Peringatan Keamanan

There were no known overdoses of clofarabine. The highest daily dose administered to a human to date (on a mg/m2 basis) has been 70 mg/m2/day × 5 days (2 pediatric ALL patients). The toxicities included in these 2 patients included grade 4 hyperbilirubinemia, grade 2 and 3 vomiting, and grade 3 maculopapular rash.

Clofarabine

DB00631

small molecule approved investigational

Deskripsi

Clofarabine is a purine nucleoside antimetabolite that is being studied in the treatment of cancer. It is marketed as Clolar in the U.S. and Canada, or Evoltra in Europe, Australia, and New Zealand. Clofarabine is used in paediatrics to treat a type of leukaemia called relapsed or refractory acute lymphoblastic leukaemia (ALL), only after at least two other types of treatment have failed. It is not known if the drug extends life expectancy. Its potential use in acute myeloid leukaemia (AML) and juvenile myelomonocytic leukaemia (JMML) has been investigated.

Struktur Molekul 2D

Berat 303.677
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal half-life is estimated to be 5.2 hours.
Volume Distribusi * 172 L/m2
Klirens (Clearance) * 28.8 L/h/m2 [Pediatric patients (2 - 19 years old) with relapsed or refractory acute lymphoblastic leukemia (ALL) or acute myelogenous leukemia (AML) receiving 52 mg/m2 dose]

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Clofarabine is sequentially metabolized intracellularly to the 5’-monophosphate metabolite by deoxycytidine kinase and mono- and di-phosphokinases to the active 5’-triphosphate metabolite. Clofarabine has high affinity for the activating phosphorylating enzyme, deoxycytidine kinase, equal to or greater than that of the natural substrate, deoxycytidine.

Rute Eliminasi

Based on 24-hour urine collections in the pediatric studies, 49 - 60% of the dose is excreted in the urine unchanged.

Interaksi Makanan

1 Data
  • 1. Avoid echinacea. Echinacea should be used with caution, if at all, in patients receiving therapeutic immunosuppressants. Monitor for reduced efficacy of the immunosuppressant during concomitant use.

