Tegafur/gimeracil/oteracil
Combination drug
From Wikipedia, the free encyclopedia
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
| 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 | |
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]
Medical uses
Contraindications
In the European Union, tegafur/gimeracil/oteracil must not be used in the following groups:
- people receiving another fluoropyrimidine (a group of anticancer medicines that includes tegafur/gimeracil/oteracil) or who have had severe and unexpected reactions to fluoropyrimidine therapy;[3]
- people known to have no DPD enzyme activity, as well as people who, within the previous four weeks, have been treated with a medicine that blocks this enzyme;[3]
- pregnant or breastfeeding women;[3]
- people with severe leucopenia, neutropenia, or thrombocytopenia (low levels of white cells or platelets in the blood);[3]
- people with severe kidney problems requiring dialysis;[3]
- people who should not be receiving cisplatin.[3]
Mechanism of action
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]
Research
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]
Tegafur
Gimeracil
Oteracil potassium
