Infliximab

DB00065

biotech approved

Deskripsi

Infliximab is a tumor necrosis factor (TNF-alpha or TNF-?) blocker and a chimeric monoclonal IgG1 antibody composed of human constant (75%) and murine variable (25%) regions A31469. Infliximab is produced by a recombinant cell line cultured by continuous perfusion. Tumor necrosis factor-alpha (TNF-?) is a key proinflammatory cytokine involved in chronic inflammatory diseases A31469. Its hyperactivity and enhanced signalling pathways can be observed in inflammatory diseases where it activates further pro-inflammatory cascades. By binding to both the soluble subunit and the membrane-bound precursor of TNF-? A106, infliximab disrupts the interaction of TNF-? with its receptors and may also cause lysis of cells that produce TNF-? A106.

Infliximab was first approved by the FDA in 1998 under the market name Remicade as an intravenous injection. It is indicated for the treatment of various inflammatory disorders such as adult or pediatric Chron's disease, adult or pediatric ulcerative colitis, rheumatoid arthritis in combination with methotrexate, ankylosing spondyliti, psoriatic arthritis, and plaque psoriasis FDA Label. In clinical trials, multiple infusions of infliximab displayed in a reduction of signs and symptoms of inflammatory diseases and induction of remission in patients who have had an inadequate response to alternative first-line therapies for that disorder FDA Label.

There are currently two biosilimars of infliximab available in the US market that demonstrate a high degree of similarity to the reference product, Remicade. They are approved for all eligible indications of the reference product. Inflectra, a first biosimilar drug product, was approved in 2016. In December 2017, Ixifi, a second biosimilar that was developed by Pfizer, was granted approval by the FDA.

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 median terminal half-life of infliximab is 7.7 to 9.5 days. The data is based on a pharmacokinetic study in patients with Crohn's disease, plaque psoriasis and rheumatoid arthritis receiving a single dose of infliximab [FDA Label].
Volume Distribusi Based on a pharmacokinetic study of adult patients, the distribution at steady state was independent of dose and indicated that infliximab was distributed primarily within the vascular compartment [FDA Label]. In patients with Crohn's disease, the apparent volume of distribution at steady state (Vss) of infliximab following single doses of 5 mg/kg and 10 mg/kg was 80 mL/kg and 65 mL/kg, respectively. In a maintenance therapy study, multiple infusions of infliximab (at week 0, 2 and 6) at the same dose of 5 mg/kg and 10 mg/kg resulted in Vss of 70 mL/kg and 81 mL/kg , respectively [A31469]. In patients with rheumatoid arthritis, the Vss of infliximab following a single dose infusion of 5 mg/kg, 10 mg/kg and 20 mg/kg were 4.3±2.5 L, 3.2±0.7 L, and 3.1±0.6 L, respectively [A31469].
Klirens (Clearance) In patients with Crohn's disease, the total body clearance (CL) of infliximab following single doses of 5 mg/kg and 10 mg/kg was 18.4 mL/h and 14.3 mL/h, respectively. In a maintenance therapy study, multiple infusions of infliximab (at week 0, 2 and 6) at the same dose of 5 mg/kg and 10 mg/kg resulted in CL of 15.2 mL/h and 15.2 mL/h, respectively [A31469]. In patients with rheumatoid arthritis, the CL of infliximab following a single dose infusion of 5 mg/kg, 10 mg/kg and 20 mg/kg were 11±7.5 mL/h, 11.4±5 mL/h, and 11±8.9 mL/h, respectively [A31469]. Development of antibodies to infliximab increased infliximab clearance [FDA Label].

Absorpsi

Following a single intravenous infusion, infliximab absorption displays a linear relationship between the dose administered and the maximum serum concentration FDA Label. In patients with Crohn's disease, the maximum plasma concentration (Cmax) of infliximab following single doses of 5 mg/kg and 10 mg/kg was 75 µg/mL and 181 µg/mL, respectively. In a maintenance therapy study, multiple infusions of infliximab (at week 0, 2 and 6) at the same dose of 5 mg/kg and 10 mg/kg resulted in Cmax of 120 µg/mL and 189 µg/mL , respectively A31469. In patients with rheumatoid arthritis, the Cmax of infliximab following a single dose infusion of 5 mg/kg, 10 mg/kg and 20 mg/kg were 192±51 µg/mL, 427±106 µg/mL, and 907±183 µg/mL, respectively A31469.

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Therapeutic monoclonal antibodies including infliximab are predicted to be nonspecifically metabolized to peptides and amino acids that can be re-used in the body for de novo synthesis of proteins or arc excreted by the kidney A19126. The reticuloendothelial system (RES) are phagocytic cells of the immune system such as macrophages and monocytes that play a role in the elimination of endogenous IgG antibodies. Although administered infliximab accounts for a small fraction of total endogenous IgG and this route is not likely saturated by therapeutic mAbs, infliximab may be removed by opsonization via RES following binding of the Fc part of the antibody to Fcy-receptors expressed on the RES A19126.

