2-fluorofucose

SGN-2FF (2-fluorofucose) is an orally bioavailable small molecule inhibitor of glycoprotein fucosylation. It acts by depleting the fucosylation substrate GDP-fucose and directly inhibiting fucosyltransferase enzymes, resulting in the production of afucosylated glycoproteins, including antibodies[1][5]. By altering glycoprotein fucosylation, SGN-2FF modulates cell-cell interactions within the tumor microenvironment and enhances immune-mediated antitumor activity through both direct and indirect effects on immune cells and tumor cells[2]. Preclinical studies demonstrated antitumor activity in multiple mouse models. In a phase I clinical trial for advanced solid tumors, SGN-2FF showed proof-of-mechanism and preliminary antitumor activity but was associated with thromboembolic events that led to study termination[6].

Other names

2-fluorofucose