CIMZIA
Clinical safety rating
cautionComprehensive clinical and safety monograph for CIMZIA (CIMZIA).
Comprehensive clinical and safety monograph for CIMZIA (CIMZIA).
Crohn's disease (FDA approved for adults with moderately to severely active disease)Rheumatoid arthritis (FDA approved for adults with moderately to severely active disease)Psoriatic arthritis (FDA approved for adults)Ankylosing spondylitis (FDA approved for adults)Plaque psoriasis (off-label use)Axial spondyloarthritis (off-label use)
Certolizumab pegol is a recombinant, humanized antibody Fab' fragment conjugated to polyethylene glycol (PEG) that binds and neutralizes human tumor necrosis factor alpha (TNFα), preventing its interaction with cell surface TNF receptors (TNFR p55 and p75). It also modulates immune responses by inhibiting TNFα-induced pro-inflammatory cytokine production and adhesion molecule expression.
| Metabolism | Certolizumab pegol is a monoclonal antibody fragment that is not metabolized by cytochrome P450 enzymes. It is degraded by proteolysis into small peptides and amino acids. |
| Excretion | Primarily eliminated via reticuloendothelial system and proteolytic catabolism; no significant renal or biliary excretion. Clinical pharmacokinetic studies show no dose adjustment needed in renal impairment. |
| Half-life | 14 days (range 11-17 days) following subcutaneous administration; supports every 2-week or monthly dosing intervals. |
| Protein binding | Not applicable (monoclonal antibody); typically does not bind to serum proteins other than target antigen. |
| Volume of Distribution | ~5.7 L (approx. 0.08 L/kg for a 70 kg patient), indicating predominant distribution in vascular space with limited extravascular penetration. |
| Bioavailability | Subcutaneous: ~80% (range 63-92%) relative to intravenous administration. |
| Onset of Action | Subcutaneous: Clinical response observed within 2-4 weeks in rheumatoid arthritis and psoriatic arthritis; 2-4 weeks in Crohn's disease; 2-4 weeks in plaque psoriasis. |
| Duration of Action | Subcutaneous: Maintains therapeutic effect for full dosing interval (2 weeks or monthly); steady-state achieved by 10-12 weeks with regular dosing. |
| Molecular Weight | 147.8 |
400 mg subcutaneously at weeks 0, 2, and 4, then 200 mg every 2 weeks or 400 mg every 4 weeks.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for renal impairment. Not studied in severe renal impairment. |
| Liver impairment | No dose adjustment required for hepatic impairment. Not studied in severe hepatic impairment (Child-Pugh C). |
| Pediatric use | Not approved for use in pediatric patients. Safety and efficacy not established. |
| Geriatric use | No specific dose adjustment in elderly; use with caution due to increased infection risk. |
| 1st trimester | Limited data; risk cannot be excluded. Use only if clearly needed. |
| 2nd trimester | Placental transfer increases; may cause fetal exposure. Use if benefit outweighs risk. |
| 3rd trimester | May lead to detectable levels in newborn; avoid unless essential. |
Clinical note
Comprehensive clinical and safety monograph for CIMZIA (CIMZIA).
| Placental transfer | Active placental transfer, especially in second and third trimesters; concentrations in cord blood can exceed maternal levels. |
| Breastfeeding | Minimal excretion into breast milk; consider risk-benefit, especially in preterm or high-risk infants. |
| Lactation Rating | L3 |
| Teratogenic Risk | CIMZIA (certolizumab pegol) is a PEGylated Fc-free anti-TNF monoclonal antibody. Due to minimal placental transfer (low Fc receptor binding), first trimester exposure shows no increased risk of major birth defects. Limited data in second and third trimesters; theoretical risk of immunosuppression in fetus. No known teratogenic effect in animal studies. |
| Fetal Monitoring | Monitor for maternal infections, tuberculosis reactivation (screen before and during therapy). No specific fetal monitoring required; standard prenatal care. Newborns exposed in utero should be monitored for infection for 6 months. |
| Fertility Effects | May improve fertility in patients with autoimmune conditions by reducing disease activity. No direct negative effect on fertility known. |
■ FDA Black Box Warning
Increased risk of serious infections leading to hospitalization or death, including tuberculosis (TB), bacterial sepsis, invasive fungal infections (such as histoplasmosis), and infections due to opportunistic pathogens. Malignancies, including lymphoma, have been reported in children and adolescents treated with TNF blockers.
| Serious Effects |
History of hypersensitivity to certolizumab pegol or any componentActive serious infection (e.g., tuberculosis, sepsis)
| Precautions | Serious infections (reactivation of TB, fungal infections, bacterial sepsis), malignancies (including lymphoma and non-melanoma skin cancer), hepatitis B virus reactivation, demyelinating disease (e.g., multiple sclerosis), congestive heart failure (new onset or exacerbation), hematologic abnormalities (pancytopenia, aplastic anemia), hypersensitivity reactions (including anaphylaxis), and lupus-like syndrome. |
| Food/Dietary | No known food interactions. Take with or without food. No dietary restrictions required. |
| Clinical Pearls | CIMZIA (certolizumab pegol) is a PEGylated Fc-free anti-TNF monoclonal antibody. It lacks an Fc region, which reduces placental transfer, making it a preferred biologic for rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, and Crohn's disease during pregnancy. Administer subcutaneously. Monitor for infections, including TB reactivation. Do not administer live vaccines concurrently. Injection site reactions are common; pre-medication with antihistamines may reduce them. |
| Patient Advice | Do not receive live vaccines (e.g., MMR, nasal flu, yellow fever) while on CIMZIA. Discuss vaccination schedule with your doctor. · Report any signs of infection (fever, cough, painful urination) or allergic reactions (rash, difficulty breathing) immediately. · Store CIMZIA in the refrigerator at 2°C to 8°C. Do not freeze. Protect from light. Allow to reach room temperature before injection. · Use proper injection technique; rotate injection sites (abdomen, thigh). Discard unused portions in a sharps container. · Tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. CIMZIA has low placental transfer and may be used during pregnancy. |
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