PXS-5505 (hydrochloride)

PXS-5505 is a pan inhibitor of lysyl oxidase (LOX) and LOX-like oxidases (LOXL; IC₅₀s = 0.493, 0.159, 0.57, 0.18, and 0.19 µM for fibroblast LOX and recombinant human LOXL1-4, respectively).¹ It is selective for LOX and LOXL1-4 over other recombinant human oxidases, including diamine oxidase (DAO), vascular adhesion protein-1 (VAP-1), monoamine oxidase A (MAO-A), and MAO-B (IC₅₀s = >30 µM for all). PXS-5505 (15 mg/kg) reduces bleomycin-induced increases in dermal thickness and the levels of α-smooth muscle actin in a mouse model of systemic sclerosis.² It reduces fibrosis in rodent models of bleomycin-induced pulmonary fibrosis, cardiac ischemia-reperfusion injury, renal unilateral ureteral obstruction, and carbon tetrachloride-induced liver fibrosis. It also reduces collagen crosslinking in KPC cancer-associated fibroblast (CAF) 3D organotypic matrices.¹ PXS-5505 (20 mg/kg) increases survival to a greater extent than gemcitabine alone when administered in combination with the anticancer nucleoside derivative gemcitabine (Item Nos. 11690 | 9003096), reduces gemcitabine-induced increases in collagen levels and stiffness, and reduces liver metastatic burden in autochthonous KPC pancreatic ductal adenocarcinoma mouse models.

WARNING This product is not for human or veterinary use.

1. Chitty, J.L., Yam, M., Perryman, L., et al. A first-in-class pan-lysyl oxidase inhibitor impairs stromal remodeling and enhances gemcitabine response and survival in pancreatic cancer. Nat. Cancer 4(9), 1326-1344 (2023).

2. Yao, Y., Findlay, A., Stolp, J., et al. Pan-lysyl oxidase inhibitor PXS-5505 ameliorates multiple-organ fibrosis by inhibiting collagen crosslinks in rodent models of systemic sclerosis. Int. J. Mol. Sci. 23(10), 5533 (2022).