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Golimumab

Pronunciation

(goe LIM ue mab)

Index Terms

  • CNTO-148

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Intravenous [preservative free]:

Simponi Aria: 50 mg/4 mL (4 mL) [latex free; contains polysorbate 80]

Solution Auto-injector, Subcutaneous [preservative free]:

Simponi: 50 mg/0.5 mL (0.5 mL); 100 mg/mL (1 mL) [contains polysorbate 80]

Solution Prefilled Syringe, Subcutaneous [preservative free]:

Simponi: 50 mg/0.5 mL (0.5 mL); 100 mg/mL (1 mL) [contains polysorbate 80]

Brand Names: U.S.

  • Simponi
  • Simponi Aria

Pharmacologic Category

  • Antipsoriatic Agent
  • Antirheumatic, Disease Modifying
  • Monoclonal Antibody
  • Tumor Necrosis Factor (TNF) Blocking Agent

Pharmacology

Human monoclonal antibody that binds to human tumor necrosis factor alpha (TNFα), thereby interfering with endogenous TNFα activity. Biological activities of TNFα include the induction of proinflammatory cytokines (interleukin [IL]-6, IL-8, Granulocyte-colony stimulating factor, granulocyte-macrophage colony stimulating factor), expression of adhesion molecules (E-selectin, vascular cell adhesion molecule [VCAM]-1, intercellular adhesion molecule [ICAM]-1) necessary for leukocyte infiltration, activation of neutrophils and eosinophils.

Distribution

Vd: IV: 151 ± 61 mL/kg (distributed primarily to circulatory system with limited extravascular distribution)

Metabolism

Pathway unknown

Time to Peak

SubQ: 2-6 days

Half-Life Elimination

~2 weeks

Special Populations Note

Weight: Following IV administration, patients with higher body weights tended to have higher serum golimumab concentrations (compared to lower body weights).

Use: Labeled Indications

Ankylosing spondylitis (Simponi): Treatment of adults with active ankylosing spondylitis

Psoriatic arthritis (Simponi): Treatment of adults with active psoriatic arthritis (alone or in combination with methotrexate)

Rheumatoid arthritis (Simponi, Simponi Aria): Treatment of adults with moderately-to-severely active rheumatoid arthritis (in combination with methotrexate)

Ulcerative colitis (Simponi): Treatment of adults with moderately-to-severely active ulcerative colitis in patients with corticosteroid dependence or who are refractory or intolerant to oral aminosalicylates, oral corticosteroids, azathioprine, or 6-mercaptopurine (to induce and maintain clinical response, improve mucosal appearance during induction, induce clinical remission, and achieve and sustain remission in induction responders)

Contraindications

There are no contraindications listed in the manufacturer’s US labeling.

Canadian labeling: Hypersensitivity to golimumab, latex, or any other component of formulation or packaging; patients with severe infections (eg, sepsis, tuberculosis, opportunistic infections); moderate or severe heart failure (NYHA class III/IV)

Dosage

Note: Corticosteroids, nonbiologic disease-modifying antirheumatic drugs (DMARDs), and/or NSAIDs may be continued for the treatment of rheumatoid arthritis, psoriatic arthritis, or ankylosing spondylitis. Golimumab should not be used in combination with biologic DMARDs.

Ankylosing spondylitis: Adults: SubQ: 50 mg once a month (either alone or in combination with methotrexate or other nonbiologic DMARDs)

Psoriatic arthritis: Adults: SubQ: 50 mg once a month (either alone or in combination with methotrexate or other nonbiologic DMARDs)

Rheumatoid arthritis: Adults:

IV: 2 mg/kg at weeks 0, 4, and then every 8 weeks thereafter (in combination with methotrexate)

SubQ: 50 mg once a month (in combination with methotrexate)

Ulcerative colitis: Adults:

US labeling: SubQ: Induction: 200 mg at week 0, then 100 mg at week 2, followed by maintenance therapy of 100 mg every 4 weeks

Canadian labeling: SubQ: Induction: 200 mg at week 0, then 100 mg at week 2, followed by maintenance therapy of 50 mg every 4 weeks (maintenance dose may be increased to 100 mg every 4 weeks if needed)

Dosage adjustment in renal impairment: There are no dosage adjustments provided in manufacturer’s labeling (has not been studied).

Dosage adjustment in hepatic impairment: There are no dosage adjustments provided in manufacturer’s labeling (has not been studied).

Reconstitution

Intact solution should be colorless to light yellow; solution may develop a few fine, translucent particles.

