- Injection, solution 50 mg per 0.5 mL
Binds to soluble and transmembrane bioactive forms of human tumor necrosis factor (TNF)–alpha, preventing the binding of TNF-alpha to its receptors, thereby inhibiting the biological activity of TNF-alpha.
Following subcutaneous injection, T max ranges from 2 to 6 days. C max is approximately 2.5 mcg/mL. Absolute bioavailability is approximately 53%.
Distributed primarily in the circulatory system with limited extravascular distribution. Mean Vd is 58 to 126 mL/kg (IV). Serum concentrations reach steady state by 12 weeks. When coadministered with methotrexate, steady-state trough serum concentrations were 0.4 to 0.6 mcg/mL, 0.5 mcg/mL, and 0.8 mcg/mL in rheumatoid arthritis (RA), psoriatic arthritis, and ankylosing spondylitis patients, respectively. Steady-state trough concentrations of golimumab were 52%, 36%, and 21% higher in patients treated with golimumab and methotrexate for RA, psoriatic arthritis and ankylosing spondylitis, respectively, compared with patients treated with golimumab only.
Mean terminal half-life is approximately 2 wk. Mean systemic Cl is 4.9 to 6.7 mL/day/kg.
Special PopulationsRenal Function Impairment
No studies have been conducted.Hepatic Function Impairment
No studies have been conducted.Elderly
No differences were observed based on age.Gender
No dosage adjustment is needed based on gender.Race
No differences in pharmacokinetics have been observed based on race.
Indications and Usage
Treatment of moderate to severe active RA in combination with methotrexate; treatment of active psoriatic arthritis as monotherapy or in combination with methotrexate; treatment of active ankylosing spondylitis.
None well documented.
Dosage and AdministrationAdults
50 mg subcutaneously once per month.
- Evaluate patients for active tuberculosis (TB) and latent infection, prior to initiating and periodically during therapy.
- Prior to initiating therapy, test patients for hepatitis B viral infection.
- Prior to injection, allow the prefilled syringe or autoinjector to sit at room temperature for 30 minutes. Do not warm any other way. Do not shake.
- Discard any leftover product remaining in the prefilled syringe or prefilled autoinjector.
- Do not inject into areas where the skin is tender, bruised, red, or hard.
- Injection sites should be rotated.
- Give with methotrexate for RA. Give with or without methotrexate for ankylosing spondylitis or psoriatic arthritis.
- Corticosteroids, nonbiologic disease-modifying antirheumatic drugs (DMARDs), and/or NSAIDs may be continued during treatment with golimumab.
Store between 36° and 46°F. Do not freeze. Do not shake. Protect from light.
Drug InteractionsAbatacept, anakinra, rituximab, tocilizumab
The risk of serious infection may be increased. Do not coadminister with golimumab.CYP-450 substrates with a narrow therapeutic index (eg, cyclosporine, theophylline, warfarin)
Monitor the response and drug concentrations of CYP-450 substrates with a narrow therapeutic index when starting or stopping golimumab. Dosage adjustments may be needed.Live vaccines
Do not coadminister live vaccines.TNF antagonists (eg, adalimumab, certolizumab, etanercept, infliximab)
Risk of infection may be increased; do not coadminister golimumab and another TNF agonist.
Dizziness, paresthesia (2%).
Aplastic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia (postmarketing).
Increased ALT (4%); increased AST (3%).
Injection-site reactions (injection-site erythema, urticaria, induration, pain, bruising, pruritis, irritation, or paresthesia) (6%).
Laryngitis, nasopharyngitis, pharyngitis, rhinitis, upper respiratory tract infection (16%); bronchitis, sinusitis (2%).
Infections (28%); viral infections (eg, influenza, herpes) (5%); golimumab antibodies (4%); superficial fungal infections (2%); serious systemic hypersensitivity reactions (including anaphylactic reactions) (postmarketing).
Patients treated with golimumab are at an increased risk for developing serious infections that may lead to hospitalization or death. Most patients who developed these infections were taking concomitant immunosuppressants (eg, corticosteroids, methotrexate). Golimumab should be discontinued if the patient develops a serious infection. Reported infections with TNF-blockers, of which golimumab is a member, include active TB, including reactivation of latent TB; invasive fungal infections; and bacterial, viral, or other infections caused by opportunistic pathogens, including Legionella and Listeria .Malignancy
Lymphoma and other malignancies, some fatal, have been reported in children and adolescents treated with TNF blockers.
Closely monitor for development of signs or symptoms of infection during and after treatment, including possible development of TB in patients who tested negative for latent TB infection prior to initiating therapy. Closely monitor patients who are carriers of hepatitis B virus for signs of active hepatitis B virus infection throughout therapy and for several months after completion of therapy. Closely monitor patients with CHF and discontinue treatment if new or worsening symptoms of CHF appear.
Category B . Immunoglobulin G (IgG) antibodies are known to cross the placenta during pregnancy and have been detected in the serum of infants of patients treated with these antibodies. Since golimumab is an IgG antibody, infants born to mothers treated with golimumab during their pregnancy may be at increased risk of infection for up to 6 months. Administration of live vaccines to infants exposed to golimumab in utero is not recommended for 6 months following the mother's last golimumab injection during pregnancy.
Safety and efficacy not established.
Use with caution. May be at greater risk for infections.
Worsening of CHF and new-onset CHF have been reported with TNF-blockers.
Use of TNF-blockers has been associated with new onset or exacerbation of CNS demyelinating disorders (eg, multiple sclerosis) and peripheral demyelinating disorders (eg, Guillain-Barré).
Pancytopenia, leukopenia, neutropenia, aplastic anemia, and thrombocytopenia have been reported with TNF-blockers during postmarketing experience.
Hepatitis B reactivation
Reactivation of hepatitis B virus has been reported in patients who are chronic hepatitis B carriers.
Antibodies to golimumab have been detected.
Needle cover on the prefilled syringe and the prefilled syringe on the autoinjector contain natural rubber, a derivative of latex, which should not be handled by persons sensitive to latex.
Switching between biological DMARDs
Use care when switching patients from one biologic agent to another because overlapping biologic activity may increase the risk of infection.
Patients may receive vaccinations, except for live vaccines.
- Instruct patients to notify their health care provider if they develop any symptoms of infection.
- Counsel patients about the risk of lymphoma and other malignancies while receiving golimumab.
- Advise patients sensitive to latex that the needle cover on the prefilled syringe and the prefilled autoinjector contain natural rubber, a derivative of latex.
- Advise patients to report any signs or worsening medical conditions, such as autoimmune disease, CHF, cytopenias, demyelinating disorders, liver disease, or psoriasis.
- After proper training in subcutaneous injection technique, a patient may self-inject with golimumab if a health care provider determines that it is appropriate. Instruct patients to follow the directions provided in the Medication Guide.
Copyright © 2009 Wolters Kluwer Health.