Navarixin

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Navarixin is a small molecule drug that acts as a selective antagonist of the CXCR2 receptor, which is a chemokine receptor involved in the recruitment of neutrophils to sites of inflammation. It is being investigated for its potential use in treating inflammatory diseases and certain types of cancer.

Mechanism of Action

Navarixin works by inhibiting the activity of the CXCR2 receptor, which is a G protein-coupled receptor (GPCR) that binds to chemokines such as interleukin-8 (IL-8). By blocking this receptor, navarixin prevents the chemotactic migration of neutrophils, thereby reducing inflammation and tissue damage associated with excessive neutrophil infiltration.

Pharmacokinetics

Navarixin is administered orally and has a bioavailability of approximately 50%. It is metabolized primarily in the liver by the cytochrome P450 enzyme system, particularly CYP3A4. The half-life of navarixin is approximately 12 hours, allowing for once or twice daily dosing.

Clinical Trials

Navarixin has been evaluated in several clinical trials for its efficacy and safety in treating conditions such as chronic obstructive pulmonary disease (COPD), asthma, and cystic fibrosis. In these trials, navarixin demonstrated a reduction in neutrophil counts in the lungs and improved lung function in patients with COPD and asthma.

Adverse Effects

Common adverse effects of navarixin include headache, nausea, and dizziness. Some patients may experience elevated liver enzymes, which necessitates monitoring of liver function during treatment.

Research and Development

Navarixin is currently in the investigational stage and has not yet received approval from major regulatory agencies such as the Food and Drug Administration (FDA) or the European Medicines Agency (EMA). Ongoing research is focused on optimizing its therapeutic potential and minimizing side effects.

Also see

• CXCR2
• Chemokine receptor
• Neutrophil
• Inflammation
• Chronic obstructive pulmonary disease
• Asthma