Simponi vs Cimzia is a comparison of the two novel TNF-inhibitors. Both the drugs can be administered as slow intravenous infusions or subcutaneous injections.
This article explains the comparative pharmacokinetics, mechanism of action, and efficacies of two TNF inhibitors Simponi (golimumab) and Cimzia (certolizumab) in various conditions. Both of these drugs are indicated in chronic inflammatory and immune-related conditions.
Simponi vs Cimzia Uses
Golimumab (Simponi) and Certolizumab (Cimzia) are used to treat the following conditions:
Simponi VS Cimzia Pharmacokinetics:
|Half-life||14 days||14 days|
|Absorption||Achieves a maximum concentration after 2-6 days of subcutaneous administration||Achieves maximum concentration within 54-171 hours.|
|Clearance||4.9-6.7Ml/day/kg after 1 dose||
Mechanism of action (MOA): Simponi Vs Cimzia:
- Golimumab (Simponi) is a human monoclonal antibody, it binds to transmembrane TNF-α and inhibits its secretion. In this way, it prevents the binding of TNF-α to its receptors. This ultimately stops leukocyte infiltration by inhibiting E-selectins, ICAM-1, and VCAM-1. It also inhibits IL-6 and IL-8 (pro-inflammatory cytokines). This aids in preventing inflammation in chronic inflammatory conditions.
- Certolizumab activates TNF-α with high affinity, which inhibits the inflammation process. It acts by binding to soluble membrane portions of TNF-α without inducing antibody-dependent cytotoxicity. Certolizumab does not present any activity against TNF-β. It is more significantly distributed in inflamed tissues as compared to Simponi and other TNF inhibitors.
Simponi vs Cimzia Use in pregnancy and lactation:
All the TNF inhibitors including Simponi and Cimzia are marked as B category drugs during pregnancy and breastfeeding. No adverse reactions have been reported but the clinical trials on the use of TNF inhibitors in such conditions are very low. During such conditions, these drugs should be administered only if needed. In some conditions such as Psoriasis, certolizumab is administered in pregnant females but limited data is available regarding its use.
Simponi vs Cimzia efficacy in different conditions:
Simponi (Golimumab) vs Cimzia (Certolizumab) in patients with Rheumatoid arthritis:
- Certolizumab (Cimzia) is clinically beneficial in improving overall disease condition, quality of life and is associated with an increased chance of remission. Reduced radiographic damage is also associated with the use of certolizumab in RA patients. But the minimum dosage of certolizumab for rheumatoid arthritis is 200mg administered subcutaneously. Discontinuation of drug use is observed in various trials due to adverse side effects like tuberculosis and hypertension. This suggests that although it is effective in treating RA, certolizumab must be used with caution.[Ref]
- Golimumab a new TNF-α inhibitor is safe and effective in treating rheumatoid arthritis. In various clinical trials in which golimumab was studied in the treatment of RA, results showed that there is a low rate of discontinuation, low immunogenicity along with low production of antibodies. It is a preferred drug due to the convenient dosage scheme and low injection site reactions. A high dose is associated with possible adverse side effects. [Ref]
- In comparison with Golimumab and etanercept in Rheumatoid arthritis, golimumab showed a superior two-year drug survival and had a better retention time owing to the fewer drug-related side effects [Ref].
Simponi (Golimumab) vs Cimzia (Certolizumab) in patients with Ankylosing Spondylitis:
- Certolizumab is effective in treating ankylosing spondylitis as well as axial spondyloarthritis. A dose of 400 mg is administered subcutaneously as two injections of 200 mg. It is generally well-tolerated and most of the adverse events that occur are non-serious infections. In one study, non-serious adverse events were 86% while serious side effects were 12% in patients taking Certolizumab.[Ref]
- Although it is effective, however, most recently a case has been reported. The case includes a young woman with a paradoxical skin reaction with clinical manifestations of both pyoderma, gangrenosum, and psoriasis due to long-term treatment with certolizumab. That’s why this must be used with great caution and clinicians must properly access people prone to such infections.[Ref]
- Another Cochrane review evaluated the safety of various biological agents in patients treated for an immune-related condition. The authors found that Certolizumab Pegol use was associated with an increased risk of serious adverse events compared to abatacept, adalimumab (Humira), etanercept (Enbrel), golimumab (Simponi), and rituximab (Rituxan) [Ref].
- Golimumab therapy is effective in the treatment of Ankylosing spondylitis. It is associated with reduced back pain and a decrease in inflammation with an overall improvement in quality of life. Less adverse events have been associated with the use of golimumab as compare to certolizumab. [Ref]
- An indirect comparison of the five commonly used TNF inhibitors was done in patients treated for Ankylosing spondylitis. Golimumab compared to placebo proved to be superior in patients with ankylosing spondylitis as assessed by the ASAS20 score at week 12. The author suggested golimumab, rather than the etanercept, infliximab, certolizumab pegol, and adalimumab, for the treatment of patients with Ankylosing spondylitis who were naive to biological agents [Ref].
Simponi (Golimumab) vs Cimzia (Certolizumab) in patients with Psoriatic arthritis:
Certolizumab Pegol (Cimzia):
- Certolizumab is approved by FDA for the treatment of mild to severe forms of psoriasis. In various trials, it has been effective for the treatment of psoriasis and psoriatic arthritis. It is associated with rapid onset of action and improvement of PsA symptoms. Discontinuation of the drug in various trials was mainly due to the loss of effectiveness of the drug.[Ref]
- Golimumab is effective in both axial and peripheral psoriatic arthritis. It is approved for IV administration in PsA patients. Therapy with golimumab in PsA patients is associated with slow progression of the disease and effective treatment of Enthesitis and nail disease however, dactylitis is improved with a 100mg dose of golimumab.[Ref]
Golimumab Vs Certolizumab in other immune-mediated conditions:
Golimumab and Certolizumab have also been studied in other conditions. These two TNF-inhibitors have a better safety profile compared to most other TNF inhibitors and can be easily tolerated.
- Golimumab and Certolizumab were investigated in the treatment of patients with non-infectious Uveitis. The majority of the patients were already treated previously with other TNF inhibitors. The 34-months drug survival was 54.5% with Certolizumab and 50% with Golimumab. Both the drugs significantly reduced the disease flares and were better tolerated [Ref].
- In a case series of patients with Crohn’s disease who had a refractory clinical course with other TNF-inhibitor drugs (including adalimumab, Certolizumab, and Infliximab), Golimumab (Simponi) resulted in a significant clinical response [Ref].
- It is important to note that some TNF-inhibitors have been associated with an increased incidence of Ulcerative Colitis and Crohn’s disease. This is particularly true for Enbrel (Etanercept) with an adjusted hazard ratio of 2.0 [95% CI: 1.4-2.8] and 2.0 [95% CI: 1.5-2.8], respectively for Crohn’s disease and Ulcerative Colitis [Ref].
It is concluded that golimumab is a better treatment option in the above-mentioned disease conditions due to the low incidence of serious side effects and a convenient dosage scheme as compared to certolizumab.
Certolizumab pegol is associated with a significantly higher risk of serious infections compared to other TNF inhibitors. And due to this reason, it has a high discontinuation rate among other TNF inhibitors. Apart from side effects, a very high dose (400mg) of certolizumab is administered at the start of therapy.