Golimumab

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

Trade Names

Simponi
- Injection, solution 50 mg per 0.5 mL

Pharmacology

Binds to both 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).

Elimination

Mean terminal half-life is approximately 2 wk. Mean systemic clearance 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 rheumatoid arthritis 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

Subcutaneous 50 mg once per month.

General Advice

• Prior to injection, allow the prefilled syringe or auto injector to sit at room temperature for 30 minutes. Do not warm any other way. Do not shake.
• For subcutaneous use.
• Discard any leftover product remaining in the prefilled syringe or prefilled auto injector.
• Do not inject into areas where the skin is tender, bruised, red, or hard.
• Injection sites should be rotated.
• Corticosteroids, nonbiologic disease-modifying antirheumatic drugs, and/or NSAIDs may be continued during treatment with golimumab.

Storage/Stability

Store at 36° to 46°F. Do not freeze. Protect from light.

Drug Interactions

Abatacept, anakinra, rituximab

Do not coadminister with golimumab.

CYP substrates with a narrow therapeutic index (eg, cyclosporine, theophylline, warfarin)

Monitor the response and drug concentrations of CYP 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.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Dizziness (2%); paresthesia, pyrexia (1%).

Dermatologic

New-onset psoriasis, including pustular psoriasis and palmoplantar psoriasis.

EENT

Nasopharyngitis (6%); pharyngitis, rhinitis (1%).

Lab Tests

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

Local

Injection-site reactions (6%); injection-site erythema (3%).

Respiratory

Upper respiratory tract infection (7%); bronchitis, sinusitis (2%).

Miscellaneous

Infections (28%); golimumab antibodies (4%); hypertension (3%); influenza (2%); oral herpes (1%).

Precautions

Warnings Patients treated with golimumab are at increased risk for developing serious infections that may lead to hospitalization or death. These patients are frequently taking concomitant immunosuppressants (eg, corticosteroids, methotrexate). Infections include active tuberculosis (TB), invasive fungal infections, or bacterial, viral, or other infections caused by opportunistic pathogens. Discontinue treatment in patients who develop serious infection or sepsis. 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 .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Use with caution.

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).

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 auto injector contain natural rubber, a derivative of latex, which should not be handled by persons sensitive to latex.

Vaccinations

Patients may receive vaccinations, except for live vaccines.

Overdosage

Symptoms

There were no overdoses in clinical studies.

Patient Information

• Instruct patients to read the Medication Guide before starting therapy and to read it each time the prescription is refilled.
• 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 auto injector 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.