Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C6428H9912N1694O1987S46
Độ tan chảy
61 °C (FAB fragment), 71 °C (whole mAb)
Dược Lực Học :
Infliximab is a chimeric human-murine anti-human tumor necrosis factor (TNF) monoclonal antibody. It binds to tumor necrosis factor alpha (TNFa) and inhibits binding of TNFa with its receptors. This reduces production of pro-inflammatory cytokines such as interleukins (IL) 1 and 6. This also limits leukocyte migration and expression of adhesion molecules by endothelial cells and leukocytes. Infliximab also limits the activation of neutrophil and eosinophil functional activity, reduces production of tissue degrading enzymes produced by synoviocytes and/or chondrocytes. Infliximab decreases synovitis and joint erosions in collagen-induced arthritis and allows eroded joints to heal.
Cơ Chế Tác Dụng :
Tumor necrosis factor (TNF-alpha) binding antibody (chimeric IgG1). It is composed of human constant and murine variable regions. Infliximab is produced by a recombinant cell line cultured by continuous perfusion
Infliximab neutralizes the biological activity of TNFa by binding with high affinity to the soluble and transmembrane forms of TNFa and inhibits binding of TNFa with its receptors. Infliximab does not neutralize TNFb (lymphotoxin a), a related cytokine that utilizes the same receptors as TNFa. TNFa activation normally induces the release of proinflammatory cytokines, the enhancement of leukocyte migration and activation of neutrophils among others. Neutralization of the biological activity of TNFa leads to an overall reduction in inflammation.
Dược Động Học :
▧ Absorption :
Onset of action occurs in about 2 weeks in Crohn's disease.
▧ Volume of Distribution :
3-6 L
▧ Metabolism :
Most likely removed by opsonization via the reticuloendothelial system when bound to T lymphocytes, or by human antimurine antibody production. Not metabolized by the CYP enzymes.
▧ Half Life :
9.5 days (7-12 days) in patients with Crohn's disease, plaque psoriasis and rheumatoid arthritis
Chỉ Định :
To manage the signs and symptoms, as well as to induce and maintain clinical remission in adults with moderate to severe active Crohn's disease or ulcerative colitis. Also used to manage signs and symptoms of rheumatoid arthritis (in conjunction with methotrexate), ankylosing spondylitis, psoriatic arthritis, and juvenile arthritis.
Tương Tác Thuốc :
-
Abatacept
The combination shoould be avoided as there have been reports of increased risk of serious infections.
-
Adalimumab
Both bind to TNF alfa and thus combination results in enhanced immunosuppressive effect. It is recommended that simultaneous use of both agents be avoided.
-
Anakinra
Combination may enhance the toxic effect of Anakinra and should be avoided otherwise there may be an increased risk of infection
-
Canakinumab
Avoid combination due to increased risk of infection as anti-TNF agents enhance adverse effects of Canakinumab.
-
Certolizumab pegol
Avoid combination because anti-TNF agents increase adverse effects of certolizumab pegol
-
Denosumab
Therapy should be monitored when combination is initiated as there may be an increase in serious infections.
-
Etanercept
Avoid combination because etanercept may increase immunosuppressive effects of infliximab.
-
golimumab
Avoid combination with infliximab due to the potential increased immunosuppression of infliximab.
-
Leflunomide
Therapy modification should be considered in order to reduce the risk of hematologic toxicities.
-
Natalizumab
Increase adverse effects of natalizumab. Avoid combination
-
Pimecrolimus
Pimecrolimus enhances the adverse effects of immune suppressants thus the combination should be avoided.
-
Rilonacept
Anti-TNF alfa agents enhance adverse effects of rilonacept thus combination should be avoided.
-
Roflumilast
Roflumilast enhances the adverse effects of immune suppressants thus a therapy modification should be considered.
-
Sipuleucel-T
Monitoring is required because immunosuppressants can decrease the therapeutic effect of Sipuleucel-T.
-
Tacrolimus
Avoid combination because of risk of enhance adverse effects of immunosuppressants
-
Tocilizumab
Avoid combination because enhanced immunosuppression by anti-TNF agents.
-
Tofacitinib
Avoid combination with infliximab and other anti-TNF drugs due to the potential enhancement of tofacitinib related adverse effects.
-
Trastuzumab
Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Liều Lượng & Cách Dùng :
Powder, for solution - Intravenous