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

Prostaglandin D₂ (PGD₂) is a major cyclooxygenase mediator that is synthesized by activated human mast cells and other immune cells. The biological effects of PGD₂ are mediated by D-prostanoid (DP₁), DP₂ (CRTH2) and thromboxane prostanoid (TP) receptors that are expressed on several immune and non-immune cells involved in allergic inflammation. PGD₂ exerts various proinflammatory effects relevant to the pathophysiology of allergic disorders. Several selective, orally active, DP₂ receptor antagonists and a small number of DP₁ receptor antagonists are being developed for the treatment of allergic disorders.

The role of DP₂ and DP₁ receptor antagonists in the treatment of asthma and allergic rhinitis.

Head-to-head studies that compare DP₁ antagonists with the standard treatment for allergic rhinitis are necessary to verify the role of these novel drugs as mono- or combination therapies. Further clinical trials are necessary to verify whether DP₂ antagonists as monotherapies or, more likely, as add-on therapies, will be effective for the treatment of different phenotypes of adult and childhood asthma. Long-term studies are necessary to evaluate the safety of targeted anti-PGD₂ treatments.