Peringatan Keamanan

Risk for tumor-lysis syndrome.
Discontinue use in the event of severe/progressive skin reactions.
Hematologic malignancies of different forms reported.
Discontinue use in the case of severe infusion reactions.
May cause extravasation.
Mild to moderate renal impairment.
Mild hepatic impairment.
Sepsis (infections) may occur.
Avoid use if pregnant.
Possibility of anaphylaxis or infusion reactions- severe in rare cases.

Bendamustine

DB06769

small molecule approved investigational

Deskripsi

Bendamustine is a nitrogen mustard drug which has been used in the treatment of chronic lymphocytic leukemia (CLL) and indolent B-cell non-Hodgkin lymphoma (NHL). Bendamustine is a bifunctional mechlorethamine derivative capable of forming electrophilic alkyl groups that covalently bond to other molecules. Through this function as an alkylating agent, bendamustine causes intra- and inter-strand crosslinks between DNA bases resulting in cell death. It is active against both active and quiescent cells, although the exact mechanism of action is unknown.

Struktur Molekul 2D

Berat 358.263
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 40 minutes
Volume Distribusi The mean steady-state volume of distribution (Vss) of bendamustine was approximately 20-25 L. Steady-state volume of distribution for total radioactivity was approximately 50 L, indicating that neither bendamustine nor total radioactivity are extensively distributed into the tissues.
Klirens (Clearance) 700 mL/min

Absorpsi

Following a single IV dose of bendamustine hydrochloride Cmax typically occurred at the end of infusion. The dose proportionality of bendamustine has not been studied.

Metabolisme

In vitro data indicate that bendamustine is primarily metabolized via hydrolysis to monohydroxy (HP1) and dihydroxy-bendamustine (HP2) metabolites with low cytotoxic activity. Two active minor metabolites, M3 and M4, are primarily formed via CYP1A2. However, concentrations of these metabolites in plasma are 1/10th and 1/100th that of the parent compound, respectively, suggesting that the cytotoxic activity is primarily due to bendamustine. Results of a human mass balance study confirm that bendamustine is extensively metabolized via hydrolytic, oxidative, and conjugative pathways.

Rute Eliminasi

Mean recovery of total radioactivity in cancer patients following IV infusion of 14C bendamustine hydrochloride was approximately 76% of the dose. Approximately 50% of the dose was recovered in the urine and approximately 25% of the dose was recovered in the feces. Urinary excretion was confirmed as a relatively minor pathway of elimination of bendamustine, with approximately 3.3% of the dose recovered in the urine as parent. Less than 1% of the dose was recovered in the urine as M3 and M4, and less than 5% of the dose was recovered in the urine as HP2.

Interaksi Obat

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

Target Protein

DNA

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17599772
    Hartmann JT, Mayer F, Schleicher J, Horger M, Huober J, Meisinger I, Pintoffl J, Kafer G, Kanz L, Grunwald V: Bendamustine hydrochloride in patients with refractory soft tissue sarcoma: a noncomparative multicenter phase 2 study of the German sarcoma group (AIO-001). Cancer. 2007 Aug 15;110(4):861-6.
  • PMID: 17726779
    Bagchi S: Bendamustine for advanced sarcoma. Lancet Oncol. 2007 Aug;8(8):674.
  • PMID: 20110042
    Dennie TW, Kolesar JM: Bendamustine for the treatment of chronic lymphocytic leukemia and rituximab-refractory, indolent B-cell non-Hodgkin lymphoma. Clin Ther. 2009;31 Pt 2:2290-311. doi: 10.1016/j.clinthera.2009.11.031.
  • PMID: 16957931
    Teichert J, Baumann F, Chao Q, Franklin C, Bailey B, Hennig L, Caca K, Schoppmeyer K, Patzak U, Preiss R: Characterization of two phase I metabolites of bendamustine in human liver microsomes and in cancer patients treated with bendamustine hydrochloride. Cancer Chemother Pharmacol. 2007 May;59(6):759-70. Epub 2006 Sep 7.
  • PMID: 25829094
    Darwish M, Bond M, Hellriegel E, Robertson P Jr, Chovan JP: Pharmacokinetic and pharmacodynamic profile of bendamustine and its metabolites. Cancer Chemother Pharmacol. 2015 Jun;75(6):1143-54. doi: 10.1007/s00280-015-2727-6. Epub 2015 Apr 1.

Contoh Produk & Brand

Produk: 41 • International brands: 2
Produk
  • Belrapzo
    Injection • 100 mg/4mL • Intravenous • US • Approved
  • Bendamustine
    Injection, powder, lyophilized, for solution • 25 mg/5mL • Intravenous • US • Generic • Approved
  • Bendamustine
    Injection, powder, lyophilized, for solution • 100 mg/20mL • Intravenous • US • Generic • Approved
  • Bendamustine Hydrochloride
    Injection, powder, lyophilized, for solution • 25 mg/5mL • Intravenous • US • Generic • Approved
  • Bendamustine Hydrochloride
    Injection, powder, lyophilized, for solution • 100 mg/20mL • Intravenous • US • Generic • Approved
  • Bendamustine Hydrochloride
    Injection • 100 mg/1 • Intravenous • US • Approved
  • Bendamustine Hydrochloride
    Injection, powder, lyophilized, for solution • 25 mg/5mL • Intravenous • US • Generic • Approved
  • Bendamustine Hydrochloride
    Injection, powder, lyophilized, for solution • 100 mg/20mL • Intravenous • US • Generic • Approved
Menampilkan 8 dari 41 produk.
International Brands
  • Levact — NAPP Pharmaceuticals
  • Treakisym — Teva Pharmaceutical Industries Ltd.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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