PXS-6302 is an irreversible inhibitor of lysyl oxidase with IC50s of 3.7 μM for Bovine LOX, 3.4 μM for rh LOXL1, 0.4 μM for rh LOXL2, 1.5 μM for rh LOXL3, 0.3 μM for rh LOXL4, respectively. PXS-6302 can readily penetrate the skin, reduces collagen deposition and cross-linking, and significantly improves scar appearance without reducing tissue strength. PXS-6302 also has potentially broader applications in other fibrotic diseases.

PXS-6302 exhibits high permeability to across a monolayer of cells, for example, Caco-2 or MDCKII cells [1].

Topical treatment with PXS-6302 inhibits LOX, reduces crosslinking, and improves scar appearance in excisional and burn injury porcine models [1]. PXS-6302 (1.5%; oil in water cream; 500 mg applied to 16 cm²; external application; once daily for 28 days) reduces collagen deposition and crosslinking in a murine model of injury and fibrosis [1]. In porcine injury models, PXS-6302 (0.5, 1.5, or 3%; oil in water cream; 400 mg applied to 16 cm²; external application; once daily for 12 weeks) significantly improves scar appearance without reducing tissue strength [1]. In a porcine excision injury model (female juvenile pigs, 18-20 kg) [1], dosages of 0.5, 1.5, or 3% (oil in water cream; 400 mg applied to 16 cm²) were administered externally once daily for 12 weeks, starting at 1, 2, and 3 weeks post-injury, resulting in significantly higher scores for the 3% treated scars, indicating significant improvement in scar appearance.