Target: CRTh2 | Indication: Asthma

Introduction / Brief Description

ARRY-502 is an oral, potent and highly selective CRTh2 antagonist designed to treat patients with Th2-driven allergic diseases.  The CRTh2 receptor is expressed on Th2 T cells, basophils and eosinophils, and its ligand, prostaglandin D2 (PGD2), is released by mast cells.  Results of a Phase 2 study with ARRY-502 in patients with mild to moderate Th2-driven asthma demonstrate that antagonism of the PGD2/CRTh2 axis results in significant improvements in lung function, asthma control, symptoms, and patient-reported quality-of-life outcomes.  ARRY-502 provided control of allergic inflammation and clinically meaningful benefit to these asthma patients.  Because current asthma therapies do not fully control the Th2 pathophysiology, antagonism of CRTh2 represents an exciting new approach to enhance disease control in asthma and other allergic inflammatory diseases. 

Based on its mechanism of action, ARRY-502 will provide the greatest patient benefit in a Th2 signature-enriched population.  Several baseline Th2-related biomarkers were evaluated in the Phase 2 study, including fractional exhaled nitric oxide (FENO).  The Th2 signature, which is present in about half of the asthma population, spans mild, moderate and severe disease and suggests broad applicability for ARRY-502 in these patients as well as in other Th2-driven diseases such as allergic rhinitis and atopic dermatitis.  Array is seeking a partner for further development of ARRY-502. 

About Asthma

It is estimated that approximately 25 million people in the United States have asthma, causing significant morbidity and mortality.  The worldwide estimates are approximately 235 million people with 180,000 deaths annually.  Mild to moderate persistent allergic asthma represents more than 12 million patients in the U.S, and while only 10% of all asthmatics are considered severe, they are responsible for a disproportionate share of asthma-related expenditures due to frequent exacerbations that result in emergency room visits and hospitalization.  Despite the range of available asthma treatments, there remains a significant need for a convenient, safe and effective therapy for patients.  Specifically, oral medications may facilitate treatment compliance relative to inhaled and injectable therapies. 

Clinical Trials

None at this time




American Academy of Allergy, Asthma & Immunology Annual Meeting

Safety and Efficacy of ARRY-502, a Potent, Selective, Oral CRTh2 Antagonist, in Patients with Mild to Moderate Th2-Driven Asthma

S. Wenzel, et al.



American Thoracic Society International Conference

Th2 Signature Selection Strategies for CRTh2 Antagonists: Baseline Characteristics of a Mild to Moderate Persistent Asthma Population

D. Chantry, et al.



World Congress on Inflammation

Potent, Selective, and Orally Active CRTh2 Antagonists for Allergic Disease

L. Burgess, et al.



Inflammation Research Association International Conference

Safety, PK and PD of ARRY-502, a CRTh2 Antagonist, in Healthy Subjects with a History of Seasonal Allergies

L. Burgess, et al.



European Respiratory Society Annual Congress

Safety, PK and PD of ARRY-502, a CRTh2 Antagonist, in Healthy Subjects with a History of Seasonal Allergies

S. Bell, et al.


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