Golimumab; Uses, Dosage, Side Effects, Interactions

Golimumab

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

Contra-Indications of Golimumab

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

More common

Rare

Drug Interactions of Golimumab

Golimumab may interact with the following drugs, supplements, & may change the efficacy of the drug

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.

References

Golimumab