Peringatan Keamanan

High doses of tegafur are reported to present unique central nervous system toxicity. The oral administration of tegafur has been reported to present toxicity but the usage of the combo product tegafur/uracil have presented higher levels of 5-fluorouracil without the toxic effects or oral tegafur.L1565

Tegafur-uracil

DB09327

small molecule approved investigational

Deskripsi

Tegafur-uracil is an anti-tumor compound containing tegafur (1-(2-tetrahydrofuryl)-5-fluorouracil) and uracil in a molar ratio of 1:4. It was developed as an anti-cancer therapy by Taiho Pharmaceutical Co Ltd.A32073 It is approved in different countries but it is not yet approved by the FDA, Health Canada or EMA.

Struktur Molekul 2D

Berat 312.257
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The presence of uracil generates an increase in the half-life of tegafur and it is registered to be of 11 hours.[A1821] The elimination half-life of uracil is of 20-40 minutes.[L934]
Volume Distribusi The volume of distribution of tegafur is reported to be 59 L while the uracil volume of distribution of 474 L.[T122]
Klirens (Clearance) The reported clearance of tegafur when administered in the form of tegafur/uracil ranged from 47 to 175 ml/min

Absorpsi

The absorption into systemic circulation is very rapid and the peak concentration is reached within 1-2 hours. After a single dose of tegafur/uracil of 300 mg/m2/day in three divided doses, tegafur plasma concentration of >1000 ng/ml are maintained throughout the 8-hour dosing interval, whereas uracil concentrations decline rapidly following the peak concentration. The plasma concentration of 5-fluorouracil peaks at 30-60 min after administration with 200 ng/ml and remain detectable for 8-hour dosing interval. There is no significant long-term accumulation of either uracil, tegafur or 5-fluorouracil.L934

Metabolisme

Tegafur is bioactivated to 5-fluorouracil by the liver microsomal cytochrome P450 enzymes, mainly the CYP 2A6. This bioactivation is marked by the presence of C-5' oxidation and C-2' hydrolysis.L934 The 5-fluorouracil is later transformed into its active metabolite 5-fluorodeoxyuridine-monophosphate and 5-fluorouridine-triphosphate.L1557 More than 80% of the administered dose is eliminated due to the metabolism of dihydropyridine dehydrogenase.A1821 Some other metabolic products include 3'-hydroxy tegafur, 4'-hydroxy tegafur and dihydro tegafur which all of them are significantly less cytotoxic than 5-fluorouracil.T122

Rute Eliminasi

Less than 20% of the administered dose of tegafur is excreted intact in the urine following the oral administration.L934

