Peringatan Keamanan

LD50=230mg/kg (orally in mice)

Fluorouracil

DB00544

small molecule approved

Deskripsi

A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the thymidylate synthetase conversion of deoxyuridylic acid to thymidylic acid.

Struktur Molekul 2D

Berat 130.0772
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 10-20 minutes
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

28-100%

Metabolisme

Hepatic. The catabolic metabolism of fluorouracil results in degradation products ( e.g., CO2, urea and ?-fluoro-ß-alanine) which are inactive.

Rute Eliminasi

Seven percent to 20% of the parent drug is excreted unchanged in the urine in 6 hours; of this over 90% is excreted in the first hour. The remaining percentage of the administered dose is metabolized, primarily in the liver.

Farmakogenomik

12 Varian
TYMS (rs34743033)

Patients with this genotype have increased risk of severe neutropenia or severe diarrhea with drug; fluorouracil.

DPYD (rs1801265)

Patients with this genotype have reduced metabolism of fluorouracil and increased risk of toxicity.

GSTP1 (rs1695)

Patients with this genotype have increased risk of toxicity with fluorouracil

DPYD (rs3918290)

Patients with this genotype have reduced metabolism of fluorouracil and increased risk of toxicity.

DPYD (rs67376798)

Patients with this genotype have reduced metabolism of fluorouracil and increased risk of toxicity.

DPYD (rs3918290)

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

DPYD (rs55886062)

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

DPYD (rs67376798)

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

DPYD (rs1801158)

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

DPYD (rs1801159)

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

DPYD (rs1801160)

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

DPYD (rs1801265)

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

Interaksi Obat

1327 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Fluorouracil.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Fluorouracil.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Fluorouracil.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Fluorouracil.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Fluorouracil.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Fluorouracil.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Fluorouracil.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Fluorouracil.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Fluorouracil.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Fluorouracil.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Fluorouracil.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Fluorouracil.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Fluorouracil.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Fluorouracil.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Fluorouracil.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Fluorouracil.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Fluorouracil.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Fluorouracil.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Fluorouracil.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Fluorouracil.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Fluorouracil.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Fluorouracil.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Fluorouracil.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Fluorouracil.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Fluorouracil.
Cladribine Fluorouracil may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Fluorouracil.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Fluorouracil.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Fluorouracil.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Fluorouracil.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Fluorouracil.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Fluorouracil.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Fluorouracil.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Fluorouracil.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Fluorouracil.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Fluorouracil.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Fluorouracil.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Fluorouracil.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Fluorouracil.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Fluorouracil.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Fluorouracil.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Fluorouracil.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Fluorouracil.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Fluorouracil.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Fluorouracil.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Fluorouracil.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Fluorouracil.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Fluorouracil.
Propylthiouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Propylthiouracil.
Pentostatin The risk or severity of adverse effects can be increased when Fluorouracil is combined with Pentostatin.
Carbamazepine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Carbamazepine.
Vinblastine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Vinblastine.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluorouracil is combined with Fluocinolone acetonide.
Linezolid The risk or severity of adverse effects can be increased when Fluorouracil is combined with Linezolid.
Triamcinolone The risk or severity of adverse effects can be increased when Fluorouracil is combined with Triamcinolone.
Clofarabine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Clofarabine.
Pemetrexed The risk or severity of adverse effects can be increased when Fluorouracil is combined with Pemetrexed.
Fludrocortisone The risk or severity of adverse effects can be increased when Fluorouracil is combined with Fludrocortisone.
Daunorubicin The risk or severity of adverse effects can be increased when Fluorouracil is combined with Daunorubicin.
Irinotecan The risk or severity of adverse effects can be increased when Fluorouracil is combined with Irinotecan.
Etoposide The risk or severity of adverse effects can be increased when Fluorouracil is combined with Etoposide.
Sulfasalazine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Sulfasalazine.
Dacarbazine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Dacarbazine.
Temozolomide The risk or severity of adverse effects can be increased when Fluorouracil is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Penicillamine.
Prednisolone The risk or severity of adverse effects can be increased when Fluorouracil is combined with Prednisolone.
Sirolimus The risk or severity of adverse effects can be increased when Fluorouracil is combined with Sirolimus.
Mechlorethamine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Azacitidine.
Carboplatin The risk or severity of adverse effects can be increased when Fluorouracil is combined with Carboplatin.
Methylprednisolone The risk or severity of adverse effects can be increased when Fluorouracil is combined with Methylprednisolone.
Dactinomycin The risk or severity of adverse effects can be increased when Fluorouracil is combined with Dactinomycin.
Cytarabine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Cytarabine.
Azathioprine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Azathioprine.
Doxorubicin The risk or severity of adverse effects can be increased when Fluorouracil is combined with Doxorubicin.
Hydroxyurea The risk or severity of adverse effects can be increased when Fluorouracil is combined with Hydroxyurea.
Busulfan The risk or severity of adverse effects can be increased when Fluorouracil is combined with Busulfan.
Mycophenolic acid The risk or severity of adverse effects can be increased when Fluorouracil is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Fluorouracil is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Mercaptopurine.
Thalidomide The risk or severity of adverse effects can be increased when Fluorouracil is combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Fluorouracil is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Flucytosine.
Trilostane The risk or severity of adverse effects can be increased when Fluorouracil is combined with Trilostane.
Procarbazine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Procarbazine.
Arsenic trioxide The risk or severity of adverse effects can be increased when Fluorouracil is combined with Arsenic trioxide.
Idarubicin The risk or severity of adverse effects can be increased when Fluorouracil is combined with Idarubicin.
Estramustine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Estramustine.
Mitoxantrone The risk or severity of adverse effects can be increased when Fluorouracil is combined with Mitoxantrone.
Lomustine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Lomustine.
Budesonide The risk or severity of adverse effects can be increased when Fluorouracil is combined with Budesonide.
Docetaxel The risk or severity of adverse effects can be increased when Fluorouracil is combined with Docetaxel.
Dasatinib The risk or severity of adverse effects can be increased when Fluorouracil is combined with Dasatinib.
Eculizumab The risk or severity of adverse effects can be increased when Fluorouracil is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Decitabine.
Nelarabine The risk or severity of adverse effects can be increased when Fluorouracil is combined with Nelarabine.
Corticotropin The risk or severity of adverse effects can be increased when Fluorouracil is combined with Corticotropin.
Cortisone acetate The risk or severity of adverse effects can be increased when Fluorouracil is combined with Cortisone acetate.
Paramethasone The risk or severity of adverse effects can be increased when Fluorouracil is combined with Paramethasone.

