Simponi vs Enbrel is a comparison of the two TNF-inhibitors, Golimumab and Etanercept. Both Simponi (Golimumab) and Enbrel (Etanercept) aim to reduce the process of inflammation by decreasing the production of Interleukin-6 and Interleukin-8.
Owing to their strong immune-modulatory effects, these drugs are commonly used to treat autoimmune rheumatic conditions like ankylosing spondylitis, psoriatic arthritis, rheumatoid arthritis, and ulcerative colitis.
Mechanism of action of Simponi (Golimumab) and Enbrel (Etanercept):
Golimumab (Simponi) is a human monoclonal antibody, it binds to soluble and transmembrane TNFα and inhibits its secretion. By doing so, it prevents the binding of TNFα to its receptors which stops leukocyte infiltration by inhibiting E-selectins, ICAM-1 and VCAM-1. It also inhibits IL-6 and IL-8 which are pro-inflammatory cytokines. This in turn reduces or prevents inflammation in chronic inflammatory conditions.
Etanercept (Enbrel) is a dimeric soluble form p75 TNF receptor which can bind two TNF molecules thereby removing TNF from the circulation. Etanercept is only capable of binding to the active trimeric form of tumor necrotic factor. Etanercept binds to TNF and inhibits its binding with cell surface receptors
Generic Names and dosage forms:
|Dosage form||Simponi: Injection, solution||Enbrel: Subcutaneous injection|
|Generic name||Simponi: Golimumab 50mg in 0.5mL||Enbrel: ETANERCEPT 50mg in 1mL|
Simponi Vs Enbrel – Approved Indications of Using these two TNF inhibitors:
|Ankylosing Spondylitis||Approved for the treatment of active ankylosing spondylitis in adults, as a single agent or in combination with methotrexate||Approved in patients with Ankylosing Spondylitis|
|Psoriatic arthritis||FDA-Approved for the treatment of psoriatic arthritis in adults||FDA approved for the treatment of psoriatic arthritis to prevent structural joint damage and inducing major clinical response|
|Rheumatoid arthritis||Approved for the treatment of patients with Rheumatoid Arthritis in combination with methotrexate||Approved for the treatment of RA as monotherapy or in combination with methotrexate to prevent joint damage and improve physical function in moderately to severely active RA|
|Ulcerative colitis||Simponi is indicated to treat moderate to severely active ulcerative colitis in patients with corticosteroid dependence, patients who are unable to tolerate oral corticosteroids, oral aminosalicylates, azathioprine, or 6-mercaptopurine||Etanercept is not indicated for the treatment of Inflammatory Bowel disease.
Rather, studies have shown that IBDs may be provoked by using Enbrel (Etanercept) [Ref].
|Plaque psoriasis:||Golimumab is used in the treatment of psoriatic arthritis.
However various case reports of paradoxical reactions resulting in the development of psoriasis pustulosa have been published [Ref].
|Enbrel is indicated for the treatment of patients of 4 years or above age with chronic plaque psoriasis who are receiving phototherapy or systemic therapy.|
|Polyarticular juvenile idiopathic arthritis:||Golimumab has been recently approved by the FDA for the treatment of polyarticular Juvenile idiopathic arthritis.||Enbrel is indicated in the treatment of polyarticular juvenile idiopathic arthritis for reducing signs and symptoms in patients with 2 years of age or above.|
Pharmacokinetics of Simponi Vs Enbrel (Golimumab Vs Etanercept):
|Absorption||Golimumab (Simponi) achieves maximum concentrations in 2-6 days after subcutaneous administration.||It is absorbed slowly and reaches the maximum concentration in 69 hours|
|Bioavailability||It has an approximate bioavailability of 53%||It has a bioavailability of 56.9%|
|Half-life||About 2 weeks||Mean half-life in adults: 68 hours
In children: 70-90 hours
|Clearance||After one dose the clearance was 4.9-6.7Ml/day/kg||The clearance rate is 160mL/h in Rheumatoid arthritis and 0.057 L/h in pediatric JIA patients|
Simponi Vs Enbrel in Pregnancy and breastfeeding:
|In pregnancy||Simponi is under pregnancy category B of drugs.
No adverse events have been reported and limited data is available on the use of golimumab during pregnancy.
Monoclonal antibodies cross the placenta during the third trimester, these can be present in the newborn’s serum for 6 months
Exposure to golimumab in utero possess a greater risk.
|No category has been assigned to Enbrel
No adverse events have been reported
|During lactation||The Secretion of golimumab in breast milk is unknown.