Interaksi Obat

80 Data
Pentobarbital The metabolism of Tegafur-uracil can be increased when combined with Pentobarbital.
Tranylcypromine The metabolism of Tegafur-uracil can be decreased when combined with Tranylcypromine.
Letrozole The metabolism of Tegafur-uracil can be decreased when combined with Letrozole.
Miconazole The metabolism of Tegafur-uracil can be decreased when combined with Miconazole.
Ketoconazole The metabolism of Tegafur-uracil can be decreased when combined with Ketoconazole.
Amiodarone The metabolism of Tegafur-uracil can be decreased when combined with Amiodarone.
Metreleptin The metabolism of Tegafur-uracil can be increased when combined with Metreleptin.
Amphetamine The metabolism of Tegafur-uracil can be decreased when combined with Amphetamine.
Methimazole The metabolism of Tegafur-uracil can be decreased when combined with Methimazole.
Memantine The metabolism of Tegafur-uracil can be decreased when combined with Memantine.
Fenofibrate The metabolism of Tegafur-uracil can be decreased when combined with Fenofibrate.
Ethambutol The metabolism of Tegafur-uracil can be decreased when combined with Ethambutol.
Methoxsalen The metabolism of Tegafur-uracil can be decreased when combined with Methoxsalen.
Clofibrate The metabolism of Tegafur-uracil can be decreased when combined with Clofibrate.
Isoniazid The metabolism of Tegafur-uracil can be decreased when combined with Isoniazid.
Metyrapone The metabolism of Tegafur-uracil can be decreased when combined with Metyrapone.
Fomepizole The metabolism of Tegafur-uracil can be decreased when combined with Fomepizole.
Seratrodast The metabolism of Tegafur-uracil can be decreased when combined with Seratrodast.
Triclabendazole The metabolism of Tegafur-uracil can be decreased when combined with Triclabendazole.
Eletriptan The metabolism of Tegafur-uracil can be increased when combined with Eletriptan.
Phenobarbital The metabolism of Tegafur-uracil can be increased when combined with Phenobarbital.
Progesterone The metabolism of Tegafur-uracil can be increased when combined with Progesterone.
Prednisone The metabolism of Tegafur-uracil can be increased when combined with Prednisone.
Hydrocortisone The metabolism of Tegafur-uracil can be increased when combined with Hydrocortisone.
Prednisolone phosphate The metabolism of Tegafur-uracil can be increased when combined with Prednisolone phosphate.
Nevirapine The metabolism of Tegafur-uracil can be decreased when combined with Nevirapine.
Acetaminophen The metabolism of Tegafur-uracil can be decreased when combined with Acetaminophen.
Chlorzoxazone The metabolism of Tegafur-uracil can be decreased when combined with Chlorzoxazone.
Clozapine The metabolism of Tegafur-uracil can be decreased when combined with Clozapine.
Montelukast The metabolism of Tegafur-uracil can be decreased when combined with Montelukast.
Zidovudine The metabolism of Tegafur-uracil can be decreased when combined with Zidovudine.
Cinnarizine The metabolism of Tegafur-uracil can be decreased when combined with Cinnarizine.
Cisapride The metabolism of Tegafur-uracil can be decreased when combined with Cisapride.
Flurazepam The metabolism of Tegafur-uracil can be decreased when combined with Flurazepam.
Metronidazole The metabolism of Tegafur-uracil can be decreased when combined with Metronidazole.
Formoterol The metabolism of Tegafur-uracil can be decreased when combined with Formoterol.
Methoxyflurane The metabolism of Tegafur-uracil can be decreased when combined with Methoxyflurane.
Selegiline The metabolism of Tegafur-uracil can be decreased when combined with Selegiline.
Nifedipine The metabolism of Tegafur-uracil can be decreased when combined with Nifedipine.
Halothane The metabolism of Tegafur-uracil can be decreased when combined with Halothane.
Ifosfamide The metabolism of Tegafur-uracil can be decreased when combined with Ifosfamide.
Sevoflurane The metabolism of Tegafur-uracil can be decreased when combined with Sevoflurane.
Arformoterol The metabolism of Tegafur-uracil can be decreased when combined with Arformoterol.
Antipyrine The metabolism of Tegafur-uracil can be decreased when combined with Antipyrine.
Flunitrazepam The metabolism of Tegafur-uracil can be decreased when combined with Flunitrazepam.
Phenacetin The metabolism of Tegafur-uracil can be decreased when combined with Phenacetin.
Flunarizine The metabolism of Tegafur-uracil can be decreased when combined with Flunarizine.
Lorcaserin The metabolism of Tegafur-uracil can be decreased when combined with Lorcaserin.
Clomethiazole The metabolism of Tegafur-uracil can be decreased when combined with Clomethiazole.
Vortioxetine The metabolism of Tegafur-uracil can be decreased when combined with Vortioxetine.
Propacetamol The metabolism of Tegafur-uracil can be decreased when combined with Propacetamol.
Asunaprevir The metabolism of Asunaprevir can be decreased when combined with Tegafur-uracil.
Plitidepsin The metabolism of Tegafur-uracil can be decreased when combined with Plitidepsin.
Cenobamate The metabolism of Tegafur-uracil can be decreased when combined with Cenobamate.
Azelastine The metabolism of Tegafur-uracil can be decreased when combined with Azelastine.
Nicotine The metabolism of Tegafur-uracil can be decreased when combined with Nicotine.
Valproic acid The metabolism of Tegafur-uracil can be decreased when combined with Valproic acid.
Cyclophosphamide The metabolism of Cyclophosphamide can be decreased when combined with Tegafur-uracil.
Fluorouracil The metabolism of Fluorouracil can be decreased when combined with Tegafur-uracil.
Tamoxifen The metabolism of Tamoxifen can be decreased when combined with Tegafur-uracil.
Tegafur The metabolism of Tegafur can be decreased when combined with Tegafur-uracil.
Phenytoin The serum concentration of Phenytoin can be increased when it is combined with Tegafur-uracil.
Fosphenytoin The serum concentration of Fosphenytoin can be increased when it is combined with Tegafur-uracil.
Etanercept The metabolism of Tegafur-uracil can be increased when combined with Etanercept.
Anakinra The metabolism of Tegafur-uracil can be increased when combined with Anakinra.
Adalimumab The metabolism of Tegafur-uracil can be increased when combined with Adalimumab.
Infliximab The metabolism of Tegafur-uracil can be increased when combined with Infliximab.
Abatacept The metabolism of Tegafur-uracil can be increased when combined with Abatacept.
Afelimomab The metabolism of Tegafur-uracil can be increased when combined with Afelimomab.
Apremilast The metabolism of Tegafur-uracil can be increased when combined with Apremilast.
Canakinumab The metabolism of Tegafur-uracil can be increased when combined with Canakinumab.
Tocilizumab The metabolism of Tegafur-uracil can be increased when combined with Tocilizumab.
Rilonacept The metabolism of Tegafur-uracil can be increased when combined with Rilonacept.
Golimumab The metabolism of Tegafur-uracil can be increased when combined with Golimumab.
Certolizumab pegol The metabolism of Tegafur-uracil can be increased when combined with Certolizumab pegol.
Secukinumab The metabolism of Tegafur-uracil can be increased when combined with Secukinumab.
Siltuximab The metabolism of Tegafur-uracil can be increased when combined with Siltuximab.
Emapalumab The metabolism of Tegafur-uracil can be increased when combined with Emapalumab.
Ropeginterferon alfa-2b The metabolism of Tegafur-uracil can be decreased when combined with Ropeginterferon alfa-2b.
Bimekizumab The metabolism of Tegafur-uracil can be increased when combined with Bimekizumab.

