Metabolism of bioconjugate therapeutics: why, when, and how?

abstract：:In summary, we have shown that steroid D-ring, but not steroid A-ring, glucuronide conjugates act at the level of the bile canaliculus to decrease bile-acid-dependent flow, initially; and subsequently, bile-acid-independent flow. These data indicate that glucuronide conjugates are not necessarily inactive; the present...

journal_title：Drug metabolism reviews

authors： Vore M,Montgomery C,Meyers M

更新日期：1983-01-01 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：:Psilocybin and psilocin are controlled substances in many countries. These are the two main hallucinogenic compounds of the "magic mushrooms" and both act as agonists or partial agonists at 5-hydroxytryptamine (5-HT)2A subtype receptors. During the last few years, psilocybin and psilocin have gained therapeutic releva...

journal_title：Drug metabolism reviews

authors： Dinis-Oliveira RJ

更新日期：2017-02-01 00:00:00

abstract：:By inhibiting ACE, captopril blocks the conversion of AI or AII and augments the effects of bradykinin both in vitro and in vivo. In rats, dogs, and monkeys with 2-kidney renal hypertension, orally administered captopril rapidly and markedly reduces blood pressure; this antihypertensive effect apparently occurs via a ...

journal_title：Drug metabolism reviews

authors： Migdalof BH,Antonaccio MJ,McKinstry DN,Singhvi SM,Lan SJ,Egli P,Kripalani KJ

更新日期：1984-01-01 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：:Global statistical data shed light on an alarming trend that every year thousands of people die due to adverse drug reactions as each individual responds in a different way to the same drug. Pharmacogenomics has come up as a promising field in drug development and clinical medication in the past few decades. It has em...

journal_title：Drug metabolism reviews

authors： Chaudhary R,Singh B,Kumar M,Gakhar SK,Saini AK,Parmar VS,Chhillar AK

更新日期：2015-08-01 00:00:00

abstract：:The lung, which is in intimate contact with the external environment, is exposed to a number of toxicants both by virtue of its large surface area and because it receives 100% of the cardiac output. Lung diseases are a major disease entity in the U.S. population ranking third in terms of morbidity and mortality. Despi...

journal_title：Drug metabolism reviews

authors： Buckpitt A,Boland B,Isbell M,Morin D,Shultz M,Baldwin R,Chan K,Karlsson A,Lin C,Taff A,West J,Fanucchi M,Van Winkle L,Plopper C

更新日期：2002-11-01 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：: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：:Glutathione S-transferase P1-1 (GSTP) is one member of the family of GSTs and is ubiquitously expressed in human tissues. The literature is replete with reports of high levels of GSTP linked either with cancer incidence or drug resistance, and yet no entirely cogent explanation for these correlations exists. The catal...

journal_title：Drug metabolism reviews

authors： Tew KD,Townsend DM

更新日期：2011-05-01 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：:The high rate of attrition during drug development and its associated high research and development (R&D) cost have put pressure on pharmaceutical companies to ensure that candidate drugs going to clinical testing have the appropriate quality such that the biological hypothesis could be evaluated. To help achieve this...

journal_title：Drug metabolism reviews

authors： Ballard P,Brassil P,Bui KH,Dolgos H,Petersson C,Tunek A,Webborn PJ

更新日期：2012-08-01 00:00:00

abstract：:Hepatotoxicity is a serious problem during drug development and for the use of many established drugs. For example, acetaminophen overdose is currently the most frequent cause of acute liver failure in the United States and Great Britain. Evaluation of the mechanisms of drug-induced liver injury indicates that mitocho...

journal_title：Drug metabolism reviews

authors： Jaeschke H,McGill MR,Ramachandran A

更新日期：2012-02-01 00:00:00

abstract：:Mineral fibers, including asbestos, are ubiquitous contaminants of the environment. Asbestos fibers are generally present at levels below 1 fiber/L in air though 10 fibers/L may be found in cities; these levels do not appear to be high enough to present a hazard to health. These fibers come mostly from the use of fibr...