The decision to breastfeed during golimumab therapy depends upon the risk of infant exposure, benefits of treatment on the mother, and benefits of breastfeeding.
|It is present in breast milk in low concentrations and is minimally absorbed by the infant.|
Simponi Vs Enbrel in the Various Disease States:
Simponi Vs Enbrel use in Rheumatoid arthritis:
- Various clinical trials done on the efficacy of Simponi in the treatment of rheumatoid arthritis suggest that golimumab therapy showed a significant reduction in symptoms and improved physical function. Golimumab+ methotrexate has more beneficial effects than golimumab therapy alone in rheumatoid arthritis patients. It seems to be a good choice also due to low levels of immunogenicity and low rate of drug discontinuation as compared to Enbrel or other TNF inhibitors. (ref)
- Clinical trials are done to know the efficacy of Enbrel in the treatment of RA showed that Enbrel is also safe and effective in the treatment of rheumatoid arthritis. It has been shown to reduce disease activity and slow its progression. Etanercept along with methotrexate is more effective in reducing joint damage. (Ref)
Simponi Vs Enbrel use in Psoriatic Arthritis:
- Enbrel has been shown to reduce symptoms of psoriatic arthritis in various clinical trials and meta-analyses. The drug is effective in axial disease and also reduces psoriatic disease in the skin and nails. Enbrel is as effective as other TNF inhibitors, except in cost-effectiveness where Enbrel is more effective. (Ref)
- Simponi is approved by FDA for the treatment of psoriatic arthritis. According to studies the drug is well tolerated and is associated with improved disease activity. (Ref)
Simponi Vs Enbrel use in Ankylosing spondylitis
- Studies suggest that subcutaneous injections of golimumab once every 4 weeks are effective in treating and reducing signs and symptoms of AS along with improvement in physical function. (Ref)
- In random clinical trials and open-label extension studies, the efficacy of etanercept has been confirmed in Ankylosing spondylitis. It is effective in different manifestations of the disease like back pain, psoriasis, enthesitis, and peripheral arthritis. However, the efficacy of etanercept is low in uveitis as compared to other TNF inhibitors. Etanercept is effective even after discontinuation, meta-analysis shows that the risk/benefit ratio is favorable with low toxicity. (Ref)
Simponi Vs Enbrel Use in patients with COVID-19 infection:
Simponi vs Enbrel and COVID-19 Simponi and Enbrel both are TNF inhibitors. Some studies suggest that TNF inhibitors might have a protective role against the complications of COVID-19. Although COVID-19 initially starts from the upper respiratory tract, TNF inhibitors might have a protective role because TNF is one of the cytokines that can initiate a cytokine storm which is a dangerous overactive immune response in patients with COVID-19 a TNF inhibitor might aid to prevent that. But still, further studies are being conducted in this regard.
Serious Conditions associated with Simponi and Enbrel Use that need monitoring:
- In patients using TNF inhibitors, autoimmune disorders such as lupus-like syndrome are seen rarely. Symptoms must be regularly monitored and in presence of any such symptoms, the therapy must be stopped.
- These medications can lead to demyelination disorders like multiple sclerosis, polyneuropathy, optic neuritis, and Guillain-Barré syndrome. Therapy must be withdrawn in patients with any such disorders. If these conditions are pre-existing, therapy must be used with caution.
- TNF blockers are known to cause worsening and new-onset heart failure. Strict monitoring and withdrawal of therapy may be necessary with the onset or worsening of symptoms. TNF blockers are known to cause myocardial toxicity
- TNF blockers can lead to aplastic anemia. They can also cause leukopenia, neutropenia, pancytopenia, and thrombocytopenia. Therapy should be withdrawn if these conditions exist.
- For patients receiving immunosuppressants, reactivation of the hepatitis B virus can occur. Before starting the therapy, HBV status must be checked.
- IV or Sub-cutaneous administration can lead to severe systemic hypersensitivity reactions such as anaphylaxis presenting with dyspnea, hives, nausea, and pruritus. Reactions occur during and within 1 hour of the start of IV infusion.
Malignancy [US Boxed Warning]:
- TNF blockers are known to cause lymphoma and other malignancies which might be life-threatening. A high risk of lymphoma is found in patients with rheumatoid arthritis.
- TNF blockers may lead to melanoma and Merkel cell carcinoma.
Tuberculosis: [US Boxed Warning]:
- Before therapy, patients should be monitored for tuberculosis risk factors and latent tuberculosis infection.
- Patients having therapy can have tuberculosis (disseminated or extrapulmonary) both reactivation of latent infection and new infections. Before therapy, treatment of latent tuberculosis must be provided. Monitoring should be done throughout the treatment. Proper evaluation should be done in patients who have been exposed to tuberculosis