Interaksi Obat

1508 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Clofarabine.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Clofarabine.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Clofarabine.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Clofarabine.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Clofarabine.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Clofarabine.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Clofarabine.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Clofarabine.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Clofarabine.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Clofarabine.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Clofarabine.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Clofarabine.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Clofarabine.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Clofarabine.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Clofarabine.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Clofarabine.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Clofarabine.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Clofarabine.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Clofarabine.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Clofarabine.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Clofarabine.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Clofarabine.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Clofarabine.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Clofarabine.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Clofarabine.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Clofarabine.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Clofarabine.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Clofarabine.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Clofarabine.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Clofarabine.
Cladribine Clofarabine may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Clofarabine.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Clofarabine.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Clofarabine.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Clofarabine.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Clofarabine.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Clofarabine.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Clofarabine.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Clofarabine.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Clofarabine.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Clofarabine.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Clofarabine.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Clofarabine.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Clofarabine.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Clofarabine.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Clofarabine.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Clofarabine.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Clofarabine.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Clofarabine.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Clofarabine.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Clofarabine.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Clofarabine.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Clofarabine.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Clofarabine.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Clofarabine.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Clofarabine.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Clofarabine.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Clofarabine.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Clofarabine.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Clofarabine.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Clofarabine.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Clofarabine.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Clofarabine.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Clofarabine.
Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Clofarabine.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Clofarabine.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Clofarabine.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Clofarabine.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Clofarabine.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Clofarabine.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Clofarabine.
Prednisone The risk or severity of adverse effects can be increased when Clofarabine is combined with Prednisone.
Pemetrexed The risk or severity of adverse effects can be increased when Clofarabine is combined with Pemetrexed.
Fludrocortisone The risk or severity of adverse effects can be increased when Clofarabine is combined with Fludrocortisone.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Clofarabine is combined with Mycophenolate mofetil.
Daunorubicin The risk or severity of adverse effects can be increased when Clofarabine is combined with Daunorubicin.
Irinotecan The risk or severity of adverse effects can be increased when Clofarabine is combined with Irinotecan.
Methimazole The risk or severity of adverse effects can be increased when Clofarabine is combined with Methimazole.
Etoposide The risk or severity of adverse effects can be increased when Clofarabine is combined with Etoposide.
Sulfasalazine The risk or severity of adverse effects can be increased when Clofarabine is combined with Sulfasalazine.
Dacarbazine The risk or severity of adverse effects can be increased when Clofarabine is combined with Dacarbazine.
Temozolomide The risk or severity of adverse effects can be increased when Clofarabine is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Clofarabine is combined with Penicillamine.
Prednisolone The risk or severity of adverse effects can be increased when Clofarabine is combined with Prednisolone.
Sirolimus The risk or severity of adverse effects can be increased when Clofarabine is combined with Sirolimus.
Mechlorethamine The risk or severity of adverse effects can be increased when Clofarabine is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Clofarabine is combined with Azacitidine.
Carboplatin The risk or severity of adverse effects can be increased when Clofarabine is combined with Carboplatin.
Methylprednisolone The risk or severity of adverse effects can be increased when Clofarabine is combined with Methylprednisolone.
Dactinomycin The risk or severity of adverse effects can be increased when Clofarabine is combined with Dactinomycin.
Cytarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Cytarabine.
Azathioprine The risk or severity of adverse effects can be increased when Clofarabine is combined with Azathioprine.
Doxorubicin The risk or severity of adverse effects can be increased when Clofarabine is combined with Doxorubicin.
Hydroxyurea The risk or severity of adverse effects can be increased when Clofarabine is combined with Hydroxyurea.
Busulfan The risk or severity of adverse effects can be increased when Clofarabine is combined with Busulfan.
Mycophenolic acid The risk or severity of adverse effects can be increased when Clofarabine is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Clofarabine is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Clofarabine is combined with Mercaptopurine.
Thalidomide The risk or severity of adverse effects can be increased when Clofarabine is combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Clofarabine is combined with Melphalan.

Target Protein

DNA
Ribonucleoside-diphosphate reductase subunit M2 B RRM2B
Ribonucleoside-diphosphate reductase subunit M2 RRM2
DNA polymerase alpha catalytic subunit POLA1
Ribonucleoside-diphosphate reductase large subunit RRM1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 20631817
    Pession A, Masetti R, Kleinschmidt K, Martoni A: Use of clofarabine for acute childhood leukemia. Biologics. 2010 Jun 24;4:111-8.
  • PMID: 18728851
    Harned TM, Gaynon PS: Treating refractory leukemias in childhood, role of clofarabine. Ther Clin Risk Manag. 2008 Apr;4(2):327-36.
  • PMID: 19519505
    Lech-Maranda E, Korycka A, Robak T: Clofarabine as a novel nucleoside analogue approved to treat patients with haematological malignancies: mechanism of action and clinical activity. Mini Rev Med Chem. 2009 Jun;9(7):805-12.
  • PMID: 19463072
    Larson ML, Venugopal P: Clofarabine: a new treatment option for patients with acute myeloid leukemia. Expert Opin Pharmacother. 2009 Jun;10(8):1353-7. doi: 10.1517/14656560902997990.
  • PMID: 19576186
    Zhenchuk A, Lotfi K, Juliusson G, Albertioni F: Mechanisms of anti-cancer action and pharmacology of clofarabine. Biochem Pharmacol. 2009 Dec 1;78(11):1351-9. doi: 10.1016/j.bcp.2009.06.094. Epub 2009 Jul 1.

Contoh Produk & Brand

Produk: 23 • International brands: 1
Produk
  • Clofarabine
    Injection • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Clofarabine
    Injection • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Clofarabine
    Injection, solution • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Clofarabine
    Injection • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Clofarabine
    Injection • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Clofarabine
    Injection • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Clofarabine
    Injection • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Clofarabine
    Injection • 1 mg/1mL • Intravenous • US • Generic • Approved
Menampilkan 8 dari 23 produk.
International Brands
  • Clofazic — Raffo

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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