Download Adalimumab

Adalimumab
Drugbank ID : DB00051
Protein chemical formula : C6428H9912N1694O1987S46
Protein average weight : 144190.3000
Half-life : 10-20 days.
Description
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
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:
DIQMTQSPSSLSASVGDRVTITCRASQGIRNYLAWYQQKPGKAPKLLIYAASTLQSGVPSRFSGSGSGTD
FTLTISSLQPEDVATYYCQRYNRAPYTFGQGTKVEIKRTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPRE
AKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRG
EC
Heavy chain:
EVQLVESGGGLVQPGRSLRLSCAASGFTFDDYAMHWVRQAPGKGLEWVSAITWNSGHIDYADSVEGR
FTISRDNAKNSLYLQMNSLRAEDTAVYYCAKVSYLSTASSLDYWGQGTLVTVSSASTKGPSVFPLAPSSKST
SGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKP
SNTKVDKKVEPKSC
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. 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&comp
ression=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