Combination of | |
---|---|
Tegafur | Antineoplastic drug |
Gimeracil | Enzyme inhibitor |
Oteracil | Enzyme inhibitor |
Clinical data | |
Trade names | Teysuno |
Other names | S-1 [1] |
AHFS/ Drugs.com | UK Drug Information |
Pregnancy category |
|
Routes of administration | By mouth |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
CAS Number | |
PubChem CID | |
KEGG |
Tegafur/gimeracil/oteracil, sold under the brand name Teysuno among others is a fixed-dose combination medication used for the treatment of advanced gastric cancer when used in combination with cisplatin, [3] and also for the treatment of head and neck cancer, colorectal cancer, non–small-cell lung, breast, pancreatic, and biliary tract cancers. [4]: 213
The most common severe side effects when used in combination with cisplatin include neutropenia (low levels of neutrophils, a type of white blood cell), anaemia (low red blood cell counts) and fatigue (tiredness). [3]
Tegafur/gimeracil/oteracil (Teysuno) was approved for medical use in the European Union in March 2011. [3]
In the European Union, tegafur/gimeracil/oteracil is indicated for the treatment of advanced gastric cancer when given in combination with cisplatin. [3]
In the European Union, tegafur/gimeracil/oteracil must not be used in the following groups:
Tegafur is the chemotherapeutic agent. It is a prodrug of the active substance fluorouracil (5-FU). [3] Tegafur, is a cytotoxic medicine (a medicine that kills rapidly dividing cells, such as cancer cells) that belongs to the ‘anti-metabolites’ group. Tegafur is converted to the medicine fluorouracil in the body, but more is converted in tumor cells than in normal tissues. [3] Fluorouracil is very similar to pyrimidine. [3] Pyrimidine is part of the genetic material of cells (DNA and RNA). [3] In the body, fluorouracil takes the place of pyrimidine and interferes with the enzymes involved in making new DNA. [3] As a result, it prevents the growth of tumor cells and eventually kills them. [3]
Gimeracil inhibits the degradation of fluorouracil by reversibly blocking the dehydrogenase enzyme dihydropyrimidine dehydrogenase (DPD). This results in higher 5-FU levels and a prolonged half-life of the substance. [5]
Oteracil mainly stays in the gut because of its low permeability, where it reduces the production of 5-FU by blocking the enzyme orotate phosphoribosyltransferase. Lower 5-FU levels in the gut result in a lower gastrointestinal toxicity. [5]
Within the medication, the molar ratio of the three components (tegafur:gimeracil:oteracil) is 1:1:0.4. [6]
It is being developed for the treatment of hepatocellular carcinoma. [7] and has activity in esophageal,(Perry Chapter 33) breast,[ citation needed] cervical,[ citation needed] and colorectal cancer. [8]