Advances in the development and use of human tissue-based techniques for drug toxicity testing.

abstract：:In adapting to the challenge to make more informed selection of compounds for development, the pharmaceutical industry is increasingly embracing the application of mechanism-based models and prediction tools for prediction of pharmacokinetic parameters. This review first outlines the concepts and application of the ma...

journal_title：Expert opinion on drug metabolism & toxicology

authors： De Buck SS,Mackie CE

更新日期：2007-12-01 00:00:00

abstract：INTRODUCTION:Hemophilia A is a bleeding disorder resulting from a lack of clotting factor VIII (FVIII), and treatment typically consists of prophylactic replacement of the deficient factor. However, high between subject variability precludes the development of a 'one size fits all' dosing strategy and necessitates an i...

journal_title：Expert opinion on drug metabolism & toxicology

authors： McEneny-King A,Iorio A,Foster G,Edginton AN

更新日期：2016-11-01 00:00:00

abstract：INTRODUCTION:. Membrane transporters are integral to the maintenance of cellular integrity of all tissue and cell types. While transporters play an established role in the systemic pharmacokinetics of therapeutic drugs, tissue specific expression of uptake transporters can serve as an initiating mechanism that governs ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Huang KM,Uddin ME,DiGiacomo D,Lustberg MB,Hu S,Sparreboom A

更新日期：2020-06-01 00:00:00

abstract：BACKGROUND:Sertindole is a second-generation antipsychotic recently reintroduced in the market for the treatment of schizophrenia after a reevaluation of its risks and benefits. OBJECTIVE:This article provides an overview of the pharmacological properties of sertindole as well as of its efficacy, tolerability and safe...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Spina E,Zoccali R

更新日期：2008-05-01 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: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

abstract：INTRODUCTION:The absorption, distribution, metabolism, excretion and toxicity (ADME-tox) processes of drugs are of importance and require preclinical investigation intestine in addition to the liver. Various models have been developed for prediction of ADME-tox in the intestine. In this review, precision-cut intestinal...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Li M,de Graaf IA,Groothuis GM

更新日期：2016-01-01 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：:Three first-line antituberculosis drugs, isoniazid, rifampicin and pyrazinamide, may induce liver injury, especially isoniazid. This antituberculosis drug-induced liver injury ranges from a mild to severe form, and the associated mortality cases are not rare. The major drug-metabolizing enzyme of isoniazid is N-acetyl...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Huang YS

更新日期：2007-02-01 00:00:00

abstract：INTRODUCTION:Sepsis remains a leading cause of death worldwide. Despite years of extensive research, effective drugs that inhibit the pro-inflammatory effects of lipopolysaccharide (LPS) and improve outcome when added to conventional sepsis treatments are lacking. Eritoran tetrasodium (E5564) is a promising candidate t...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Barochia A,Solomon S,Cui X,Natanson C,Eichacker PQ

更新日期：2011-04-01 00:00:00

abstract：INTRODUCTION:The pharmacokinetic properties of anti-infective drugs are a determinant part of treatment success. Pathogen replication is inhibited if adequate drug levels are achieved in target sites, whereas excessive drug concentrations linked to toxicity are to be avoided. Anti-infective distribution can be predicte...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Moss DM,Marzolini C,Rajoli RK,Siccardi M

更新日期：2015-01-01 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:Telaprevir is one of the first direct-acting antiviral drugs approved for the treatment of the hepatitis C virus (HCV) genotype 1. Following its approval in 2011, new data regarding the pharmacokinetics and pharmacodynamics were reported, leading to important clinical applications. AREAS COVERED:This arti...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Rivero-Juarez A,Camacho A,Rivero A

更新日期：2015-07-01 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: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：INTRODUCTION:Co-medication, gene polymorphisms and co-morbidity are main causes for high variability in expression and function of the CYP3A isoenzymes. Pharmacokinetic variability is a major source of interindividual variability of drug effect and response of CYP3A substrates. While CYP3A genotyping is of limited use,...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hohmann N,Haefeli WE,Mikus G

