Modifications of human carboxylesterase for improved prodrug activation.

abstract：:Introduction: In quantitative modeling, the resolving of underpredictions and overpredictions of hepatic clearance (CLh) makes a top priority for pharmacokinetic modelers. Clearly, the 'protein-mediated hepatic uptake' is a violation of 'the free drug hypothesis', but the lack of its consideration in CLh-predictive ap...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Bteich M,Poulin P,Haddad S

更新日期：2019-08-01 00:00:00

abstract：INTRODUCTION:Chemoprevention of cancer refers to the use of natural or synthetic compounds to abolish or perturb a variety of steps in tumor initiation, promotion, and progression. This can be realized through different mechanisms, including activation of free radical scavenging enzymes, control of chronic inflammation...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Ismail T,Donati-Zeppa S,Akhtar S,Turrini E,Layla A,Sestili P,Fimognari C

更新日期：2021-01-01 00:00:00

abstract：INTRODUCTION:The key feature of the newborn is its fast age-dependent maturation, resulting in extensive variability in pharmacokinetics and -dynamics, further aggravated by newly emerging covariates like treatment modalities, environmental issues or pharmacogenetics. This makes clinical research in neonates relevant a...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Samardzic J,Turner MA,Bax R,Allegaert K

更新日期：2015-07-01 00:00:00

abstract：INTRODUCTION:Medullary thyroid carcinoma (MTC) is a rare endocrine malignancy accounting for a significant percentage of thyroid cancer-related fatal events. Traditional treatment modalities used in the other types of thyroid carcinomas have been proved largely ineffective in advanced MTC. Better understanding of the m...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Karras S,Anagnostis P,Krassas GE

更新日期：2014-03-01 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: Overactive bladder (OAB) has a heterogeneous presentation that varies between individuals and by gender. Treatment with antimuscarinic medications is standard first line pharmacotherapy for most patients with OAB. However, gender specific differences in the pharmacokinetics and pharmacodynamics of antimu...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hartigan SM,Dmochowski RR

更新日期：2020-02-01 00:00:00

abstract：BACKGROUND:The intestinal epithelial membrane expresses ATP-binding cassette (ABC) transporters such as P-glycoprotein (P-gp), multi-drug resistance-associated proteins (MRPs) and breast cancer resistance protein (BCRP), in addition to various solute carrier (SLC) transporters. These ABC transporters affect the oral bi...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Murakami T,Takano M

更新日期：2008-07-01 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：:Introduction: Although the hepatotoxicity of acetaminophen is a well-known problem, the search for reliable biomarker of toxicity is still a current issue as clinical tools are missing to assess patients intoxicated following chronic use, sequential ingestion, use of modified release formulations or in case of delayed...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Gloor Y,Schvartz D,F Samer C

更新日期：2019-08-01 00:00:00

abstract：INTRODUCTION:Multiple myeloma (MM) patients who relapse, or become refractory to currently available novel agents, have limited treatment options with poor outcomes. The introductions of the newer proteasome inhibitor carfilzomib and the immunomodulatory agent pomalidomide have provided new treatment strategies within ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Gay F,Mina R,Troia R,Bringhen S

更新日期：2013-11-01 00:00:00

abstract：BACKGROUND:The number of patients eligible for cardiovascular therapies in general is forecast to increase substantially in the coming decades. However, the current list of potential future cardiovascular blockbuster drugs is alarmingly short. There is thus a clear need for innovative strategies to increase the efficie...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Jänis MT,Laaksonen R,Oresic M

更新日期：2008-06-01 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:Pregabalin is an alternative compound to SSRIs and SNRIs for the first-line treatment of generalized anxiety disorder (GAD). Areas covered: We describe the pharmacokinetic properties of pregabalin and their implications for the treatment of GAD. A search in the main database sources (Medline, ISI, Web of K...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Buoli M,Caldiroli A,Serati M

