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Golimumab

Pronunciation: goe-LIM-ue-mab
Class: Immunomodulator

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Trade Names

Simponi
- Injection, solution 50 mg per 0.5 mL

Pharmacology

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.

Pharmacokinetics

Absorption

Following subcutaneous injection, T _max ranges from 2 to 6 days. C _max is approximately 2.5 mcg/mL. Absolute bioavailability is approximately 53%.

Distribution

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.

Elimination

Mean terminal half-life is approximately 2 wk. Mean systemic Cl is 4.9 to 6.7 mL/day/kg.

Special Populations

Renal 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.

Contraindications

None well documented.

Dosage and Administration

Adults

50 mg subcutaneously once per month.

General Advice

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.

Storage/Stability

Store between 36° and 46°F. Do not freeze. Do not shake. Protect from light.

Drug Interactions

Abatacept, 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.

Adverse Reactions

Cardiovascular

Hypertension (3%).

CNS

Dizziness, paresthesia (2%).

GI

Constipation (1%).

Hematologic

Aplastic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia (postmarketing).

Lab Tests

Increased ALT (4%); increased AST (3%).

Local

Injection-site reactions (injection-site erythema, urticaria, induration, pain, bruising, pruritis, irritation, or paresthesia) (6%).

Respiratory

Laryngitis, nasopharyngitis, pharyngitis, rhinitis, upper respiratory tract infection (16%); bronchitis, sinusitis (2%).

Miscellaneous

Infections (28%); viral infections (eg, influenza, herpes) (5%); golimumab antibodies (4%); superficial fungal infections (2%); serious systemic hypersensitivity reactions (including anaphylactic reactions) (postmarketing).

Precautions

Warnings

Serious infections

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.

Monitor

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.

Pregnancy

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.

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Use with caution. May be at greater risk for infections.

CHF

Worsening of CHF and new-onset CHF have been reported with TNF-blockers.

Demyelinating disorders

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).

Hematologic events

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.

Immunogenicity

Antibodies to golimumab have been detected.

Latex

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.

Vaccinations

Patients may receive vaccinations, except for live vaccines.

Patient Information

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.