| Primary information |
|---|
| ThPP ID | Th1078 |
| Therapeutic Peptide/Protein Name | Efalizumab |
| Sequence | Light Chain:DIQMTQSPSSLSASVGDRVTITCRASKTISKYLAWXQQ view full sequnce in fasta |
| Functional Classification | IIa |
| Molecular Weight | 150000 |
| Chemical Formula | N.A. |
| Isoelectric Point | N.A. |
| Hydrophobicity | N.A. |
| Melting Point (℃) | 61 (FAB f |
| Half Life | 5 days |
| Description | Efalizumab 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/Disease | Indcated in treatment of adult patients with moderate to severe chronic plaque psoriasis, who are candidates for phototherapy or systemic therapy. |
| Pharmacodynamics | In 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 Action | Efalizumab 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. |
| Toxicity | N.A. |
| Metabolism | N.A. |
| Absorption | Average efalizumab bioavailability following subcutaneous administration was estimated at 30 to 50%. |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | Immunosuppressive Agents |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| Drug Interaction | Ergonovine is the antiretroviral agent may increase the ergot derivative |
| Target | Iduronic acid |
| Information of corresponding available drug in the market |
|---|
| Brand Name | RAPTIVA |
| Company | Genentech, Inc. |
| Brand Discription | RAPTIVA 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 for | RAPTIVA (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 Name | N.A. |
| Formulation | Each 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 Appearnce | RAPTIVA (efalizumab) is supplied as a sterile, white to off-white, lyophilized powder in single-use glass vials |
| Route of Administration | Subcutaneous (Subcutaneous) Injection. |
| Recommended Dosage | The 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). |
| Contraindication | RAPTIVA (efalizumab) should not be administered to patients with known hypersensitivity to RAPTIVA (efalizumab) or any of its components. |
| Side Effects | he 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 Link | http://www.rxlist.com/raptiva-drug.htm |
| PubMed ID | 17053736, 24897146 |
| 3-D Structure | Th1078 (View) or (Download) |