Prostaglandin D2 receptor antagonists in allergic disorders: safety, efficacy, and future perspectives

Childhood Asthma Clusters Reveal Neutrophil-Predominant Phenotype with Distinct Gene Expression

(2018) Ming-Wei Su et al.   ALLERGY

Important and specific role for basophils in acute allergic reactions

(2018) P. Korošec et al.   CLINICAL AND EXPERIMENTAL ALLERGY

Innate effector cells in angiogenesis and lymphangiogenesis

(2018) Gilda Varricchi et al.   CURRENT OPINION IN IMMUNOLOGY

Prostaglandin D 2 generation from human lung mast cells is catalysed exclusively by cyclooxygenase-1

(2018) Bandar K. Baothman et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Fevipiprant in the treatment of asthma

(2018) Christobelle White et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

The contribution of mast cells to bacterial and fungal infection immunity

(2018) Adrian M. Piliponsky et al.   IMMUNOLOGICAL REVIEWS

Human mast cells and basophils-How are they similar how are they different?

(2018) Gilda Varricchi et al.   IMMUNOLOGICAL REVIEWS

Hypersensitivity reactions to therapeutic monoclonal antibodies: Phenotypes and endotypes

(2018) Ghislaine Annie C. Isabwe et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

The pathogenicity of IL-33 on steroid-resistant eosinophilic inflammation via the activation of memory-type ST2+ CD4+ T cells

(2018) Kiyoshi Hirahara et al.   JOURNAL OF LEUKOCYTE BIOLOGY

A genome-wide cross-trait analysis from UK Biobank highlights the shared genetic architecture of asthma and allergic diseases

(2018) Zhaozhong Zhu et al.   NATURE GENETICS

Efficacy and Safety of Dupilumab in Glucocorticoid-Dependent Severe Asthma

(2018) Klaus F. Rabe et al.   NEW ENGLAND JOURNAL OF MEDICINE

Dupilumab Efficacy and Safety in Moderate-to-Severe Uncontrolled Asthma

(2018) Mario Castro et al.   NEW ENGLAND JOURNAL OF MEDICINE

PGD2/DP2 receptor activation promotes severe viral bronchiolitis by suppressing IFN- λ production

(2018) Rhiannon B. Werder et al.   Science Translational Medicine

Thymic Stromal Lymphopoietin Isoforms, Inflammatory Disorders, and Cancer

(2018) Gilda Varricchi et al.   Frontiers in Immunology

Fevipiprant, an oral prostaglandin DP2receptor (CRTh2) antagonist, in allergic asthma uncontrolled on low-dose inhaled corticosteroids

(2017) Eric D. Bateman et al.   EUROPEAN RESPIRATORY JOURNAL

Decreased Prostaglandin D2 Levels in Major Depressive Disorder Are Associated with Depression-Like Behaviors

(2017) Cuilin Chu et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel CRTH2 Antagonist BI 1021958 at Single Oral Doses in Healthy Men and Multiple Oral Doses in Men and Women With Well-Controlled Asthma

(2017) Andy Fowler et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Oral Glucocorticoid–Sparing Effect of Benralizumab in Severe Asthma

(2017) Parameswaran Nair et al.   NEW ENGLAND JOURNAL OF MEDICINE

Personalized Medicine in Allergy

(2017) Matteo Ferrando et al.   Allergy Asthma & Immunology Research

Efficacy of mepolizumab add-on therapy on health-related quality of life and markers of asthma control in severe eosinophilic asthma (MUSCA): a randomised, double-blind, placebo-controlled, parallel-group, multicentre, phase 3b trial

(2017) Geoffrey L Chupp et al.   Lancet Respiratory Medicine

Are Mast Cells MASTers in Cancer?

(2017) Gilda Varricchi et al.   Frontiers in Immunology

Eosinophils: The unsung heroes in cancer?

