5-azaorotic Acid
5-azaorotic Acid Uses, Dosage, Side Effects, Food Interaction and all others data.
5-azaorotic Acid is an adjunct to antineoplastic therapy, used to reduce the toxic side effects associated with chemotherapy. Approved by the European Medicines Agency (EMA) in March 2011, 5-azaorotic Acid is available in combination with Gimeracil and Tegafur within the commercially available product "Teysuno". The main active ingredient in Teysuno is Tegafur, a pro-drug of Fluorouracil (5-FU), which is a cytotoxic anti-metabolite drug that acts on rapidly dividing cancer cells. By mimicking a class of compounds called "pyrimidines" that are essential components of RNA and DNA, 5-FU is able to insert itself into strands of DNA and RNA, thereby halting the replication process necessary for continued cancer growth.
5-azaorotic Acid's main role within Teysuno is to reduce the activity of 5-FU within normal gastrointestinal mucosa, and therefore reduce's gastrointestinal toxicity . It functions by blocking the enzyme orotate phosphoribosyltransferase (OPRT), which is involved in the production of 5-FU.
| Trade Name | 5-azaorotic Acid |
| Generic | Oteracil |
| Oteracil Other Names | 5-azaorotic acid, Allantoxanic acid, Oteracil, Oxonate, Oxonic Acid |
| Type | |
| Formula | C4H3N3O4 |
| Weight | Average: 157.0843 Monoisotopic: 157.012355599 |
| Protein binding | Oteracil, gimeracil, 5-FU, and tegafur are 8.4%, 32.2%, 18.4%, and 52.3% protein bound, respectively . |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
5-azaorotic Acid is a chemotherapy agent used in combination with tegafur, cisplatin and gimeracil to treat advanced gastric cancer.
5-azaorotic Acid is used as an adjunct to antineoplastic therapy. When used within the product Teysuno, oteracil is indicated for the treatment of adults with advanced gastric (stomach) cancer when given in combination with cisplatin.
5-azaorotic Acid is also used to associated treatment for these conditions: Advanced Gastric Cancer
How 5-azaorotic Acid works
5-azaorotic Acid's main role within Teysuno is to reduce the activity of 5-FU within normal gastrointestinal mucosa, and therefore reduce's gastrointestinal toxicity . It functions by blocking the enzyme orotate phosphoribosyltransferase (OPRT), which is involved in the production of 5-FU.
Food Interaction
- Take separate from meals. 5-azaorotic Acid should be separated from meals by at least one hour before and after eating.
Volume of Distribution
Although no intravenous data are available for Teysuno in humans, the volume of distribution could be roughly estimated from the apparent volume of distribution and urinary excretion data as 16 l/m2, 17 l/m2, and 23 l/m2 for tegafur, gimeracil and oteracil, respectively .
Elimination Route
After administration of a single dose of 50 mg Teysuno (expressed as tegafur content), median Tmax for Teysuno components tegafur, gimeracil, and oteracil was 0.5, 1.0, and 2.0 hours, respectively .
Half Life
Following a single dose of Teysuno, T1/2 values ranged from 6.7 to 11.3 hours for tegafur, from 3.1 to 4.1 hours for gimeracil, and from 1.8 to 9.5 hours for oteracil .
Elimination Route
Following a single dose of Teysuno, approximately 3.8% to 4.2% of administered tegafur, 65% to 72% of administered gimeracil, and 3.5% to 3.9% of administered oteracil were excreted unchanged in the urine .
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