Icalcaprant

Icalcaprant_structure.png

Icalcaprant is a pharmaceutical compound that acts as a selective antagonist of the prostaglandin D2 receptor 2 (DP2), also known as the CRTh2 receptor. It is primarily investigated for its potential therapeutic effects in treating inflammatory conditions such as asthma and allergic rhinitis.

Mechanism of Action

Icalcaprant functions by selectively blocking the DP2 receptor, which is a G-protein coupled receptor involved in the inflammatory response. The DP2 receptor is activated by prostaglandin D2 (PGD2), a lipid compound that plays a significant role in mediating allergic and inflammatory responses. By inhibiting this receptor, icalcaprant reduces the recruitment and activation of eosinophils, basophils, and Th2 lymphocytes, which are key players in the pathophysiology of allergic diseases.

Pharmacokinetics

Icalcaprant is administered orally and exhibits a favorable pharmacokinetic profile with good bioavailability. It is metabolized primarily in the liver and excreted via the kidneys. The half-life of icalcaprant allows for once-daily dosing, which is advantageous for patient compliance.

Clinical Trials

Icalcaprant has undergone several clinical trials to evaluate its efficacy and safety in treating asthma and other allergic conditions. In phase II trials, icalcaprant demonstrated a significant reduction in asthma exacerbations and improved lung function compared to placebo. However, further studies are needed to confirm these findings and to assess long-term safety.

Adverse Effects

The most common adverse effects reported in clinical trials include headache, nausea, and dizziness. These side effects are generally mild and transient. Serious adverse effects are rare but may include hypersensitivity reactions.

Regulatory Status

As of the latest update, icalcaprant is not yet approved by major regulatory agencies such as the FDA or EMA. It remains an investigational drug undergoing further clinical evaluation.

Research and Development

Research on icalcaprant is ongoing, with studies focusing on its potential use in other inflammatory conditions beyond asthma, such as chronic obstructive pulmonary disease (COPD) and atopic dermatitis.

Also see

• Prostaglandin D2 receptor 2
• Asthma treatment
• Allergic rhinitis
• Eosinophil
• G-protein coupled receptor