In vivo antidiabetic drug discovery.

abstract：BACKGROUND:Despite exciting progress and growth in the understanding of molecular and cellular mechanisms of chronic pain, osteoarthritis (OA) pain remains a challenging clinical entity to treat. There is an emerging diversity of algogenic mechanisms suggesting heterogeneity in pain aetiology in the OA patient populati...

journal_title：Expert opinion on investigational drugs

authors： Read SJ,Dray A

更新日期：2008-05-01 00:00:00

abstract：INTRODUCTION:Rheumatoid arthritis (RA) is a chronic inflammatory auto-immune disease that can lead to permanent disability and deformity. Despite current treatment modalities, many patients are still unable to reach remission. Interleukin-1 receptor-associated kinase 4 (IRAK-4) inhibitors are novel agents designed to s...

journal_title：Expert opinion on investigational drugs

authors： Wiese MD,Manning-Bennett AT,Abuhelwa AY

更新日期：2020-05-01 00:00:00

abstract：:The focus of this meeting was the interface between eating disorders and obesity. A symposium at this meeting dealt with advances in treatment for bulimia nervosa (BN) and binge eating disorder. There were two presentations in this symposium that addressed pharmacological treatments. One reviewed drug treatments for B...

journal_title：Expert opinion on investigational drugs

authors： Kaplan AS

更新日期：2003-08-01 00:00:00

abstract：:The discovery of peroxisome proliferator-activated receptor gamma (PPARgamma) as the molecular target for antidiabetic thiazolidinediones has heralded a new era in the approach to understanding the pathophysiology of insulin resistance and its relationship to cardiovascular disease. However, the subsequent discovery o...

journal_title：Expert opinion on investigational drugs

authors： Pershadsingh HA

更新日期：1999-11-01 00:00:00

abstract：:Leukotriene B(4) (LTB(4)) is a lipid inflammatory mediator derived from membrane phospholipids by the sequential actions of cytosolic phospholipase A2 (PLA2), 5-lipoxygenase (5-LO) and leukotriene A(4) (LTA(4)) hydrolase. Several inflammatory diseases, including asthma, chronic obstructive pulmonary disease, arthritis...

journal_title：Expert opinion on investigational drugs

authors： Hicks A,Monkarsh SP,Hoffman AF,Goodnow R Jr

更新日期：2007-12-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Antiangiogenic strategies are affording considerable interest and have become a major milestone in therapeutics of various adult cancers. However, progress has been slow to expand such therapies to patients with pediatric solid malignancies. AREAS COVERED IN THIS REVIEW:This review discusses th...

journal_title：Expert opinion on investigational drugs

authors： Taylor M,Rössler J,Geoerger B,Vassal G,Farace F

更新日期：2010-07-01 00:00:00

abstract：:Neural cell transplantation is an emerging therapy that may provide an effective treatment for neurodegenerative disorders. The most extensive work with neural transplants has been carried out for Parkinson's and Huntington's diseases. However, intensive efforts are also being made for the treatment of other neurologi...

journal_title：Expert opinion on investigational drugs

authors： Dinsmore JH

更新日期：1998-04-01 00:00:00

abstract：INTRODUCTION:Posttraumatic stress disorder (PTSD) is a prevalent, chronic and disabling anxiety disorder that may develop following exposure to a traumatic event. There is currently no effective pharmacotherapy for PTSD and therefore the discovery of novel, evidence-based treatments is particularly important. This revi...

journal_title：Expert opinion on investigational drugs

authors： Ragen BJ,Seidel J,Chollak C,Pietrzak RH,Neumeister A

更新日期：2015-05-01 00:00:00

abstract：:Cyclooxygenase-2 (COX-2) is constitutively expressed in the central nervous system, and is thought to have an important functional role therein. COX-2 interacts with neurotransmitters such as acetylcholine, 5-hydroxytryptamine and glutamate but is also involved in the regulation of the central nervous system immune sy...

journal_title：Expert opinion on investigational drugs

authors： Müller N,Strassnig M,Schwarz MJ,Ulmschneider M,Riedel M

更新日期：2004-08-01 00:00:00

abstract：:TNP-470, an analogue of fumagillin, has been shown to inhibit angiogenesis in vitro and in vivo. In 1992, TNP-470 entered clinical development for cancer as an anti-angiogenic agent. It is currently in Phase I/II trials in Kaposi's sarcoma, renal cell carcinoma, brain cancer, breast cancer, cervical cancer and prostat...

