Investigational PPAR-gamma agonists for the treatment of Type 2 diabetes.

Abstract:

:The tremendous increase in the global prevalence of Type 2 diabetes (T2D) and its conglomeration of metabolic disorders has dramatically intensified the search for innovative therapies to fight this emerging epidemic. Over the last decade, the family of nuclear receptors, especially the peroxisome proliferator-activated receptors (PPARs), has emerged as one of the most important drug targets aimed at combating the metabolic syndrome. Consequently, compounds that activate the PPARs have served as potential therapeutics for the treatment of T2D and the metabolic anomalies associated with this disorder. This review focuses on the currently marketed compounds and also describes the discovery and development of the next generation of PPAR ligands that are under investigation for the potential treatment of T2D and the metabolic syndrome.

authors

Savkur RS,Miller AR

doi

10.1517/13543784.15.7.763

subject

Has Abstract

pub_date

2006-07-01 00:00:00

pages

763-78

issue

7

eissn

1354-3784

issn

1744-7658

journal_volume

15

pub_type

杂志文章,评审
  • Glutamatergic fine tuning with ADX-10059: a novel therapeutic approach for migraine?

    abstract:IMPORTANCE OF THE FIELD:Migraine is an episodic, substantially inherited brain disorder affecting 15% of adults in Western Europe and North America, and is one of the commonest reasons for patients to see their physicians. While the World Health Organization considers that severe migraine can be as disabling as quadrip...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543781003691832

    authors: Marin JC,Goadsby PJ

    更新日期:2010-04-01 00:00:00

  • Glucokinase activators in diabetes management.

    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

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.17.2.145

    authors: Coghlan M,Leighton B

    更新日期:2008-02-01 00:00:00

  • Novel approaches for the prevention of restenosis.

    abstract::Restenosis, the re-narrowing of the lumen of the coronary artery, in the months following a successful percutaneous balloon angioplasty or stenting, remains the main limitation to percutaneous coronary revascularisation. Serial intravascular ultrasound studies have shown that restenosis after conventional balloon angi...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.9.11.2555

    authors: Gruberg L,Waksman R,Satler LF,Pichard AD,Kent KM

    更新日期:2000-11-01 00:00:00

  • Ganetespib for small cell lung cancer.

    abstract:INTRODUCTION:Heat shock proteins (Hsps) are part of a complex network of chaperone proteins that are critically involved in the conformational maturation of intracellular proteins and regulate their degradation via the proteasome system Hsps (especially Hsp70 and Hsp90) are upregulated in many cancers and are potential...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1080/13543784.2017.1268599

    authors: Subramaniam DS,Warner EA,Giaccone G

    更新日期:2017-01-01 00:00:00

  • Emerging therapeutic strategies for minimal change disease and focal and segmental glomerulosclerosis.

    abstract:INTRODUCTION:Minimal change disease (MCD) and Focal and segmental glomerulosclerosis (FSGS) are two of the major causes of nephrotic syndrome (NS) in children and adults. According to KDIGO (Kidney Disease: Improving Global Outcomes) guidelines, the treatment of adult primary MCD and FSGS should be based on immunosuppr...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1080/13543784.2018.1540587

    authors: Siligato R,Cernaro V,Nardi C,De Gregorio F,Gembillo G,Costantino G,Conti G,Buemi M,Santoro D

    更新日期:2018-11-01 00:00:00

  • Histone deacetylase inhibitors in clinical development.

    abstract::In addition to a variety of other novel agents, interest in histone deacetylase inhibitors (HDACIs) as antineoplastic drugs has recently accelerated and increasing numbers of these compounds have entered clinical trials in humans. HDACIs represent a prototype of molecularly targeted agents that perturb signal transduc...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.13.1.21

    authors: Rosato RR,Grant S

    更新日期:2004-01-01 00:00:00

  • Olaparib for the treatment of breast cancer.

