Bioaccessibility of polycyclic aromatic hydrocarbons: relevance to toxicity and carcinogenesis.

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:Immunosuppressive drugs have a narrow therapeutic range and large inter-individual response variability. This has prompted pharmacogenetic studies, mostly with regard to their dose-concentration relationships, but also about proteins involved in their pharmacodynamics. Some polymorphisms of genes involved ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Picard N,Marquet P

更新日期：2011-06-01 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:Obesity is an epidemic associated with significant morbidity. Lorcaserin , a novel serotonin 2C receptor antagonist, was recently approved as an adjunct to lifestyle modification for long-term weight loss and maintenance. Clinical studies in patients without diabetes demonstrated 5.8% mean weight loss from...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Berlie HD,Hurren KM

更新日期：2013-08-01 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:This meeting report presents a brief summary on the 4th Annual Predictive Toxicology Summit 2012, which was held on 15 - 16 February 2012 in London. AREAS COVERED:The majority of presentations came from global pharmaceutical companies, although small and medium enterprise (SME) and academic researchers we...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Cui Z

更新日期：2013-08-01 00:00:00

abstract：INTRODUCTION:Treatments for hepatitis C virus (HCV) infection have advanced rapidly in the last decade. Pegylated interferon alpha 2a (PEG-IFN alpha 2a) alone, in combination with ribavirin and with or without direct acting antivirals (DAAs) is modestly effective in the treatment of chronic HCV infection. Areas covered...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Maughan A,Ogbuagu O

更新日期：2018-02-01 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：INTRODUCTION:Capecitabine , an oral prodrug of 5-fluorouracil (5-FU), is adsorbed in its intact form through the intestine and metabolized to 5-FU in tumour cells. In metastatic breast cancer (MBC), capecitabine is an effective and well-tolerated therapeutic option both in monotherapy and in combination with chemothera...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Daniele G,Gallo M,Piccirillo MC,Giordano P,D'Alessio A,Del Giudice A,La Porta ML,Perrone F,Normanno N,De Luca A

更新日期：2013-02-01 00:00:00

abstract：:Introduction: The target concentration strategy uses PKPD information for dose determination. Models have also quantified exposure-response relationships, improved understanding of developmental pharmacokinetics, rationalized dose prescription, provided insight into the importance of covariate information, explained d...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Anderson BJ,Morse JD,Hannam JA,Cortinez LI

更新日期：2020-04-01 00:00:00

abstract：INTRODUCTION:Small molecule tyrosine and serine-threonine kinase inhibitors (TKIs and STKIs) are emerging drugs that interfere with downstream signaling pathways involved in cancer proliferation, invasion, metastasis and angiogenesis. The understanding of their pharmacokinetics, the identification of their transporters...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Da Silva CG,Honeywell RJ,Dekker H,Peters GJ

更新日期：2015-05-01 00:00:00

abstract：:The in vitro pharmacological profiling of drugs using a large panel of cloned receptors (e.g., G protein-coupled receptors, ligand-gated ion channels, Na(+)-dependent monoamine transporters), an approach that has come to be known as 'receptorome screening', has unveiled novel molecular mechanisms responsible for the a...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Setola V,Roth BL

更新日期：2005-10-01 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:Within recent years, glucagon-like peptide 1 receptor agonists (GLP-1-RA) have emerged as a new treatment option for type 2 diabetes. The GLP-1-RA are administered subcutaneously and differ substantially in pharmacokinetic profiles. AREAS COVERED:This review describes the pharmacokinetics and safety aspec...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Jespersen MJ,Knop FK,Christensen M

更新日期：2013-01-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:genetic and pharmacologically-driven variations in common mechanisms involved in the disposition of antidepressant medications may contribute to variable interpatient response. This review describes the pharmacological properties underlying the safety and efficacy of desvenlafaxine, a second-gen...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Nichols AI,Tourian KA,Tse SY,Paul J

更新日期：2010-12-01 00:00:00

abstract：INTRODUCTION:First- and second-generation epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs), such as gefitinib, erlotinib, icotinib, and afatinib are the standard-of-care for first-line therapy of non-small-cell lung cancer (NSCLC) harboring activating EGFR mutations. Unfortunately, after initial ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Rossi A,Muscarella LA,Di Micco C,Carbonelli C,D'alessandro V,Notarangelo S,Palomba G,Sanpaolo G,Taurchini M,Graziano P,Maiello E

