PXS-4787 is a potent and selective inhibitor of lysyl oxidase (LOX) with broad-spectrum activity. It effectively suppresses lysyl oxidase activity by acting on its mechanisms. The compound displays inhibitory effects with IC50 values of 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), and 0.2 μM (rh LOXL4), respectively [1].

PXS-4787, in a concentration and time-dependent manner, inhibits lysyl oxidase—a key enzyme in stabilizing collagen in scar tissue, thereby affecting scar stiffness and appearance. This compound exhibits consistent inhibitory effects across different species. When tested on primary human dermal fibroblasts, PXS-4787 is well-tolerated, and specific dosages (e.g., 10 μM for up to 11 days) can significantly reduce collagen formation, deposition, and crosslinking in these cells. Additionally, a particular dose (10 μM for 48 hours) alters the expression of certain genes in fibroblasts and keratinocytes, such as COL1A1, LOX, GAPDH, and PGK1, indicating its potential for modifying cellular responses related to scarring. Immunofluorescence and RT-PCR studies further confirm the compound's efficacy in reducing collagen in treated groups and in inducing gene expression changes, underscoring its therapeutic potential in managing scar formation and appearance.

PXS-4787, a 3% oil-in-water cream applied topically once daily, reduces collagen deposition and cross-linking in murine injury and fibrosis models over 28 days and enhances scar appearance without compromising tissue strength in porcine injury models over 12 weeks, suggesting a target-driven benefit. In a specific porcine excision injury model using female juvenile pigs weighing 18-20 kg, a 400 mg dose of the cream was applied externally to a 16 cm^2 area once daily starting 1, 2, and 3 weeks post-injury for a duration of 12 weeks. The results indicate an improved scar appearance in relevant in vivo models, supporting the compound's therapeutic potential in wound healing and fibrosis.