Farmakogenomik

1 Varian
FCGR3A (rs1801274)

Patients with this genotype have increased ACR20 response when using infliximab to treat rheumatoid arthritis.

Interaksi Obat

1383 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Infliximab.
Etanercept Etanercept may increase the immunosuppressive activities of Infliximab.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Infliximab.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Infliximab.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Infliximab.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Infliximab.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Infliximab.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Infliximab.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Infliximab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Infliximab.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Infliximab.
Interferon beta-1b The risk or severity of adverse effects can be increased when Infliximab is combined with Interferon beta-1b.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Infliximab is combined with Interferon alfacon-1.
Rituximab The risk or severity of adverse effects can be increased when Infliximab is combined with Rituximab.
Basiliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Basiliximab.
Muromonab The risk or severity of adverse effects can be increased when Infliximab is combined with Muromonab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Infliximab is combined with Ibritumomab tiuxetan.
Tositumomab The risk or severity of adverse effects can be increased when Infliximab is combined with Tositumomab.
Alemtuzumab The risk or severity of adverse effects can be increased when Infliximab is combined with Alemtuzumab.
Alefacept The risk or severity of adverse effects can be increased when Infliximab is combined with Alefacept.
Efalizumab The risk or severity of adverse effects can be increased when Infliximab is combined with Efalizumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Infliximab is combined with Antithymocyte immunoglobulin (rabbit).
Interferon alfa-2b The risk or severity of adverse effects can be increased when Infliximab is combined with Interferon alfa-2b.
Daclizumab The risk or severity of adverse effects can be increased when Infliximab is combined with Daclizumab.
Phenylalanine The risk or severity of adverse effects can be increased when Infliximab is combined with Phenylalanine.
Cladribine Infliximab may increase the immunosuppressive activities of Cladribine.
Amsacrine The risk or severity of adverse effects can be increased when Infliximab is combined with Amsacrine.
Bleomycin The risk or severity of adverse effects can be increased when Infliximab is combined with Bleomycin.
Chlorambucil The risk or severity of adverse effects can be increased when Infliximab is combined with Chlorambucil.
Raltitrexed The risk or severity of adverse effects can be increased when Infliximab is combined with Raltitrexed.
Mitomycin The risk or severity of adverse effects can be increased when Infliximab is combined with Mitomycin.
Floxuridine The risk or severity of adverse effects can be increased when Infliximab is combined with Floxuridine.
Tioguanine The risk or severity of adverse effects can be increased when Infliximab is combined with Tioguanine.
Dexrazoxane The risk or severity of adverse effects can be increased when Infliximab is combined with Dexrazoxane.
Streptozocin The risk or severity of adverse effects can be increased when Infliximab is combined with Streptozocin.
Trifluridine The risk or severity of adverse effects can be increased when Infliximab is combined with Trifluridine.
Gemcitabine The risk or severity of adverse effects can be increased when Infliximab is combined with Gemcitabine.
Epirubicin The risk or severity of adverse effects can be increased when Infliximab is combined with Epirubicin.
Chloramphenicol The risk or severity of adverse effects can be increased when Infliximab is combined with Chloramphenicol.
Lenalidomide The risk or severity of adverse effects can be increased when Infliximab is combined with Lenalidomide.
Altretamine The risk or severity of adverse effects can be increased when Infliximab is combined with Altretamine.
Cisplatin The risk or severity of adverse effects can be increased when Infliximab is combined with Cisplatin.
Oxaliplatin The risk or severity of adverse effects can be increased when Infliximab is combined with Oxaliplatin.
Propylthiouracil The risk or severity of adverse effects can be increased when Infliximab is combined with Propylthiouracil.
Pentostatin The risk or severity of adverse effects can be increased when Infliximab is combined with Pentostatin.
Linezolid The risk or severity of adverse effects can be increased when Infliximab is combined with Linezolid.
Clofarabine The risk or severity of adverse effects can be increased when Infliximab is combined with Clofarabine.
Methimazole The risk or severity of adverse effects can be increased when Infliximab is combined with Methimazole.
Sulfasalazine The risk or severity of adverse effects can be increased when Infliximab is combined with Sulfasalazine.
Temozolomide The risk or severity of adverse effects can be increased when Infliximab is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Infliximab is combined with Penicillamine.
Mechlorethamine The risk or severity of adverse effects can be increased when Infliximab is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Infliximab is combined with Azacitidine.
Carboplatin The risk or severity of adverse effects can be increased when Infliximab is combined with Carboplatin.
Dactinomycin The risk or severity of adverse effects can be increased when Infliximab is combined with Dactinomycin.
Hydroxyurea The risk or severity of adverse effects can be increased when Infliximab is combined with Hydroxyurea.
Mycophenolic acid The risk or severity of adverse effects can be increased when Infliximab is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Infliximab is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Infliximab is combined with Mercaptopurine.
Melphalan The risk or severity of adverse effects can be increased when Infliximab is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Infliximab is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Infliximab is combined with Flucytosine.
Procarbazine The risk or severity of adverse effects can be increased when Infliximab is combined with Procarbazine.
Arsenic trioxide The risk or severity of adverse effects can be increased when Infliximab is combined with Arsenic trioxide.
Mitoxantrone The risk or severity of adverse effects can be increased when Infliximab is combined with Mitoxantrone.
Lomustine The risk or severity of adverse effects can be increased when Infliximab is combined with Lomustine.
Eculizumab The risk or severity of adverse effects can be increased when Infliximab is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Infliximab is combined with Decitabine.
Nelarabine The risk or severity of adverse effects can be increased when Infliximab is combined with Nelarabine.
Stepronin The risk or severity of adverse effects can be increased when Infliximab is combined with Stepronin.
Castanospermine The risk or severity of adverse effects can be increased when Infliximab is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Infliximab is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Infliximab is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Infliximab is combined with Brequinar.
Afelimomab The risk or severity of adverse effects can be increased when Infliximab is combined with Afelimomab.
Interferon alfa The risk or severity of adverse effects can be increased when Infliximab is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Infliximab is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Infliximab is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Infliximab is combined with Human interferon omega-1.
Mepolizumab The risk or severity of adverse effects can be increased when Infliximab is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Infliximab is combined with Abetimus.
Golimumab The risk or severity of adverse effects can be increased when Infliximab is combined with Golimumab.
Belatacept The risk or severity of adverse effects can be increased when Infliximab is combined with Belatacept.
Pralatrexate The risk or severity of adverse effects can be increased when Infliximab is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Infliximab is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Infliximab is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Infliximab is combined with Belimumab.
Teriflunomide The risk or severity of adverse effects can be increased when Infliximab is combined with Teriflunomide.
Carfilzomib The risk or severity of adverse effects can be increased when Infliximab is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Infliximab is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Infliximab is combined with Obinutuzumab.
Secukinumab The risk or severity of adverse effects can be increased when Infliximab is combined with Secukinumab.
Siltuximab The risk or severity of adverse effects can be increased when Infliximab is combined with Siltuximab.
Blinatumomab The risk or severity of adverse effects can be increased when Infliximab is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Infliximab is combined with Dinutuximab.
Tixocortol The risk or severity of adverse effects can be increased when Infliximab is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Infliximab is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Infliximab is combined with Antilymphocyte immunoglobulin (horse).
Tepoxalin The risk or severity of adverse effects can be increased when Infliximab is combined with Tepoxalin.
Ixekizumab The risk or severity of adverse effects can be increased when Infliximab is combined with Ixekizumab.