Target Protein

Telomerase reverse transcriptase TERT
Dihydropyrimidine dehydrogenase [NADP(+)] DPYD
Thymidylate synthase TMP1
DNA
RNA
Thymidylate synthase TYMS

Referensi & Sumber

Synthesis reference: Leroy B. Townsend, Robert A. Earl, Steven J. Manning, "Method of synthesizing 1-(tetrahydro-2-furanyl)-5-fluorouracil." U.S. Patent US3960864, issued October, 1969.
Artikel (PubMed)
  • PMID: 12724731
    Longley DB, Harkin DP, Johnston PG: 5-fluorouracil: mechanisms of action and clinical strategies. Nat Rev Cancer. 2003 May;3(5):330-8.
  • PMID: 15032669
    Petty RD, Cassidy J: Novel fluoropyrimidines: improving the efficacy and tolerability of cytotoxic therapy. Curr Cancer Drug Targets. 2004 Mar;4(2):191-204.

Contoh Produk & Brand

Produk: 93 • International brands: 4
Produk
  • Actikerall
    Solution • - • Topical • Canada • Approved
  • Adrucil
    Injection, solution • 2.5 g/50mL • Intravenous • US • Generic • Approved
  • Adrucil
    Injection, solution • 5 g/100mL • Intravenous • US • Generic • Approved
  • Adrucil
    Injection, solution • 50 mg/1mL • Intravenous • US • Generic • Approved
  • Adrucil
    Solution • 50 mg / mL • Intravenous • Canada • Approved
  • Adrucil Inj 50mg/ml
    Liquid • 500 mg / 10 mL • Intravenous • Canada • Approved
  • Carac
    Cream • 5 mg/1g • Topical • US • Approved
  • Carac
    Cream • 5 mg/1g • Topical • US • Approved
Menampilkan 8 dari 93 produk.
International Brands
  • Carzonal — Tobishi
  • Efudix — Meda
  • Efurix — Valeant
  • Ftoruracil — Verofarm

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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