(2017) Gilda Varricchi et al.   OncoImmunology

IL-33 restricts tumor growth and inhibits pulmonary metastasis in melanoma-bearing mice through eosinophils

(2017) Valeria Lucarini et al.   OncoImmunology

Generation and characterization of an antagonistic monoclonal antibody against an extracellular domain of mouse DP2 (CRTH2/GPR44) receptors for prostaglandin D2

(2017) Nanae Nagata et al.   PLoS One

T follicular helper (Tfh) cells in normal immune responses and in allergic disorders

(2016) G. Varricchi et al.   ALLERGY

Emergence of Biomolecular Pathways to Define Novel Asthma Phenotypes. Type-2 Immunity and Beyond

(2016) Sally E. Wenzel   AMERICAN JOURNAL OF RESPIRATORY CELL AND MOLECULAR BIOLOGY

Phase 3 Study of Reslizumab in Patients With Poorly Controlled Asthma

(2016) Jonathan Corren et al.   CHEST

Reslizumab for Inadequately Controlled Asthma With Elevated Blood Eosinophil Levels

(2016) Leif Bjermer et al.   CHEST

Mast cells in asthma - state of the art

(2016) P. Bradding et al.   CLINICAL AND EXPERIMENTAL ALLERGY

Long-term Efficacy and Safety of Mepolizumab in Patients With Severe Eosinophilic Asthma: A Multi-center, Open-label, Phase IIIb Study

(2016) Njira Lugogo et al.   CLINICAL THERAPEUTICS

Interleukin-5 pathway inhibition in the treatment of eosinophilic respiratory disorders

(2016) Gilda Varricchi et al.   Current Opinion in Allergy and Clinical Immunology

Controversial role of mast cells in skin cancers

(2016) Gilda Varricchi et al.   EXPERIMENTAL DERMATOLOGY

Are emerging PGD2 antagonists a promising therapy class for treating asthma?

(2016) Hugo Farne et al.   EXPERT OPINION ON EMERGING DRUGS

Investigational prostaglandin D2receptor antagonists for airway inflammation

(2016) Giuseppe Santini et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

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

(2016) Pierachille Santus et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Are Basophils and Mast Cells Masters in HIV Infection?

(2016) Gianni Marone et al.   INTERNATIONAL ARCHIVES OF ALLERGY AND IMMUNOLOGY

A Critical Evaluation of Anti-IL-13 and Anti-IL-4 Strategies in Severe Asthma

(2016) Diego Bagnasco et al.   INTERNATIONAL ARCHIVES OF ALLERGY AND IMMUNOLOGY

Activated prostaglandin D2 receptors on macrophages enhance neutrophil recruitment into the lung

(2016) Katharina Jandl et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Thymic stromal lymphopoietin controls prostaglandin D 2 generation in patients with aspirin-exacerbated respiratory disease

(2016) Kathleen M. Buchheit et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Efficacy and safety of benralizumab for patients with severe asthma uncontrolled with high-dosage inhaled corticosteroids and long-acting β2-agonists (SIROCCO): a randomised, multicentre, placebo-controlled phase 3 trial

(2016) Eugene R Bleecker et al.   LANCET

Benralizumab, an anti-interleukin-5 receptor α monoclonal antibody, as add-on treatment for patients with severe, uncontrolled, eosinophilic asthma (CALIMA): a randomised, double-blind, placebo-controlled phase 3 trial

(2016) J Mark FitzGerald et al.   LANCET

Pharmacological characterization of CRTh2 antagonist LAS191859: Long receptor residence time translates into long-lasting in vivo efficacy

(2016) Marta Calbet et al.   PHARMACOLOGICAL RESEARCH

The oral CRTh2 antagonist QAW039 (fevipiprant): A phase II study in uncontrolled allergic asthma

(2016) Veit J. Erpenbeck et al.   PULMONARY PHARMACOLOGY & THERAPEUTICS

Two Phase II randomized trials on the CRTh2 antagonist AZD1981 in adults with asthma

(2016) Piotr Kuna et al.   Drug Design Development and Therapy

Effect of prostaglandin D2 on VEGF release by nasal polyp fibroblasts

(2016) Kengo Kanai et al.   ALLERGOLOGY INTERNATIONAL

Fevipiprant, a prostaglandin D 2 receptor 2 antagonist, in patients with persistent eosinophilic asthma: a single-centre, randomised, double-blind, parallel-group, placebo-controlled trial

(2016) Sherif Gonem et al.   Lancet Respiratory Medicine

Therapeutic interventions in severe asthma

(2016) Giorgio Walter Canonica et al.   World Allergy Organization Journal

Effect of the potent and selective DP1 receptor antagonist, asapiprant (S-555739), in animal models of allergic rhinitis and allergic asthma

(2015) Go Takahashi et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

D prostanoid receptor 2 (chemoattractant receptor–homologous molecule expressed on TH2 cells) protein expression in asthmatic patients and its effects on bronchial epithelial cells

