Selectin inhibitors: a patent review

Importance of the field: Selectins play a significant and well-documented role in inflammation and immune response. They initiate tethering and rolling of blood borne leukocytes leading to their activation, adhesion and subsequent extravazation into tissues. This is important for healthy immune response and tissue repair. However, dysregulation of selectins leads to exacerbation of disease. Atherosclerosis, restenosis, deep venous thrombosis and tumor metastasis are just a few of the diseases in which selectin blockade has been demonstrated to ameliorate disease pathology. Thus, selectins remain attractive targets for amelioration of disease. Areas covered in this review: Summarized here are new patents/patent applications on selectin inhibition published since our last review in 2003 and any significant changes or progress made in demonstrating clinical safety and efficacy of therapeutics covered by patents/ patent applications reviewed in 2003. What the reader will gain: A comprehensive review of new developments in the field of selectin inhibition through discussion of patents/ patent applications from 2003 to August 2009, reports on clinical results where available and selected literature. Take home message: The field of selectin inhibition has matured significantly in recent years in the ability to inhibit selectin/ligand interactions with drug-like molecules and to demonstrate disease modification in human trials.