Adalimumab Drugbank ID : DB00051

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Presentation transcript:

Adalimumab Drugbank ID : DB00051 Protein chemical formula : C6428H9912N1694O1987S46 Protein average weight : 144190.3000 Half-life : 10-20 days.

Description Indication Pharmacodynamics Mechanism Of Action Adalimumab is a human monoclonal antibody against TNF-alpha. It is produced by recombinant DNA technology using a mammalian cell expression system. It consists of 1330 amino acids and has a molecular weight of approximately 148 kilodaltons. Indication For treatment of rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, and Crohn's disease. Pharmacodynamics Used in the treatment of immune system mediated diseases, adalimumab binds specifically to TNF-alpha and blocks its general cytokine effects, thereby reducing TNF-induced inflammation and halting tissue destruction. Mechanism Of Action Adalimumab binds to TNF-alpha and blocks its interaction with the p55 and p75 cell surface TNF receptors. Adalimumab also lyses surface TNF expressing cells in vitro in the presence of complement.

Metabolism Clearance Categories Affected Organism Patents Most likely removed by opsonization via the reticuloendothelial system. Clearance 12 mL/hr [RA patients with dose 0.25-10 mg/kg] Categories Antirheumatic Agents and Anti-Inflammatory Agents and Immunosuppressive Agents Affected Organism Humans and other mammals Patents Country Patent Number Approved Expires Canada 2243459 2002-09-17 2017-02-10

Drug interaction Canakinumab : Increases immunosuppressive effects and risk of infection. Infliximab : Both bind to TNF alfa and thus combination results in enhanced immunosuppressive effect. It is recommended that simultaneous use of both agents be avoided. Rilonacept : results in increased immunosuppressive effects; increases the risk of infection. Tofacitinib : Adalimumab (and other anti-TNF immunosuppressants), when used in combination with tofacitinib, may increase the risk of added immunosuppression. It is recommended to avoid concurrent therapy. Trastuzumab : Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.

Sequence Light chain: DIQMTQSPSSLSASVGDRVTITCRASQGIRNYLAWYQQKPGKAPKLLIYAASTLQSGVPSRFSGSGSGTDFTLTISSLQPEDVATYYCQRYNRAPYTFGQGTKVEIKRTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC Heavy chain: EVQLVESGGGLVQPGRSLRLSCAASGFTFDDYAMHWVRQAPGKGLEWVSAITWNSGHIDYADSVEGRFTISRDNAKNSLYLQMNSLRAEDTAVYYCAKVSYLSTASSLDYWGQGTLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSC

Targets Tumor necrosis factor, Low affinity immunoglobulin gamma Fc region receptor III-B, Complement C1r subcomponent, Complement C1q subcomponent subunit A, Complement C1q subcomponent subunit B, Complement C1q subcomponent subunit C, Low affinity immunoglobulin gamma Fc region receptor III-A, Complement C1s subcomponent, High affinity immunoglobulin gamma Fc receptor I, Low affinity immunoglobulin gamma Fc region receptor II-a, Low affinity immunoglobulin gamma Fc region receptor II-b, Low affinity immunoglobulin gamma Fc region receptor II-c

Brands : Humira and Humira Pen Company : Abbott Laboratories Description : HUMIRA (adalimumab) is a recombinant human IgG1 monoclonal antibody specific for human tumor necrosis factor (TNF). HUMIRA was created using phage display technology resulting in an antibody with human derived heavy and light chain variable regions and human IgG1:k constant regions. Adalimumab is produced by recombinant DNA technology in a mammalian cell expression system and is purified by a process that includes specific viral inactivation and removal steps. It consists of 1330 amino acids and has a molecular weight of approximately 148 kilodaltons. Used For/Prescribed for : Humira is used to treat rheumatoid arthritis, juvenile idiopathic arthritis, psoriatic arthritis, ankylosing spondylitis, and plaque psoriasis. It is also used to treat Crohn's disease or ulcerative colitis, after other drugs have been tried without successful treatment of symptoms.

Formulation : It is supplied for a single use Formulation : It is supplied for a single use. Each prefilled syringe delivers 0.8 mL (40 mg) of drug product. Each 0.8 mL of HUMIRA contains 40 mg adalimumab, 4.93 mg sodium chloride, 0.69 mg monobasic sodium phosphate dihydrate, 1.22 mg dibasic sodium phosphate dihydrate, 0.24 mg sodium citrate, 1.04 mg citric acid monohydrate, 9.6 mg mannitol, 0.8 mg polysorbate 80, and Water for Injection, USP. Sodium hydroxide added as necessary to adjust pH. Each pediatric prefilled syringe delivers 0.4 mL (20 mg) of drug product. Each 0.4 mL of HUMIRA contains 20 mg adalimumab, 2.47 mg sodium chloride, 0.34 mg monobasic sodium phosphate dihydrate, 0.61 mg dibasic sodium phosphate dihydrate, 0.12 mg sodium citrate, 0.52 mg citric acid monohydrate, 4.8 mg mannitol, 0.4 mg polysorbate 80, and Water for Injection, USP. Sodium hydroxide added as necessary to adjust pH. Form : sterile, preservative-free solution Route of administration : subcutaneous administration Dosage : The recommended dose of HUMIRA for adult patients with rheumatoid arthritis (RA), psoriatic arthritis (PsA), or ankylosing spondylitis (AS) is 40 mg administered every other week. Methotrexate (MTX), other non-biologic DMARDS, glucocorticoids, nonsteroidal anti-inflammatory drugs (NSAIDs), and/or analgesics may be continued during treatment with HUMIRA. In the treatment of RA, some patients not taking concomitant MTX may derive additional benefit from increasing the dosing frequency of HUMIRA to 40 mg every week. Contraindication : hypersensitivity

Side effects : signs of infection - fever, chills, sore throat, vomiting, diarrhea, flu symptoms, pain or burning when you urinate; signs of tuberculosis - fever with ongoing cough, weight loss (fat or muscle); pale skin, easy bruising or bleeding (nosebleeds, bleeding gums); numbness, tingly feeling, weakness or prickly feeling; vision problems; shortness of breath with swelling of your ankles or feet; or new or worsening psoriasis (raised, silvery flaking of the skin). headache; nausea; cold symptoms such as stuffy nose, sinus pain, sneezing, sore throat; rash; or redness, bruising, itching, or swelling where the injection was given. Drug Interaction : A total of 297 drugs (941 brand and generic names) are known to interact with Humira (adalimumab). 168 major drug interactions (523 brand and generic names) 114 moderate drug interactions (348 brand and generic names) 15 minor drug interactions (70 brand and generic names)

Genral References # PDB sequence "Link":http://www.rcsb.org/pdb/download/downloadFile.do?fileFormat=FASTA&compression=NO&structureId=1IGT # Patent Information "Link":http://www.freepatentsonline.com/6090382.html

Refrence https://www.humira.com/ http://www.drugs.com/humira.html http://www.rxlist.com/humira-drug.htm