journal_title：Drug metabolism reviews

authors： Hoskins JA,Brown RC

更新日期：1994-01-01 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：:Drug transporters and drug metabolism enzymes govern drug absorption, distribution, metabolism and elimination. Many literature works presenting important aspects related to stereochemistry of drug metabolism are available. However, there is very little literature on stereoselectivity of chiral drug transport and enan...

journal_title：Drug metabolism reviews

authors： Zhou Q,Yu LS,Zeng S

更新日期：2014-08-01 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：: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：: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：:The reabsorptive and excretory capacity of the kidney has an important influence on the systemic concentration of drugs. Multidrug resistance proteins (MRP/ABCC) expressed in the kidney play a critical role in the tubular efflux of a wide variety of drugs and toxicants, and, in particular, of their negatively charged ...

journal_title：Drug metabolism reviews

authors： van de Water FM,Masereeuw R,Russel FG

更新日期：2005-01-01 00:00:00

abstract：:In summary, the concerns that environmental and other agents are causing adverse effects on reproductive function in humans are real, although the risk is not necessarily well characterized. The range of concerns for the types of effect that agents might have on reproduction span the full range of reproductive events....

journal_title：Drug metabolism reviews

authors： Schwetz BA

更新日期：1996-02-01 00:00:00

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 multiple functions of NAD(P)H:quinone oxidoreductase 1 (NQO1, DT-diaphorase) in the cell are reviewed. NQO1 has long been viewed as a chemoprotective enzyme involved in cellular defense against the electrophilic and oxidizing metabolites of xenobiotic quinones. It also participates in reduction of endogenous quino...

journal_title：Drug metabolism reviews

authors： Ross D

更新日期：2004-10-01 00:00:00

abstract：:N-acetyltransferase 1 (NAT1), a polymorphic Phase II enzyme, plays an essential role in metabolizing heterocyclic and aromatic amines, which are implicated in urinary bladder cancer (BCa). This systematic review investigates a possible association between the different NAT1 genetic polymorphisms and BCa risk. Medline,...

journal_title：Drug metabolism reviews

authors： Dhaini HR,El Hafi B,Khamis AM

更新日期：2018-05-01 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：:Indirect evidence for the participation of cytochrome P450 (P450) in the microsomal N-oxygenation of primary and N-substituted amine functions is presented by studies employing diagnostic modifiers of the hemoprotein system as well as immunochemical approaches. Experiments with recombinant hemoproteins or isozymes pur...

journal_title：Drug metabolism reviews

authors： Hlavica P

更新日期：2002-08-01 00:00:00

abstract：:Acetaminophen (APAP, paracetamol, N-acetyl-p-aminophenol) is a widely used analgesic that is safe at therapeutic doses but is a major cause of acute liver failure (ALF) following overdose. APAP-induced hepatotoxicity is related to the formation of an electrophilic reactive metabolite, N-acetyl-p-benzoquinone imine (NA...

journal_title：Drug metabolism reviews

authors： Coen M

更新日期：2015-02-01 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：:Traditional Chinese medicine (TCM) has a long history of medical use in China and is still used worldwide. Unexpected herb-drug interactions (HDIs) may lead to adverse drug reactions or loss of therapeutic efficacy of the victim drug. Here, based on searches of Medline, EBSCO, Science Direct and Web of Science using v...

journal_title：Drug metabolism reviews

authors： Ma BL,Ma YM

更新日期：2016-01-01 00:00:00

abstract：:The recent progresses in molecular biology and pharmacology approaches allowed the characterization of a series of nuclear receptors (NRs) as efficient regulators of uridine diphosphate glucuronosyltransferase (UGT) genes activity. These regulatory processes ensure an optimized UGT expression in response to specific e...

journal_title：Drug metabolism reviews

authors： Bigo C,Caron S,Dallaire-Théroux A,Barbier O

更新日期：2013-02-01 00:00:00