Screening the receptorome reveals molecular targets responsible for drug-induced side effects: focus on 'fen-phen'.

abstract：INTRODUCTION:Maintaining effective antiretroviral treatment for life is a major problem in both resource-limited and resource-rich countries. Despite the progress observed in paediatric antiretroviral therapy, approximately 12% of children still experience treatment failure due to drug resistance, inadequate dosing and...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Piana C,Danhof M,Della Pasqua O

更新日期：2017-05-01 00:00:00

abstract：INTRODUCTION:The N-acetylation polymorphism has been the subject of comprehensive reviews describing the role of arylamine N-acetyltransferase 2 (NAT2) in the metabolism of numerous aromatic amine and hydrazine drugs. AREAS COVERED:We describe and review data that more clearly defines the effects of NAT2 haplotypes an...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hein DW,Millner LM

更新日期：2021-01-01 00:00:00

abstract：BACKGROUND:CYP enzymes from the CYP2C and CYP2J subfamilies metabolize arachidonic acid in a regiospecific and stereoselective manner to eight epoxyeicosatrienoic acids (EETs). Various EETs have been detected in the liver, as well as in many extrahepatic tissues, and have been implicated in numerous physiological funct...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Kaspera R,Totah RA

更新日期：2009-07-01 00:00:00

abstract：INTRODUCTION:Bioaccessibility is a growing area of research in the field of risk assessment. As polycyclic aromatic hydrocarbons (PAHs) are ubiquitous environmental pollutants, they are the toxicants of focus to establish cancer risks in humans. Orally ingested PAHs also cause toxicity and even affect the pharmacokinet...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Harris KL,Banks LD,Mantey JA,Huderson AC,Ramesh A

更新日期：2013-11-01 00:00:00

abstract：:Introduction: Graft-versus-host disease (GVHD) is the most common complication of hematopoietic stem cell transplantation (HSCT); therefore, the prevention of GVHD is important for a successful treatment. Tacrolimus (Tac), a calcineurin inhibitor, has been widely used for the prophylaxis of GVHD in HSCT recipients. Ar...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Gao Y,Ma J

更新日期：2019-10-01 00:00:00

abstract：INTRODUCTION:Pediatric critical illness and associated alterations in organ function can change drug pharmacokinetics (PK). Extracorporeal membrane oxygenation (ECMO), a life-saving therapy for severe cardiac and/or respiratory failure, causes additional PK alterations that affect drug disposition. AREAS COVERED:The p...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Himebauch AS,Kilbaugh TJ,Zuppa AF

更新日期：2016-10-01 00:00:00

abstract：INTRODUCTION:Integration of targeted therapy and additional chemotherapy options has improved median overall survival (OS) in patients with unresectable metastatic colorectal cancer (mCRC). Cetuximab and panitumumab are examples of targeted therapies, specifically against the epidermal growth factor receptor (EGFR). Th...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Lo L,Patel D,Townsend AR,Price TJ

更新日期：2015-01-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:many promising targeted agents and combination therapies are being investigated for brain cancer. However, the results from recent clinical trials have been disappointing. A better understanding of the disposition of drug in the brain early in drug development would facilitate appropriate channe...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Blakeley J,Portnow J

更新日期：2010-12-01 00:00:00

abstract：INTRODUCTION:Mortality from invasive fungal disease involving the central nervous system (CNS) is excessive. Achieving therapeutic drug concentrations at the site of infection within the CNS is always difficult and its evaluation is complex due to anatomical barriers and variable pathophysiological lesions. Areas cover...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Stott KE,Hope W

更新日期：2018-08-01 00:00:00

abstract：INTRODUCTION:Antiepileptic drugs (AEDs) are widely used for the treatment of epilepsy. However, ∼ 30% of patients do not remain seizure free. It is possible that methylxanthine derivatives (e.g., caffeine and theophylline) may partially account for this outcome. AREAS COVERED:Data on the convulsive activity of methylx...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Chrościńska-Krawczyk M,Radzik I,Miziak B,Czuczwar SJ

