==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb

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1028 details
Primary information
ThPP IDTh1005
Therapeutic Peptide/Protein NameEtanercept
SequenceLPAQVAFTPYAPEPGSTCRLREYYDQTAQMCCSKCSPGQHAKVFCTKTSD view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight51234.9
Chemical FormulaC2224H3475N621O698S36
Isoelectric Point7.89
Hydrophobicity-0.529
Melting Point (℃)71
Half Life102 ± 30 hrs
DescriptionIt is a dimeric fusion protein (934 amino acids) consisting of extracellular ligand-binding portion of the human 75 kilodalton (p75) tumor necrosis factor receptor (TNFR) linked to Fc portion of human IgG1 produced by recombinant DNA technology in a Chinese hamster ovary (CHO) mammalian cell expression system.. The Fc component of etanercept contains the CH2 domain, the CH3 domain and hinge region, but not the CH1 domain of IgG1.
Indication/DiseaseUsed to treat severe rheumatoid arthritis in adults, severe juvenile idiopathic arthritis, ankylosing spondylitis, and severe plaque psoriasis.
PharmacodynamicsTNF, a naturally occurring cytokine is involved in normal inflammatory and immune responses. Elevated levels of TNF are found in tissues and fluids of patients suffering from rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis (AS), and plaque psoriasis. Etanercept binds specifically to tumor necrosis factor (TNF) and blocks its interaction with cell surface TNF receptors.
Mechanism of ActionThere are two distinct receptors for TNF (TNFRs), a 55 kilodalton (p55) and a 75 kilodalton receptor (p75). The biological activity of TNF is dependent upon binding to either of the cell surface receptors p75 or p55. Etanercept is a dimeric soluble form of the p75 TNF receptor that can bind to two TNF molecules, thereby effectively removing them from circulation.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
Clearance160 ± 80 mL/hr [RA patients]
CategoriesImmunosuppressive Agents
Patents NumberCA2476934
Date of Issue16/06/09
Date of Expiry27/02/23
Drug InteractionRilonacept results in increased immunosuppressive effects; increases the risk of infection.
TargetTumor necrosis factor,Tumor necrosis factor receptor superfamily member 1B,Low affinity immunoglobulin gamma Fc region receptor II-b,Low affinity immunoglobulin gamma Fc region receptor II-c,Lymphotoxin-alpha,Low affinity immunoglobulin gamma Fc region re
Information of corresponding available drug in the market
Brand NameEnbrel
CompanyImmunex Corp
Brand DiscriptionEnbrel is a 934 amino acid fusion protein (dimeric) weighing approximately 150 kilodaltons and containing the extracellular ligand-binding part of the human 75 kilodalton (p75) tumor necrosis factor receptor linked to the Fc part of human IgG1. The Fc com
Prescribed forUsed to treat rheumatoid arthritis, psoriatic arthritis, or ankylosing spondylitis, and prevent joint damage caused by these conditions. Enbrel is also used to treat plaque psoriasis in adults and polyarticular juvenile idiopathic arthritis (in children a
Chemical NameN.A.
FormulationSupplied in a multiple-use vial as a sterile, white, preservative-free, lyophilized powder. Reconstitution with 1 mL of the supplied Sterile Bacteriostatic Water for Injection, USP (containing 0.9% benzyl alcohol) yields a multiple-use, clear, and colorle
Physcial AppearnceLyophilized powder.
Route of AdministrationSubcutaneous Injection
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsSigns of infection (fever, chills, sore throat, body aches, confusion, neck stiffness, flu symptoms); shortness of breath with swelling, rapid weight gain; chest pain, ongoing cough, coughing up mucus or blood; signs of skin infection such as itching, sw
Useful Linkhttp://www.genome.jp/dbget-bin/www_bget/D00742
PubMed ID20080922, 25651776, 23620660, 16713481
3-D StructureTh1005 (View) or (Download)