Efavirenz in the therapy of HIV infection.

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：:Rats are an important tool in pharmacology and toxicology. The authors focus on rat P450s in relation to diazepam metabolism. In particular, considerable attention is devoted to the CYP2D subfamily, which is a group of highly polymorphic enzymes. First, the metabolic profiles of diazepam of humans and other animals ar...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Sakai N,Ishizuka M

更新日期：2009-11-01 00:00:00

abstract：INTRODUCTION:Assessments of the pharmacokinetic/pharmacodynamic (PK/PD) characteristics are an integral part in the development of novel therapeutic agents. Compared with traditional small molecule drugs, therapeutic proteins possess many distinct PK/PD features that necessitate the application of modified or separate ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Diao L,Meibohm B

更新日期：2015-07-01 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：:Psychiatric disorders are a leading cause of disability worldwide and despite significant pharmacologic advances, often remain difficult to diagnose correctly and treat fully. Factors which contribute to these difficulties include imprecise understanding of etiology, syndromal nature of many disorders and overlap in d...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Lombard J,Doraiswamy PM

更新日期：2013-01-01 00:00:00

abstract：:Toxicogenomics is the application of gene expression profiling technology to toxicology. This results in the generation of very large and complex gene expression data sets associated with the development of toxicities. It is widely assumed that this data can be deconvoluted to reveal novel insights into toxicological ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Huby R,Tugwood JD

更新日期：2005-08-01 00:00:00

abstract：INTRODUCTION:Sesamin is a major lignan found in sesame and is known to have various biological effects. Some of these biological effects occur following its metabolic conversion to corresponding catechols and, therefore, the study of sesamin metabolism is quite important. There is currently a need to identify the enzym...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Yasuda K,Sakaki T

更新日期：2012-01-01 00:00:00

abstract：BACKGROUND:Anticancer drugs are characterized by a narrow therapeutic window and significant inter-patient variability in therapeutic and toxic effects. Current body surface area (BSA)-based dosing fails to standardize systemic anticancer drug exposure and other alternative dosing strategies also have their limitations...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Gao B,Klumpen HJ,Gurney H

更新日期：2008-10-01 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:. 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：INTRODUCTION:Chronic constipation is a frequent condition often treated pharmacologically. The laxatives available belong to very different pharmacologic groups. AREAS COVERED:This is a short but comprehensive review of the pharmacology, efficacy and safety of currently available laxatives for chronic constipation. Pe...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Müller-Lissner S

更新日期：2013-04-01 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: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：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:A growing body of evidence suggests that everolimus might offer effective immunosuppressive activity together with antiproliferative effects that may address some of the unmet needs in the long-term therapeutic management of the post-transplant patient. OBJECTIVE:To summarize the emerging evidence for emplo...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Sánchez-Fructuoso AI

更新日期：2008-06-01 00:00:00

abstract：OBJECTIVE:To investigate the metabolic routes and metabolites of myricitrin, an important active ingredient of traditional herbal medicine, yielded by the isolated human intestinal bacteria, which have not been reported previously. METHODS:Fresh human fecal samples were collected from a healthy female volunteer and ab...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Du LY,Zhao M,Xu J,Qian DW,Jiang S,Shang EX,Guo JM,Liu P,Su SL,Duan JA,Leng XJ

更新日期：2014-07-01 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: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:Peripheral T-cell lymphomas (PTCLs) are a heterogeneous group of T-cell neoplasms. Most patients with PTCL have a poor outcome with conventional therapies and are not cured without stem-cell transplantation. Pralatrexate, a novel antifolate chemotherapeutic agent, was rationally designed to impede folate m...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Foss FM

更新日期：2011-09-01 00:00:00

abstract：INTRODUCTION:Arterial and venous thrombotic states, including myocardial infarction (MI), stroke and deep vein thrombosis with subsequent pulmonary embolism, are a significant cause of cardiovascular mortality and morbidity. Factor Xa (FXa) plays a pivotal role in thrombus formation. Its inhibition following acute coro...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Gopalakrishnan L,Kumar V,Kohli P,Singh P,Rastogi U,Gibson CM

更新日期：2012-07-01 00:00:00

abstract：INTRODUCTION:Oral mucositis, one of the major side effects of chemotherapy and irradiation, is still a burden of modern oncology. The keratinocyte growth factor (KGF) palifermin has been approved as a new, targeted therapy for the prevention of severe oral mucositis. AREAS COVERED:The authors review the literature on ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Weigelt C,Haas R,Kobbe G

更新日期：2011-04-01 00:00:00

abstract：BACKGROUND:The activity of various CYP isoforms is critical for maintaining the clinical effectiveness of many medications. Therefore, determining the sex-dependent activity of clinically relevant CYP families is highly important for optimal therapeutic effectiveness. OBJECTIVE:This review examined the sex-dependent a...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Scandlyn MJ,Stuart EC,Rosengren RJ

更新日期：2008-04-01 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：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: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:Drug-induced cholestasis, intrahepatic cholestasis of pregnancy and viral hepatitis are acquired forms of liver disease. Cholestasis is a pathophysiologic state with impaired bile formation and subsequent accumulation of bile salts in hepatocytes. The bile salt export pump (BSEP) (ABCB11) is the key export...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Stieger B,Geier A

更新日期：2011-04-01 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：: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

abstract：:Changes in mammalian diets alter the hepatic expression of CYP drug-metabolising enzymes and endobiotic oxidases. Thus, dietary constituents may significantly influence the duration of action of chemicals in tissues. Recent improvements in the mechanistic information on the regulation of constitutive and inducible exp...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Murray M

更新日期：2007-04-01 00:00:00

abstract：INTRODUCTION:Dosing of antibiotics in people with cystic fibrosis (CF) is challenging, due to altered pharmacokinetics, difficulty of lung tissue penetration, and increasing presence of antimicrobial resistance. AREAS COVERED:The purpose of this work is to critically review original data as well as previous reviews an...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Akkerman-Nijland AM,Akkerman OW,Grasmeijer F,Hagedoorn P,Frijlink HW,Rottier BL,Koppelman GH,Touw DJ

更新日期：2021-01-01 00:00:00