journal_title：Expert opinion on investigational drugs

authors： Kruger EA,Figg WD

更新日期：2000-06-01 00:00:00

abstract：:Liver targeted therapy is designed to deliver a substance preferentially to the organ in order to increase the accumulation, improve the therapeutic effect and reduce toxicity to other organs. The aim of selective targeting is to deliver a substance to a specific cell type in the liver. A variety of vehicles have been...

journal_title：Expert opinion on investigational drugs

authors： Wu J,Wu GY,Zern MA

更新日期：1998-11-01 00:00:00

abstract：INTRODUCTION:Sorafenib is an oral multikinase inhibitor with anti-angiogenic and anti-proliferative activity that is indicated for use in hepatocellular and renal cell carcinomas. Sorafenib is being developed in a number of solid tumors, including breast cancer (BC). AREAS COVERED:A series of four randomized, double-b...

journal_title：Expert opinion on investigational drugs

authors： Gradishar WJ

更新日期：2012-08-01 00:00:00

abstract：INTRODUCTION:IL-6 is a key cytokine in the pathogenesis of rheumatoid arthritis (RA). The clinical efficacy of tocilizumab (TCZ), a humanized anti-IL6-receptor mAb, confirmed the value of IL-6 blockade in this disease. A number of new anti-IL-6 biologics are currently in Phase I - III of clinical development for RA. A...

journal_title：Expert opinion on investigational drugs

authors： Semerano L,Thiolat A,Minichiello E,Clavel G,Bessis N,Boissier MC

更新日期：2014-07-01 00:00:00

abstract：:Two methods of using tumour located enzymes have been described. These are antibody directed enzyme prodrug therapy (ADEPT) and macromolecule directed enzyme prodrug therapy (MDEPT), where the tumour located enzyme converts a non-toxic prodrug into a cytotoxic drug at tumour sites. The alternative use of tumour locate...

journal_title：Expert opinion on investigational drugs

authors： Bagshawe KD,Burke PJ,Knox RJ,Melton RG,Sharma SK

更新日期：1999-02-01 00:00:00

abstract：:AGI-1067 is a derivative of probucol that is a promising new development for the treatment of restenosis and possibly atherosclerosis. In monkeys fed a high-fat diet for 1 year, AGI-1067 prevented the development of atherosclerosis. In these monkeys, AGI-1067 lowered plasma levels of low-density lipoprotein (LDL)-chol...

journal_title：Expert opinion on investigational drugs

authors： Doggrell SA

更新日期：2003-11-01 00:00:00

abstract：:Therapeutic angiogenesis is a novel approach to the treatment of ischaemic or occlusive coronary and peripheral vascular disease. The therapeutic concept is based on the restoration of distal blood flow by the enlargement of existing vessels and tissue perfusion by the induction of new capillaries. Initial studies hav...

journal_title：Expert opinion on investigational drugs

authors： Tarzami ST,Singh JP

更新日期：2004-10-01 00:00:00

abstract：:It is now widely accepted that the renin-angiotensin system (RAS) not only contributes to pathological mechanisms involved, e.g. in hypertension or hypertensive and diabetic end-organ damage, but also harbors a "protective arm" represented mainly by two receptors, the AT2 (angiotensin type 2) receptor and the Mas rece...

journal_title：Expert opinion on investigational drugs

authors： Steckelings UM,Unger T

更新日期：2012-06-01 00:00:00

abstract：BACKGROUND:Histone deacetylases (HDACs), which target histones as well as non-histone proteins as substrates, have the potential to regulate aberrant gene expression and restore normal growth control in malignancies. OBJECTIVE:This review provides an updated summary of preclinical and clinical experience with the oral...

journal_title：Expert opinion on investigational drugs

authors： Le Tourneau C,Siu LL

更新日期：2008-08-01 00:00:00

abstract：:Since the introduction of the first through the skin (TTS) therapeutic in 1980, a total of 34 TTS products have been marketed and numerous drugs have been tested by more than 50 commercial organisations for their suitability for TTS delivery. Most of the agents which have been tested have had low molecular weights, du...

journal_title：Expert opinion on investigational drugs

authors： Cevc G

更新日期：1997-12-01 00:00:00

abstract：BACKGROUND:The hypereosinophilic syndrome (HES) comprises a heterogeneous group of disorders characterized by chronic, unexplained hypereosinophilia with organ involvement. The discovery of novel molecular targets has changed the therapeutic paradigm in HES. OBJECTIVE:This article reviews the current medical managemen...

