Peringatan Keamanan

Toxicity information regarding rituximab is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as fatal infusion-related reactions and severe mucocutaneous reactions. Symptomatic and supportive measures are recommended. No long-term animal studies have been performed to establish the carcinogenic or mutagenic potential of rituximab or to determine potential effects on fertility in males or females L26641. The maximum tolerated dose of rituximab in mice administered intraperitoneally is higher than 100 mg/kg.L42045

Rituximab

DB00073

biotech approved

Deskripsi

Rituximab is a genetically engineered chimeric murine/human monoclonal antibody directed against the CD20 antigen found on the surface of normal and malignant B lymphocytes. The antibody is an IgG1 kappa immunoglobulin containing murine light and heavy-chain variable region sequences and human constant region sequences A40017, FDA label. It was originally approved by the U.S. FDA in 1997 as a single agent to treat patients with B-cell Non-Hodgkin's Lymphoma (NHL) L4811, however, has now been approved for a variety of conditions FDA label. On November 28, 2018, the US FDA approved Truxima, the first biosimilar to Rituxan (Rituximab) L4808.

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In patients with non-Hodgkin's lymphoma (NHL) treated with rituximab once a week or once every three weeks (n=298), the median terminal elimination half-life was 22 days (range of 6.1-52 days).[L26641] In patients with chronic lymphocytic leukemia (CLL) treated with rituximab (n=21), the estimated median terminal half-life was 32 days (range of 14-62 days).[L26641] Based on a pharmacokinetic analysis that included 2005 patients with rheumatoid arthritis (RA), the mean terminal elimination half-life of rituximab is 18.0 days.[L26641] In pediatric patients (6-17 years old) with granulomatosis with polyangiitis (GPA) or microscopic polyangiitis (MPA) given four doses of 375 mg/m<sup>2</sup> of rituximab intravenously once a week, the terminal half-life was 22 days (range from 11 to 42 days). In adult patients given the same dose, the terminal half-life was 25 days (range from 11 to 52 days).[L26641] In patients with pemphigus vulgaris given an intravenous infusion of 1000 mg of rituximab, the terminal half-life was 21.1 days (range from 9.3 to 36.2 days) in the first infusion cycle (days 1 and 15), and 26.2 days (range from 16.4 to 42.8 days) in the second infusion cycle (days 168 and 182).[L26641]
Volume Distribusi Based on a pharmacokinetic analysis that included 2005 patients with rheumatoid arthritis (RA), the volume of distribution of rituximab is 3.1 L.[L26641] In pediatric patients (6-17 years old) with granulomatosis with polyangiitis (GPA) or microscopic polyangiitis (MPA) given four doses of 375 mg/m<sup>2</sup> of rituximab intravenously once a week, the volume of distribution was 2.28 L (range from 1.43 to 3.17 L). In adult patients given the same dose, the volume of distribution was 3.12 L (range from 2.42 to 3.91 L).[L26641] In patients with pemphigus vulgaris given an intravenous infusion of 1000 mg of rituximab on days 1, 15, 168, and 182, the volume of distribution was 3.49 L (range from 2.48 to 5.22 L).[L26641]
Klirens (Clearance) In patients with non-Hodgkin’s lymphoma (NHL), those with higher CD19-positive cell counts or larger measurable tumor lesions at pretreatment had higher rituximab clearance [L26641]. Based on a pharmacokinetic analysis that included 2005 patients with rheumatoid arthritis (RA), the clearance of rituximab is 0.335 L/day.[L26641] In pediatric patients (6-17 years old) with granulomatosis with polyangiitis (GPA) or microscopic polyangiitis (MPA) given four doses of 375 mg/m<sup>2</sup> of rituximab intravenously once a week, clearance was 0.222 L/day (range from 0.0996 to 0.381 L/day). In adult patients given the same dose, clearance was 0.279 L/day (range from 0.113 to 0.653 L/day).[L26641] In patients with pemphigus vulgaris given an intravenous infusion of 1000 mg of rituximab, clearance was 0.30 L/day (range from 0.16 to 1.51 L/day) in the first infusion cycle (days 1 and 15), and 0.24 L/day (range from 0.13 to 0.45 L/day) in the second infusion cycle (days 168 and 182).[L26641]

Absorpsi

Rituximab follows a linear pharmacokinetic model.A40006 In patients with non-Hodgkin’s lymphoma (NHL) administered 4 doses of 375 mg/m2 of rituximab (IV) weekly, detectable levels were observed 3-6 months after treatment completion. The pharmacokinetic profile of rituximab administered in combination with 6 cycles of CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisone) chemotherapy was similar to the one observed when administered alone.L26641 In patients with rheumatoid arthritis (RA) administered 2 doses of 500 mg of rituximab, the Cmax of the first and second infusions were 157 (SD ± 46) and 183 (SD ± 55) mcg/mL. In patients administered 2 doses of 1,000 mg of rituximab, the Cmax of the first and second infusions were 318 (SD ± 86) and 381 (SD ± 98) mcg/mL.L26641 In pediatric patients (6-17 years old) with granulomatosis with polyangiitis (GPA) or microscopic polyangiitis (MPA) given four doses of 375 mg/m2 of rituximab intravenously once a week, the AUC0-180 was 9787 µg/mL?day (range from 4838 to 20446 µg/mL?day). In adult patients given the same dose, the AUC0-180 of rituximab was 10302 µg/mL?day (range from 3653 to 21874 µg/mL?day).L26641 The bioavailability of rituximab administered intravenously is expected to be close to 100%. Compared to rituximab administered intravenously, the bioavailability of RITUXAN HYCELA, a combination product of rituximab and hyaluronidase (human recombinant), is 64.6% in patients with follicular lymphoma and 63.4% in patients with chronic lymphocytic leukemia (CLL).L42040

Metabolisme

As a monoclonal antibody, rituximab is expected to be metabolized by proteases throughout the body.