SubQ: Bring to room temperature by allowing syringe/autoinjector to sit at room temperature outside the carton for 30 minutes prior to administration (do not warm in any other way). Do not use if discolored, cloudy, or if foreign particles are present.

IV: Do not use if solution is discolored, or contains opaque or foreign particles. Dilute for infusion by slowly adding calculated dose/volume to sodium chloride 0.9% to a total volume of 100 mL. Gently mix.

Discard unused portion of vial/syringe/autoinjector.

Administration

IV: Dilute prior to use. Infuse over 30 minutes, using an infusion set with an in-line low protein-binding 0.22 micron filter. Do not infuse in the same line with other medications.

Subcutaneous injection: Hold autoinjector firmly against skin and inject subcutaneously into thigh, lower abdomen (below navel), or upper arm. A loud click is heard when injection has begun. Continue to hold autoinjector against skin until second click is heard (may take 3-15 seconds). Following second click, lift autoinjector from injection site. Rotate injection sites and avoid injecting into tender, red, scaly, hard, or bruised skin, or areas with scars or stretch marks. If multiple injections are required for a single dose, administer at different sites on body.

Compatibility

Stable in NS.

Storage

Store intact vials and syringes refrigerated at 2°C to 8°C (36°F to 46°F); do not freeze. Do not shake. Store product in original carton to protect from light.

IV: Solutions diluted for infusion may be stored at room temperature for 4 hours.

Drug Interactions

Abatacept: Anti-TNF Agents may enhance the adverse/toxic effect of Abatacept. An increased risk of serious infection during concomitant use has been reported. Avoid combination

Anakinra: Anti-TNF Agents may enhance the adverse/toxic effect of Anakinra. An increased risk of serious infection during concomitant use has been reported. Avoid combination

BCG (Intravesical): Immunosuppressants may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

Belimumab: Monoclonal Antibodies may enhance the adverse/toxic effect of Belimumab. Avoid combination

Canakinumab: Anti-TNF Agents may enhance the adverse/toxic effect of Canakinumab. Specifically, the risk for serious infections and/or neutropenia may be increased. Avoid combination

Certolizumab Pegol: Anti-TNF Agents may enhance the immunosuppressive effect of Certolizumab Pegol. Avoid combination

Coccidioides immitis Skin Test: Immunosuppressants may diminish the diagnostic effect of Coccidioides immitis Skin Test. Monitor therapy

Denosumab: May enhance the adverse/toxic effect of Immunosuppressants. Specifically, the risk for serious infections may be increased. Monitor therapy

Echinacea: May diminish the therapeutic effect of Immunosuppressants. Consider therapy modification

Fingolimod: Immunosuppressants may enhance the immunosuppressive effect of Fingolimod. Management: Avoid the concomitant use of fingolimod and other immunosuppressants when possible. If combined, monitor patients closely for additive immunosuppressant effects (eg, infections). Consider therapy modification

InFLIXimab: Golimumab may enhance the immunosuppressive effect of InFLIXimab. Avoid combination

Leflunomide: Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly. Consider therapy modification

Natalizumab: Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Avoid combination

Pimecrolimus: May enhance the adverse/toxic effect of Immunosuppressants. Avoid combination

Rilonacept: Anti-TNF Agents may enhance the adverse/toxic effect of Rilonacept. Avoid combination

Roflumilast: May enhance the immunosuppressive effect of Immunosuppressants. Consider therapy modification

Sipuleucel-T: Immunosuppressants may diminish the therapeutic effect of Sipuleucel-T. Monitor therapy

Tacrolimus (Topical): May enhance the adverse/toxic effect of Immunosuppressants. Avoid combination

Tocilizumab: May enhance the immunosuppressive effect of Anti-TNF Agents. Avoid combination

Tofacitinib: Anti-TNF Agents may enhance the adverse/toxic effect of Tofacitinib. Avoid combination

Tofacitinib: Immunosuppressants may enhance the immunosuppressive effect of Tofacitinib. Management: Concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted, and this warning seems particularly focused on more potent immunosuppressants. Avoid combination

Trastuzumab: May enhance the neutropenic effect of Immunosuppressants. Monitor therapy

Vaccines (Inactivated): Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Management: Vaccine efficacy may be reduced. Complete all age-appropriate vaccinations at least 2 weeks prior to starting an immunosuppressant. If vaccinated during immunosuppressant therapy, revaccinate at least 3 months after immunosuppressant discontinuation. Consider therapy modification

