Last updated: November 24, 2014
Trade Name: Cimzia
Drug Class: Biologic DMARD, TNF antagonist
Preparations: For subcutaneous injection 200 mg vial lyophilized powder for reconstitution or 200 mg pre-filled syringe
Dose: 400 mg by subcutaneous injection at weeks 0, 2 , 4 and then either 200 mg every 2 weeks or 400 mg every 4 weeks. For Crohn’s, the maintenance dose of 400 mg every 4 weeks is recommended in the FDA label.
Mechanism of Action: A recombinant humanized Fab fragment (lacks Fc region) of a monoclonal antibody to human TNF alpha conjugated to polyethylene glycol. It binds to TNF alpha neutralizing it.
Contraindications: Hypersensitivity, untreated tuberculosis and other opportunistic infections, sepsis, active infection, chronic localized or recurrent infections, demyelinating disease, optic neuritis, moderate-to-severe heart failure.
Precautions: Increased risk of serious infections including TB and fungal. Exclude latent or active TB with a skin test or TB blood test (interferon-gamma release assays or IGRA). Caution in debilitated or high risk of infection. Exclude active hepatitis B infection or carriage. Avoid live virus vaccines and BCG. Do not use with other biologics. May exacerbate pre-exisiting demyelinating disease and heart failure.
Monitoring: Monitor clinically for infection. Periodic CBC. After therapy started, additional TB testing may be indicated for individuals likely to have exposure to TB.
Pregnancy Risk: B
Common: Injection site reactions, positive antinuclear antibody, positive antinuclear and double stranded DNA antibody.
Less common: Allergy, infection (bacterial, but particularly opportunistic infections such as tuberculosis, listeriosis, and histoplasmosis).
Rare: Lymphoma (including fatal hepatosplenic T-cell lymphoma), hepatitis, demyelinating CNS disorders, optic neuritis, seizures, pancytopenia, drug-induced lupus, reactivation of hepatitis B, new onset psoriasis. Certolizumab pegol may cause falsely elevated activated partial thromboplastin time (aPTT) results in some assays.
Drug Interactions: Concurrent use of high-dose steroids and other immunosuppressants may increase risk of infection.
Patient Instructions: Avoid live virus vaccines; avoid pregnancy; stop injections and call your doctor if an infection or fever develops that lasts more than a few days.
Comments: TNF antagonists are among the most effective treatments for RA. Patients start to respond quickly, usually within 4–6 weeks, but maximum response may take 4-6 months. In RA, increasing the dose of certolizumab from 200 mg every 2 weeks to 400 mg every 2 weeks did not result in additional benefit. Combined therapy of an anti-TNF with MTX is more effective than either drug alone. TNF antagonists are being explored in a range of diseases such as sarcoidosis and inflammatory eye disease. Risk of tuberculosis may be lower with etanercept than other TNF antagonists; comparative risk of adverse effects among individual TNF antagonists is not clear and side effects likely a class effect. Patients may form antibodies to anti-TNF drugs that decrease their effect. Concurrent treatment with MTX may reduce the frequency of this.
Clinical Pharmacology: Half-life is 14 days. Biologic agents are not metabolized and thus have few drug interactions.
Singh JA, Furst DE, Bharat A. et al.2012 Update of the 2008 American College of Rheumatology recommendations for the use of disease-modifying antirheumatic drugs and biologic agents in the treatment of rheumatoid arthritis.Arthritis Care Res 2012;64(5):625-39. PMID:22473917
Curtis JR, Chen L, Luijtens K, et al. Dose escalation of certolizumab pegol from 200 mg to 400 mg every other week provides no additional efficacy in rheumatoid arthritis: an analysis of individual patient-level data. Arthritis Rheum 2011;63:2203-8. PMID: 21484766.