Mechanism of effect
As a human monoclonal antibody, golimumab binds and inhibits soluble and transmembrane human TNFα. Inhibition of TNFα prevents it binding to its receptors, which prevents both leukocyte infiltration through prevention of cell adhesion proteins such as E-selectin, ICAM-1 and VCAM-1, and pro-inflammatory cytokine secretion such as IL-6, IL-8, G-CSF and GM-CSF in vitro.
Consequently, in patients with chronic inflammatory conditions, decreases in ICAM-1 and IL-6 as well as C-reactive protein (CRP), matrix metalloproteinase 3 (MMP-3), and vascular endothelial growth factor (VEGF) were observed.
Pharmacodynamic
Golimumab inhibits the activity of the cytokine, tumor necrosis factor alpha (TNFα). In areas such as the joints and blood, increased TNFα is associated with chronic inflammation seen in patients with rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis. Thus golimumab decreases the inflammation in these conditions.
Pharmacokinetics
Absorption
Bioavailability: 53% (SC)
Peak plasma time (50 mg dose): 2-6 days
Peak plasma concentration: 44.4 mcg/mL (Golimumab Aria)
Distribution
Vd: 115 mL/kg (healthy subjects); 151 mL/kg (RA)
Elimination
Half-life: 14 days
Clearance: 6.9 mL/day/kg (healthy subjects); 7.6 mL/day/kg (RA)
Dosage
Adult
Rheumatoid Arthritis
Golimumab: 50 mg SC qMonth
Golimumab Aria: 2 mg/kg IV infused over 30 minutes at weeks 0 and 4, then q8weeks
Psoriatic Arthritis
Golimumab:50 mg SC qMonth
Golimumab Aria:2 mg/kg IV infused over 30 minutes at weeks 0 and 4, then q8Weeks
Ankylosing Spondylitis
Golimumab: 50 mg SC qMonth
Golimumab Aria: 2 mg/kg IV infused over 30 minutes at weeks 0 and 4, then q8Weeks
Ulcerative Colitis
Golimumab only
Initial: 200 mg SC at Week 0, followed by 100 mg SC at Week 2, THEN
Maintenance: 100 mg SC q4Weeks
Pediatric
<18 years: Safety and efficacy not established
Side effects
Sinusitis , flu , Pain , vertigo , urticaria , Hypertension , Increased ALT , itching , Rash , rhinitis , Herpes SimplexInteractions
Thymoglubin , Melphalan , Chlorambucil , prednisone , Azathioprine , Everolimus , Infliximab , Pneumovax , Tacrolimus , Sirolimus , Anakinra , Measles vaccine , Rubella Vaccines , Tocilizumab , Canakinumab , Basiliximab , Alefacept , Cyclosporine , Glatiramer acetate , Hydroxychloroquine , Human papillomma virus vaccine , Adalimumab , Certolizumab , Hib vaccine , Clofarabine , Tositumomab , Ibritumomab tiuxetan , Bendamustine , Aflibercept , Axicabtagene ciloleucel , Pralatrexate , trabectedine , Duvelisib , Nelarabine , Dupilumab , Ocrelizumab , Ofatumumab , vedolizumab , Brodalumab , Rilonacept , Hepatitis B Vaccine , Dasatinib , Typhoid vaccine (live), oral , Meningococcal conjugate vaccine , Rabies Vaccine , Daclizumab , alirocumab , Famtrastuzumab , NiraparibAlerts
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:
1) 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
2) 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
3) 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
Points of recommendation
Follow all directions on your prescription label. Do not use this medicine in larger or smaller amounts or for longer than recommended.
Golimumab may also be injected under the skin once every 2 to 4 weeks. You may be shown how to use injections at home. Do not self-inject this medicine if you do not understand how to give the injection and properly dispose of used needles and syringes.
Your care provider will show you the best places on your body to inject golimumab. Use a different place each time you give an injection. Do not inject into the same place two times in a row.
Each single-use prefilled syringe or auto-injector device is for one use only. Throw away after one use, even if there is still some medicine left in it after injecting your dose.
Store in the refrigerator, do not freeze. Protect from light. Keep the medication in its original carton until you are ready to give an injection.
Take the prefilled syringe or auto-injector out of the refrigerator and place it at room temperature for 30 minutes before giving your injection. Do not warm the medication with water or heat.
Golimumab can weaken your immune system. Your blood will need to be tested often.
Ask a Pharmacist