更新日期：2017-12-01 00:00:00

abstract：:Irritable bowel syndrome (IBS) is a chronic disease characterized by complex interactions between genetic predisposition and the environment. Current treatments for IBS are characterized by a highly variable response. Gene variations may result from insertions or deletions, gene rearrangements, splice variants or copy...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Acosta A,Camilleri M

更新日期：2015-01-01 00:00:00

abstract：INTRODUCTION:Mathematical models of dermal transport offer the advantages of being much faster and less expensive than in vitro or in vivo studies. The number of methods used to create such models has been increasing rapidly, probably due to the steady rise in computational power. Although each of the various approache...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Selzer D,Neumann D,Schaefer UF

更新日期：2015-01-01 00:00:00

abstract：INTRODUCTION:Pharmacokinetic and pharmacodynamic drug interactions (DIs) can occur between antiepileptics (AEDs) and second-generation antipsychotics (SGAPs). Some AED and SGAP pharmacodynamic mechanisms are poorly understood. AED-SGAP combinations are used for treating comorbid illnesses or increasing efficacy, partic...

journal_title：Expert opinion on drug metabolism & toxicology

authors： de Leon J,Santoro V,D'Arrigo C,Spina E

更新日期：2012-03-01 00:00:00

abstract：INTRODUCTION:Variations in the human genome sequence sometimes play an important role in pharmacokinetics and/or pharmacodynamics. Previous studies have demonstrated a high degree of variation both between and within different ethnic populations. Areas covered: This review sought to summarize key SNPs in CYP2B6, CYP3A ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Neary M,Owen A

更新日期：2017-11-01 00:00:00

abstract：INTRODUCTION:Catechins of green tea extract (GTE) have been associated with the rare risk of hepatotoxicity in a few individuals. As GTE were coadministered with synthetic drugs in some hepatotoxicity cases, uncertainty emerged whether GTE are a risk factor of drug-induced liver injury (DILI). AREAS COVERED:Case repor...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Teschke R,Zhang L,Melzer L,Schulze J,Eickhoff A

更新日期：2014-12-01 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:It is widely accepted that current practice of polypharmacy inevitably increases the incidence of drug-drug interactions (DDIs). Serious DDIs are a major liability for new molecular entities entering the pharmaceutical market. Various strategies are employed to avoid problematic compounds for clinical deve...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Riley RJ,Wilson CE

更新日期：2015-04-01 00:00:00

abstract：INTRODUCTION:Neonatal patients, because of the inability of their immune system to properly respond to microbial challenge, are highly susceptible to viral infections. Immunoglobulins, monoclonal antibody and antiviral drugs are used for prophylaxis and treatment of viral diseases in neonates. Neonates and, especially,...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Enioutina EY,Constance JE,Stockmann C,Linakis MW,Yu T,Rower JE,Balch AH,Sherwin CM

更新日期：2015-01-01 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：INTRODUCTION:For orally administered drugs, their intestinal absorption and hepatic metabolism are key players for determining a drug's systemic bioavailability and thus therapeutic effect. Drug absorption and metabolism are both complicated processes, with many physicochemical and physiological factors involved. Under...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Alqahtani S,Mohamed LA,Kaddoumi A

更新日期：2013-10-01 00:00:00

abstract：INTRODUCTION:The prevalence of obesity and associated co-morbid conditions is increasing globally. Physiological changes accompanying obesity are likely to result in altered drug pharmacokinetics; however, there is paucity of information on how to best dose adjust for the obese. AREAS COVERED:This review presents mate...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Morrish GA,Pai MP,Green B

更新日期：2011-06-01 00:00:00

abstract：:There is an increasing recognition within the pharmaceutical industry of the importance of the ADME studies in drug registration. Consequently, there has been a drive in recent times to conduct the ADME studies as early as possible in the development programme. There are, however, regulatory barriers, particularly in ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Lappin G,Garner RC

更新日期：2005-06-01 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：INTRODUCTION:Over the past decade, zebrafish have been tasked to play important roles from modeling human diseases to finding cures for them. Inadvertently, these fish now find themselves swimming along the drug development pipeline. A number of studies have been conducted to see if these small fish are up to the task ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Sukardi H,Chng HT,Chan EC,Gong Z,Lam SH

更新日期：2011-05-01 00:00:00