| Identification | Back Directory | [Name]
Certolizumab | [CAS]
428863-50-7 | [Synonyms]
Cdp870
Cimzia
Pha 738144
Unii-umd07X179e
CERTOLIZUMAB PEGOL
Research Grade Certolizumab(DHB94401)
(2S)-1-((2S)-6-aMino-2-((hydroxy(4-phenylbutyl)phosphoryl)oxy)hexanoyl)pyrrolidine-2-carboxylic acid
Immunoglobulin, anti-(human tumor necrosis factor alpha) fab' fragment (human-mouse monoclonal cdp870 heavy chain), disulfide with human-mouse monoclonal cdp870 light chain, pegylated | [Molecular Formula]
C24H22F3N | [MOL File]
428863-50-7.mol | [Molecular Weight]
381.433 |
| Hazard Information | Back Directory | [Description]
Certolizumab pegol, a tumor necrosis factor α(TNF-α) blocker, was
launched for the treatment of moderate-to-severe Crohn’s
disease. It is specifically indicated for reducing signs and symptoms and
maintaining clinical response in adult patients who have had an
inadequate response to conventional therapy. Certolizumab pegol is
the third anti-TNF-α biologic to be marketed for this indication behind
infliximab (Remicade) and adalimumab (Humira). Certolizumab
pegol is a recombinant, humanized antibody Fab’ fragment linked to
approximately 40 kDa polyethylene glycol (PEG). The Fab’ fragment is
composed of a light chain with 214 amino acids and a heavy chain with
229 amino acids. It is manufactured in E.coli and is subsequently
subjected to purification and conjugation to PEG, to generate certolizumab pegol. The addition of PEG moiety significantly enhances the
plasma half-life of the antibody, allowing for less frequent dosing. Certolizumab pegol neutralizes both soluble and membrane-associated forms of human TNF-a. It binds to human TNF-a with slightly higher affinity (KD 0.09 nM) than infliximab (KD 0.23 nM) and adalimumab (KD 0.16 nM). In addition, in cellular assays, certolizumab pegol is more potent in preventing TNF-a-induced killing of L929 fibroblasts than infliximab and adalimumab (IC50 0.35 ng/mL versus 5 and 6 ng/mL, 592 Shridhar Hegde and Michelle Schmidt respectively). | [Originator]
UCB Celltech (United Kingdom) | [Uses]
Certolizumab pegol increases nonexudative age-related macular degeneration diagnosis among medicare beneficiaries with rheumatoid arthritis. | [Uses]
Treatment of rheumatoid
arthritis and inflammatory bowel disease. | [Brand name]
Cimzia | [Clinical Use]
#N/A | [Side effects]
The most common adverse reactions with certolizumab were upper respiratory infections (20%), urinary tract infections (7%), and anthralgias (6%). TNF-a blockers as a class have been linked to increased risk of opportunistic infections and malignancy. Tuberculosis, invasive fungal infections, and other serious infections have occurred in patients receiving certolizumab pegol, and the drug label contains a black-box warning of the risk. | [Drug interactions]
Potentially hazardous interactions with other drugs
Anakinra and abatacept: avoid concomitant use.
Live vaccines: avoid concomitant use. | [Metabolism]
The Fab fragment comprises protein compounds and is
expected to be degraded to peptides and amino acids by
proteolysis. The de-conjugated PEG component is rapidly
eliminated from plasma and is to an unknown extent
excreted renally. |
|
| Company Name: |
AntibodySystem
|
| Tel: |
027-65279366 18162686757 |
| Website: |
www.antibodysystem.com |
|