Dosing & Uses
Dosage Forms & Strengths
SC solution (single-dose prefilled syringe/autoinjector)
- 50mg/0.5mL (Simponi)
- 100mg/1mL (Simponi)
IV solution (single-dose vial)
- 50mg/4mL (Simponi Aria)
Rheumatoid Arthritis
Indicated for moderately-to-severely active rheumatoid arthritis in combination with methotrexate
Simponi: 50 mg SC qMonth
Simponi Aria: 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
Simponi
- 50 mg SC qMonth
Simponi Aria
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
Simponi
- 50 mg SC qMonth
Simponi Aria
2 mg/kg IV at weeks 0 and 4, then q8Weeks
Corticosteroids, NSAIDs, and/or analgesics may be continued during treatment
Ulcerative Colitis
Simponi
- 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
Dosage Modifications
Renal and hepatic impairment
- No formal trial of the effect of renal or hepatic impairment on pharmacokinetics was conducted
Dosing Considerations
Evaluate for active tuberculosis and test for latent infection prior to initiating treatment and periodically during therapy
Before initiating treatment, test patients for hepatitis B viral infection
Safety and efficacy of switching between IV and SC formulations and routes of administration not established
<18 years: Safety and efficacy not established
Polyarticular Juvenile Idiopathic Arthritis (Orphan)
Orphan designation for treatment of polyarticular juvenile idiopathic arthritis in pediatric patients aged ≤16 yr
Sponsor
- Janssen Research & Development, LLC; Welsh & McKean Roads; P. O. Box 776; Spring House, PA 19477
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Simponi
- Upper respiratory tract infection (eg, upper respiratory tract infection, nasopharyngitis, pharyngitis, laryngitis, and rhinitis) (16%)
Simponi Aria
- Upper respiratory tract infection (eg, upper respiratory tract infection, nasopharyngitis, pharyngitis, laryngitis, and rhinitis) (12%)
1-10%
Simponi
- 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%)
Simponi Aria
- Viral infections (eg, influenza and herpes) (3%)
- Hypertension (2%)
- Rash (1%)
- Pyrexia (1%)
- Bronchitis (1%)
Frequency Not Defined
Simponi
- Infections and infestations: Septic shock, atypical mycobacterial infection, pyelonephritis, arthritis bacterial, bursitis infective
- Neoplasms benign, malignant and unspecified: Leukemia
- Skin and subcutaneous tissue disorders: Psoriasis (new onset or worsening, palmar/plantar and pustular), vasculitis (cutaneous)
- Vascular disorders: Vasculitis (systemic)
Simponi Aria
- Infections and infestations: Superficial fungal infection, sinusitis, abscess, lower respiratory tract infection (pneumonia), pyelonephritis
- Investigations: Alanine aminotransferase (ALT) increased, aspartate aminotransferase (AST) increased, neutrophil count decreased
- Nervous system disorders: Dizziness, paresthesia
- Gastrointestinal disorders: Constipation
Postmarketing Reports
Simponi
- Immune system disorders: Serious systemic hypersensitivity reactions (including anaphylactic reaction), sarcoidosis
- Respiratory, thoracic and mediastinal disorders: Interstitial lung disease
- Skin and subcutaneous tissue disorders: Skin exfoliation, rash, bullous skin reactions
Simponi Aria
- General disorders and administration site conditions: Infusion-related reactions
- Neoplasm benign and malignant: Melanoma, Merkel cell carcinoma
- Immune system disorders: Serious systemic hypersensitivity reactions (including anaphylactic reaction), sarcoidosis
- Respiratory, thoracic and mediastinal disorders: Interstitial lung disease
- Skin and SC tissue disorders: Skin exfoliation, lichenoid reactions, bullous skin reactions
Warnings
Black Box Warnings
Serious infection risk
- Increased risk for developing serious infections resulting in hospitalization or death; most patients were taking concomitant immunosuppressants (eg, methotrexate, corticosteroids)
- Patients older than 65 years may be at greater risk
- Discontinue if patient develops serious infection or sepsis
-
Reported infections include:
- Active TB, including reactivation of latent TB (frequently present with disseminated or extrapulmonary disease); test for latent TB before use and during therapy; treat latent infection prior to use
- Invasive fungal infections (eg, histoplasmosis, coccidioidomycosis, candidiasis, aspergillosis, blastomycosis, pneumocystosis); may present with disseminated, rather than localized, disease; antigen/antibody testing for histoplasmosis may be negative in some patients with active infection; initiate empiric antifungal therapy if severe systemic illness develops
- Other bacterial (eg, Legionella, Listeria), mycobacterial (eg, tuberculosis), and viral (eg, hepatitis B) opportunistic pathogens
Malignancy
- Lymphoma and other malignancies, some fatal, have been reported in children and adolescents treated with TNF blockers
- Manufacturer required to report all malignancies to FDA in order for complete and consistent analysis
Contraindications
None
Cautions
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)
- Rare postmarketing cases reported primarily in adolescent and young adult patients with Crohn disease and ulcerative colitis treated with TNF blockers
- Reports have also included a patient being treated for psoriasis and 2 patients being treated for rheumatoid arthritis
- HSTCL is an aggressive, rare type of T-cell lymphoma (usually fatal)
- Most reported cases with TNF blockers have occurred with concomitant treatment with azathioprine or 6-mercaptopurine, although there have been cases reported receiving azathioprine or mercaptopurine alone
Drug interactions overview
- 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
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
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
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)
Absorption
Bioavailability: 53% (Simponi)
Peak plasma time: 2-6 days (Simponi)
Peak plasma concentration: 44.4 mcg/mL (Simponi Aria); 3.2 mcg/mL (Simponi)
Distribution
Vd: 58-126 mL/kg (Simponi); 115 mL/kg (Simponi Aria, healthy subjects); 151 mL/kg (Simponi Aria, RA)
Metabolism
Exact metabolic pathway unknown
Elimination
Clearance: 4.9-6.7 mL/day/kg (Simponi); 6.9 mL/day/kg (Simponi Aria, healthy subjects); 7.6 mL/day/kg (Simponi Aria, RA)
Half-life: ~ 2 weeks
Administration
IV Preparation
Simponi Aria only
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
Simponi Aria only
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
Simponi only
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
Storage
Refrigerate unopened IV and SC products at 2-8ºC (36-46ºF); do not freeze
Keep the product in the original carton to protect from light until the time of use
Once diluted, IV infusion solution may be stored for 4 hr at room temperature
Images
Patient Handout
Formulary
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