Certolizumab pegol

Certolizumab pegol is a pegylated monoclonal antibody from the drug class of TNF-alpha blockers. Certolizumab pegol binds specifically to the cytokine TNF-alpha, thus preventing the triggering of an inflammatory cascade reaction. Pegylation means that polyethylene glycol (PEG) moieties are incorporated into the antibody. This can prolong the half-life of the drug.

The absence of the Fc IgG moiety in this monoclonal antibody is considered an advantage in that some potential side effects of monoclonal antibodies are thought to be related to the Fc moiety. At the same time, the pegylation changes the so-called pharmacokinetics of the antibody, i.e. the behavior of the drug in the organism.

Certolizumab pegol was officially approved as ^Cimzia® for the treatment of rheumatoid arthritis (chronic polyarthritis) in countries throughout the European Union on October 1, 2009. In the United States, approval was granted by the U.S. Food and Drug Administration (FDA) in April 2008 initially for Crohn's disease, followed by approval for rheumatoid arthritis (M06.9) in May 2009.

Certolizumab has been approved since June 2018 based on 3 phase III studies (CIMPASI-1/-2 as well as CIMPACT), for the treatment of moderate-to-severe plaque psoriasis (Gottlieb AB et al. 2018). In the CIMPACT trial, the PASI 75 at week 12 of therapy under 200mg was 61.3% under 400mg was 66.7% (Lebwohl M et al. 2018). Also for the DLQI after 16 weeks every 2nd patient reached the best score: impairment of quality of life. There is minimal to no transfer of certolizumab into breast milk (CRIB/CRADDLE). It therefore offers a potential treatment option for breastfeeding psoriatic mothers.

Certolizumab pegol is used to treat adults with moderate to severe active rheumatoid arthritis for which conventional disease-modifying antirheumatic drugs(DMARDs), including methotrexate (MTX), have not responded or have not responded adequately. To ensure maximum efficacy, certolizumab is usually used in combination with methotrexate. Patients who are intolerant to methotrexate or for whom further treatment with methotrexate is not reasonable for other reasons may also be treated monotherapeutically with Cimzia without MTX.

Certolizumab is approved for the treatment of moderate to severe plaque psoriasis. Dosages and type of application are based on the many years of experience in the treatment of rheumatoid arthritis.

The therapy with Certolizumab Pegol is performed as a subcutaneous injection (see c).

In the therapy of rheumatoid arthritis the usual dose is 200 mg Certolizumab/14 days. In the initial phase of therapy, the dose is doubled, i.e. 400 mg are administered on the first day, as well as after 14 and after 28 days.

The significantly improved efficacy of certolizumab compared to conventional DMARDs has been convincingly demonstrated in extensive clinical studies for the therapy of rheumatoid arthritis.

Rapid-1 and Rapid-2 studies have shown that Certolizumab Pegol in combination with methotrexate has been shown to stop radiologically detectable progression in more than 2/3 of patients. The maximum clinical efficacy is usually achieved after 8-12 weeks.

The most frequent ADRs include infections, whereby the increased risk of infection is mostly banal infections of the upper respiratory tract such as normal colds, furthermore also bronchitis, sore throat or sinusitis. Local intolerances are low. 0

Severe side effects during therapy with Certolizumab are rare. They mainly concern infectious complications. A special warning concerns the possible occurrence of tuberculosis. This is usually a reactivation of already existing latent infections.

Cimzia®

Tuberculosis must be ruled out before starting therapy with certolizumab (Amerio P et al. 2013). This also applies to hepatitis B virus infections. A particularly strict indication applies to HBV carriers, i.e. persons who do not show symptoms of an active hepatitis B infection but are carriers of the hepatitis B virus. For them, very close monitoring during the course of therapy is also necessary.

Certolizumab must not be used in patients with moderate or severe heart failure (NYHA Grade III/IV) or in patients with untreated, active acute or chronic infections.

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