Golimumab

Indications

Golimumab is used for: Rheumatoid Arthritis, Psoriatic Arthritis, Ankylosing Spondylitis, Ulcerative Colitis

Adult Dose

Rheumatoid Arthritis Indicated for moderately-to-severely active rheumatoid arthritis in combination with methotrexate SC solution: 50 mg SC qMonth IV solution: 2 mg/kg IV at weeks 0 and 4, then q8Weeks Psoriatic Arthritis Indicated for moderately-to-severely active rheumatoid arthritis in combination with methotrexate SC solution 50 mg SC qMonth IV solution 2 mg/kg IV at weeks 0 and 4, then q8Weeks Corticosteroids, nonsteroidal anti-inflammatory drugs (NSAIDs), and/or analgesics may be continued during treatment Ankylosing Spondylitis Indicated for active ankylosing spondylitis with or without methotrexate SC solution 50 mg SC qMonth IV solution 2 mg/kg IV at weeks 0 and 4, then q8Weeks Corticosteroids, NSAIDs, and/or analgesics may be continued during treatment Ulcerative Colitis SC solution Indicated in adults with moderate to severe active ulcerative colitis who demonstrate corticosteroid dependence or who have an inadequate response to or failed to tolerate oral aminosalicylates, oral corticosteroids, azathioprine, or 6-mercaptopurine for inducing and maintaining clinical response, improving endoscopic appearance of the mucosa during induction, inducing clinical remission, achieving and sustaining clinical remission in induction responders Initial: 200 mg SC at Week 0, followed by 100 mg SC at Week 2, THEN Maintenance: 100 mg SC q4Weeks

Child Dose

Renal Dose

Renal impairment No formal trial of the effect of renal or hepatic impairment on pharmacokinetics was conducted

Administration

IV Preparation Inspect vial; solution is colorless to light yellow and opalescent Do not use if opaque particles, discoloration or other foreign particles are present Dilute calculated dose volume with 0.9% NaCl to a final volume of 100 mL; alternatively, 0.45% NaCl Injection, USP can also be used; gently mix (DO NOT SHAKE) Discard any unused drug remaining in the vials IV Administration Use only an infusion set with an in-line, sterile, nonpyrogenic, low protein-binding filter (pore size 0.22 micrometer or less) Do not administer concomitantly in same IV line with other agents Infuse over 30 minutes SC Administration Warm by sitting at room temperature for 30 min; do NOT heat or microwave If multiple injections required, administer at different site on the body Injection sites: Front of thighs (recommended), lower abdomen (except for a 2-inch area right around the navel); back of the upper arms (only if someone else is administering it) Rotate injection sites for each administration Do not administer in area where the skin is tender, bruised, red, or hard

Contra Indications

Precautions

Risk of infections, reactivation of latent hepatitis/TB; interrupt if serious infection develops (eg, bacterial sepsis, severe invasive fungal infections, opportunistic infections) Risk of exacerbation of or new onset heart failure; discontinue therapy if worsening symptoms occur; fatal outcomes reported in patients with congestive heart failure Pancytopenia, leukopenia, neutropenia, agranulocytosis, aplastic anemia, and thrombocytopenia may occur; exercise caution when using TNF-blockers in patients who have or have had significant cytopenias Use of TNF-blockers, including golimumab, has been associated with rare cases of new onset or exacerbation of central nervous system (CNS) demyelinating disorders (eg, multiple sclerosis [MS]) and peripheral demyelinating disorders (eg, Guillain Barre syndrome) Treatment with TNF blockers, including golimumab, may result in the formation of antinuclear antibodies (ANA); rarely, treatment with TNF blockers, may result in the development of a lupus-like syndrome; if a patient develops symptoms suggestive of a lupus-like syndrome following treatment, discontinue treatment Serious systemic hypersensitivity reactions including anaphylaxis may occur Severe hepatic reactions including acute liver failure in patients receiving TNF blockers reported Malignancies Increased risk of lymphoma and other cancers reported in children and adolescents Occurrence of leukemia and new-onset psoriasis in patients treated with TNF blockers Skin cancer (melanoma, Merkel cell carcinoma) reported with TNF blockers; perform periodic skin examination for all patients, particularly those with risk factors for skin cancer Hepatosplenic T-cell lymphomas (HSTCL)

Pregnancy-Lactation

Pregnancy There are no adequate and well-controlled trials in pregnant women; monoclonal antibodies are transported across the placenta during the third trimester and may affect immune response in the in utero exposed infant Use during pregnancy only if clearly needed Clinical considerations Golimumab crosses the placenta during pregnancy; another TNF-blocking monoclonal antibody administered during pregnancy detected for up to 6 months in serum of infants; consequently, infants may be at increased risk of infection Live vaccines administration to infants exposed to golimumab in utero is not recommended for 6 months following the mother’s last dose during pregnancy Lactation There is no information regarding the presence in human milk, the effects on breastfed infants, or the effects on milk production Maternal IgG is known to be present in human milk; the effects of local exposure in gastrointestinal tract and potential limited systemic exposure in the infant to golimumab are unknown; developmental and health benefits of breast-feeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breast-fed infants or from the underlying maternal condition

Interactions

Infection risk increases when coadministered with abatacept, anakinra, or rituximab; combination is not recommended Care should be taken when switching from one biologic product to another biologic product since overlapping biological activity may further increase the risk of infection May decrease humoral response to live-virus vaccines (eg, MMR) Administration of live virus vaccines and therapeutic agents (eg, BCG bladder instillation) may result in disseminated infections Formation of CYP450 enzymes may be suppressed by increased levels of cytokines (eg, TNF-alpha) during chronic inflammation; molecules (eg, golimumab) that antagonizes cytokine activity may normalize the formation of CYP450 enzymes; upon initiation or discontinuation of treatment in patients being treated with CYP450 substrates with a narrow therapeutic index, monitoring of the effects (eg, warfarin) or drug concentrations (eg, cyclosporine or theophylline) is recommended and adjusting individual doses of the drug products as needed

Adverse Effects

Side effects of Golimumab : >10% SC solution Upper respiratory tract infection (eg, upper respiratory tract infection, nasopharyngitis, pharyngitis, laryngitis, and rhinitis) (16%) IV solution Upper respiratory tract infection (eg, upper respiratory tract infection, nasopharyngitis, pharyngitis, laryngitis, and rhinitis) (12%) 1-10% SC solution Injection site reactions (eg, erythema, urticaria, induration, pain, bruising, pruritus, irritation, paresthesia) (6%) Viral infections (eg, influenza and herpes) (5%) Increased ALT (4%) Increased AST (3%) Dizziness (2%) Paresthesia (2%) Bronchitis (2%) Superficial fungal infections (2%) Sinusitis (2%) Constipation (1%) IV solution Viral infections (eg, influenza and herpes) (3%) Hypertension (2%) Rash (1%) Pyrexia (1%) Bronchitis (1%)

Mechanism of Action

Human anti-TNF-alpha monoclonal antibody, binds to both soluble and transmembrane bioactive forms of human TNFα; prevents binding of TNF-alpha to its receptors, thereby inhibiting biological activity of TNFα (a cytokine protein)