加洛他滨, Galocitabine

Galocitabine is a cytotoxic drug that inhibits DNA synthesis by inhibiting the activity of the enzyme topoisomerase II. It has been shown to be active against mouse tumor cells in vivo and is used for the treatment of various types of cancer, including lymphoma, leukemia, and carcinomas. Galocitabine also has a role in treating infectious diseases such as tuberculosis and may be useful for treating inflammatory bowel disease. Galocitabine contains a hydroxyl group, which can form non-covalent bonds with fatty acids. This is important because it increases its solubility in water, making it more suitable for use in slow-release formulations.

Galocitabine is an orally available 5-fluorouracil (5-FU) prodrug with potential antineoplastic activity. Upon administration, galocitabine is converted into 5'-deoxy-5-fluorocytidine, 5'-deoxy-fluorouridine, and 5-FU. 5-FU is further metabolized into other cytotoxic metabolites that interfere with RNA and DNA synthesis via inhibition of thymidylate synthase. As a result, this agent eventually inhibits tumor cell growth.