(2015) Sally E. Stinson et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

A novel CRTH2 antagonist: Single- and multiple-dose tolerability, pharmacokinetics, and pharmacodynamics of ACT-453859 in healthy subjects

(2015) Martine Géhin et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Human lung-resident macrophages express CB1 and CB2 receptors whose activation inhibits the release of angiogenic and lymphangiogenic factors

(2015) Rosaria I. Staiano et al.   JOURNAL OF LEUKOCYTE BIOLOGY

The prostaglandin D2 receptor CRTH2 regulates accumulation of group 2 innate lymphoid cells in the inflamed lung

(2015) E D Tait Wojno et al.   Mucosal Immunology

Eosinophils orchestrate cancer rejection by normalizing tumor vessels and enhancing infiltration of CD8+ T cells

(2015) Rafael Carretero et al.   NATURE IMMUNOLOGY

The immunology of asthma

(2015) Bart N Lambrecht et al.   NATURE IMMUNOLOGY

Mast cells in human and experimental cardiometabolic diseases

(2015) Guo-Ping Shi et al.   Nature Reviews Cardiology

Efficacy of BI 671800, an oral CRTH2 antagonist, in poorly controlled asthma as sole controller and in the presence of inhaled corticosteroid treatment

(2015) Ian P. Hall et al.   PULMONARY PHARMACOLOGY & THERAPEUTICS

Heightened response of eosinophilic asthmatic patients to the CRTH2 antagonist OC000459

(2014) R. Pettipher et al.   ALLERGY

Setipiprant, a selective CRTH2 antagonist, reduces allergen-induced airway responses in allergic asthmatics

(2014) Z. Diamant et al.   CLINICAL AND EXPERIMENTAL ALLERGY

Role of prostaglandin D2and CRTH2 blockade in early- and late-phase nasal responses

(2014) Y. Shiraishi et al.   CLINICAL AND EXPERIMENTAL ALLERGY

Immunopharmacological modulation of mast cells

(2014) Francesco Borriello et al.   CURRENT OPINION IN PHARMACOLOGY

Anti-inflammatory actions of Chemoattractant Receptor-homologous molecule expressed on Th2 by the antagonist MK-7246 in a novel rat model of Alternaria alternata elicited pulmonary inflammation

(2014) Malgorzata A. Gil et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Outcomes after cessation of mepolizumab therapy in severe eosinophilic asthma: A 12-month follow-up analysis

(2014) Pranabashis Haldar et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Safety and Efficacy Of ARRY-502, a Potent, Selective, Oral CRTh2 Antagonist, In Patients With Mild To Moderate Th2-Driven Asthma

(2014) Sally E. Wenzel et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Prostaglandin D2 activates group 2 innate lymphoid cells through chemoattractant receptor-homologous molecule expressed on TH2 cells

(2014) Luzheng Xue et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Lessons learned from the fate of AstraZeneca's drug pipeline: a five-dimensional framework

(2014) David Cook et al.   NATURE REVIEWS DRUG DISCOVERY

Oral Glucocorticoid-Sparing Effect of Mepolizumab in Eosinophilic Asthma

(2014) Elisabeth H. Bel et al.   NEW ENGLAND JOURNAL OF MEDICINE

Mepolizumab Treatment in Patients with Severe Eosinophilic Asthma

(2014) Hector G. Ortega et al.   NEW ENGLAND JOURNAL OF MEDICINE

Expression of DP2 (CRTh2), a Prostaglandin D2 Receptor, in Human Mast Cells

(2014) Tae Chul Moon et al.   PLoS One

The role of prostaglandins in allergic lung inflammation and asthma

(2014) Dru Claar et al.   Expert Review of Respiratory Medicine

Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases

(2013) David A. Sandham et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Inhibition of antigen-induced airway inflammation and hyperresponsiveness in guinea pigs by a selective antagonist of “chemoattractant receptor homologous molecule expressed on Th2 cells” (CRTH2)

(2013) Mamoru Tasaki et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Update on the status of DP2 receptor antagonists; from proof of concept through clinical failures to promising new drugs

(2013) Peter Norman   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Risk of childhood asthma following infant bronchiolitis during the respiratory syncytial virus season

(2013) Kristina M. James et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Prostaglandin D2 pathway upregulation: Relation to asthma severity, control, and TH2 inflammation

