Simponi

Golimumab is approved and clinically used for the treatment of several autoimmune and inflammatory diseases, including:

• Rheumatoid Arthritis (RA):
  • For adults with moderately to severely active RA, usually in combination with methotrexate, to reduce signs and symptoms, inhibit structural damage, and improve physical function.
• Ankylosing Spondylitis (AS):
  • For adults with active AS to reduce symptoms and improve spinal mobility.
• Psoriatic Arthritis (PsA):
  • For adults with active PsA to reduce signs and symptoms, improve physical function, and inhibit structural joint damage.
• Ulcerative Colitis (UC):
  • For adults with moderately to severely active UC to induce and maintain clinical remission and mucosal healing, particularly in patients with inadequate response to conventional therapy.
• Plaque Psoriasis:
  • For adults with moderate to severe chronic plaque psoriasis who are candidates for systemic therapy or phototherapy.
• Other Off-label/Clinically Accepted Uses:
  • Occasionally used off-label for other TNF-alpha mediated inflammatory conditions where anti-TNF therapy is indicated.

• Route:
  • Administered by subcutaneous injection.
• Rheumatoid Arthritis, Psoriatic Arthritis, Ankylosing Spondylitis, Plaque Psoriasis:
  • Initial dose: 50 mg subcutaneously once monthly.
  • For RA and PsA, often given with methotrexate.
  • For patients over 100 kg or with insufficient response, dose may be increased to 100 mg once monthly.
• Ulcerative Colitis:
  • Induction: 200 mg subcutaneously at week 0, then 100 mg at week 2.
  • Maintenance: 100 mg every 4 weeks starting at week 6.
• Pediatrics:
  • Safety and efficacy not established; not routinely recommended.
• Elderly:
  • No specific dose adjustments; use with caution due to increased infection risk.
• Renal/Hepatic Impairment:
  • No dose adjustment required; however, monitor patients carefully.
• Administration Notes:
  • Rotate injection sites with each administration.
  • Patient or caregiver may self-inject after proper training.
  • Use sterile technique and dispose of needles safely.

Golimumab is a fully human monoclonal antibody that selectively binds to tumor necrosis factor-alpha (TNF-α), a pro-inflammatory cytokine central to the pathogenesis of autoimmune diseases. By binding with high affinity to both soluble and transmembrane forms of TNF-α, golimumab neutralizes its biological activity, preventing TNF-α from interacting with its cell surface receptors. This blockade inhibits downstream inflammatory signaling pathways, leading to reduced inflammation, decreased joint and tissue destruction, and amelioration of clinical symptoms in diseases such as rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, and ulcerative colitis.

• Absorption:
  • Subcutaneous administration results in slow absorption; peak serum concentrations occur approximately 2 to 6 days post-dose.
• Bioavailability:
  • Approximately 53% after subcutaneous injection.
• Distribution:
  • Volume of distribution is about 6.4 L, limited to the vascular and extracellular space.
• Metabolism:
  • Metabolized via proteolytic enzymes into small peptides and amino acids.
• Elimination Half-life:
  • Approximately 14 days, supporting once-monthly dosing.
• Excretion:
  • No renal or hepatic excretion; clearance primarily via reticuloendothelial system.

• Pregnancy:
  • Classified as FDA Pregnancy Category B. Animal studies showed no teratogenicity, but adequate well-controlled human studies are lacking. Use only if clearly needed, balancing benefits and risks.
• Lactation:
  • Limited data available; monoclonal antibodies may be present in breast milk in low amounts but are unlikely absorbed orally by the infant. Caution advised.

• Primary Class: Tumor Necrosis Factor (TNF) inhibitor
• Subclass: Monoclonal antibody, anti-TNF biologic agent

• Known hypersensitivity to golimumab or any excipients.
• Active serious infections including tuberculosis, sepsis, opportunistic infections.
• Moderate to severe heart failure (NYHA class III/IV).
• Concurrent use with other biologic TNF inhibitors or live vaccines.

• Infections:
  • Increased risk of serious infections including tuberculosis, fungal, viral, and bacterial infections. Screen for latent TB before initiation. Monitor patients closely.
• Malignancies:
  • Possible increased risk of lymphoma and other malignancies.
• Heart Failure:
  • Use caution; may worsen congestive heart failure.
• Immunizations:
  • Avoid live vaccines during and shortly after treatment.
• Neurological Reactions:
  • Rare cases of demyelinating disorders reported.
• Hypersensitivity:
  • Anaphylaxis and serious allergic reactions possible; monitor closely during administration.

• Common:
  • Upper respiratory tract infections, nasopharyngitis, headache, injection site reactions, nausea.
• Serious/Rare:
  • Serious infections (e.g., pneumonia, TB), malignancies, congestive heart failure exacerbation, demyelinating disease, pancytopenia, liver enzyme elevations, anaphylaxis.
• Onset:
  • Infections and hypersensitivity reactions can occur anytime; injection site reactions typically appear shortly after administration.

• Major interactions:
  • Avoid concomitant use with other biologic immunosuppressants (e.g., other anti-TNF agents, abatacept).
  • Immunosuppressive drugs (e.g., methotrexate) may increase infection risk but often used together with close monitoring.
• Drug-Food and Drug-Alcohol:
  • No significant known interactions.
• Metabolic Pathways:
  • Not metabolized by CYP450 enzymes; minimal interaction potential via CYP pathways.

• Updated guidelines recommend screening and treatment for latent tuberculosis before starting golimumab.
• Increased emphasis on infection risk monitoring and patient education.
• Recent studies support golimumab's efficacy in early and moderate disease stages for approved indications.
• No major recent changes in approved dosing schedules.

• Store refrigerated at 2°C to 8°C (36°F to 46°F).
• Protect from light; do not freeze.
• Allow to reach room temperature before injection (approximately 15–30 minutes outside the refrigerator).
• Do not shake the solution.
• Keep out of reach of children.