Tetrahydrodeoxyhypusine

Tetrahydrodeoxyfluorouracil, also known as Tetrahydro-DFUR or THDFUR, is a prodrug of 5-fluorouracil (5-FU). It is a derivative of the pyrimidine analog 5-fluorouracil, which is a widely used chemotherapy agent. Tetrahydrodeoxyfluorouracil is metabolized in the body to 5-FU, which then exerts its cytotoxic effects by interfering with DNA and RNA synthesis. This mechanism of action makes it effective against various types of cancer, particularly solid tumors.

The development of Tetrahydrodeoxyfluorouracil aimed to improve the therapeutic index of 5-FU by potentially reducing its systemic toxicity while maintaining or enhancing its anti-cancer activity. This prodrug approach often involves modifications that alter the drug's absorption, distribution, metabolism, or excretion, thereby influencing its pharmacokinetic profile. Tetrahydrodeoxyfluorouracil is typically administered orally.

Once absorbed, Tetrahydrodeoxyfluorouracil undergoes enzymatic conversion within the body to release the active 5-FU. This conversion process can be influenced by various factors, including the specific enzymes present in tumor cells and healthy tissues. The subsequent action of 5-FU involves its incorporation into RNA, leading to the production of faulty proteins, and its inhibition of thymidylate synthase, an enzyme crucial for DNA synthesis. This dual action ultimately leads to cell death, particularly in rapidly dividing cancer cells. Clinical trials have evaluated the efficacy and safety of Tetrahydrodeoxyfluorouracil in treating various malignancies, and it has been utilized in some regions as part of cancer treatment regimens.