Vaccines (Live): Immunosuppressants may enhance the adverse/toxic effect of Vaccines (Live). Immunosuppressants may diminish the therapeutic effect of Vaccines (Live). Management: Avoid use of live organism vaccines with immunosuppressants; live-attenuated vaccines should not be given for at least 3 months after immunosuppressants. Avoid combination

Vedolizumab: Anti-TNF Agents may enhance the adverse/toxic effect of Vedolizumab. Avoid combination

Adverse Reactions

>10%:

Hematologic & oncologic: Positive ANA titer (≥1:160 titer, newly positive; 17% intravenous, 4% subcutaneous)

Infection: Infection (27% to 28%)

Respiratory: Upper respiratory tract infection (includes laryngitis, nasopharyngitis, pharyngitis, and rhinitis; 13% to 16%)

1% to 10%:

Cardiovascular: Hypertension (3%)

Central nervous system: Dizziness (<1% to 2%), paresthesia (<1% to 2%)

Dermatologic: Skin rash (3%)

Gastrointestinal: Constipation (≤1%)

Hematologic & oncologic: Leukopenia (≤1%)

Hepatic: Increased serum ALT (subcutaneous 4%; ≥3 x ULN: 2%; ≥5 x ULN: <1%), increased serum AST (<1% to 3%)

Immunologic: Antibody development (3% to 7%)

Infection: Viral infection (4% to 5%; includes herpes and influenza), fungal infection (superficial; <1% to 2%), bacterial infection (intravenous 1%), serious infection (≤1%)

Local: Injection site reaction (subcutaneous 3% to 6%)

Respiratory: Bronchitis (2% to 3%)

Miscellaneous: Fever (2%), infusion related reaction (intravenous 1%)

<1% (Limited to important or life-threatening): Anaphylaxis, antibody development (anti-dsDNA), aspergillosis, atypical mycobacterial infection (subcutaneous), blastomycosis, bullous skin disease, candidiasis, cardiac failure (worsening or new onset), cellulitis, coccidioidomycosis, demyelinating disease of the central nervous system, hepatotoxicity (idiosyncratic) (Chalasani 2014), histoplasmosis, Hodgkin lymphoma (initiation of therapy ≤18 years old), hypersensitivity angiitis (subcutaneous), hypersensitivity reaction, infective bursitis (subcutaneous), interstitial pulmonary disease (subcutaneous), leukemia, lupus-like syndrome, malignant lymphoma, malignant melanoma, malignant neoplasm (other than nonmelanoma skin cancer), Merkel cell carcinoma, multiple sclerosis, non-Hodgkin lymphoma (initiation of therapy ≤18 years old), neutropenia, optic neuritis, pancytopenia, peripheral demyelinating polyneuropathy, pneumocystosis, pneumonia, psoriasis (subcutaneous) including new onset, palmoplantar, pustular, or exacerbation), pyelonephritis, reactivation of HBV, sarcoidosis, sepsis, septic arthritis (subcutaneous), septic shock (subcutaneous), serious infection, thrombocytopenia, tuberculosis (including reactivation of latent and new infection), vasculitis (subcutaneous)

ALERT: U.S. Boxed Warning

Serious infection:

Patients treated with golimumab are at an increased risk of developing serious infections that may lead to hospitalization or death. Most patients who developed these infections were taking concomitant immunosuppressants, such as methotrexate or corticosteroids.

Discontinue golimumab if a patient develops a serious infection.

Reported infections with tumor necrosis factor (TNF) blockers include the following:

Active tuberculosis (TB), including reactivation of latent TB. Patients with TB have frequently presented with disseminated or extrapulmonary disease. Test patients for latent TB before golimumab use and during therapy. Initiate treatment for latent infection prior to golimumab use.

Invasive fungal infections, including histoplasmosis, coccidioidomycosis, candidiasis, aspergillosis, blastomycosis, and pneumocystosis. Patients with histoplasmosis or other invasive fungal infections may present with disseminated, rather than localized, disease. Antigen and antibody testing for histoplasmosis may be negative in some patients with active infection. Consider empiric antifungal therapy in patients at risk of invasive fungal infections who develop severe systemic illness.

Bacterial, viral, and other infections due to opportunistic pathogens, including Legionella and Listeria.

Consider the risks and benefits of treatment prior to initiating therapy in patients with chronic or recurrent infection.

Monitor patients closely for the development of signs and symptoms of infection during and after treatment, including the possible development of TB in patients who tested negative for latent TB infection prior to initiating therapy.

