Peringatan Keamanan

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.

Tegafur

DB09256

small molecule approved investigational

Deskripsi

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.

Struktur Molekul 2D

Berat 200.169
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half life of tegafur is approximately 11 hours [L934].
Volume Distribusi The volume of distribution based on apparent volume of distribution and urinary excretion data of tegafur is 16 L/m^2 [L933].
Klirens (Clearance) No pharmacokinetic data available.

Absorpsi

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.

Metabolisme

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.

Rute Eliminasi

Following oral administration, about less 20% of total tegafur is excreted unchanged in the urine L934.

Farmakogenomik

7 Varian
DPYD (rs3918290)

The presence of this genotype in DPYD is associated with an increased risk of drug-related toxicity from tegafur therapy.

DPYD (rs55886062)

The presence of this genotype in DPYD is associated with an increased risk of drug-related toxicity from tegafur therapy.

DPYD (rs67376798)

The presence of this genotype in DPYD may be associated with an increased risk of drug-related toxicity from tegafur therapy.

DPYD (rs1801158)

The presence of this genotype in DPYD may be associated with an increased risk of drug-related toxicity from tegafur therapy.

DPYD (rs1801159)

The presence of this genotype in DPYD may be associated with an increased risk of drug-related toxicity from tegafur therapy.

DPYD (rs1801160)

The presence of this genotype in DPYD may be associated with an increased risk of drug-related toxicity from tegafur therapy.

DPYD (rs1801265)

The presence of this genotype in DPYD may be associated with an increased risk of drug-related toxicity from tegafur therapy.

Interaksi Makanan

2 Data
  • 1. Drink plenty of fluids. Drinking water is important to prevent dehydration when taking Teysuno.
  • 2. Take on an empty stomach. Food does not impact the bioavailability of tegafur. Food does affect other ingredients in the combination product Teysuno. Take Teysuno at least 1 hour before or after eating.

Interaksi Obat

1268 Data
Deferasirox The serum concentration of Tegafur can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Tegafur can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Tegafur can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Tegafur can be decreased when it is combined with Teriflunomide.
Mifepristone The serum concentration of Tegafur can be increased when it is combined with Mifepristone.
Cimetidine The serum concentration of Tegafur can be increased when it is combined with Cimetidine.
Gemcitabine The serum concentration of Tegafur can be increased when it is combined with Gemcitabine.
Sorafenib The risk or severity of QTc prolongation can be increased when Sorafenib is combined with Tegafur.
Abiraterone The metabolism of Tegafur can be decreased when combined with Abiraterone.
Cyproterone acetate The metabolism of Tegafur can be increased when combined with Cyproterone acetate.
Metronidazole The serum concentration of Tegafur can be increased when it is combined with Metronidazole.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Tegafur.
Dicoumarol The risk or severity of bleeding can be increased when Tegafur is combined with Dicoumarol.
Phenindione The risk or severity of bleeding can be increased when Tegafur is combined with Phenindione.
4-hydroxycoumarin The risk or severity of bleeding can be increased when Tegafur is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of bleeding can be increased when Tegafur is combined with Coumarin.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Tegafur is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of bleeding can be increased when Tegafur is combined with Fluindione.
Clorindione The risk or severity of bleeding can be increased when Tegafur is combined with Clorindione.
Diphenadione The risk or severity of bleeding can be increased when Tegafur is combined with Diphenadione.
Tioclomarol The risk or severity of bleeding can be increased when Tegafur is combined with Tioclomarol.
Albendazole The metabolism of Tegafur can be increased when combined with Albendazole.
Primidone The metabolism of Tegafur can be increased when combined with Primidone.
Osimertinib The serum concentration of Tegafur can be decreased when it is combined with Osimertinib.
Vemurafenib The serum concentration of Tegafur can be increased when it is combined with Vemurafenib.
Icosapent Icosapent may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Tegafur which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Tegafur which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Tegafur which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Tegafur which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Tegafur which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Tegafur which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Tegafur which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Tegafur which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Tegafur which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Tegafur which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Tegafur which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Tegafur which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Tegafur which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Tegafur which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Tegafur which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Tegafur which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Tegafur which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Tegafur which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Tegafur which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Tegafur which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Tegafur which could result in a higher serum level.
Meloxicam The risk or severity of methemoglobinemia can be increased when Tegafur is combined with Meloxicam.
Carprofen Carprofen may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Tegafur which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Tegafur which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Tegafur which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Tegafur which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Tegafur which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Tegafur which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Tegafur which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Tegafur which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Tegafur which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Tegafur which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Tegafur which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Tegafur which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Tegafur which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Tegafur which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Tegafur which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Tegafur which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Tegafur which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Tegafur which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Tegafur which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Tegafur which could result in a higher serum level.
Cephalothin Group Cephalothin Group may decrease the excretion rate of Tegafur which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Tegafur which could result in a higher serum level.
Latamoxef Latamoxef may decrease the excretion rate of Tegafur which could result in a higher serum level.
Nimesulide Nimesulide may decrease the excretion rate of Tegafur which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Tegafur which could result in a higher serum level.
Metamizole Metamizole may decrease the excretion rate of Tegafur which could result in a higher serum level.
Zomepirac Zomepirac may decrease the excretion rate of Tegafur which could result in a higher serum level.
Ceftobiprole Ceftobiprole may decrease the excretion rate of Tegafur which could result in a higher serum level.

Target Protein

Thymidylate synthase TYMS

Referensi & Sumber

Artikel (PubMed)
  • PMID: 22824079
    Tsuburaya A, Morita S, Kodera Y, Kobayashi M, Shitara K, Yamaguchi K, Yoshikawa T, Yoshida K, Yoshino S, Sakamoto J: A randomized phase II trial to elucidate the efficacy of capecitabine plus cisplatin (XP) and S-1 plus cisplatin (SP) as a first-line treatment for advanced gastric cancer: XP ascertainment vs. SP randomized PII trial (XParTS II). BMC Cancer. 2012 Jul 23;12:307. doi: 10.1186/1471-2407-12-307.
  • PMID: 25206296
    Yang J, Zhou Y, Min K, Yao Q, Xu CN: S-1-based vs non-S-1-based chemotherapy in advanced gastric cancer: a meta-analysis. World J Gastroenterol. 2014 Sep 7;20(33):11886-93. doi: 10.3748/wjg.v20.i33.11886.
  • PMID: 11098484
    Kohne CH, Peters GJ: UFT: mechanism of drug action. Oncology (Williston Park). 2000 Oct;14(10 Suppl 9):13-8.
Textbook
  • ISBN: 978-0-7020-3471-8
    55. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 680-681). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 5 • International brands: 22
Produk
  • Teysuno
    Capsule • - • Oral • EU • Approved
  • Teysuno
    Capsule • - • Oral • EU • Approved
  • Teysuno
    Capsule • - • Oral • EU • Approved
  • Teysuno
    Capsule • - • Oral • EU • Approved
  • Teysuno
    Capsule • - • Oral • EU • Approved
International Brands
  • Ai Yi — Hengrui
  • ESUEEW AN T — Sawai Seiyaku
  • Fimer — LKM
  • Ftorafur — Grindeks
  • Furil — Lotus Pharmaceuticals
  • Futraful — Taiho
  • Icarus — Koa Isei
  • Lunacin — Sawai Seiyaku
  • NKS-1 T — Nippon Kayaku
  • Qi Xing — Hualu Pharmaceutical

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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