BI-1467335

BI-1467335 is an inhibitor of vascular adhesion protein-1 (VAP-1; IC₅₀ = <100 nM), also known as semicarbazide-sensitive amine oxidase (SSAO), an enzyme with roles in leukocyte adhesion and transmigration.¹ It is selective for VAP-1 over monoamine oxidase B (MAO-B) and diamine oxidase (DAO; IC₅₀s = >1,000 and >10,000 nM, respectively). Oral administration of BI-1467335 (10 mg/kg per day) reduces plasma total cholesterol, LDL, and glucose levels, as well as decreases the recruitment of macrophages to atherosclerotic lesions and the area of atherosclerotic plaques, in a cholesterol-fed rabbit model.² It reduces neutrophil lung infiltration induced by K. pneumoniae in mice when administered at a dose of 6 mg/kg.³ It also reduces airway hyperreactivity in a mouse model of rhinovirus-exacerbated allergy-induced asthma.

WARNING This product is not for human or veterinary use.

1. Deodhar, M., Findlay, A.D., Foot, J.S., et al. Substituted 3-haloallylamine inhibitors of SSAO and uses thereof. (2020).

2. Wang, S.-H., Yu, T.-Y., Hung, C.-S., et al. Inhibition of semicarbazide-sensitive amine oxidase reduces atherosclerosis in cholesterol-fed New Zealand white rabbits. Sci. Rep. 8(1), 9249 (2018).

3. Schilter, H.C., Collison, A., Russo, R.C., et al. Effects of an anti-inflammatory VAP-1/SSAO inhibitor, PXS-4728A, on pulmonary neutrophil migration. Respir. Res. 16(1), 42 (2018).