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 cream applied to 16 cm 2; external application; once daily, for 28 days) reduces collagen deposition and cross-linkin in a topically applied murine model of injury and fibrosis [1]. PXS-6302 (0.5, 1.5, or 3%, oil in water cream; 400 mg cream applied to 16 cm 2; external application; once daily, for 12 weeks) also significantly improves scar appearance without reducing tissue strength in porcine injury models when applied topically [1]. Animal Model: Porcine excision injury model (female Juvenile pigs, 18-20 kg) [1] Dosage: 0.5, 1.5, or 3%, oil in water cream; 400 mg cream applied to 16 cm 2 Administration: External application; 1, 2 and 3 weeks post-injury; once dayly, for 12 weeks Result: Exhibited significantly higher scores for the 3% treated scars indicating significant improvement in scar appearance.