Novel CRTH2 antagonists: a review of patents from 2006 to 2009

Abstract

Many diverse potent CRTH2 antagonists are now available, and several are in or on the way into the clinic. It is still early to draw final conclusions, but preliminary results give reason for optimism, and the prospect that we will see new CRTH2 antagonists reaching the market for the treatment of asthma, rhinitis, atopic dermatitis and/or COPD seems good.

D-type prostanoid receptor enhances the signaling of chemoattractant receptor–homologous molecule expressed on TH2 cells

“…48 Consistently, numerous pharmaceutical companies are engaged in programs developing CRTH2 antagonists, including bivalent CRTH2/DP antagonists. 49 Our data demonstrate remarkable cooperativity between PGD 2 receptors, CRTH2, and DP. Because several native cells expressing CRTH2, such as eosinophils, basophils, and T H 2 lymphocytes, also express the DP receptor, 15,23 it is tempting to speculate that CRTH2 activity essentially depends on functional DP receptors in vivo by ''hijacking'' its signaling machinery.…”

The immunology of atopic dermatitis and its reversibility with broad-spectrum and targeted therapies

“…158,159 Polymorphisms in CRTH2 have been associated with allergic sensitization. 160 CRTH2 blockade (Figure 2B) via the small molecules fevipiprant (QAW039, NCT01785602) and OC000459 (NCT02002208) are currently being assessed in clinical trials.…”

Allergic rhinitis: An update on disease, present treatments and future prospects

“…Thus, CRTH2 also promotes the production of Th2 cytokines and IgE. CRTH2 receptor antagonists are being assessed for the treatment of chronic allergic diseases including AR [91]. The orally active CRTH2 antagonists AM-211 and AM-461 (Amira) are under clinical development.…”