Target Protein

Dihydropyrimidine dehydrogenase [NADP(+)] DPYD
Thymidylate synthase TYMS
RNA
DNA

Referensi & Sumber

Artikel (PubMed)
  • PMID: 3139892
    Yamashita K, Sutou H, Maruden A, Takenouchi T, Morita K, Ariyoshi T: A nine-month chronic toxicity study of tegafur-uracil mixture (UFT) in dogs. J Toxicol Sci. 1988 May;13(2):97-132.
  • PMID: 12950123
    Kim DJ, Kim TI, Suh JH, Cho YS, Shin SK, Kang JK, Kim NK, Kim WH: Oral tegafur-uracil plus folinic acid versus intravenous 5-fluorouracil plus folinic acid as adjuvant chemotherapy of colon cancer. Yonsei Med J. 2003 Aug 30;44(4):665-75. doi: 10.3349/ymj.2003.44.4.665.
  • PMID: 8400672
    Inada T, Ogata Y, Kubota T, Ozawa I, Hishinuma S, Shimizu H, Kotake K, Ikeda T, Koyama Y: A pharmacodynamic and pharmacokinetic study of fluoropyrimidines in a nude mouse system and in postoperative patients with gastric cancer. Surg Today. 1993;23(8):687-92.
  • PMID: 15280932
    Milano G, Ferrero JM, Francois E: Comparative pharmacology of oral fluoropyrimidines: a focus on pharmacokinetics, pharmacodynamics and pharmacomodulation. Br J Cancer. 2004 Aug 16;91(4):613-7.
  • PMID: 28765689
    Martini G, Troiani T, Cardone C, Vitiello P, Sforza V, Ciardiello D, Napolitano S, Della Corte CM, Morgillo F, Raucci A, Cuomo A, Selvaggi F, Ciardiello F, Martinelli E: Present and future of metastatic colorectal cancer treatment: A review of new candidate targets. World J Gastroenterol. 2017 Jul 14;23(26):4675-4688. doi: 10.3748/wjg.v23.i26.4675.
Textbook
  • Ashley C. and Dunleavy A. (2014). The renal drug handbook. Caroline Ashley and Aileen Dunleavy.
  • Wellington K. and Goa K. (2001). Drugs and aging. Springer .

Contoh Produk & Brand

Produk: 0 • International brands: 1
International Brands
  • Ftorafur — Taj pharma

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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