journal_title：Expert opinion on investigational drugs

authors： Quintás-Cardama A,Cortes J

更新日期：2008-07-01 00:00:00

abstract：:Type 2 diabetes is a chronic metabolic disease that adversely affects both the quality and longevity of life. The disease is characterised by elevated blood glucose (hyperglycaemia) that is associated with microvascular complications and increased macrovascular risk. Existing oral agents, either alone or in combinatio...

journal_title：Expert opinion on investigational drugs

authors： Coghlan M,Leighton B

更新日期：2008-02-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Aspirin, an irreversible inhibitor of thromboxane A(2) production, in combination with clopidogrel, an inhibitor of PY(12) ADP platelet receptors, represents the current standard-of-care of antiplatelet therapy for patients with acute coronary syndrome and those undergoing percutaneous coronary ...

journal_title：Expert opinion on investigational drugs

authors： Tomasello SD,Angiolillo DJ,Goto S

更新日期：2010-12-01 00:00:00

abstract：:Introduction: The armamentarium of antileishmanial drugs is small. It is further being threatened by the development of resistance and decreasing sensitivity to the available drugs. The development of newer drugs is sorely needed. Areas covered: The authors have based their review on a literature search performed usin...

journal_title：Expert opinion on investigational drugs

authors： Sundar S,Chakravarty J

更新日期：2015-01-01 00:00:00

abstract：INTRODUCTION:Glioblastoma is a primary brain tumor with a poor prognosis despite multimodal therapy including surgery, radiotherapy and alkylating chemotherapy. Novel therapeutic options are therefore urgently needed; however, there have been various drug failures in late-stage clinical development. The proteasome repr...

journal_title：Expert opinion on investigational drugs

authors： Roth P,Mason WP,Richardson PG,Weller M

更新日期：2020-10-01 00:00:00

abstract：:Introduction: Therapeutic oligonucleotides have emerged as a promising new class of drug that could silence undruggable targets; they can potentially treat metabolic liver diseases such as nonalcoholic fatty liver disease (NAFLD), hereditary hemochromatosis and alpha 1 antitrypsin deficiency. Areas covered: This artic...

journal_title：Expert opinion on investigational drugs

authors： Alkhouri N,Gawrieh S

更新日期：2021-01-29 00:00:00

abstract：BACKGROUND:In the past years the bone seeking radiopharmaceutical samarium lexidronam ((153)Sm-EDTMP) has been increasingly used alone or in conjunction with chemotherapy and/or bisphosphonates for the treatment of painful bone metastasis. OBJECTIVE:Its use has been explored in different solid tumours. In this report ...

journal_title：Expert opinion on investigational drugs

authors： Abruzzese E,Iuliano F,Trawinska MM,Di Maio M

更新日期：2008-09-01 00:00:00

abstract：:Sitagliptin is a once-daily, orally active, competitive and fully reversible inhibitor of dipeptidyl peptidase 4, the enzyme that is responsible for the rapid degradation of the incretin hormone glucagon-like peptide-1. It is the first in this new class of antihyperglycaemic agents to gain regulatory approval for the ...

journal_title：Expert opinion on investigational drugs

authors： Deacon CF

更新日期：2007-04-01 00:00:00

abstract：:This review highlights some important advances that have taken place in cannabinoid research over the last four years. It focuses on novel ligands that are of interest either as experimental tools or as lead compounds for therapeutic agents and possible clinical applications for some of these ligands. The molecular ta...

journal_title：Expert opinion on investigational drugs

authors： Pertwee RG

更新日期：2000-07-01 00:00:00

abstract：:The main cause of illness and death after the first year of heart transplantation is vasculopathy of the cardiac allograft, probably initiated by early immunological and non-immunological endothelial damage. The incidence of multiple episodes of grade 3A rejection 6 months after primary heart transplantation was lower...

journal_title：Expert opinion on investigational drugs

authors： Doggrell SA

更新日期：2004-02-01 00:00:00

abstract：:Fatty acid synthase (FASN) is the enzyme that catalyzes the de novo synthesis of fatty acids in cells. Because of the strong expression in many cancers, FASN is an attractive and tractable target for therapeutic intervention. The discovery and development of pharmacologic agents that block FASN activity highlight the ...

journal_title：Expert opinion on investigational drugs

authors： Kridel SJ,Lowther WT,Pemble CW 4th

更新日期：2007-11-01 00:00:00