更新日期：2014-07-01 00:00:00

abstract：INTRODUCTION:Replacement therapy for FVIII/IX in hemophilia A/B is more than 50 years old following the discovery of cryoprecipitate by Judith Pool in 1964. On-demand therapy and prophylaxis to treat or prevent bleedings is very demanding owing to the short half-life (HL) of factor concentrates (no more than 12-14 h fo...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Morfini M

更新日期：2016-11-01 00:00:00

abstract：:Acute kidney injury is a common condition and is associated with a high mortality rate. It has been recognised that routinely used measures of renal function, such as levels of blood urea nitrogen and serum creatinine, increase significantly only after substantial kidney injury occurs and then with a time delay. Insen...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Vaidya VS,Bonventre JV

更新日期：2006-10-01 00:00:00

abstract：INTRODUCTION:Luteinizing hormone-releasing hormone agonists such as leuprolide acetate (LA) are the most frequently utilized treatment of advanced prostate cancer as the regimen for achieving androgen deprivation therapy (ADT). The efficacy of LA is determined by extent of testosterone (T) suppression in prostate cance...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Crawford ED,Moul JW,Sartor O,Shore ND

更新日期：2015-01-01 00:00:00

abstract：INTRODUCTION:Therapeutic hypothermia is being employed clinically due to its neuro-protective benefits. Both critical illness and therapeutic hypothermia significantly affect drug disposition, potentially contributing to drug-therapy and drug-disease interactions. Currently, there is limited information on the known al...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Zhou J,Poloyac SM

更新日期：2011-07-01 00:00:00

abstract：INTRODUCTION:The fixed-dose combination of three direct-acting antivirals (DAA), namely sofosbuvir, velpatasvir and voxilaprevir is the first pangenotypic, single tablet regimen developed for the treatment of HCV infection. Areas covered: The pharmacokinetics, pharmacodynamics, efficacy and safety of the co-formulation...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Soriano V,Benítez-Gutiérrez L,Arias A,Carrasco I,Barreiro P,Peña JM,de Mendoza C

更新日期：2017-09-01 00:00:00

abstract：INTRODUCTION:Picoplatin was developed as platinum coordination complex to overcome development of resistance, through conjugation to thioles, by the introduction of a methyl-pyridine moiety into the cisplatin parent structure. Pharmacokinetic parameters of the drug, after intravenous and oral application, were studied ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hamilton G

更新日期：2013-10-01 00:00:00

abstract：INTRODUCTION:Cervical cancer is the second-most common malignancy in women worldwide. Cisplatin was introduced as a radiosensitizer in 1999 to improve chances of survival. Tumor cell hypoxia, however, remains a major limiting factor in the treatment of solid tumors with chemotherapy and radiation. There has since been ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Ghatage P,Sabagh H

更新日期：2012-12-01 00:00:00

abstract：INTRODUCTION:Iron overload is an inevitable consequence of transfusion therapy for a variety of underlying anemias. Iron overload, without effective chelation, will lead to significant morbidity and mortality. Deferasirox (Exjade®) is an oral tridentate iron chelator used for reducing iron overload. AREAS COVERED:In a...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Galanello R,Campus S,Origa R

更新日期：2012-01-01 00:00:00

abstract：INTRODUCTION:Extensive within-population variability is the essence of neonatal pharmacology. Despite this, infants remain one of the last therapeutic orphans. Together with additional legal initiatives, tailoring of already available tools (modeling, covariates, pharmacovigilance) may significantly improve pharmacothe...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Allegaert K

更新日期：2014-08-01 00:00:00

abstract：INTRODUCTION:The review aims to discuss effects of vitrectomy on pharmacokinetics of anti-vascular endothelial growth factor (anti-VEGF) agents, and attempt to provide treatment guidance. Areas covered: An Embase search was conducted using the terms 'anti-VEGF', 'pegaptanib', 'ranibizumab', 'bevacizumab', 'aflibercept'...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Edington M,Connolly J,Chong NV

