Golimumab

• Rheumatoid Arthritis
• Psoriatic Arthritis
• Ankylosing Spondylitis
• Ulcerative Colitis

Golimumab is a fully human monoclonal antibody that targets tumor necrosis factor alpha (TNF-α), used in the treatment of several inflammatory autoimmune conditions. This biologic offers once-monthly subcutaneous or intravenous dosing for sustained TNF inhibition.

Mechanism of Action

Golimumab is a human IgG1κ monoclonal antibody that binds with high affinity and specificity to both soluble and transmembrane forms of human tumor necrosis factor alpha (TNF-α), neutralizing its biological activity. TNF-α is a pro-inflammatory cytokine that plays a central role in the pathogenesis of inflammatory diseases by activating immune cells, inducing other pro-inflammatory cytokines, promoting angiogenesis, and stimulating tissue degradation. By binding to TNF-α, golimumab prevents it from interacting with its cell surface receptors, thereby reducing inflammation, joint damage, and disease activity in autoimmune conditions.

Available Formulations

Golimumab is available for subcutaneous injection in prefilled syringes and autoinjectors (Simponi) containing 50 mg/0.5 mL or 100 mg/mL, and for intravenous infusion (Simponi Aria) as 50 mg/4 mL vials. The SC formulation can be self-administered after proper training. The medication requires refrigeration.

Medical Uses

Golimumab is FDA-approved for moderately to severely active rheumatoid arthritis (with methotrexate), active psoriatic arthritis (alone or with methotrexate), active ankylosing spondylitis, moderately to severely active ulcerative colitis (in patients with inadequate response to prior therapy or requiring continuous corticosteroids), and active polyarticular juvenile idiopathic arthritis (IV formulation, ages 2+). Clinical trials demonstrated significant improvements in signs and symptoms, physical function, and quality of life.

Dosing Guidelines

For rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis, the SC dose is 50 mg once monthly. For ulcerative colitis, the SC dose is 200 mg initially, 100 mg at week 2, then 100 mg every 4 weeks; patients under 80 kg with inadequate response may continue 100 mg, while those 80 kg or over may increase to 200 mg. For IV administration (RA), 2 mg/kg is given at weeks 0 and 4, then every 8 weeks. SC injections should be given in the thigh, lower abdomen, or upper arm.

Important Safety Information

Golimumab carries boxed warnings for serious infections (including tuberculosis, invasive fungal infections, bacterial/viral infections, and opportunistic infections) and malignancy (including lymphoma and other malignancies, some fatal, in children and adolescents). All patients should be tested for latent TB before starting therapy. Treatment should not be initiated during active infections. Other serious risks include hepatitis B reactivation, heart failure worsening, demyelinating disease, cytopenias, lupus-like syndrome, and serious allergic reactions.

Drug Interactions

Concurrent use with anakinra or abatacept is not recommended due to increased serious infection risk. Live vaccines should not be given concurrently. No formal drug interaction studies have been conducted. The formation of CYP450 enzymes may be altered by chronic inflammation; monitoring is recommended for narrow therapeutic index drugs when starting or stopping golimumab.

Special Populations

There are limited data on golimumab use during pregnancy. Animal studies showed no evidence of harm. Use during pregnancy only if clearly needed. It is unknown whether golimumab is excreted in human breast milk; caution is advised. Safety and efficacy of IV golimumab have been established in children 2 years and older with polyarticular juvenile idiopathic arthritis; SC golimumab is not approved for pediatric patients. Elderly patients may be at increased risk for infections. No dose adjustment is needed for renal or hepatic impairment based on available data.