Peringatan Keamanan

Repeat dose exposure has been shown to produce a partially reversible decrease in neutrophil count and a reversible decrease in fibrinogen.L1000

Sarilumab

DB11767

biotech approved investigational

Deskripsi

Sarilumab is a fully human anti-interleukin 6 (IL-6) receptor monoclonal IgG1 antibody that binds to both membrane-bound and soluble IL-6 receptor forms, thus blocking the cis- and trans-inflammatory signalling cascades of IL-6.A27262 Sarilumab was developed by Sanofi and Regeneron Pharmaceuticals, Inc; it was US FDA-approved in May 2017 and followed by EU approval in June 2017 for the treatment of moderate to severe rheumatoid arthritis (RA) in combination with methotrexate.A27265 RA is a chronic inflammatory disease characterized by polyarthritis, and its treatment has been challenged by the different responses in every patient.A27264 Subcutaneous administration of sarilumab has been shown to decrease acute-phase reactant levels and improve clinical RA symptoms.A27263

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) The half-life will depend on the administered concentration. At 200 mg every 2 weeks, half-life is up to 10 days in patients with rheumatoid arthritis (RA) at steady state. At 150 mg every 2 weeks, half-life is up to 8 days in patients with RA at steady state. After the last steady state dose of 150 and 200 mg, the time to reach nondetectable concentration is 28 and 43 days, respectively.[L45454]
Volume Distribusi In patients with rheumatoid arthritis, the apparent volume of distribution at steady state was 7.3 L.[L45454]
Klirens (Clearance) Sarilumab is not eliminated via renal or hepatic pathways. Patients with rheumatoid arthritis have shown a trend toward higher clearance in the presence of anti-sarilumab antibodies.[L45454]

Absorpsi

Sarilumab is shown to be well absorbed in patients with rheumatoid arthritis after single subcutaneous administration, with a maximum serum concentration presented after 2 to 4 days. For the 150 mg every two weeks dose regimen, the AUC, Cmin and Cmax of sarilumab were 202 ± 120 mg.day/L, 6.35 ± 7.54 mg/L, and 20.0 ± 9.20 mg/L, respectively. For the 200 mg every two weeks dose regimen, the AUC, Cmin and Cmax of sarilumab were 395 ± 207 mg.day/L, 16.5 ± 14.1 mg/L, and 35.6 ± 15.2 mg/L, respectively.L45454

Metabolisme

The metabolism of sarilumab has not been characterized. As a monoclonal antibody, it is thought to be degraded into small peptides and amino acids.L45454

Rute Eliminasi

At high concentrations, sarilumab is thought to be eliminated predominantly through a non-saturated proteolytic pathway, while at lower concentrations, the elimination will be done by saturable target-mediated elimination.A27262 As a monoclonal antibody, sarilumab is not eliminated through renal or hepatic pathways.L45454

Interaksi Obat

852 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Sarilumab.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Sarilumab.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Sarilumab.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Sarilumab.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Sarilumab.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Sarilumab.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Sarilumab.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Sarilumab.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Sarilumab.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Sarilumab.
Adalimumab The risk or severity of infection can be increased when Adalimumab is combined with Sarilumab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Sarilumab.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Sarilumab.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Sarilumab.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Sarilumab.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Sarilumab.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Sarilumab.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Sarilumab.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Sarilumab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Sarilumab.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Sarilumab.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Sarilumab.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Sarilumab.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Sarilumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Sarilumab.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Sarilumab.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Sarilumab.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Sarilumab.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Sarilumab.
Cladribine Sarilumab may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Sarilumab.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Sarilumab.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Sarilumab.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Sarilumab.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Sarilumab.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Sarilumab.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Sarilumab.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Sarilumab.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Sarilumab.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Sarilumab.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Sarilumab.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Sarilumab.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Sarilumab.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Sarilumab.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Sarilumab.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Sarilumab.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Sarilumab.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Sarilumab.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Sarilumab.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Sarilumab.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Sarilumab.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Sarilumab.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Sarilumab.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Sarilumab.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Sarilumab.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Sarilumab.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Sarilumab.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Sarilumab.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Sarilumab.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Sarilumab.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Sarilumab.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Sarilumab.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Sarilumab.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Sarilumab.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Sarilumab.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Sarilumab.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Sarilumab.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Sarilumab.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Sarilumab.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Sarilumab.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Sarilumab.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Sarilumab.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Sarilumab.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Sarilumab.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Sarilumab.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Sarilumab.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Sarilumab.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Sarilumab.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Sarilumab.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Sarilumab.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Sarilumab.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Sarilumab.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Sarilumab.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Sarilumab.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Sarilumab.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Sarilumab.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Sarilumab.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Sarilumab.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Sarilumab.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Sarilumab.
Mitoxantrone The risk or severity of adverse effects can be increased when Mitoxantrone is combined with Sarilumab.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Sarilumab.
Dexamethasone The risk or severity of adverse effects can be increased when Dexamethasone is combined with Sarilumab.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Sarilumab.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Sarilumab.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Sarilumab.
Abatacept The risk or severity of adverse effects can be increased when Abatacept is combined with Sarilumab.
Corticotropin The risk or severity of adverse effects can be increased when Corticotropin is combined with Sarilumab.
Cortisone acetate The risk or severity of adverse effects can be increased when Cortisone acetate is combined with Sarilumab.
Paramethasone The risk or severity of adverse effects can be increased when Paramethasone is combined with Sarilumab.

Target Protein

Interleukin-6 receptor subunit alpha IL6R
High affinity immunoglobulin gamma Fc receptor I FCGR1A
Low affinity immunoglobulin gamma Fc region receptor II-a FCGR2A
Low affinity immunoglobulin gamma Fc region receptor II-b FCGR2B
Low affinity immunoglobulin gamma Fc region receptor III-A FCGR3A
Low affinity immunoglobulin gamma Fc region receptor III-B FCGR3B

Referensi & Sumber

Artikel (PubMed)
  • PMID: 24297381
    Huizinga TW, Fleischmann RM, Jasson M, Radin AR, van Adelsberg J, Fiore S, Huang X, Yancopoulos GD, Stahl N, Genovese MC: Sarilumab, a fully human monoclonal antibody against IL-6Ralpha in patients with rheumatoid arthritis and an inadequate response to methotrexate: efficacy and safety results from the randomised SARIL-RA-MOBILITY Part A trial. Ann Rheum Dis. 2014 Sep;73(9):1626-34. doi: 10.1136/annrheumdis-2013-204405. Epub 2013 Dec 2.
  • PMID: 25733246
    Genovese MC, Fleischmann R, Kivitz AJ, Rell-Bakalarska M, Martincova R, Fiore S, Rohane P, van Hoogstraten H, Garg A, Fan C, van Adelsberg J, Weinstein SP, Graham NM, Stahl N, Yancopoulos GD, Huizinga TW, van der Heijde D: Sarilumab Plus Methotrexate in Patients With Active Rheumatoid Arthritis and Inadequate Response to Methotrexate: Results of a Phase III Study. Arthritis Rheumatol. 2015 Jun;67(6):1424-37. doi: 10.1002/art.39093.
  • PMID: 26860742
    Cooper S: Sarilumab for the treatment of rheumatoid arthritis. Immunotherapy. 2016;8(3):249-50. doi: 10.2217/imt.15.127. Epub 2016 Feb 9.
  • PMID: 28890641
    Kaufman MB: Pharmaceutical Approval Update. P T. 2017 Sep;42(9):562-580.

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