Certolizumab pegol

Summary

Certolizumab pegol (Cimzia) is a PEGylated humanized anti-TNF-α Fab' fragment approved for the treatment of moderate-to-severe Crohn's disease, rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, non-radiographic axial spondyloarthritis, and plaque psoriasis. Its unique Fc-free, PEGylated structure is associated with minimal placental transfer, making it notable for use in pregnancy when anti-TNF therapy is required.

Mechanism of Action

Selectively binds and neutralizes human tumor necrosis factor alpha (TNF-α), blocking its interaction with TNF receptors p55 and p75. As a PEGylated Fab' fragment lacking an Fc region, it does not fix complement or induce antibody-dependent cellular cytotoxicity. PEGylation extends half-life and may reduce placental transfer.

Routes of Administration

Goals & Uses

• Rheumatoid arthritis disease activity reductionRheumatologyHigh
• Ankylosing spondylitis and non-radiographic axial spondyloarthritis treatmentRheumatologyHigh
• Moderate-to-severe plaque psoriasisDermatologyHigh
• Crohn's disease remission induction and maintenanceGastroenterologyHigh
• Psoriatic arthritis symptom controlRheumatologyHigh
• Pregnancy-compatible anti-TNF therapyObstetrics/RheumatologyModerate

Contraindications

• Hypersensitivity to certolizumab pegol or excipientsAllergy/ImmunologyHigh
• Moderate-to-severe heart failure (NYHA class III/IV)CardiovascularHigh
• Active tuberculosis or other severe infectionsInfectious DiseaseHigh
• Demyelinating disordersNeurologyModerate
• Active hepatitis B infectionInfectious DiseaseHigh

Adverse Effects

• Injection site reactionsLocalCommon
• Hypersensitivity/anaphylaxisImmunologicalRare
• Malignancies (lymphoma, solid tumors)OncologicRare
• Autoimmune reactions (drug-induced lupus, autoantibody formation)ImmunologicUncommon
• Headache and nasopharyngitisGeneral/RespiratoryCommon
• Serious infections (bacterial, fungal, viral, opportunistic)InfectiousUncommon

Drug Interactions

• Other biologic DMARDs (e.g., rituximab, tocilizumab)Moderate
• AnakinraHigh
• Live vaccinesHigh
• AbataceptHigh
• MethotrexateLow

Population Constraints

• PregnancyReproductive SafetyRelative
• Pediatric patients (<18 years)AgeRelative
• Immunocompromised patientsImmunologicRelative
• Elderly patientsAgeRelative
• Patients with latent tuberculosisInfectious DiseaseRelative
• BreastfeedingReproductiveRelative

Regulatory Status

• European UnionApprovedApproved: Crohn's disease, Rheumatoid arthritis, Psoriatic arthritis, Axial spondyloarthritis (ankylosing spondylitis and non-radiographic), Plaque psoriasisApproved by EMA; marketed as Cimzia. Subject to additional monitoring.
• United StatesApprovedApproved: Moderately to severely active Crohn's disease, Moderately to severely active rheumatoid arthritis, Active psoriatic arthritis, Active ankylosing spondylitis, Active non-radiographic axial spondyloarthritis, Moderate-to-severe plaque psoriasisFirst approved by FDA in April 2008 for Crohn's disease. Boxed warning for serious infections and malignancy.
• United KingdomApprovedApproved: Crohn's disease, Rheumatoid arthritis, Psoriatic arthritis, Axial spondyloarthritis, Plaque psoriasisApproved by MHRA post-Brexit; NICE guidance supports use in specific indications with criteria.

Approved by the FDA in 2008 for Crohn's disease; subsequent approvals for rheumatoid arthritis (2009), psoriatic arthritis and ankylosing spondylitis (2013), plaque psoriasis (2018), and non-radiographic axial spondyloarthritis (2019). Carries a boxed warning for serious infections and malignancies. EMA-approved (Cimzia) with similar indications.

Evidence & Sources

No sources recorded yet.