Malignancy:

Lymphoma and other malignancies, some fatal, have been reported in children and adolescents treated with TNF blockers.

Warnings/Precautions

Concerns related to adverse effects:

• Autoimmune disorder: Positive antinuclear antibody titers have been detected in patients (with negative baselines). Rare cases of autoimmune disorder, including lupus-like syndrome, have been reported; monitor and discontinue if symptoms develop.

• Demyelinating disease: Rare cases of new-onset or exacerbation of demyelinating disorders (eg, multiple sclerosis, optic neuritis, Guillain-Barré syndrome, polyneuropathy) have been reported. Consider discontinuing in patients who develop peripheral or central nervous system demyelinating disorders during treatment. Use with caution in patients with pre-existing or recent onset central or peripheral nervous system demyelinating disorders.

• Heart failure (HF): Worsening and new-onset HF (some fatal) have been reported with golimumab and other TNF-blockers. Monitor closely and discontinue with onset or worsening of symptoms. Use with caution in patients with heart failure or decreased left ventricular function. The Canadian labeling contraindicates use in moderate or severe heart failure (NYHA class III/IV).

• Hematologic effects: Cases of pancytopenia and other significant cytopenias, including aplastic anemia, have been reported with TNF-blocking agents. Pancytopenia, leukopenia, neutropenia, and thrombocytopenia have occurred with golimumab. Consider discontinuing with significant hematologic abnormalities. Use with caution in patients with underlying hematologic disorders.

• Hepatitis B: Rare reactivation of hepatitis B virus (HBV), sometimes fatal, has occurred in chronic virus carriers, usually in patients receiving concomitant immunosuppressants; evaluate for HBV prior to initiation in all patients. Patients who test positive for HBV surface antigen should be referred for hepatitis B evaluation/treatment prior to golimumab initiation. Monitor for clinical and laboratory signs of active infection during and for several months following discontinuation of golimumab treatment in HBV carriers; interrupt therapy if reactivation occurs and treat appropriately with antiviral therapy; if resumption of therapy is deemed necessary, exercise caution and monitor patient closely.

• Hypersensitivity reactions: Severe systemic hypersensitivity reactions (including anaphylaxis) have been reported (some have occurred with the first dose) following subcutaneous administration; discontinue immediately if signs develop and initiate appropriate treatment.

• Infections: [US Boxed Warning]: Patients receiving golimumab are at increased risk for serious infections which may result in hospitalization and/or fatality; infections usually developed in patients receiving concomitant immunosuppressive agents (eg, methotrexate or corticosteroids). Active tuberculosis (or reactivation of latent tuberculosis), invasive fungal (including aspergillosis, blastomycosis, candidiasis, coccidioidomycosis, histoplasmosis, and pneumocystosis) and bacterial, viral or other opportunistic infections (including legionellosis and listeriosis) have been reported in patients receiving TNF-blocking agents, including golimumab. May present as disseminated (rather than local) disease. Histoplasmosis testing (antigen or antibody) may be negative in some patients with active infection. Monitor closely for signs/symptoms of infection. Discontinue for serious infection or sepsis. Consider risks versus benefits prior to use in patients with a history of chronic or recurrent infection. Consider empiric antifungal therapy in patients who are at risk for invasive fungal infection and develop severe systemic illness. Caution should be exercised (consider risks versus benefits) when considering use in the elderly, patients taking concomitant immunosuppressants, patients with chronic or recurrent infection, patients who have been exposed to tuberculosis, patients with a history of opportunistic infection, patients with comorbid conditions that predispose them to infections (eg, diabetes), or residence/travel from areas of endemic mycoses (blastomycosis, coccidioidomycosis, histoplasmosis). Do not initiate golimumab therapy in patients with active infection, including localized infection which is clinically important. Patients who develop a new infection while undergoing treatment should be monitored closely.