更新日期：2017-03-01 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：BACKGROUND:Testosterone replacement therapy in hypogonadal men has been used for > 60 years. The use of testosterone substitution is continuously growing and is given to aging men to improve the quality of life. Because testosterone use is associated with muscle strength enhancing effects, it has become a popular drug ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Schulze JJ,Rane A,Ekström L

更新日期：2009-07-01 00:00:00

abstract：:It has increasingly been recognized that few molecules move across the cell membrane without the assistance of transporter proteins. Large superfamilies of transporter proteins have been identified in every living cell, including microorganisms and mitochondria. This report reviews the role of transporters in physiolo...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Lee EJ,Lean CB,Limenta LM

更新日期：2009-11-01 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:Although naturally occurring peptides have been widely used as drugs, their rapid in vivo degradation by proteolysis and their interactions at multiple receptors are part of the reason for the limitation of their clinical applications. AREAS COVERED:This paper reviews peptide-metabolizing enzymes in the b...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Pernot M,Vanderesse R,Frochot C,Guillemin F,Barberi-Heyob M

更新日期：2011-07-01 00:00:00

abstract：:Introduction: The treatment of psoriasis with conventional topical therapies and disease-modifying anti-rheumatic drugs (DMARDs) is often linked to unsatisfactory outcomes and the risk of serious adverse events. Over the last decades, research advances in understanding the role of tumor necrosis factor alpha (TNF α) a...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Campanati A,Paolinelli M,Diotallevi F,Martina E,Molinelli E,Offidani A

更新日期：2019-11-01 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：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:There are profound changes that take place in drug metabolism enzymes during fetal and postnatal development. These changes may significantly impact drug therapy in children. AREAS COVERED:A combination of focused and comprehensive literature searches using PubMed and reference lists (from inception to 7 ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： de Wildt SN

更新日期：2011-08-01 00:00:00

abstract：:Background: The liver plays a central role in human drug metabolism. To model drug metabolism, the major cell type of the liver, the hepatocyte, is commonly used. Hepatocytes can be derived from human and animal sources, including pluripotent stem cells. Cell-based models have shown promise in modeling human drug expo...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Zhou W,Graham K,Lucendo-Villarin B,Flint O,Hay DC,Bagnaninchi P

更新日期：2019-01-01 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：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:Chronic low back pain (CLBP) is a common and difficult illness to manage. Some individuals with CLBP have pain processing disorders and are also at risk for opioid abuse, misuse; addiction and diversion. Guidelines have been published to guide management; neuromodulation, exercise, mindfulness-based stress...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Davis MP

更新日期：2016-07-01 00:00:00

abstract：INTRODUCTION:Cardiovascular disease is still the leading cause of death worldwide. There are many environmental and genetic factors that play a role in the development of cardiovascular disease. The treatment of cardiovascular disease is beginning to move in the direction of personalized medicine by using biomarkers fr...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Berinstein E,Levy A

更新日期：2017-09-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:The use of the first generation non-nucleoside reverse transcriptase inhibitor efavirenz (EFV) as a component of first-line antiretroviral therapy has been accepted worldwide. EFV is the only antiretroviral agent currently on the market that has been combined with emtricitabine and tenofovir dis...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Rakhmanina NY,van den Anker JN

更新日期：2010-01-01 00:00:00

abstract：INTRODUCTION:Despite initial patient benefit, drug resistance to first-generation EGFR tyrosine kinase inhibitors (TKIs) is inevitable. One of the key mechanisms responsible for the development of acquired drug resistance is the secondary T790M missense mutation in exon 20 of the EGFR kinase domain. Afatinib is an ATP-...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Yap TA,Popat S

更新日期：2013-11-01 00:00:00

abstract：BACKGROUND:5-Aminosalicylate (5-ASA) agents are the mainstay of oral therapy for ulcerative colitis (UC). Balsalazide, a prodrug of 5-ASA, has recently been approved for the treatment of UC. OBJECTIVE:To summarize current data on balsalazide and to discuss its impact on management of UC. METHODS:A systematic review o...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Wiggins JB,Rajapakse R

更新日期：2009-10-01 00:00:00