and in vivo. P-glycoprotein and MRP null mice have been used to examine many aspects of xenobiotic distribution and bioavailability. Their advantage over conventional models is that they allow the exclusion ...

journal_title：Drug metabolism reviews

authors： Stanley LA,Horsburgh BC,Ross J,Scheer N,Wolf CR

更新日期：2009-01-01 00:00:00

abstract：:Human tumors arise from multiple genetic changes that gradually transform growth-limited cells into highly invasive cells that are unresponsive to growth controls. The genetic evolution of normal cells into cancer cells is largely determined by the fidelity of DNA replication, repair, and division. Cell-cycle arrest i...

journal_title：Drug metabolism reviews

authors： Flatt PM,Pietenpol JA

更新日期：2000-08-01 00:00:00

abstract：:The aim of this study was to evaluate diazepam and oxazepam as cytochrome P450 inducers at doses previously shown to cause liver tumors in mice but not rats. In rats, diazepam and oxazepam induced CYP2B, and were as effective as phenobarbital despite lacking phenobarbital's tumor-promoting effect in rats. In mice, dia...

journal_title：Drug metabolism reviews

authors： Parkinson A,Leonard N,Draper A,Ogilvie BW

更新日期：2006-01-01 00:00:00

abstract：:Most foreign compounds, including nonnutrients in foods and vapors in air, undergo extensive metabolism before they are eliminated from the body. Included in this paper are discussions of the urinary clearance of various kinds of foreign compounds, the nonspecific enzymes that catalyze the formation of many metabolite...

journal_title：Drug metabolism reviews

authors： Gillette JR

更新日期：1979-01-01 00:00:00

abstract：:The body is considered as a system composed of a number of subsystems. The response(s) of a drug is a complicated function of the concentration in the blood plasma, which in turn is some function of the dosage input. The dose-response curve of a drug in a subsystem (e.g., isolated organ) is, over a limited concentrati...

journal_title：Drug metabolism reviews

authors： van Rossum JM,Burgers JP

更新日期：1984-01-01 00:00:00

abstract：:The present paper has discussed available test systems for determination of the response of G-6-PD-deficient human erythrocytes to environmental agents. The limitations and advantages of each model have been examined, and the results of research using each model have been presented. The future development of suitable ...

journal_title：Drug metabolism reviews

authors： Horton HM,Calabrese EJ

更新日期：1986-01-01 00:00:00

abstract：:The Pharmacogenetics and Pharmacogenomics Knowledge Base (PharmGKB: http://www.pharmgkb.org) is devoted to disseminating primary data and knowledge in pharmacogenetics and pharmacogenomics. We are annotating the genes that are most important for drug response and present this information in the form of Very Important ...

journal_title：Drug metabolism reviews

authors： Sangkuhl K,Berlin DS,Altman RB,Klein TE

更新日期：2008-01-01 00:00:00

abstract：:Enormous efforts toward predicting the metabolic fate of a drug have been driven by the high attrition rate in drug development. To accelerate such efforts, it is critical to elucidate the molecular mechanisms of drug recognition by drug-metabolizing enzymes. Therefore, it is not surprising that an increasing number o...

journal_title：Drug metabolism reviews

authors： Dong D,Wu B

更新日期：2012-02-01 00:00:00

abstract：:Bioconjugation of therapeutic agents has been used as a selective drug delivery platform for many therapeutic areas. Bioconjugates are prepared by the covalent linkage of active compounds (small or large molecule) to a carrier molecule (lipids, proteins, peptides, carbohydrates, and polymers) through a chemical linker...

journal_title：Drug metabolism reviews

authors： Liu H,Bolleddula J,Nichols A,Tang L,Zhao Z,Prakash C

更新日期：2020-02-01 00:00:00