更新日期：2017-12-01 00:00:00

abstract：INTRODUCTION:The blood-brain barrier (BBB) is a selectively permeable micro-vascular unit which prevents many central nervous system (CNS)-targeted compounds from reaching the brain. A significant problem in CNS drug development is the ability to model BBB permeability in a timely, reproducible and cost-effective manne...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Geldenhuys WJ,Allen DD,Bloomquist JR

更新日期：2012-06-01 00:00:00

abstract：INTRODUCTION:Drug-disease interactions include the impact of a drug and a particular disease condition on each other. However, the current practice in addressing drug-disease interaction is unbalanced and mostly limited to how the drug worsens the disease or health condition. AREAS COVERED:Aspirin and gastric ulcer in...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Nwose EU,Yee KC

更新日期：2016-09-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:There are few true international meetings dedicated to covering multiple areas of toxicology. The XII International Congress of Toxicology (IUTOX) held from 19 to 23 July 2010 in Barcelona, Spain is one such meeting. The IUTOX is important as its emphasis is on chemical safety and integrating ap...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Anadón A,Valerio LG Jr

更新日期：2010-11-01 00:00:00

abstract：INTRODUCTION:The second-line treatment of endometriosis-related pain symptoms includes injectable depot formulations of gonadotropin-releasing hormone analogs (GnRH-as). These drugs improve the symptomatology by inducing a hypoestrogenic status and a consequent regression of endometriotic implants. However, GnRH-a may ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Della Corte L,Barra F,Mercorio A,Evangelisti G,Rapisarda AMC,Ferrero S,Bifulco G,Giampaolino P

更新日期：2020-09-01 00:00:00

abstract：BACKGROUND:Carboxylesterases (CEs) are ubiquitous enzymes responsible for the hydrolysis of numerous clinically useful drugs. As ester moieties are frequently included in molecules to improve their water solubility and bioavailability, de facto they become substrates for CEs. OBJECTIVE:In this review, we describe the ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hatfield JM,Wierdl M,Wadkins RM,Potter PM

更新日期：2008-09-01 00:00:00

abstract：INTRODUCTION:Coumadin (R/S-warfarin) is the most widely prescribed oral anticoagulant in the world; nevertheless, its clinical use is complicated by unpredictability in dose requirements to achieve and maintain optimal anticoagulation. Variations in warfarin metabolism among patients contribute to unpredictability in t...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Jones DR,Miller GP

更新日期：2011-07-01 00:00:00

abstract：:The pharmaceutical relevance of proton-coupled peptide transporters is currently under intense investigation in many laboratories. Studies have shown that these membrane proteins, expressed in intestine, kidney, choroid plexus and other tissues, accept many peptidomimetic drugs and prodrugs as substrates. The focus of...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Brandsch M

更新日期：2009-08-01 00:00:00

abstract：INTRODUCTION:Nucleosidic analogs such as pyrimidine and purine derivatives are mainstay in the field of treating cancers, both in adults and in children. All these drugs act as antimetabolite compounds, that is, they interfere with the ability of cancer cells to synthesize the nucleosides or the nucleotides necessary f...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Serdjebi C,Milano G,Ciccolini J

更新日期：2015-05-01 00:00:00

abstract：INTRODUCTION:In preliminary clinical studies, aleglitazar, a new dual PPAR-α-γ agonist, has been demonstrated to improve hyperglycemia and dyslipidemia in patients with type 2 diabetes mellitus. This review will provide up-to-date information on the clinical safety and efficacy of aleglitazar, which is currently under ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Younk LM,Uhl L,Davis SN

更新日期：2011-06-01 00:00:00

abstract：INTRODUCTION:Whereas in the past, (Q)SAR methods have been largely used to support the design of new drugs, in the last few decades, there has been a new interest in its applications for the assessment of drug safety. In particular, the ICH M7 guideline has introduced the concept that (Q)SAR predictions for the Ames mu...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Benigni R,Bassan A,Pavan M

更新日期：2020-08-01 00:00:00