| Primary information |
|---|
| ThPP ID | Th1153 |
| Therapeutic Peptide/Protein Name | Alefacept |
| Sequence | Heavy Chain: CFSQQIYGVVYGNVTFHVPSNVPLKEVLWKKQKDKVA view full sequnce in fasta |
| Functional Classification | IIa |
| Molecular Weight | 51801.1 |
| Chemical Formula | C2306H3594N610O694S26 |
| Isoelectric Point | 7.86 |
| Hydrophobicity | -0.432 |
| Melting Point (℃) | N.A. |
| Half Life | 270 hrs |
| Description | Immunosuppressive dimeric fusion protein that consists of the extracellular CD2-binding portion of the human leukocyte function antigen-3 (LFA-3) linked to the Fc (hinge, CH2 and CH3 domains) portion of human IgG1. Produced by CHO cells, mW is 91.4 kD. |
| Indication/Disease | As an immunosuppressive drug, Alefacept can be used for treatment of moderate to severe chronic plaque psoriasis |
| Pharmacodynamics | Interferes with lymphocyte activation by specifically binding to the lymphocyte antigen, CD2, and inhibiting LFA-3/CD2 interaction. Activation of T lymphocytes involving the interaction between LFA-3 on antigen-presenting cells and CD2 on T lymphocytes plays a role in the pathophysiology of chronic plaque psoriasis. Also causes a reduction in subsets of CD2+ T lymphocytes as well as CD4+ and CD8+ T lymphocytes. |
| Mechanism of Action | Inhibits T-lymphocyte activation and production by binding to the CD2 lymphocyte antigen. |
| Toxicity | While it has been found to cross the placenta in monkeys, it is not yet known if it also diffuses into breast milk. |
| Metabolism | N.A. |
| Absorption | Bioavailability after IM administration is 63%. |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | Dermatologic and Immunosupressive agents |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| Drug Interaction | Canakinumab, Rilonacept- Increases immunosupressive effects |
| Target | T-cell surface antigen CD2, Complement C1r subcomponent, Complement C1q subcomponent subunit A, B, C, Low affinity immunoglobulin gamma Fc region receptor III-A,III-B, II-a, II-b, II-c |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Amevive |
| Company | Astellas Pharma Inc. |
| Brand Discription | AMEVIVE (alefacept) is a CD2-directed LFA-3/Fc fusion protein that consists of the extracellular CD2-binding portion of the human leukocyte function antigen-3 (LFA-3) linked to the Fc (hinge, CH2 and CH3 domains) portion of human IgGl. Alefacept is produced by recombinant DNA technology in a Chinese Hamster Ovary (CHO) mammalian cell expression system. The molecular weight of alefacept is 91.4 kilodaltons. |
| Prescribed for | AMEVIVE is indicated for the treatment of adult patients with moderate to severe chronic plaque psoriasis who are candidates for systemic therapy or phototherapy. |
| Chemical Name | N.A. |
| Formulation | It contains alefacept (15 mg), citric acid monohydrate (0.06 mg), glycine (5 mg), sodium citrate dehydrate (3.6 mg), and sucrose (12.5 mg) per 0.5 mL of reconstituted solution. |
| Physcial Appearnce | AMEVIVE is supplied as a sterile, white-to-off-white, preservative-free, lyophilized powder |
| Route of Administration | Intramuscular Injection |
| Recommended Dosage | The recommended dose of AMEVIVE® is 15 mg intramuscularly once weekly for 12 weeks. The CD4+ T lymphocyte counts should be measured before initiating dosing. |
| Contraindication | AMEVIVE should not be administered to patients infected with HIV. AMEVIVE reduces CD4+ T lymphocyte counts, which might accelerate disease progression or increase complications of disease in these patients |
| Side Effects | Lymphopenia, Malignancies, Serious Infections reuiring hospitalization, Hypersenstivity reactions. |
| Useful Link | http://www.rxlist.com/amevive-drug.htm |
| PubMed ID | 16865867, 16713481 |
| 3-D Structure | Th1153 (View) or (Download) |