Mast cell stabilizers prevent or control certain allergic disorders. In particular, Lodoxamide is a mast cell stabilizer. Furthermore, Lodoxamide inhibits mast cell degranulation in vitro and in vivo.

Lodoxamide is effective in reducing tryptase and histamine levels and the recruitment of inflammatory cells in the tear fluid after allergen challenge, as well as tear eosinophil cationic protein and leukotrienes (BLT and CysLT1). Moreover, Lodoxamide downregulates ICAM-1 expression on the continuously cultured, differentiated conjunctival cell line.

In this study, researchers evaluated the effect of Lodoxamide eye drops on the inflammatory early-phase reaction changes induced by an allergen-specific conjunctival challenge. Lodoxamide is potent in the prevention of histamine release in several animal models. Lodoxamide has the additional effects of being a hydroxyl radical scavenger and an inhibitor of xanthine oxidase and neutrophil chemotaxis. On the basis of these properties, Lodoxamide tromethamine decreases ischemia-reperfusion injury in cardiac and spinal cord models.

Lodoxamide strongly inhibits the release of eosinophil peroxidase after IgA-dependent activation and, to a lesser extent, the release of eosinophil cationic protein and eosinophil-derived neurotoxin. Moreover, the release of cytotoxic mediators evaluated in an antibody-dependent cytotoxicity assay against parasitic targets was also significantly reduced, not only in the case of human eosinophils but also in a rat eosinophil-mast cell model of cytotoxicity. Lodoxamide induces a reduction in the total number of inflammatory cells and neutrophils during the early-phase reaction. In addition, Lodoxamide reduces early clinical events and cellular changes after ASCC consistently with its activity as a mast-cell stabilizer.

Taken together, Lodoxamide is an antiallergic drug acting as a mast-cell stabilizer, which is effective in the treatment of allergic conjunctivitis.

G Ciprandi, et al. Antiallergic activity of topical lodoxamide on in vivo and in vitro models. Allergy. 1996 Dec;51(12):946-51.