(2013) Merritt L. Fajt et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Efficacy of the oral chemoattractant receptor homologous molecule on TH2 cells antagonist BI 671800 in patients with seasonal allergic rhinitis

(2013) Norbert Krug et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Pharmacological characterization of the late phase reduction in lung functions and correlations with microvascular leakage and lung edema in allergen-challenged Brown Norway rats

(2013) Peter J. Mauser et al.   PULMONARY PHARMACOLOGY & THERAPEUTICS

UGT2B17 Genetic Polymorphisms Dramatically Affect the Pharmacokinetics of MK-7246 in Healthy Subjects in a First-in-Human Study

(2012) Y-H Wang et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Transcript profiling of CD16-positive monocytes reveals a unique molecular fingerprint

(2012) Marion Frankenberger et al.   EUROPEAN JOURNAL OF IMMUNOLOGY

Inhibition of the asthmatic allergen challenge response by the CRTH2 antagonist OC000459

(2012) D. Singh et al.   EUROPEAN RESPIRATORY JOURNAL

Safety and efficacy of the prostaglandin D2 receptor antagonist AMG 853 in asthmatic patients

(2012) William W. Busse et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Mepolizumab for severe eosinophilic asthma (DREAM): a multicentre, double-blind, placebo-controlled trial

(2012) Ian D Pavord et al.   LANCET

Asthma phenotypes: the evolution from clinical to molecular approaches

(2012) Sally E Wenzel   NATURE MEDICINE

A randomized, double-blind, placebo-controlled study of the CRTH2 antagonist OC000459 in moderate persistent asthma

(2011) N. Barnes et al.   CLINICAL AND EXPERIMENTAL ALLERGY

Prostanoid DP receptor antagonists suppress symptomatic asthma-like manifestation by distinct actions from a glucocorticoid in rats

(2011) Yosuke Hirano et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

A novel DP2receptor antagonist (AM-461): a patent evaluation of WO2011085033

(2011) Peter Norman   EXPERT OPINION ON THERAPEUTIC PATENTS

Pharmacodynamics, Pharmacokinetics, and Safety of AM211: A Novel and Potent Antagonist of the Prostaglandin D2Receptor Type 2

(2011) G. Bain et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Eosinophils as a Novel Cell Source of Prostaglandin D2: Autocrine Role in Allergic Inflammation

(2011) T. Luna-Gomes et al.   JOURNAL OF IMMUNOLOGY

Pharmacology of AM211, a Potent and Selective Prostaglandin D2 Receptor Type 2 Antagonist That Is Active in Animal Models of Allergic Inflammation

(2011) G. Bain et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Discovery of AMG 853, a CRTH2 and DP Dual Antagonist

(2011) Jiwen Liu et al.   ACS Medicinal Chemistry Letters

Mast Cell Phenotype, Location, and Activation in Severe Asthma

(2010) Silvana Balzar et al.   AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE

Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases

(2010) Michel Gallant et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Pharmacological Characterization of MK-7246, a Potent and Selective CRTH2 (Chemoattractant Receptor-Homologous Molecule Expressed on T-Helper Type 2 Cells) Antagonist

(2010) F. G. Gervais et al.   MOLECULAR PHARMACOLOGY

The safety and side effects of monoclonal antibodies

(2010) Trevor T. Hansel et al.   NATURE REVIEWS DRUG DISCOVERY

CRTH2 and D-Type Prostanoid Receptor Antagonists as Novel Therapeutic Agents for Inflammatory Diseases

(2010) Rufina Schuligoi et al.   PHARMACOLOGY

Interaction between prostaglandin D2and chemoattractant receptor-homologous molecule expressed on Th2 cells mediates cytokine production by Th2 lymphocytes in response to activated mast cells

(2009) L. Xue et al.   CLINICAL AND EXPERIMENTAL IMMUNOLOGY

Clinical studies of the DP1 antagonist laropiprant in asthma and allergic rhinitis

(2009) George Philip et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Wheezing Rhinovirus Illnesses in Early Life Predict Asthma Development in High-Risk Children

(2008) Daniel J. Jackson et al.   AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE

Lipopolysaccharide Induces Macrophage Migration via Prostaglandin D2 and Prostaglandin E2

(2008) T. Tajima et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Role of Prostaglandin D2 and Its Receptors in the Pathophysiology of Asthma

(2008) Tsuyoshi Oguma et al.   ALLERGOLOGY INTERNATIONAL