OGT 719

OGT 719 is a novel, orally and intravenously bioavailable **nucleoside analogue** that consists of a galactose moiety covalently attached to the N1 position of 5-fluorouracil (5-FU)[1][2][3][5][7]. It is designed to selectively target hepatocytes and hepatocellular carcinoma (HCC) cells through the **asialoglycoprotein receptor (ASGP-R)**, aiming to enhance activity against primary and metastatic liver cancers while reducing systemic toxicity typically observed with standard 5-FU therapy[1][3][5]. OGT 719 is a **poorly metabolized prodrug** of 5-fluorouracil; it localizes preferentially in the liver, where it is slowly converted to 5-FU, resulting in a localized cytotoxic effect[2][3][5]. Activity stems primarily from inhibition of thymidylate synthase (TYMS), mirroring the mechanism of its parent compound, 5-FU[1][3][5]. Clinical studies in advanced cancers, primarily hepatocellular carcinoma and colorectal liver metastases, used both oral and intravenous routes with a typical oral bioavailability around 25%, an elimination half-life between 1.5 and 4 hours, and demonstrated acceptable safety, although efficacy was limited and no objective tumor responses were observed[5][7]. Development of OGT 719 has since been discontinued[3].

Other names

1-galactopyranosyl-5-fluorouracil