    abstract:INTRODUCTION:Basal-like breast cancer is characterized by being triple negative and aggressive. Defects in DNA repair is a promising therapeutic target as BRCA alterations are found in 11 to 42% of these tumors, with a frequency varying according to family history and ethnicity. The oral PARP inhibitors exploit this de...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1080/13543784.2017.1318847

    authors: Robert M,Frenel JS,Gourmelon C,Patsouris A,Augereau P,Campone M

    更新日期:2017-06-01 00:00:00

  • Inhibitors of cholesteryl ester transfer protein--a new approach to coronary artery disease.

    abstract::Despite the use of the statins to lower low-density lipoprotein-cholesterol, leading to major reductions in the mortality and morbidity that is associated with coronary artery disease, considerable mortality and morbidity remains. Increasing high-density lipoprotein (HDL)-cholesterol levels has been associated with re...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.15.2.99

    authors: Doggrell SA

    更新日期:2006-02-01 00:00:00

  • Bromocriptine improves glycaemic control and serum lipid profile in obese Type 2 diabetic subjects: a new approach in the treatment of diabetes.

    abstract::Bromocriptine, a potent dopamine D(2) receptor agonist, has been shown to reduce insulin resistance, glucose intolerance and hyperlipidaemia in both numerous animal studies and in Phase II studies. Bromocriptine has been used worldwide for over 20 years to treat Parkinson's disease, macroprolactinoma and other disorde...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1517/13543784.8.10.1683

    authors: Cincotta AH,Meier AH,Cincotta M Jr

    更新日期:1999-10-01 00:00:00

  • Investigational therapies for Ewing sarcoma: a search without a clear finding.

    abstract:INTRODUCTION:Ewing sarcoma family tumors (ESFT) are a group of aggressive diseases, characterized histologically by small, round, blue cells and genetically by translocation involving EWS and ETS partner genes. The current treatment of localized Ewing sarcoma (ES) requires a multi-disciplinary approach, including multi...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2016.1168398

    authors: Vornicova O,Bar-Sela G

    更新日期:2016-06-01 00:00:00

  • Dehydroaltenusin is a specific inhibitor of mammalian DNA polymerase α.

    abstract:INTRODUCTION:We carried out a screen for small molecule selective inhibitors of eukaryotic DNA polymerases (pols). Dehydroaltenusin, isolated from a fungus (Alternaria tenuis), was found to be a specific inhibitor of pol α. AREAS COVERED:We succeeded in chemically synthesizing dehydroaltenusin along with five analogs....

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2011.619977

    authors: Mizushina Y,Maeda N,Kuriyama I,Yoshida H

    更新日期:2011-11-01 00:00:00

  • Discontinued drugs in 2006: pulmonary-allergy, dermatological, gastrointestinal and arthritis drugs.

    abstract::This perspective is the second in a series discussing drugs dropped from development in 2006, with a focus on pulmonary-allergy, dermatological, gastrointestinal and arthritis drugs. A survey of discontinued drugs from 2006 is provided, based on data from the Pharmaprojects database, along with an analysis of biology,...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.16.9.1327

    authors: Ozdemir C,Akdis CA

    更新日期:2007-09-01 00:00:00

  • Tirofiban: an investigational platelet glycoprotein IIb/IIIa receptor antagonist.

    abstract::The deposition of a platelet rich thrombus on an atherosclerotic plaque is a critical step in the development of unstable coronary syndromes. Currently available therapeutic agents such as aspirin and ticlopidine are relatively weak inhibitors of platelet aggregation. Recently, antagonists to platelet glycoprotein IIb...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1517/13543784.6.9.1257

    authors: Kumar A,Herrmann HC

    更新日期:1997-09-01 00:00:00

  • How to treat patients with relapsed/refractory multiple myeloma: evidence-based information and opinions.

