Certolizumab pegol

Certolizumab pegol, sold under the brand name Cimzia, is a biopharmaceutical medication for the treatment of Crohn's disease,^[3][4] rheumatoid arthritis, psoriatic arthritis and ankylosing spondylitis. It is a fragment of a monoclonal antibody specific to tumor necrosis factor alpha (TNF-α) and is manufactured by UCB.^[5][6][1]

Certolizumab pegol

Syringe with 200mg Certolizumab pegol
Monoclonal antibody
Type	Fab' fragment
Source	Humanized (from mouse)
Target	TNF alpha
Clinical data
Trade names	Cimzia
Other names	CDP870
AHFS/Drugs.com	Monograph
MedlinePlus	a608041
License data	US DailyMed: Certolizumab pegol
Pregnancy category	AU: C
Routes of administration	Subcutaneous
ATC code	L04AB05 (WHO)
Legal status
Legal status	AU: S4 (Prescription only) US: ℞-only[1] EU: Rx-only[2]
Pharmacokinetic data
Elimination half-life	about 11 days
Excretion	Kidney (PEG only)
Identifiers
CAS Number	428863-50-7 N
DrugBank	DB08904 Y
ChemSpider	none
UNII	UMD07X179E
KEGG	D03441 Y
ChEMBL	ChEMBL1201831 N
Chemical and physical data
Formula	C2115H3252N556O673S16
Molar mass	47749.46 g·mol−1
NY (what is this?)  (verify)

It is on the World Health Organization's List of Essential Medicines.^[7]

Medical uses

Crohn's Disease

On April 22, 2008, the U.S. Food and Drug Administration (FDA) approved Cimzia for the treatment of Crohn's disease in people who did not respond sufficiently or adequately to standard therapy.^[6][8][9]

Rheumatoid arthritis

On June 26, 2009, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) issued a positive opinion recommending that the European Commission grant a marketing authorisation for Cimzia for the treatment of rheumatoid arthritis only - the CHMP refused approval for the treatment of Crohn's disease. The marketing authorisation was granted to UCB Pharma SA in October 2009.^[2]

Psoriatic arthritis

On September 27, 2013, the U.S. FDA approved Cimzia for the treatment of adult patients with active psoriatic arthritis.^[10]

Method of action

Three certolizumab molecules (blue) binding a homotrimer of TNF-alpha (tan). Certolizumab can block TNF in both its soluble form (freely circulating in the bloodstream) and its transmembrane form (bound to the membrane of a cell). From PDB: 5WUX​.^[11]

Certolizumab pegol is a monoclonal antibody directed against tumor necrosis factor alpha. More precisely, it is a PEGylated Fab' fragment of a humanized TNF inhibitor monoclonal antibody.^[12]

Clinical trials

Crohn's disease

Positive results have been demonstrated in two phase III trials (PRECiSE 1 and 2) of certolizumab pegol versus placebo in moderate to severe active Crohn's disease.^{[3][12][13][14]}

Axial spondyloarthritis

In 2013, a phase 3 double blind randomized placebo-controlled study found significantly positive results in patient self-reported questionnaires, with rapid improvement of function and pain reduction, in patients with axial spondyloarthritis.^[15]

Rheumatoid arthritis

Certolizumab appears beneficial in those with rheumatoid arthritis.^[16]