Golimumab is a human monoclonal antibody which is used as an immunosuppressive drug. Golimumab targets tumor necrosis factor alpha (TNF-alpha), a pro-inflammatory molecule and hence is a TNF inhibitor. Profound reduction in C-reactive protein (CRP) levels, interleukin (IL)-6, intercellular adhesion molecules (ICAM)-1, matrix metalloproteinase (MMP)-3, and vascular endothelial growth factor(VEGF) demonstrates golimumab as an effective modulator of inflammatory markers and bone metabolism.
Golimumab is a human IgG1қ monoclonal antibody derived from immunizing genetically engineered mice with human TNFα. Golimumab binds and inhibits soluble and transmembrane human TNFα. Increased TNFα is associated with chronic inflammation. Thus golimumab is indicated for use in adults (i) as an adjunct to methotrexate treatment in patients with moderate to severe active rheumatoid arthritis (RA), (ii) alone or as an adjunct to methotrexate treatment in patients with active psoriatic arthritis (PsA), (iii) as a single agent in patients with active ankylosing spondylitis (AS), and (iv) as a single agent in patients with moderate to severe ulcerative colitis (UC) who require chronic steroids or have experienced intolerance or only a partial response to previous medications.
Mechanism of Action of Golimumab
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.
Indications of Golimumab
- Rheumatoid arthritis
- Severe, active rheumatoid arthritis
- Ankylosing spondylitis
- Psoriatic arthritis
- Ulcerative Colitis
- Juvenile idiopathic arthritis
- Juvenile rheumatoid arthritis
- Plaque Psoriasis
- Psoriasis
- Moderate to severe ulcerative colitis
Contra-Indications of Golimumab
- Tuberculosis
- Infection caused by Blastomyces dermatitidis Fungus
- Opportunistic fungal infection
- Pneumonia
- Severe infection
- Infection that lasts a long time
- Malignant melanoma
- Leukemia
- Diabetes that is not under control
- Reduction in the body’s resistance to infection
- The acquired decrease of all cells in the blood
- Low blood counts due to bone marrow failure
- Decreased neutrophils a type of white blood cell
- Multiple sclerosis
- Demyelinating Disease
- Sudden blindness and pain Upon moving the eye
- Heart failure
- Decreased Blood Platelets
- Decreased white blood cells
- Low Level of Granulocytes in the Blood
- Chronic heart failure
- Pneumonia caused by Legionella pneumophila bacteria
- Hardening of the liver caused by alcohol
- Liver inflammation caused by the body’s own immune response
- Seizures
- Reactivated tuberculosis
- Sepsis syndrome
- Malignant lymphoma
- Relapse of hepatitis B infection symptoms
- Hepatitis B
- Hepatosplenic T-cell lymphoma
Dosage of Golimumab
Strengths: 50 mg/0.5 mL; 100 mg/mL; 50 mg/4 mL
Rheumatoid Arthritis
Subcutaneous
- 50 mg once a month
- IV: 2 mg/kg over 30 minutes at Weeks 0 and 4, then every 8 weeks thereafter
Ankylosing Spondylitis
Subcutaneous
- 50 mg once a month
- IV: 2 mg/kg over 30 minutes at weeks 0 and 4, then every 8 weeks thereafter
Psoriatic Arthritis
Subcutaneous
- 50 mg once a month
- IV: 2 mg/kg over 30 minutes at weeks 0 and 4, then every 8 weeks thereafter
Ulcerative Colitis
Subcutaneous
- Initial dose: 200 mg subcutaneously at week 0, followed by 100 mg at week 2
- Maintenance dose: 100 mg subcutaneously every 4 weeks.
Side Effects of Golimumab
The most common
- Nausea and vomiting
- Severe stomach ache
- multiple sclerosis,
- Severe diarrhea
- Vaginal thrush
- Skin rash redness or itching, pain, or swelling at the injection site
- A headache
- chest pain
- constipation
- a cough
- diarrhea or loose stools
- difficulty with breathing
- dizziness
- heartburn
- muscle pain
More common
- Abdominal or stomach pain, discomfort, or tenderness
- chills or fever
- difficulty with moving
- a headache, severe and throbbing
- joint or back pain
- Loss of energy or weakness
- pain or burning in the throat
- runny or stuffy nose
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in the chest
- discomfort in arms, shoulders, neck or upper back
- excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- rust colored urine
- decreased amount of urine
Rare
- Anxiety
- change in vision
- seizures
- abnormal or fast heart rate
- tremors
- weight loss
- chest pain or tightness
- confusion
- a cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- fainting
- hallucinations
- a headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
- muscle spasm or jerking of all extremities
Drug Interactions of Golimumab
Golimumab may interact with the following drugs, supplements, & may change the efficacy of the drug
- abatacept
- anakinra
- bacillus Calmette-Guérin (BCG)
- belimumab
- canakinumab
- certolizumab pegol
- cyclophosphamide
- denosumab
- fingolimod
- immunosuppressants (e.g., cyclosporine, mycophenolate, tacrolimus)
- medications that weaken the immune system (e.g., medications for cancer or organ transplants)
- other biologics (e.g., abatacept, adalimumab, infliximab, anakinra)
- leflunomide
- nivolumab
- natalizumab
- pimecrolimus
- roflumilast
- sulfasalazine
- tacrolimus
- tocilizumab
- tofacitinib
- trastuzumab
- vaccines (e.g., yellow fever, BCG, cholera, typhoid, varicella, meningococcal, diphtheria)
- vedolizumab
Pregnancy Catagory of Golimumab
FDA Pregnancy Category B
Pregnancy
Golimumab crosses the placenta and may affect the development of the unborn child if it is used by a woman during pregnancy. Effective birth control must be used to prevent pregnancy and for 6 months after the last dose of golimumab is taken to avoid causing harm to an unborn baby. If you become pregnant while taking this medication, contact your doctor immediately.
Lactation
It is not known if this medication passes into breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. The safety and effectiveness of using this medication have not been established for children. Children, less than 18 years of age may be at an increased risk of developing certain blood cancers.
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