Golimumab - Drug Monograph

Introduction

Golimumab is a human monoclonal antibody that specifically targets tumor necrosis factor-alpha (TNF-α), a key inflammatory cytokine. Marketed under the brand name Simponi®, it is classified as a biologic disease-modifying antirheumatic drug (bDMARD) and represents an important therapeutic option for several immune-mediated inflammatory conditions. Approved by the FDA in 2009, golimumab joins the class of TNF inhibitors that have revolutionized the treatment of autoimmune disorders.

Mechanism of Action

Golimumab exerts its therapeutic effects by binding with high affinity and specificity to both soluble and transmembrane forms of human TNF-α. This binding prevents TNF-α from interacting with its receptors (TNFR1 and TNFR2), thereby inhibiting TNF-mediated cellular responses. TNF-α plays a central role in the inflammatory cascade by promoting cytokine production, endothelial activation, leukocyte migration, and tissue degradation. By neutralizing TNF-α, golimumab reduces inflammation, decreases joint damage in rheumatic conditions, and improves clinical symptoms across its approved indications.

Indications

Golimumab is FDA-approved for:

• Moderate to severe rheumatoid arthritis (in combination with methotrexate)
• Active psoriatic arthritis
• Active ankylosing spondylitis
• Ulcerative colitis (moderate to severe)
• Polyarticular juvenile idiopathic arthritis (patients aged 2 years and older)

Dosage and Administration

• Rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis: 50 mg subcutaneously once monthly
• Ulcerative colitis: Initial dose of 200 mg subcutaneously at week 0, followed by 100 mg at week 2, then maintenance dose of 100 mg every 4 weeks

• Hepatic impairment: No dose adjustment recommended
• Renal impairment: No dose adjustment recommended
• Elderly: No specific dose adjustment, but increased infection risk
• Pediatrics (≥2 years): 30 mg/m² (maximum 50 mg) every 4 weeks

• Administer subcutaneously in thigh, abdomen, or upper arm
• Rotate injection sites
• Allow prefilled syringe or autoinjector to reach room temperature (30 minutes) before administration

Pharmacokinetics

Contraindications

• Hypersensitivity to golimumab or any component of the formulation
• Active tuberculosis or other serious infections
• Sepsis or risk of sepsis
• Moderate to severe heart failure (NYHA Class III/IV)

Warnings and Precautions

• Serious infections leading to hospitalization or death
• Increased risk of tuberculosis reactivation and invasive fungal infections
• Lymphoma and other malignancies reported in children and adolescents

• Hepatitis B virus reactivation
• Neurologic events (demyelinating disorders)
• Hematologic events (pancytopenia)
• Hypersensitivity reactions
• Worsening heart failure
• Autoimmunity (lupus-like syndrome)

Drug Interactions

Adverse Effects

• Upper respiratory infections
• Injection site reactions (erythema, pain, swelling)

• Viral infections
• Hypertension
• Elevated liver enzymes
• Headache
• Dizziness
• Fatigue
• Bronchitis
• Sinusitis

• Serious infections (sepsis, pneumonia, opportunistic infections)
• Malignancies (lymphoma, skin cancer)
• Heart failure exacerbation
• Demyelinating disorders
• Hepatic reactions
• Hematologic disorders
• Severe hypersensitivity reactions

Monitoring Parameters

• Tuberculosis screening (PPD or interferon-gamma release assay)
• Hepatitis B and C serology
• Complete blood count
• Liver function tests
• Renal function
• Pregnancy test if applicable
• Cardiovascular assessment

• Signs and symptoms of infection at every visit
• CBC and LFTs every 3-6 months
• Skin examination for malignancies annually
• Clinical response assessment
• Injection site reactions
• Patient-reported outcomes

Patient Education

• Proper injection technique training
• Rotation of injection sites
• Storage requirements (refrigerate at 2-8°C, do not freeze)
• Discard unused medication appropriately

• Report any signs of infection immediately (fever, cough, sores)
• Avoid live vaccines during treatment
• Inform all healthcare providers about golimumab use

• Keep all scheduled follow-up appointments
• Report any new neurological symptoms
• Monitor for skin changes or unusual lumps

• Maintain good hygiene practices
• Consider sun protection measures
• Inform dentist about medication before procedures

• Discuss family planning with healthcare provider
• Registry available for pregnancy outcomes
• Limited data on breastfeeding - discuss risks/benefits

References

1. FDA Prescribing Information: Simponi (golimumab). 2023 2. Smolen JS, et al. EULAR recommendations for the management of rheumatoid arthritis. Ann Rheum Dis. 2020;79(6):685-699 3. Singh JA, et al. 2018 American College of Rheumatology Guideline for the Treatment of Rheumatoid Arthritis. Arthritis Rheumatol. 2018;70(3):328-352 4. Sandborn WJ, et al. Subcutaneous golimumab maintains clinical response in patients with moderate-to-severe ulcerative colitis. Gastroenterology. 2014;146(1):96-109 5. Kay J, et al. Golimumab in patients with active rheumatoid arthritis despite treatment with methotrexate: a randomized, double-blind, placebo-controlled, dose-ranging study. Arthritis Rheum. 2008;58(4):964-975 6. Inman RD, et al. Efficacy and safety of golimumab in patients with ankylosing spondylitis: results of a randomized, double-blind, placebo-controlled, phase III trial. Arthritis Rheum. 2008;58(11):3402-3412 7. Clinical Pharmacology [Internet]. Tampa (FL): Gold Standard, Inc.; 2023