| Primary information |
|---|
| ThPP ID | Th1063 |
| Therapeutic Peptide/Protein Name | Basiliximab |
| Sequence | Heavy Chain: QLQQSGTVLARPGASVKMSCKASGYSFTRYWMHWIKQ view full sequnce in fasta |
| Functional Classification | IIa |
| Molecular Weight | 143801.3 |
| Chemical Formula | C6378H9844N1698O1997S48 |
| Isoelectric Point | 8.68 |
| Hydrophobicity | -0.473 |
| Melting Point (℃) | 61 (FAB f |
| Half Life | 7.2 ± 3.2 days (adults) |
| Description | A recombinant chimeric (murine/human) monoclonal antibody (IgG1k) that functions as an immunosuppressive agent, specifically binding to and blocking the interleukin-2 receptor a-chain (IL-2R alpha, also known as CD25 antigen) on the surface of activated T-lymphocytes. It is a 144 kDa glycoprotein obtained from fermentation of an established mouse myeloma cell line genetically engineered to express plasmids containing the human heavy and light chain constant region genes and mouse heavy and light chain variable region genes encoding the RFT5 antibody that binds selectively to the IL-2R alpha. |
| Indication/Disease | For prophylactic treatment of kidney transplant rejection |
| Pharmacodynamics | Basiliximab functions as an IL-2 receptor antagonist. Specifically it inhibits IL-2-mediated activation of lymphocytes, a critical pathway in the cellular immune response involved in allograft rejection. |
| Mechanism of Action | Basiliximab binds with high-affinity to the alpha-subunit (CD25) of the high-affinity IL-2 receptor. This inhibits IL-2 binding, which inhibits T-cell activation and prevents the body from mounting an immune response against the foreign kidney. |
| Toxicity | N.A. |
| Metabolism | Most likely removed by opsonization via the reticuloendothelial system. |
| Absorption | N.A. |
| Volume of Distribution | 7.8 ± 5.1 L [Pediatric] 4.8 ± 2.1 L [Adult] |
| Clearance | 41 ± 19 mL/h [Adult patients undergoing first kidney transplantation] 17 ± 6 mL/h [pediatric patients undergoing renal transplantation] 31 ± 19 mL/h [adolescent patients undergoing renal transplantation] |
| Categories | Immunosuppressive Agents |
| Patents Number | CA2038279 |
| Date of Issue | 10/03/03 |
| Date of Expiry | 12/03/15 |
| Drug Interaction | Canakinumab, Rilonacept results in increased immunosuppressive effects; increases the risk of infection |
| Target | N.A. |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Simulect |
| Company | Novartis |
| Brand Discription | Simulect (basiliximab) is a chimeric (murine/human) monoclonal antibody(IgG1K), produced by recombinant DNA technology, that functions as animmunosuppressive agent, specifically binding to and blocking the interleukin-2 receptor α-chain (IL-2Rα, also known as CD25 antigen) on the surface of activated T-lymphocytes. Based on the amino acid sequence, the calculated molecular weight of the protein is 144 kilodaltons. It is aglycoprotein obtained from fermentation of an established mouse myeloma cell line genetically engineered to express plasmids containing the human heavy and light chain constant region genes and mouse heavy and light chain variable region genes encoding the RFT5 antibody that binds selectively to the IL-2Rα. |
| Prescribed for | Simulect (basiliximab) is indicated for the prophylaxis of acute organ rejection in patients receiving renal transplantation when used as part of an immunosuppressive regimen that includes cyclosporine, USP (MODIFIED) and corticosteroids. |
| Chemical Name | N.A. |
| Formulation | Each 10-mg vial contains 10 mg basiliximab, 3.61 mg monobasic potassium phosphate, 0.50 mg disodium hydrogen phosphate (anhydrous), 0.80 mg sodium chloride, 10 mg sucrose, 40 mg mannitol and 20 mg glycine, to be reconstituted in 2.5 mL of Sterile Water for Injection, USP. No preservatives are added. Each 20-mg vial contains 20 mg basiliximab, 7.21 mg monobasic potassium phosphate, 0.99 mg disodium hydrogen phosphate (anhydrous), 1.61 mg sodium chloride, 20 mg sucrose, 80 mg mannitol and 40 mg glycine, to be reconstituted in 5 mL of Sterile Water for Injection, USP. No preservatives are added. |
| Physcial Appearnce | Simulect (basiliximab) , is a sterile lyophilisate which is available in 6 mL colorless glass vials and is available in 10 mg and 20 mg strength powder. |
| Route of Administration | intavenous infusion mainly or bolus (if no allerg |
| Recommended Dosage | In adult patients, the recommended regimen is two doses of 20 mg each. The first 20-mg dose should be given within 2 hours prior to transplantation surgery. The recommended second 20-mg dose should be given 4 days after transplantation. |
| Contraindication | Simulect (basiliximab) is contraindicated in patients with known hypersensitivity to basiliximab or any other component of the formulation. |
| Side Effects | Gastrointestinal System: constipation, nausea, abdominal pain, vomiting, diarrhea, dyspepsia; Body as a Whole-General: pain, peripheral edema, fever, viral infection; Metabolic and Nutritional: hyperkalemia, hypokalemia, hyperglycemia, hypercholesterolemia, hypophosphatemia, hyperuricemia; Urinary System: urinary tract infection;Respiratory System: dyspnea, upper respiratory tract infection; Skin and Appendages: surgical wound complications, acne;Cardiovascular Disorders-General: hypertension; Central and Peripheral Nervous System: headache, tremor; Psychiatric: insomnia; Red Blood Cell: anemia. |
| Useful Link | http://www.rxlist.com/simulect-drug.htm http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1af01887-b69d-444b-91ed-ebfe12784440 |
| PubMed ID | 25501951, 22151353 |
| 3-D Structure | Th1063 (View) or (Download) |