Detailed description page of THPdb

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Primary information
ThPP ID	Th1005
Therapeutic Peptide/Protein Name	Etanercept
Sequence	LPAQVAFTPYAPEPGSTCRLREYYDQTAQMCCSKCSPGQHAKVFCTKTSD view full sequnce in fasta
Functional Classification	IIa
Molecular Weight	51234.9
Chemical Formula	C2224H3475N621O698S36
Isoelectric Point	7.89
Hydrophobicity	-0.529
Melting Point (℃)	71
Half Life	102 Â± 30 hrs
Description	It 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/Disease	Used to treat severe rheumatoid arthritis in adults, severe juvenile idiopathic arthritis, ankylosing spondylitis, and severe plaque psoriasis.
Pharmacodynamics	TNF, 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 Action	There 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.
Toxicity	N.A.
Metabolism	N.A.
Absorption	N.A.
Volume of Distribution	N.A.
Clearance	160 Â± 80 mL/hr [RA patients]
Categories	Immunosuppressive Agents
Patents Number	CA2476934
Date of Issue	16/06/09
Date of Expiry	27/02/23
Drug Interaction	Rilonacept results in increased immunosuppressive effects; increases the risk of infection.
Target	Tumor 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 Name	Enbrel
Company	Immunex Corp
Brand Discription	Enbrel 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 for	Used 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 Name	N.A.
Formulation	Supplied 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 Appearnce	Lyophilized powder.
Route of Administration	Subcutaneous Injection
Recommended Dosage	N.A.
Contraindication	N.A.
Side Effects	Signs 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 Link	http://www.genome.jp/dbget-bin/www_bget/D00742
PubMed ID	20080922, 25651776, 23620660, 16713481
3-D Structure	Th1005 (View) or (Download)