bilastine

Clinical trial activity

24 trials · 32 clinical orgs · 0 marketing orgs

Earliest trial started Apr 1, 2003 (NCT01108783)

Indications

Mechanism of action

• Histamine H1 receptorINVERSE AGONIST

  HRH1 inverse agonist

  Bilastine is an H1 receptor inverse agonist. The biological effects of histamine in the allergic reaction are mediated through H1 receptors that coexist in active and inactive forms of g-protein-coupled receptors which balance each other. Histamine works as an agonist that pushes the balance to the active side leading to effects such as muscular contraction, bronchospasms, upregulation of endothelial permeability, and stimulation of sensory nerves and cough receptors. H1 antihistamines, like Bilastine, work as inverse agonists that drive the balance toward the inactive side and suppress the effects of histamine. In vitro data have also shown that bilastine exerts antiinflammatory activity by inhibiting the release of histamine, IL-4 and tumor necrosis factor (TNF)-¿ from human mast cells and granulocytes. It has limited penetration across the blood-brain barrier.

  Bilastine has high specificity for H1-receptors while has negligible affinity for 30 other receptors (serotonin, bradykinin, leukotriene-D4, muscarinic M3-receptors, ¿1-adrenoceptors, ß2-adrenoceptors, and H2- and H3-histamine receptors).

  • Histamine H1 receptor (HRH1) ↗