Target Protein

Tumor necrosis factor TNF

Referensi & Sumber

Artikel (PubMed)
  • PMID: 10228190
    Present DH, Rutgeerts P, Targan S, Hanauer SB, Mayer L, van Hogezand RA, Podolsky DK, Sands BE, Braakman T, DeWoody KL, Schaible TF, van Deventer SJ: Infliximab for the treatment of fistulas in patients with Crohn's disease. N Engl J Med. 1999 May 6;340(18):1398-405.
  • PMID: 14985485
    Sands BE, Anderson FH, Bernstein CN, Chey WY, Feagan BG, Fedorak RN, Kamm MA, Korzenik JR, Lashner BA, Onken JE, Rachmilewitz D, Rutgeerts P, Wild G, Wolf DC, Marsters PA, Travers SB, Blank MA, van Deventer SJ: Infliximab maintenance therapy for fistulizing Crohn's disease. N Engl J Med. 2004 Feb 26;350(9):876-85.
  • PMID: 17655372
    Klotz U, Teml A, Schwab M: Clinical pharmacokinetics and use of infliximab. Clin Pharmacokinet. 2007;46(8):645-60. doi: 10.2165/00003088-200746080-00002.
  • PMID: 20608753
    Keizer RJ, Huitema AD, Schellens JH, Beijnen JH: Clinical pharmacokinetics of therapeutic monoclonal antibodies. Clin Pharmacokinet. 2010 Aug;49(8):493-507. doi: 10.2165/11531280-000000000-00000.
  • PMID: 29763197
    Fatima R, Bittar K, Aziz M: Infliximab. .

Contoh Produk & Brand

Produk: 54 • International brands: 1
Produk
  • Avsola
    Injection, powder, lyophilized, for solution • 100 mg/10mL • Intravenous • US • Approved
  • Avsola
    Powder, for solution • 100 mg / vial • Intravenous • Canada • Approved
  • Flixabi
    Injection, powder, for solution • 100 mg • Intravenous • EU • Approved
  • Flixabi
    Injection, powder, for solution • 100 mg • Intravenous • EU • Approved
  • Flixabi
    Injection, powder, for solution • 100 mg • Intravenous • EU • Approved
  • Flixabi
    Injection, powder, for solution • 100 mg • Intravenous • EU • Approved
  • Flixabi
    Injection, powder, for solution • 100 mg • Intravenous • EU • Approved
  • Inflectra
    Injection, powder, lyophilized, for solution • 100 mg/10mL • Intravenous • US • Approved
Menampilkan 8 dari 54 produk.
International Brands
  • Avsola — Amgen

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul