Peringatan Keamanan

Belinostat is genotoxic according to Ames test and may impair male fertility. Weekly complete blood count should be monitored during treatment to adjust the dosage as intravenous infusion of belinostat is frequently associated with hematologic toxicity such as leukopenia and thrombocytopenia. Incidences of infections such as sepsis, hepatotoxicity, tumor lysis syndrome, gastrointestinal toxicity, and embryo-fetal toxicity may occur.
No specific information is available on the treatment of overdosage of Beleodaq. There is no antidote for Beleodaq and it is not known if Beleodaq is dialyzable. If an overdose occurs, general supportive measures should be instituted as deemed necessary by the treating physician.

Belinostat

DB05015

small molecule approved investigational

Deskripsi

Belinostat is a novel agent that inhibits the enzyme histone deacetylase (HDAC) with a sulfonamide-hydroxamide structure. It was developed as an orphan drug to target hematological malignancies and solid tumors by TopoTarget. The safety and efficacy of belinostat is currently being evaluated for use in combination with traditional front-line therapies for the treatment of PTCL. Intravenous administration of the agent is available as Beleodaq as monotherapy and the dosing regimen involves a 21-day cycle. It was US-approved in July 2014 as a therapeutic agent for relapsed or refractory peripheral T-cell lymphoma.

Struktur Molekul 2D

Berat 318.35
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Displays a three-compartment pharmacokinetic property with elimination half life of 1.1 hours
Volume Distribusi The volume of distribution is 409 ± 76.7 L.
Klirens (Clearance) 1240 mL/min

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Primarily metabolized by hepatic UGT1A1. Strong UGT1A1 inhibitors are expected to increase exposure to belinostat. Belinostat also undergoes hepatic metabolism by CYP2A6, CYP2C9, and CYP3A4 enzymes to form belinostat amide and belinostat acid. The enzymes responsible for the formation of methyl belinostat and 3-(anilinosulfonyl)-benzenecarboxylic acid, (3-ASBA) are not known

Rute Eliminasi

Approximately 40% of the belinostat dose is excreted renally, primarily as metabolites and less than 2% of total dose recovered as unchanged parent drug.

Farmakogenomik

2 Varian
UGT1A1 (rs8175347)

Patients who carry this genotype in UGT1A1 are at greater risk of experiencing dose-limiting toxicity from belinostat therapy.

UGT1A1 (rs4124874)

Patients who carry this genotype in UGT1A1 may be at greater risk of experiencing dose-limiting toxicity from belinostat therapy.

Interaksi Obat

880 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Belinostat.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Belinostat.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Belinostat.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Belinostat.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Belinostat.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Belinostat.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Belinostat.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Belinostat.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Belinostat.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Belinostat.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Belinostat.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Belinostat.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Belinostat.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Belinostat.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Belinostat.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Belinostat.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Belinostat.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Belinostat.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Belinostat.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Belinostat.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Belinostat.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Belinostat.
Cladribine Belinostat may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Belinostat.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Belinostat.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Belinostat.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Belinostat.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Belinostat.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Belinostat.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Belinostat.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Belinostat.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Belinostat.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Belinostat.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Belinostat.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Belinostat.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Belinostat.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Belinostat.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Belinostat.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Belinostat.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Belinostat.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Belinostat.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Belinostat.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Belinostat.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Belinostat.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Belinostat.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Belinostat.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Belinostat.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Belinostat.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Belinostat.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Belinostat.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Belinostat.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Belinostat.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Belinostat.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Belinostat.
Sirolimus The risk or severity of adverse effects can be increased when Sirolimus is combined with Belinostat.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Belinostat.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Belinostat.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Belinostat.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Belinostat.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Belinostat.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Belinostat.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Belinostat.
Busulfan The risk or severity of adverse effects can be increased when Busulfan is combined with Belinostat.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Belinostat.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Belinostat.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Belinostat.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Belinostat.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Belinostat.
Trilostane The risk or severity of adverse effects can be increased when Trilostane is combined with Belinostat.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Belinostat.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Belinostat.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Belinostat.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Belinostat.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Belinostat.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Belinostat.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Belinostat.
Ciclesonide The risk or severity of adverse effects can be increased when Ciclesonide is combined with Belinostat.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Belinostat.
Everolimus The risk or severity of adverse effects can be increased when Everolimus is combined with Belinostat.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Hydroxychloroquine is combined with Belinostat.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Belinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Belinostat.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Belinostat.
Thiotepa The risk or severity of adverse effects can be increased when Thiotepa is combined with Belinostat.
Aldosterone The risk or severity of adverse effects can be increased when Aldosterone is combined with Belinostat.
Ixabepilone The risk or severity of adverse effects can be increased when Ixabepilone is combined with Belinostat.
Pirfenidone The risk or severity of adverse effects can be increased when Pirfenidone is combined with Belinostat.
Interferon alfa The risk or severity of adverse effects can be increased when Belinostat is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Belinostat is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Belinostat is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Belinostat is combined with Human interferon omega-1.
Temsirolimus The risk or severity of adverse effects can be increased when Belinostat is combined with Temsirolimus.
Panobinostat The risk or severity of adverse effects can be increased when Belinostat is combined with Panobinostat.
Mepolizumab The risk or severity of adverse effects can be increased when Belinostat is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Belinostat is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Belinostat is combined with Belatacept.
Bendamustine The risk or severity of adverse effects can be increased when Belinostat is combined with Bendamustine.
Cabazitaxel The risk or severity of adverse effects can be increased when Belinostat is combined with Cabazitaxel.
Pralatrexate The risk or severity of adverse effects can be increased when Belinostat is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Belinostat is combined with Wortmannin.

Target Protein

Histone deacetylase HDAC1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27813438
    Moskowitz AJ, Horwitz SM: Targeting histone deacetylases in T-cell lymphoma. Leuk Lymphoma. 2017 Jun;58(6):1306-1319. doi: 10.1080/10428194.2016.1247956. Epub 2016 Nov 4.
  • PMID: 28090369
    Hood K, Shah A: Belinostat for Relapsed or Refractory Peripheral T-Cell Lymphoma. J Adv Pract Oncol. 2016 Mar;7(2):209-218. Epub 2016 Mar 1.
  • PMID: 23382909
    Wang LZ, Ramirez J, Yeo W, Chan MY, Thuya WL, Lau JY, Wan SC, Wong AL, Zee YK, Lim R, Lee SC, Ho PC, Lee HS, Chan A, Ansher S, Ratain MJ, Goh BC: Glucuronidation by UGT1A1 is the dominant pathway of the metabolic disposition of belinostat in liver cancer patients. PLoS One. 2013;8(1):e54522. doi: 10.1371/journal.pone.0054522. Epub 2013 Jan 30.
  • PMID: 25864732
    Valiuliene G, Stirblyte I, Cicenaite D, Kaupinis A, Valius M, Navakauskiene R: Belinostat, a potent HDACi, exerts antileukaemic effect in human acute promyelocytic leukaemia cells via chromatin remodelling. J Cell Mol Med. 2015 Jul;19(7):1742-55. doi: 10.1111/jcmm.12550. Epub 2015 Apr 11.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Beleodaq
    Injection, powder, lyophilized, for solution • 500 mg/10mL • Intravenous • US • Approved
  • Beleodaq
    Injection, powder, lyophilized, for solution • 500 mg/10mL • Intravenous • US • Approved
  • Beleodaq
    Injection, powder, lyophilized, for solution • 500 mg/10mL • Intravenous • US • Approved

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