Peringatan Keamanan

Most commonly reported adverse reactions (incidence ? 30%) are fatigue, anemia, nausea, thrombocytopenia, dyspnea, diarrhea, and pyrexia. The two dose limiting toxicities are thrombocytopenia and febrile neutropenia.
Maximum tolerate dose = 15 mg/m^2

Carfilzomib

DB08889

small molecule approved investigational

Deskripsi

Carfilzomib is an injectable antineoplastic agent (IV only). Chemically, it is a modified tetrapeptidyl epoxide and an analog of epoxomicin. It is also a selective proteasome inhibitor. FDA approved carfilzomib in July 2012 for the treatment of adults with relapsed or refractory multiple myeloma as monotherapy or combination therapy.L39392

Struktur Molekul 2D

Berat 719.9099
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following intravenous administration of doses ? 15 mg/m^2, carfilzomib was rapidly cleared from the systemic circulation with a half-life of ? 1 hour on Day 1 of Cycle 1.
Volume Distribusi Vd, steady state, 20 mg/m^2 = 28 L
Klirens (Clearance) Systemic clearance = 151 - 263 L/hour. As this value exceeds hepatic blood flow, it suggests that carfilozmib is cleared extrahepatically.

Absorpsi

Cmax, single IV dose of 27 mg/m^2 = 4232 ng/mL; AUC, single IV dose of 27 mg/m^2 = 379 ng•hr/mL; Carfilzomib does not accumulation in the systemic. At doses between 20 and 36 mg/m2, there was a dose-dependent increase in exposure.

Metabolisme

Carfilzomib was rapidly and extensively metabolized by the liver. The predominant metabolites were the peptide fragments and the diol of carfilzomib which suggests that the main metabolic pathways are peptidase cleavage and epoxide hydrolysis. The cytochrome P450 enzyme system is minimally involved in the metabolism of carfilzomib. All metabolites are inactive.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

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

Target Protein

Proteasome subunit beta type-5 PSMB5
Proteasome subunit beta type-8 PSMB8
Proteasome subunit beta type-1 PSMB1
Proteasome subunit beta type-9 PSMB9
Proteasome subunit beta type-2 PSMB2
Proteasome subunit beta type-10 PSMB10

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23393020
    Kortuem KM, Stewart AK: Carfilzomib. Blood. 2013 Feb 7;121(6):893-7. doi: 10.1182/blood-2012-10-459883.
  • PMID: 17591945
    Kuhn DJ, Chen Q, Voorhees PM, Strader JS, Shenk KD, Sun CM, Demo SD, Bennett MK, van Leeuwen FW, Chanan-Khan AA, Orlowski RZ: Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma. Blood. 2007 Nov 1;110(9):3281-90. Epub 2007 Jun 25.

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