4-deoxy-4-fluorogalactose

4-deoxy-4-fluorogalactose (4DFG) is a first-generation galactose-based antimetabolite being developed for the treatment of glioblastoma (GBM). It targets the galactose scavenging pathway, which GBM cells utilize as a substrate for metabolism and glycan synthesis. 4DFG is imported into cells via glucose transporters Glut3 and Glut14 and processed through the Leloir metabolic pathway. Once inside, it acts as a potent chemotherapeutic by inhibiting glycolytic and mitochondrial flux and disrupting the synthesis of glycans, particularly the incorporation of galactose (Gal) and N-acetylgalactosamine (GalNAc) sugars. Preclinical studies at Houston Methodist have demonstrated that 4DFG can significantly increase survival in intracranial GBM models and may bolster existing therapies.

Other names

4-deoxy-4-fluoro-D-galactose4-fluoro-4-deoxygalactose