Tegafur

Tegafur is a anticancer drug.it is a fluorouracil derivative, in vitro it has no anti-tumor effect, after it goes into the human body ,by the role of the liver drug metabolism enzymes and microsomal enzymes P-450 in the liver, its tetrahydrofuran ring is taken off, fluorouracil (5-FU)is gradually released to produce cytotoxicity. Variety of tumor inhibition is similar to 5-FU, its mechanism of inhibition is inhibiting thymidine synthetase, blocking deoxy thymidylate converting to pyrimidine nucleotide, thereby interfering and blocking the synthesis of DNA, RNA and protein .
Tegafur index of chemotherapy is twice of 5-FU and toxicity is 1/6~1/5 of 5-FU ,there is cross-resistance between 5-FU and the product,it belongs to cycle-specific drugs, tegafur belongs to the time-dependent cytostatic, preferable absorption after oral , Tmax is 2h, it slowly releases 5-FU in vivo, blood level is not very high, it can maintain a longer time, so it has a low toxicity in vivo.the Intravenous infusion is better than the one-time injection. After the drug going into the body, it is evenly distributed in the liver, small intestine, spleen, lung, kidney and brain, liver and kidney having the highest concentrations. T1/2 is 5~18.6h. Inhibition of DNA, RNA synthesis can maintain 12~20h. After 24h, the content of each tissue is significantly reduced. It is Mainly excreted in the urine and respiratory tract , within 24h after administration, 23% is by the urine excretion of the prototype , 55% is excreted from the respiratory tract in the form of CO2. This product is highly fat-soluble, widely distributed, easily through the blood-brain barrier, its cerebrospinal fluid concentration is higher than 5-FU.
This product is effective against a variety of solid tumors, it is primarily used for the treatment of digestive system cancers, tegafur has a effective rate of 30% to 33% on gastric cancer ,it has a certain effect on colon cancer, colorectal cancer, lung cancer, primary and metastatic liver cancer, pancreatic cancer , cholangiocarcinoma, gallbladder cancer, prostate cancer, kidney cancer, bladder cancer . It can also be used to treat breast cancer, head and neck squamous cell carcinoma, lung cancer and liver cancer. It is Also used as a radiation sensitizer before and after surgery treatment to prevent cancer recurrence, proliferation and metastasis. Overall, the efficacy of this product is a little better than 5-FU.
The above information is edited by the Chemicalbook of Tian Ye.

this product is a derivative of 5-fluorouracil, the role and application of the product is the same as 5-fluorouracil, but it has less toxicity and its chemotherapy index is high. After the activion by the liver in vivo ,it becomes 5-fluorouracil to play a role in cancer. It is effective on Gastric cancer, colon cancer, colorectal cancer, pancreatic cancer and breast cancer, lung cancer.

Tegafur is an orally bioavailable prodrug form of 5-fluorouracil (5-FU; ). It is converted to 5-FU in vivo enzymatically or by cytochrome P450 oxidation. Tegafur inhibits proliferation of HT-29, BxPC-3, and Panc02 cells (IC₅₀s = 201, 172, and 179 μM, respectively). It also reduces tumor growth in an HT-27 colon carcinoma mouse xenograft model when administered at a dose of 50 mg/kg and in a 4-1ST gastric carcinoma mouse xenograft model when used in combination with uracil. Formulations containing tegafur, in combination with uracil, have been used in the treatment of cancer.

Poison by ingestion. Moderately toxic to humans by intravenous route. Moderately toxic experimentally by intraperitoneal, intravenous, and subcutaneous routes. Experimental teratogenic data. Human systemic effects: nausea and vomiting. Experimental reproductive effects. Questionable human carcinogen producing gastrointestinal tumors. Human mutation data reported. Used as an anti-cancer agent. When heated to decomposition it emits very toxic fumes of Fand NOx.