    abstract:INTRODUCTION:Relapsed/refractory multiple myeloma (rrMM) remains a difficult condition to treat despite the availability of new drugs. This review aims to provide evidence to guide physicians in the choice of salvage therapy in certain subgroups of patients. AREAS COVERED:The review attempts to present evidence-based ...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2011.575060

    authors: Offidani M,Corvatta L,Morabito F,Gentile M,Musto P,Leoni P,Palumbo A

    更新日期:2011-06-01 00:00:00

  • The Annual European Congress of Rheumatology: recent advances in the treatment of rheumatic diseases. Lisbon, Portugal, June 18-21, 2003.

    abstract::The topics discussed at this conference covered many aspects of the pathogenesis, epidemiology, diagnosis and treatment of rheumatic diseases, from the search of new therapeutic targets and evaluation of new diagnostic techniques to preclinical and clinical development of novel therapies. This contribution focuses pri...

    journal_title:Expert opinion on investigational drugs

    pub_type:

    doi:10.1517/13543784.12.10.1713

    authors: Hellmich B,Gross WL

    更新日期:2003-10-01 00:00:00

  • Prorenin receptor blockers: effects on cardiovascular complications of diabetes and hypertension.

    abstract::When the 'handle region' of the prorenin prosegment interacts with the (pro)renin receptor, the prorenin molecule partially changes the conformation to an enzymatically active state. On the other hand, the receptor triggers its own intracellular signalling pathways independent of the renin-angiotensin system (RAS). Th...

    journal_title:Expert opinion on investigational drugs

    pub_type: 社论,评审

    doi:10.1517/13543784.15.10.1137

    authors: Ichihara A,Kaneshiro Y,Suzuki F

    更新日期:2006-10-01 00:00:00

  • Sofinicline: a novel nicotinic acetylcholine receptor agonist in the treatment of attention-deficit/hyperactivity disorder.

    abstract:INTRODUCTION:Psychostimulants are first-line treatments for attention-deficit/hyperactivity disorder (ADHD), but their tolerability profiles and individual response variability fuel a continuing search for alternative medications. The observation that nicotinic agents improve cognition has led pharmaceutical companies ...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2014.934806

    authors: Fleisher C,McGough J

    更新日期:2014-08-01 00:00:00

  • Urokinase receptor antagonists: novel agents for the treatment of cancer.

    abstract::The interaction between the urokinase receptor (uPAR) and its ligand urokinase (uPA) mediates phenomena such as tissue remodelling, chemotaxis, tumour invasion, dissemination, proliferation, and angiogenesis. The broad-spectrum of biological processes that the uPA/uPAR interaction plays a role in has led researchers t...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1517/13543784.7.3.391

    authors: Weidle UH,König B

    更新日期:1998-03-01 00:00:00

  • Immune-adhesion molecules in the prevention of allograft rejection and reperfusion injury.

    abstract::Control of the immune system is of indispensable importance for graft acceptance and function. Immunological changes in the graft before and after organ harvesting, the transplantation procedure itself and the organ recipients clinical state contribute to the immune response. Leukocyte trafficking [1] into a graft is ...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.9.4.789

    authors: Behrend M

    更新日期:2000-04-01 00:00:00

  • The therapeutic potential of monoclonal antibodies against respiratory syncytial virus.

    abstract::Attempts to develop a vaccine against respiratory syncytial virus (RSV), the major cause of lower respiratory tract disease in infants and young children, have been unsuccessful. Passive immunisation with antibody to RSV has been found to be an effective alternative method for prophylaxis. The product currently in use...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1517/13543784.7.8.1271

    authors: Weltzin R

    更新日期:1998-08-01 00:00:00

  • Nitric oxide and the angiogenic response: can we improve the results of therapeutic angiogenesis?

    abstract::Therapeutic angiogenesis has yielded promising results in animal models, including the demonstration of newly created blood vessels, increased perfusion and functional benefits. On the other hand, clinical studies using similar methods of angiogenesis have so far been disappointing. The possibility that endothelial dy...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.14.1.37

    authors: Kapila V,Sellke FW,Suuronen EJ,Mesana TG,Ruel M

    更新日期:2005-01-01 00:00:00

  • Zolmitriptan: a new acute treatment for migraine.