• Malignancy: [US Boxed Warning]: Lymphoma and other malignancies (some fatal) have been reported in children and adolescent patients receiving TNF-blocking agents. Half of the malignancies reported in children were lymphomas (Hodgkin and non-Hodgkin) while other cases varied and included malignancies not typically observed in this population. The onset of malignancy was after a median of 30 months (range: 1 to 84 months) after the initiation of the TNF-blocking agent; most patients were receiving concomitant immunosuppressants. The impact of golimumab on the development and course of malignancy is not fully defined. Compared to the general population, an increased risk of lymphoma has been noted in clinical trials; however, rheumatoid arthritis alone has been previously associated with an increased rate of lymphoma. Lymphomas and other malignancies were also observed (at rates higher than expected for the general population) in adult patients receiving TNF-blocking agents. Hepatosplenic T-cell lymphoma (HSTCL), a rare T-cell lymphoma, has also been associated with TNF-blocking agents, primarily reported in adolescent and young adult males with Crohn disease or ulcerative colitis treated with a TNF-blocking agent and concurrent or prior azathioprine or mercaptopurine. Melanoma and Merkel cell carcinoma have been reported in patients receiving TNF-blocking agents including golimumab. Perform periodic skin examinations in all patients during therapy, particularly those at increased risk for skin cancer. Consider risks versus benefits in patients with a known malignancy (other than a successfully treated nonmelanoma skin cancer) and if considering continuing treatment in a patient who develops a malignancy.

• Tuberculosis: [US Boxed Warning]: Tuberculosis (disseminated or extrapulmonary) has been reported in patients receiving golimumab; both reactivation of latent infection and new infections have been reported. Patients should be evaluated for tuberculosis risk factors and latent tuberculosis infection (with a tuberculin skin test) prior to and during therapy. Treatment of latent tuberculosis should be initiated before use. Monitor for development of tuberculosis throughout treatment in patients with initial negative tuberculin skin tests, patients currently receiving treatment for latent tuberculosis, or patients previously treated for tuberculosis; active tuberculosis has developed in this population during treatment with TNF-blocking agents. Use with caution in patients who have resided in regions where tuberculosis is endemic. Consider antituberculosis therapy if an adequate course of treatment cannot be confirmed in patients with a history of latent or active tuberculosis or for patients with risk factors despite negative skin test. Prior to use, consider risks versus benefits in patients who have been exposed to tuberculosis.

Concurrent drug therapy issues:

• Abatacept: Due to a higher incidence of serious infections, concomitant use with abatacept is not recommended.

• Anakinra: Due to a higher incidence of neutropenia and serious infections, concomitant use with anakinra is not recommended.

• Disease-modifying antirheumatic drugs (DMARDs): Use caution when switching between biological disease modifying antirheumatic drugs (DMARDs); overlapping of biological activity may increase the risk for infection.

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

• Elderly: Use with caution; general incidence of infection is higher in elderly.

Dosage form specific issues:

• Latex: Some dosage forms may contain dry natural rubber (latex).

• Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer's labeling.

Other warnings/precautions:

• Administration formulation/route: The safety and efficacy of switching between the IV and SubQ formulations and routes have not been studied.

• Immunizations: Patients should be brought up to date with all immunizations before initiating therapy. Live vaccines should not be given concurrently; there is no data available concerning secondary transmission of infection by live vaccines in patients receiving therapy. In clinical trials, humoral response to pneumococcal vaccine was not suppressed in psoriatic arthritis patients receiving golimumab.

Monitoring Parameters

CBC with differential; latent TB screening (prior to initiating and periodically during therapy); HBV screening (prior to initiating [all patients]; during and for several months following therapy [HBV carriers]); monitor improvement of symptoms and physical function assessments; signs/symptoms of infection (prior to, during, and following therapy); signs/symptoms/worsening of heart failure signs and symptoms of hypersensitivity reaction; symptoms of lupus-like syndrome; signs/symptoms of malignancy (eg, splenomegaly, hepatomegaly, abdominal pain, persistent fever, night sweats, weight loss) including periodic skin examination

Pregnancy Risk Factor

B

Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies. Golimumab crosses the placenta. Based on data from other TNF-blockers, antibodies may be present in the newborn serum for up to 6 months and infants exposed to golimumab in utero may be at risk of increased infection. Administration of live vaccines to newborns is not recommended until 6 months after the last maternal dose. The Canadian labeling recommends that women of childbearing potential use reliable contraception during and for at least 6 months after discontinuation of golimumab therapy.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience injection site irritation. Have patient report immediately to prescriber signs of infection, signs of liver problems (dark urine, feeling tired, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or yellow skin or eyes), signs of lupus (rash on the cheeks or other body parts, sunburn easy, muscle or joint pain, chest pain or shortness of breath, or swelling in the arms or legs), angina, loss of strength and energy, burning or numbness feeling, vision changes, enlarged lymph nodes, night sweats, excessive weight gain or loss, bruising, bleeding, pale skin, severe headache, shortness of breath, swelling or arms or legs, or eczema (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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