更新日期：2016-05-01 00:00:00

abstract：OBJECTIVE:The objectives of this study are to characterize capsaicin glucuronidation using liver microsomes and to determine the contribution of individual UDP-glucuronosyltransferase (UGT) enzymes to hepatic glucuronidation of capsaicin. METHODS:The rates of glucuronidation were determined by incubating capsaicin wit...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Sun H,Wang H,Liu H,Zhang X,Wu B

更新日期：2014-10-01 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:Patients with gout often have comorbid conditions such as renal failure, cardiovascular disease and metabolic syndrome. The presence and required treatment of these conditions can make the treatment of gout challenging. Knowledge of the pharmacokinetics of the available drugs for the management of gout is ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Richette P,Frazier A,Bardin T

更新日期：2014-07-01 00:00:00

abstract：INTRODUCTION:Golimumab is a human anti-TNF monoclonal antibody that was derived from human antibody-transgenic mice. Golimumab demonstrated meaningful clinical benefit and tolerable safety in patients with active rheumatoid arthritis (RA) who were methotrexate (MTX)-naïve, or who inadequately responded to MTX or who ha...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Tanaka Y,Senoo A,Fujii H,Baker D

更新日期：2016-01-01 00:00:00

abstract：INTRODUCTION:Painful diabetic neuropathy (PDN) is a disabling pain condition. Its pathomechanism remains unknown, but a sensitization and neuronal hyperexcitabilty have been suggested. Only symptomatic pharmacological pain management treatment is currently available. AREAS COVERED:The origin of PDN is enigmatic, and t...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Tajti J,Szok D,Majláth Z,Csáti A,Petrovics-Balog A,Vécsei L

更新日期：2016-07-01 00:00:00

abstract：:The human ether-a-go-go-related gene (hERG) encodes the pore-forming alpha-subunit of a voltage-gated potassium (K(+)) channel. A variety of unrelated compounds reduce K(+ )current in the heart by blocking the pore or disrupting trafficking of the hERG channel to the membrane surface. This induces a syndrome known as ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Stansfeld PJ,Sutcliffe MJ,Mitcheson JS

更新日期：2006-02-01 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：:With the progressive ageing of the population, an increasing number of elderly patients are being exposed to multiple drugs because of co-existing morbidity states requiring pharmacological management. However, the knowledge of the effects of ageing on the pharmacokinetics and pharmacodynamics of individual drugs is f...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Mangoni AA

更新日期：2007-06-01 00:00:00

abstract：:Luminogenic cytochrome P450 (CYP) assays couple CYP enzyme activity to firefly luciferase luminescence in a technology called P450-Glo(TM) (Promega). Luminogenic substrates are used in assays of human CYP1A1, -1A2, -1B1, -2C8, -2C9, -2C19, -2D6, -2J2, -3A4, -3A7, -4A11, -4F3B, -4F12 and -19. The assays detect dose-dep...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Cali JJ,Ma D,Sobol M,Simpson DJ,Frackman S,Good TD,Daily WJ,Liu D

更新日期：2006-08-01 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：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: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：INTRODUCTION:Mepolizumab is a humanized monoclonal antibody that binds to and inactivates IL-5. It is available as a subcutaneous preparation. The practical application of mepolizumab is as an add-on therapy in the treatment of severe eosinophilic asthma. Areas covered: This article was created from a comprehensive lit...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Kallur L,Gonzalez-Estrada A,Eidelman F,Dimov V

更新日期：2017-12-01 00:00:00

abstract：:Severe adverse drug reactions (ADRs) are a major problem in drug development and clinical practice and the most common cause of market withdrawals of drugs. Individualised drug safety aims at the prospective identification of single patients who carry genetic predispositions for the development of serious or fatal ADR...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Gut J,Bagatto D

更新日期：2005-10-01 00:00:00