    abstract::Zolmitriptan is a new oral acute treatment for migraine. It is a selective and potent agonist at the serotonin (5-HT)(1B/1D) receptor and was developed to improve on the oral bioavailability, tissue selectivity and CNS penetration of earlier compounds. Animal studies confirmed that these objectives had been attained. ...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1517/13543784.7.4.633

    authors: Rolan PE,Martin GR

    更新日期:1998-04-01 00:00:00

  • Novel therapies for the treatment of inflammatory airway disease.

    abstract::Asthma and chronic obstructive pulmonary disease (COPD) are diseases of the airways with an underlying inflammatory component. The prevalence and healthcare burden of asthma and COPD is still rising and is predicted to continue to rise in the current century. The beta-agonists and corticosteroids form the basis of the...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.12.1.5

    authors: Hele DJ,Belvisi MG

    更新日期:2003-01-01 00:00:00

  • Cannabinoids against pain. Efficacy and strategies to reduce psychoactivity: a clinical perspective.

    abstract::The clinical use of cannabinoids is currently a topic of interest not exclusively, but most importantly, concerning different areas of pain therapy. One of the major obstacles in developing clinically acceptable compounds is the cannabimimetic side-effect profile of delta-9-tetrahydrocannabinol (THC) and other cannabi...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543780802691951

    authors: Karst M,Wippermann S

    更新日期:2009-02-01 00:00:00

  • Therapeutic options for patients with clonal and idiopathic hypereosinophia.

    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

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.17.7.1039

    authors: Quintás-Cardama A,Cortes J

    更新日期:2008-07-01 00:00:00

  • PF-00547659 for the treatment of Crohn's disease and ulcerative colitis.

    abstract:INTRODUCTION:Gut-specific homing is mainly mediated by the expression of MAdCAM-1 on endothelial cells. An increase in MAdCAM-1 expression has been shown in patients with inflammatory bowel disease (IBD). Areas covered: PF-00547659 is a fully human monoclonal antibody (mAb) toward MAdCAM-1 on endothelial cells, blockin...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1080/13543784.2018.1494722

    authors: Allocca M,Gilardi D,Fiorino G,Furfaro F,Argollo M,Peyrin-Biroulet L,Danese S

    更新日期:2018-07-01 00:00:00

  • The therapeutic potential of gut hormone peptide YY3-36 in the treatment of obesity.

    abstract::Many peptides are synthesised and released from the gastrointestinal tract. Although their roles in the regulation of gastrointestinal function have been known for some time, it has become increasingly evident that they also influence eating behaviour. Peptide YY (PYY) is released postprandially from gastrointestinal ...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.14.5.647

    authors: Small CJ,Bloom SR

    更新日期:2005-05-01 00:00:00

  • Investigational vasopressin receptor modulators in the pipeline.

    abstract::The vasopressin system is complex and interacts with the central nervous, cardiovascular, renal, and hematological systems. Vasopressin plays an important role in the control of blood osmolarity and vascular tone, but is also involved in many other physiological events, which are mediated mainly via three types of vas...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543780903066764

    authors: Favory R,Salgado DR,Vincent JL

    更新日期:2009-08-01 00:00:00

  • Beclabuvir for the treatment of hepatitis C.

    abstract:INTRODUCTION:About 185,000,000 people worldwide are chronically infected with hepatitis C virus (HCV). Currently, the most successful HCV infection antiviral therapies reduce the chance of progression towards the advanced phases of the hepatopathy (liver cirrhosis, hepatocellular carcinoma and death). Recently, however...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2015.1059820

    authors: Gentile I,Zappulo E,Buonomo AR,Maraolo AE,Borgia G

    更新日期:2015-01-01 00:00:00

  • Sorafenib in locally advanced or metastatic breast cancer.

    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

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2012.689824

    authors: Gradishar WJ

    更新日期:2012-08-01 00:00:00