Peringatan Keamanan

Peripheral neuropathy was the most common toxicity leading to discontinuation of eribulin (5 percent). Richard Pazdur, M.D., director of the FDA's Division of Oncology Drug Products.
Single doses of 0.75 mg/kg were lethal to rats and two doses of 0.075 mg/kg were lethal to dogs. The no-observed-adverse-effect level (NOAEL) in rats and dogs were 0.015 and 0.0045 mg/kg/day, respectively.

Eribulin

DB08871

small molecule approved investigational

Deskripsi

Eribulin is a microtubule inhibitor indicated for the treatment of patients with metastatic breast cancer who have previously received at least two chemotherapeutic regimens for the treatment of metastatic disease. Eribulin was isolated from the marine sponge Halichondria okadai. Eribulin is also being investigated for use in the treatment of advanced solid tumors A7439.

Struktur Molekul 2D

Berat 729.908
Wujud liquid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) about 40 hours
Volume Distribusi 43 L/m2 to 114 L/m2
Klirens (Clearance) 1.16 L/hr/m2 to 2.42 L/hr/m2 (dose range of 0.25 mg/m2 to 4.0 mg/m2). [FDA]

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

There are no major human metabolites of eribulin, CYP3A4 negligibly metabolizes eribulin in vitro.

Rute Eliminasi

Eribulin is eliminated primarily in feces unchanged.

Interaksi Obat

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

Target Protein

Tubulin beta-1 chain TUBB1
Apoptosis regulator Bcl-2 BCL2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23593076
    Shablak A: Eribulin for advanced breast cancer: a drug evaluation. J Breast Cancer. 2013 Mar;16(1):12-5. doi: 10.4048/jbc.2013.16.1.12. Epub 2013 Mar 31.
  • PMID: 23010853
    Devriese LA, Witteveen PO, Marchetti S, Mergui-Roelvink M, Reyderman L, Wanders J, Jenner A, Edwards G, Beijnen JH, Voest EE, Schellens JH: Pharmacokinetics of eribulin mesylate in patients with solid tumors and hepatic impairment. Cancer Chemother Pharmacol. 2012 Dec;70(6):823-32. doi: 10.1007/s00280-012-1976-x. Epub 2012 Sep 26.
  • PMID: 22953094
    Nieder C, Aandahl G, Dalhaug A: A case of brain metastases from breast cancer treated with whole-brain radiotherapy and eribulin mesylate. Case Rep Oncol Med. 2012;2012:537183. doi: 10.1155/2012/537183. Epub 2012 Aug 16.
  • PMID: 16020666
    Jordan MA, Kamath K, Manna T, Okouneva T, Miller HP, Davis C, Littlefield BA, Wilson L: The primary antimitotic mechanism of action of the synthetic halichondrin E7389 is suppression of microtubule growth. Mol Cancer Ther. 2005 Jul;4(7):1086-95.

Contoh Produk & Brand

Produk: 15 • International brands: 0
Produk
  • Eribulin Mesylate
    Injection • 0.5 mg/1mL • Intravenous • US • Generic • Approved
  • Eribulin Mesylate
    Injection • 0.5 mg/1mL • Intravenous • US • Generic • Approved
  • Eribulin Mesylate
    Solution • 0.5 mg/1mL • Intravenous • US • Generic • Approved
  • Eribulin Mesylate
    Injection • 0.5 mg/1mL • Intravenous • US • Generic • Approved
  • Eribulin Mesylate
    Injection • 0.5 mg/1mL • Intravenous • US • Generic • Approved
  • Eribulin Mesylate Injection
    Solution • 0.5 mg / mL • Intravenous • Canada • Approved
  • Halaven
    Injection • 0.5 mg/1mL • Intravenous • US • Approved
  • Halaven
    Injection, solution • 0.44 mg/ml • Intravenous • EU • Approved
Menampilkan 8 dari 15 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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