Rute Eliminasi

Monoclonal antibodies (mAb) such as rituximab trigger the formation of antidrug antibodies (ADAs) that form ADA-mAb immune complexes. The endogenous elimination of these immune complexes is mediated by the reticuloendothelial system, most likely via fragment crystallizable-gamma (Fc?)-mediated endocytosisA40006.

Farmakogenomik

1 Varian
FCGR3A (rs396991)

Patients with this genotype have increased frequency of anti-tumor response when using rituximab to treat diffuse large B-cell lymphoma, follicular lymphoma, or follicular non-Hodgkin lymphoma.

Interaksi Obat

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

Target Protein

B-lymphocyte antigen CD20 MS4A1

Referensi & Sumber

Synthesis reference: Anderson, DR., et al. (1998). Therapeutic application of chimeric and radiolabeled antibodies to human B lymphocyte restricted differentiation antigen for treatment of B cell lymphoma (U.S. Patent No. US 5,736,137 A). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/04/bf/17/b9f758df63e314/US5736137.pdf
Artikel (PubMed)
  • PMID: 9704735
    McLaughlin P, Grillo-Lopez AJ, Link BK, Levy R, Czuczman MS, Williams ME, Heyman MR, Bence-Bruckler I, White CA, Cabanillas F, Jain V, Ho AD, Lister J, Wey K, Shen D, Dallaire BK: Rituximab chimeric anti-CD20 monoclonal antibody therapy for relapsed indolent lymphoma: half of patients respond to a four-dose treatment program. J Clin Oncol. 1998 Aug;16(8):2825-33.
  • PMID: 15201414
    Edwards JC, Szczepanski L, Szechinski J, Filipowicz-Sosnowska A, Emery P, Close DR, Stevens RM, Shaw T: Efficacy of B-cell-targeted therapy with rituximab in patients with rheumatoid arthritis. N Engl J Med. 2004 Jun 17;350(25):2572-81.
  • PMID: 15795920
    Braendstrup P, Bjerrum OW, Nielsen OJ, Jensen BA, Clausen NT, Hansen PB, Andersen I, Schmidt K, Andersen TM, Peterslund NA, Birgens HS, Plesner T, Pedersen BB, Hasselbalch HC: Rituximab chimeric anti-CD20 monoclonal antibody treatment for adult refractory idiopathic thrombocytopenic purpura. Am J Hematol. 2005 Apr;78(4):275-80.
  • PMID: 16705086
    Binder M, Otto F, Mertelsmann R, Veelken H, Trepel M: The epitope recognized by rituximab. Blood. 2006 Sep 15;108(6):1975-8. Epub 2006 May 16.
  • PMID: 28653357
    Ryman JT, Meibohm B: Pharmacokinetics of Monoclonal Antibodies. CPT Pharmacometrics Syst Pharmacol. 2017 Sep;6(9):576-588. doi: 10.1002/psp4.12224. Epub 2017 Jul 29.
  • PMID: 20729962
    Emer JJ, Claire W: Rituximab: a review of dermatological applications. J Clin Aesthet Dermatol. 2009 May;2(5):29-37.
  • PMID: 20442809
    Dotan E, Aggarwal C, Smith MR: Impact of Rituximab (Rituxan) on the Treatment of B-Cell Non-Hodgkin's Lymphoma. P T. 2010 Mar;35(3):148-57.
  • PMID: 32841219
    Owczarczyk K, Cascino MD, Holweg C, Tew GW, Ortmann W, Behrens T, Schindler T, Langford CA, St Clair EW, Merkel PA, Spiera R, Seo P, Kallenberg CG, Specks U, Lim N, Stone J, Brunetta P, Prunotto M: Fc receptor-like 5 and anti-CD20 treatment response in granulomatosis with polyangiitis and microscopic polyangiitis. JCI Insight. 2020 Sep 17;5(18). pii: 136180. doi: 10.1172/jci.insight.136180.

Contoh Produk & Brand

Produk: 40 • International brands: 2
Produk
  • Blitzima
    Injection, solution, concentrate • 500 mg • Intravenous • EU • Approved
  • Blitzima
    Injection, solution, concentrate • 100 mg • Intravenous • EU • Approved
  • Mabthera
    Injection, solution, concentrate • 100 mg • Intravenous • EU • Approved
  • Mabthera
    Injection, solution, concentrate • 500 mg • Intravenous • EU • Approved
  • Mabthera
    Injection, solution • 1400 mg • Subcutaneous • EU • Approved
  • Mabthera
    Injection, solution • 1600 mg • Subcutaneous • EU • Approved
  • Riabni
    Injection, solution • 100 mg/10mL • Intravenous • US • Approved
  • Riabni
    Injection, solution • 500 mg/50mL • Intravenous • US • Approved
Menampilkan 8 dari 40 produk.
International Brands
  • MabThera — Roche
  • Riabni

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