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.

Indications: RA, psoriatic arthritis, ankylosing spondylitis, Crohn’s disease

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

Adverse Effects
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.

Adapted from: RheumaKnowledgy