Identification
- Summary
Basiliximab is a monoclonal anti-C25 antibody (interleukin-2 receptor alpha subunit) used as immunosuppressive therapy in kidney transplant patients.
- Brand Names
- Simulect
- Generic Name
- Basiliximab
- DrugBank Accession Number
- DB00074
- Background
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.
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Structure
- Protein Chemical Formula
- C6378H9844N1698O1997S48
- Protein Average Weight
- 143801.3 Da
- Sequences
>Basiliximab heavy chain QLQQSGTVLARPGASVKMSCKASGYSFTRYWMHWIKQRPGQGLEWIGAIYPGNSDTSYNQ KFEGKAKLTAVTSASTAYMELSSLTHEDSAVYYCSRDYGYYFDFWGQGTTLTVSSASTKG PSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSL SSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPPKSCDKTHTCPPCPAPELLGGPSVF LFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYR VVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKN QVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGN VFSCSVMHEALHNHYTQKSLSLSPGK
>Basiliximab light chain QIVSTQSPAIMSASPGEKVTMTCSASSSRSYMQWYQQKPGTSPKRWIYDTSKLASGVPAR FSGSGSGTSYSLTISSMEAEDAATYYCHQRSSYTFGGGTKLEIKRTVAAPSVFIFPPSDE QLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTLSK ADYEKHKVYACEVTHQGLSSPVTKSFNRGE
Download FASTA Format- Synonyms
- Basiliximab
- External IDs
- CHI-621
- SDZ-CHI-621
Pharmacology
- Indication
For prophylactic treatment of kidney transplant rejection
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- Contraindications & Blackbox Warnings
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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.
Target Actions Organism AInterleukin-2 receptor subunit alpha antibodyHumans UInterleukin-2 receptor subunit beta antibodyHumans - Absorption
Not Available
- Volume of distribution
- 7.8 ± 5.1 L [Pediatric]
- 4.8 ± 2.1 L [Adult]
- Protein binding
Not Available
- Metabolism
Most likely removed by opsonization via the reticuloendothelial system when bound to lymphocytes, or by human antimurine antibody production
- Route of elimination
Not Available
- Half-life
7.2 +/- 3.2 days (adults)
- 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]
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbatacept The risk or severity of adverse effects can be increased when Basiliximab is combined with Abatacept. Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Basiliximab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Basiliximab. Adenovirus type 7 vaccine live The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Basiliximab. Aducanumab The risk or severity of adverse effects can be increased when Basiliximab is combined with Aducanumab. Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Basiliximab. Alefacept The risk or severity of adverse effects can be increased when Basiliximab is combined with Alefacept. Alemtuzumab The risk or severity of adverse effects can be increased when Basiliximab is combined with Alemtuzumab. Alirocumab The risk or severity of adverse effects can be increased when Basiliximab is combined with Alirocumab. Allogeneic processed thymus tissue The therapeutic efficacy of Allogeneic processed thymus tissue can be decreased when used in combination with Basiliximab. 
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- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Simulect Powder, for solution 20 mg / vial Intravenous Novartis 2000-10-23 Not applicable Canada 
Simulect Injection, powder, for solution 10 mg Intravenous Novartis Europharm Limited 2016-09-08 Not applicable EU 
Simulect Injection, powder, for solution 20 mg/5mL Intravenous Novartis Pharmaceuticals Corporation 1998-05-12 Not applicable US 
Simulect Injection, powder, for solution 20 mg Intravenous Novartis Europharm Limited 2016-09-08 Not applicable EU Simulect Injection, powder, for solution 10 mg/2.5mL Intravenous Novartis Pharmaceuticals Corporation 1998-05-12 Not applicable US
Categories
- ATC Codes
- L04AC02 — Basiliximab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antineoplastic and Immunomodulating Agents
- Blood Proteins
- Globulins
- Immunoglobulins
- Immunologic Factors
- Immunoproteins
- Immunosuppressive Agents
- Interleukin 2 Receptor-directed Antibody Interactions
- Interleukin Inhibitors
- Interleukin-2 Receptor Antagonist
- Interleukin-2 Receptor Blocking Antibody
- Proteins
- Serum Globulins
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 9927MT646M
- CAS number
- 179045-86-4
References
- General References
- Not Available
- External Links
- UniProt
- P01857
- Genbank
- J00228
- PubChem Substance
- 46505169
- 196102
- ChEMBL
- CHEMBL1201439
- Therapeutic Targets Database
- DAP000388
- PharmGKB
- PA164747126
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Basiliximab
- FDA label
- Download (506 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Kidney Transplantation 1 4 Completed Prevention Adverse Side Effects / Kidney Transplantation 1 4 Completed Prevention Disorder Related to Renal Transplantation 1 4 Completed Prevention Kidney Transplantation 3 4 Completed Prevention Liver Transplantation 1 4 Completed Treatment Chronic Kidney Disease (CKD) / End Stage Renal Disease (ESRD) / Hemodialysis Treatment / Kidney Transplantation / Renal Replacement Therapies 1 4 Completed Treatment Chronic Renal Diseases 1 4 Completed Treatment Cirrhosis of the Liver / Liver Transplant Disorder 1 4 Completed Treatment Cytomegalovirus (CMV) