Prostaglandin D2 receptor antagonists in early development as potential therapeutic options for asthma.

Abstract:

INTRODUCTION:Asthma is a chronic inflammatory disease characterized by bronchial hyper-reactivity. Although many currently available treatment regimens are effective, poor symptom control and refractory severe disease still represent major unmet needs. In the last years, numerous molecular therapeutic targets that interfere with the innate inflammatory response in asthma have been identified. Promising preliminary results concern the signaling cascade promoted by prostaglandin D2 (PGD2) and its receptor antagonists. AREAS COVERED:The aim of this review is to provide the most recent clinical and preclinical data on the efficacy and safety of newly developed compounds for the treatment of allergic asthma. The authors will present an overview of the pathogenetic molecular mechanisms sustaining the chronic inflammatory response in asthma; the focus will be then directed on the mediators of the PGD2 pathway, the chemoattractant receptor-homologous molecule expressed on TH2 cells, and their latest antagonists developed. EXPERT OPINION:Bronchodilators and corticosteroids are not sufficient to achieve a satisfactory management of all asthmatic patients; the development of new specific treatments appears therefore essential. The good results in terms of cellular, functional and clinical outcomes, together with an acceptable safety of the CRTh2 antagonists represent a promising start for a tailored management of allergic asthma.

authors

Santus P,Radovanovic D

doi

10.1080/13543784.2016.1212838

subject

Has Abstract

pub_date

2016-09-01 00:00:00

pages

1083-92

issue

9

eissn

1354-3784

issn

1744-7658

journal_volume

25

pub_type

杂志文章,评审
  • The therapeutic potential of the cannabinoids in neuroprotection.

    abstract::After thousands of years of interest the last few decades have seen a huge increase in our knowledge of the cannabinoids and their mode of action. Their potential as medical therapeutics has long been known. However, very real concerns over their safety and efficacy have lead to caution and suspicion when applying the...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.11.10.1365

    authors: Grundy RI

    更新日期:2002-10-01 00:00:00

  • 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

  • A consideration of PPAR-gamma ligands with respect to lipophilicity: current trends and perspectives.

    abstract::The fact that PPAR-gamma is expressed dramatically higher in fat, regulating gene transcription in response to small lipophilic ligands, supports an essential role of increased lipophilicity for those ligands. On the other hand, the skepticism concerning high lipophilicity as a characteristic associated with undesirab...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.16.4.413

    authors: Giaginis C,Theocharis S,Tsantili-Kakoulidou A

    更新日期:2007-04-01 00:00:00

  • Atazanavir: a novel HIV-1 protease inhibitor.

    abstract::The introduction of HIV-1 protease inhibitors in 1995 ushered in the era of highly active antiretroviral therapy. For the first time, inhibition of two key enzymes responsible for HIV replication, reverse transcriptase and protease, was possible. The combination of two nucleoside reverse transcriptase inhibitors with ...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.11.9.1295

    authors: Piliero PJ

    更新日期:2002-09-01 00:00:00

  • Therapeutic potential of GP IIb/IIIa receptor antagonists in acute myocardial infarction.

    abstract::The management of acute myocardial infarction (AMI) has changed dramatically over the last two decades, with the addition of fibrinolytic agents and primary coronary intervention (PCI). The more recent development of the glycoprotein (GP) IIb/IIIa antagonists, a new class of potent antiplatelet drugs, has the potentia...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.10.11.1965

    authors: Ferguson JJ,Vaisman D

    更新日期:2001-11-01 00:00:00

  • Recent advances in protein tyrosine phosphatase 1B inhibitors.

    abstract::Type 2 diabetes and obesity are characterised by insulin and leptin resistance. Studies suggest that these may be due to defects in the insulin and leptin signalling pathways. Over the last decade, a considerable body of evidence has been amassed indicating that protein tyrosine phosphatase 1B (PTP1B) is involved in t...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.13.3.199

    authors: Taylor SD,Hill B

    更新日期:2004-03-01 00:00:00

  • The treatment of urinary tract infections and use of ciprofloxacin extended release.

    abstract::Urinary tract infections (UTIs) are one of the most common reasons people seek medical attention. There are > 50% of women who will have at least one UTI during their lifetime and most of these will require a physician visit and antibiotic treatment. The high prevalence continues to the in-patient setting where genito...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.15.5.519

    authors: Hickerson AD,Carson CC

    更新日期:2006-05-01 00:00:00

  • Recent advances in natriuretic peptides in congestive heart failure.

    abstract::Atrial natriuretic peptide (ANP) and B-type natriuretic peptide (BNP) are secreted by the heart and play important roles in the compensation of congestive heart failure with their vasodilating, natriuretic, antiproliferative, lusitropic and neurohumoral-modulating properties. Based on these beneficial properties, exog...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.13.6.643

    authors: Boerrigter G,Burnett JC Jr

    更新日期:2004-06-01 00:00:00

  • The impact of multi-targeted cyclin-dependent kinase inhibition in breast cancer cells: clinical implications.

    abstract:INTRODUCTION:The progression of the mammalian cell cycle is driven by the transient activation of complexes consisting of cyclins and cyclin-dependent kinases (CDKs). Loss of control over the cell cycle results in accelerated cell division and malignant transformation and can be caused by the upregulation of cyclins, t...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2011.628985

    authors: Węsierska-Gądek J,Kramer MP

    更新日期:2011-12-01 00:00:00

  • Heat shock protein 90 inhibitors in the treatment of cancer: current status and future directions.

    abstract:INTRODUCTION:Heat shock protein 90 (HSP90) serves as a critical facilitator for oncogene addiction. There has been augmenting enthusiasm in pursuing HSP90 as an anticancer strategy. In fact, since the initial serendipitous discovery that geldanamycin (GM) inhibits HSP90, the field has rapidly moved from proof-of-concep...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2014.902442

    authors: Jhaveri K,Ochiana SO,Dunphy MP,Gerecitano JF,Corben AD,Peter RI,Janjigian YY,Gomes-DaGama EM,Koren J 3rd,Modi S,Chiosis G

    更新日期:2014-05-01 00:00:00

  • Novel metabotropic glutamate receptor 4 and glutamate receptor 8 therapeutics for the treatment of anxiety.

    abstract:INTRODUCTION:The fast actions of the excitatory neurotransmitter glutamate are mediated by glutamate-gated ion channels (ionotropic Glu receptors). Metabotropic glutamate receptors (mGlus) are coupled to second messenger pathways via G proteins and modulate glutamatergic and GABAergic neurotransmission. Of the eight di...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2014.986264

    authors: Raber J,Duvoisin RM

    更新日期:2015-04-01 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

  • The therapeutic effects of vitamin D3 and its analogues in psoriasis.

    abstract::Psoriasis is a common skin disease which is characterised by the proliferation and abnormal differentiation of keratinocytes, coupled with complex immune disturbances. The beneficial effects of vitamin D derivatives in this disease are due to their capacity to inhibit proliferation, their ability to induce normal diff...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1517/13543784.7.1.77

    authors: Guilhou JJ

    更新日期:1998-01-01 00:00:00

  • Targeting IL-6 for the treatment of rheumatoid arthritis: Phase II investigational drugs.

    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

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2014.912276

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

    更新日期:2014-07-01 00:00:00

  • ENMD-2076 for hematological malignancies.

    abstract:INTRODUCTION:Aurora kinases are key regulators of mitosis and inhibition of Aurora kinase activity is a rational therapeutic strategy in the treatment of solid tumors and hematological malignancies. AREAS COVERED:This paper will provide an updated summary of preclinical and clinical experience with ENMD-2076 in hemato...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2012.668882

    authors: How J,Yee K

    更新日期:2012-05-01 00:00:00

  • Tumor necrosis factor alpha antagonists in the treatment of axial spondyloarthritis.

    abstract:INTRODUCTION:The introduction of therapy with tumor necrosis factor antagonists (aTNF) was a cornerstone of treatment modalities in patients with ankylosing spondylitis (AS). After > 10 years of using aTNF, the introduction of aTNF therapy was a major step forward in the medical management of patients with spondyloarth...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2014.899351

    authors: Braun J,Baraliakos X,Heldmann F,Kiltz U

    更新日期:2014-05-01 00:00:00

  • Insulin sensitizers in 2013: new insights for the development of novel therapeutic agents to treat metabolic diseases.

    abstract::Insulin-sensitizing thiazolidinediones (TZDs) correct a root cause of type 2 diabetes and potentially other diseases of metabolic dysfunction, including conditions ranging from oncologic, inflammatory, and neurodegenerative diseases. Importantly, compounds with this mode of action can modify disease progression, as op...

    journal_title:Expert opinion on investigational drugs

    pub_type: 社论,评审

    doi:10.1517/13543784.2013.839659

    authors: Colca JR,Tanis SP,McDonald WG,Kletzien RF

    更新日期:2014-01-01 00:00:00

  • A Phase I, Randomized, Double-Blind, Single-Dose, Parallel-Group Study to compare Pharmacokinetic Similarity, Safety, and Immunogenicity Between BAT2506 and Golimumab in Healthy Chinese Male Subjects.

    abstract::Background: To compare the pharmacokinetic (PK) profile, safety, and immunogenicity between golimumab and the biosimilar BAT2506 in healthy Chinese male subjects. Research design and methods: A total of 180 healthy male subjects were recruited for this randomized, double-blinded, single-dose, parallel study. They rece...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1080/13543784.2021.1851364

    authors: Wu M,Sun J,Wu D,Xu J,Wei J,Wang Z,Yu J,Li S,Zhang H,Ding Y

    更新日期:2021-01-01 00:00:00

  • Cardiac fibrosis: emerging agents in preclinical and clinical development.

    abstract:INTRODUCTION:Myocardial fibrosis is a remarkably dynamic process mediated by different molecular pathways that represent potential targets of novel therapeutic interventions. Transforming Growth Factor-beta (TGF-β), connective Tissue Growth Factor (cTGF) and Galectin-3 (Gal-3) represent the most promising targets on wh...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1080/13543784.2021.1868432

    authors: Spoladore R,Falasconi G,Fiore G,Di Maio S,Preda A,Slavich M,Margonato A,Fragasso G

    更新日期:2021-01-04 00:00:00

  • Microbial pathogens and apoptotic anticancer therapy.

    abstract::In spite of tremendous efforts to control cancer, the mortality associated with this disease has been increasing in developed countries in the recent decades. Inadequate efficiency of existing therapeutic regimens and the rise of multi-drug resistant cancer cells are the main factors which require a broadening of inve...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.9.6.1243

    authors: Pasechnik V

    更新日期:2000-06-01 00:00:00

  • Dasatinib : a novel therapy for breast cancer?

    abstract:INTRODUCTION:Dasatinib is a novel tyrosine kinase inhibitor with activity against the Src family kinases. The Src pathway is active in breast cancer and has been shown to promote cell proliferation, invasiveness, and metastases. Preclinical data support the use of dasatinib to inhibit breast cancer cell growth, modulat...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1517/13543784.2013.793308

    authors: Scher KS,Somlo G

    更新日期:2013-06-01 00:00:00

  • Investigational therapies for celiac disease.

    abstract::Celiac disease is an autoimmune condition affecting genetically susceptible individuals. It is produced by the ingestion of gluten contained in wheat, rye, barley, and related products. The only treatment currently available is strict adherence to a gluten-free diet for life. This requirement for dietary compliance is...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543780903369333

    authors: Rodrigo L

    更新日期:2009-12-01 00:00:00

  • Novel agents for the treatment of polycythemia vera: an insight into preclinical research and early phase clinical trials.

    abstract:INTRODUCTION:Current treatment for polycythemia vera (PV) is limited and primarily targets thrombosis risk. Agents targeting distinct mechanisms of action within myeloproliferation are undergoing clinical evaluation to optimize efficacy, improve tolerance and augment long term disease complications. AREA COVERED:This ...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1080/13543784.2020.1782886

    authors: Padrnos L,Mesa R

    更新日期:2020-08-01 00:00:00

  • An overview of investigational toxin-directed therapies for the adjunctive management of Bacillus anthracis infection and sepsis.

    abstract:INTRODUCTION:Sepsis with Bacillus anthracis infection has a very high mortality rate despite appropriate antibiotic and supportive therapies. Over the past 15 years, recent outbreaks in the US and in Europe, coupled with anthrax's bioterrorism weapon potential, have stimulated efforts to develop adjunctive therapies to...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2015.1041587

    authors: Ohanjanian L,Remy KE,Li Y,Cui X,Eichacker PQ

    更新日期:2015-01-01 00:00:00

  • Neuroimmunophilin ligands: evaluation of their therapeutic potential for the treatment of neurological disorders.

    abstract::Neuroimmunophilin ligands are a class of compounds that hold great promise for the treatment of nerve injuries and neurological disease. In contrast to neurotrophins (e.g., nerve growth factor), these compounds readily cross the blood-brain barrier, being orally effective in a variety of animal models of ischaemia, tr...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.9.10.2331

    authors: Gold BG

    更新日期:2000-10-01 00:00:00

  • Asimadoline in the treatment of irritable bowel syndrome.

    abstract:IMPORTANCE OF THE FIELD:Irritable bowel syndrome (IBS) represents one of the most common gastrointestinal disorders, with the diarrhea-predominant form (D-IBS) representing an area of high unmet medical need. One difficulty in identifying suitable treatments for IBS is that although there are animal models for the comp...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2010.515209

    authors: Mangel AW,Williams VS

    更新日期:2010-10-01 00:00:00

  • Second-generation epidermal growth factor tyrosine kinase inhibitors in non-small cell lung cancer.

    abstract::Inhibiting the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) has an established role in the treatment of advanced non-small cell lung cancer. The first-generation EGFR inhibitors erlotinib and gefitinib have been approved for treatment in the second- and third-line setting. Second-generation ...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543780902762843

    authors: Mukherji D,Spicer J

    更新日期:2009-03-01 00:00:00

  • Investigational drugs for hyperuricemia.

    abstract:INTRODUCTION:The unmet need and the growing prevalence of hyperuricemia and its complications worldwide have pushed investigators to identify new agents to manage hyperuricemia. AREAS COVERED:This review discusses the drugs in preclinical and early clinical trials for hyperuricemia, their mechanisms of action and avai...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2015.1051617

    authors: Shahid H,Singh JA

    更新日期:2015-01-01 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

  • The therapeutic potential of cationic peptides.

    abstract::Novel classes of antibiotics that are useful against resistant bacteria are a major need in human medicine. Cationic antimicrobial peptides are utilised as nature's antibiotics, being produced constitutively or in response to infection in virtually every type of organism from plants and insects to man. Thus, these pep...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1517/13543784.7.2.167

    authors: Hancock RE

    更新日期:1998-02-01 00:00:00