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1442 details
Primary information
ThPP IDTh1078
Therapeutic Peptide/Protein NameEfalizumab
SequenceLight Chain:DIQMTQSPSSLSASVGDRVTITCRASKTISKYLAWXQQ view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight150000
Chemical FormulaN.A.
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)61 (FAB f
Half Life5 days
DescriptionEfalizumab is Humanized IgG1 kappa isotype monoclonal antibody that binds to human CD11a. It is produced in a Chinese hamster ovary mammalian cell expression system in a nutrient medium containing the antibiotic gentamicin.
Indication/DiseaseIndcated in treatment of adult patients with moderate to severe chronic plaque psoriasis, who are candidates for phototherapy or systemic therapy.
PharmacodynamicsIn psoriatic skin, ICAM-1 cell surface expression is upregulated on endothelium and keratinocytes. Raptiva inhibits the binding of LFA-1 to the intercellular adhesion molecule-1 (ICAM-1), thereby inhibiting the adhesion of leukocytes to other cell types.
Mechanism of ActionEfalizumab binds to CD11a, a subunit of leukocyte function antigen-1 (LFA-1), which is expressed on all leukocytes. As a result efalizumab decreases cell surface expression of CD11a.
ToxicityN.A.
MetabolismN.A.
AbsorptionAverage efalizumab bioavailability following subcutaneous administration was estimated at 30 to 50%.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesImmunosuppressive Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionErgonovine is the antiretroviral agent may increase the ergot derivative
TargetIduronic acid
Information of corresponding available drug in the market
Brand NameRAPTIVA
CompanyGenentech, Inc.
Brand DiscriptionRAPTIVA is an  immunosuppressive  recombinant humanized I gG1 kappa isotype monoclonal antibody that binds to human CD11a. Efalizumab has a molecular weight of approximately 150 kilodaltons and is produced in a Chinese hamster ovary mammalian cell expression system in a nutrient medium containing the antibiotic gentamicin. Gentamicin is not detectable in the final product.
Prescribed forRAPTIVA (efalizumab) is indicated for the treatment of adult patients (18 years or older) with chronic moderate to severe plaque psoriasis who are candidates for systemic therapy or phototherapy.
Chemical NameN.A.
FormulationEach single-use vial of RAPTIVA contains 150 mg of efalizumab, 123.2 mg of sucrose, 6.8 mg of L-histidine hydrochloride monohydrate, 4.3 mg of L-histidine and 3 mg of polysorbate 20 and is designed to deliver 125 mg of efalizumab in 1.25 mL.
Physcial AppearnceRAPTIVA (efalizumab) is supplied as a sterile, white to off-white, lyophilized powder in single-use glass vials
Route of AdministrationSubcutaneous (Subcutaneous) Injection. 
Recommended DosageThe recommended dose of RAPTIVA (efalizumab) is a single 0.7 mg/kg SCconditioning dose followed by weekly SC doses of 1 mg/kg (maximum single dose not to exceed a total of 200 mg).
ContraindicationRAPTIVA (efalizumab) should not be administered to patients with known hypersensitivity to RAPTIVA (efalizumab) or any of its components.
Side Effectshe most serious adverse reactions observed during treatment with RAPTIVA (efalizumab) are serious infections, including PML, malignancies,thrombocytopenia, hemolytic anemia, arthritis events, psoriasis worsening and variants, and neurologic events. The most common adverse reactions associated with RAPTIVA (efalizumab) were a first dose reaction complex that included headache, chills, fever, nausea, and myalgia.
Useful Linkhttp://www.rxlist.com/raptiva-drug.htm
PubMed ID17053736, 24897146
3-D StructureTh1078 (View) or (Download)