Product Information
Registration Status: ActiveSIN03692P
UFT CAPSULE is approved to be sold in Singapore with effective from 1989-09-22. It is marketed by PHARMAFORTE SINGAPORE PTE LTD, with the registration number of SIN03692P.
This product contains Tegafur 100mg, and Uracil 224mg in the form of CAPSULE. It is approved for ORAL use.
This product is manufactured by TAIHO PHARMACEUTICAL CO LTD in JAPAN.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
Tegafur (INN, BAN, USAN) is a prodrug of [DB00544] (5-FU), an antineoplastic agent used as the treatment of various cancers such as advanced gastric and colorectal cancers. It is a pyrimidine analogue used in combination therapies as an active chemotherapeutic agent in conjunction with [DB09257] and [DB03209], or along with [DB00544] as [DB09327]. Tegafur is usually given in combination with other drugs that enhance the bioavailability of the 5-FU by blocking the enzyme responsible for its degradation, or serves to limit the toxicity of 5-FU by ensuring high concentrations of 5-FU at a lower dose of tegafur [L933]. When converted and bioactivated to 5-FU, the drug mediates an anticancer activity by inhibiting thymidylate synthase (TS) during the pyrimidine pathway involved in DNA synthesis. 5-FU is listed on the World Health Organization's List of Essential Medicines.
Indication
Indicated for the treatment of cancer usually in combination with other biochemically modulating drugs. Indicated in adults for the treatment of advanced gastric cancer when given in combination with [DB00515] [L933]. Indicated for the first-line treatment of metastatic colorectal cancer with [DB03419] and calcium folinate [L934].
Mechanism of Action
The transformation of 2'-deoxyurindylate (dUMP) to 2'-deoxythymidylate (dTMP) is essential in driving the synthesis of DNA and purines in cells [T28]. Thymidylate synthase catalyzes the conversion of dUMP to dTMP, which is a precursor of thymidine triphosphate (TTP), one of the four deoxyribonucleotides required for DNA synthesis [A31546]. After administration into the body, tegafur is converted into the active antineoplastic metabolite, fluorouracil (5-FU). In tumour cells, 5-FU undergoes phosphorylation to form the active anabolites, including 5-fluorodeoxyuridine monophosphate (FdUMP) [L933]. FdUMP and reduced folate are bound to thymidylate synthase leading to formation of a ternary complex which inhibits DNA synthesis [L933]. In addition, 5-fluorouridine-triphosphate (FUTP) is incorporated into RNA causing disruption of RNA functions [L933].
Pharmacokinetics
- Absorption
- Tegafur displays a dose-proportional pharmacokinetic properties. Tegafur is rapidly and well absorbed into the systemic circulation, reaching the peak plasma concentration within 1 to 2 hours of administration [L934].
- Distribution
- The volume of distribution based on apparent volume of distribution and urinary excretion data of tegafur is 16 L/m^2 [L933].
- Metabolism
- Hepatic CYP2A6 is the predominant enzyme that mediates 5-hydroxylation of tegafur to generate 5'-hydroxytegafur. This metabolite is unstable and undergoes spontaneous degradation to form 5-FU, which is an active antineoplastic agent that exerts a pharmacological action on tumours. 5-FU is rapidly metabolised by the liver enzyme dihydropyrimidine dehydrogenase (DPD) [A31546].
- Elimination
Clearance
No pharmacokinetic data available.
Toxicity
Oral LD50 value in rat, mouse and dog are 930mg/kg, 775mg/kg, and 34mg/kg, respectively [MSDS]. Continuous exposure to tegafur may cause physical defects in the developing embryo (teratogenesis). Acute toxicity from the combination use of tegafur was associated with nausea, vomiting, diarrhoea, mucositis, gastrointestinal irritation, bleeding, bone marrow depression, and respiratory failure [L933]. Overdose may lead to fatal complications [L934]. In case of overdose, appropriate therapeutic and supportive medical interventions should be implemented.
Active Ingredient/Synonyms
1-(2-Tetrahydrofuryl)-5-fluorouracil | Tegafur |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.
Description
Nitrogen mustard derivative of uracil. It is a alkylating antineoplastic agent that is used in lymphatic malignancies, and causes mainly gastrointestinal and bone marrow damage. [PubChem]
Indication
Used for its antineoplastic properties.
Mechanism of Action
After activation, it binds preferentially to the guanine and cytosine moieties of DNA, leading to cross-linking of DNA, thus inhibiting DNA synthesis and function.
Active Ingredient/Synonyms
5-(Di-2-chloroethyl)aminouracil | 5-[Bis(2-chloroethyl)amino]-2,4(1H,3H)-pyrimidinedione | 5-[Di(beta-chloroethyl)amino]uracil | 5-Aminouracil mustard | 5-N,N-Bis(2-chloroethyl)aminouracil | Aminouracil mustard | Uracil mustard | Uracil nitrogen mustard | Uramustine | Uracil mustard |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.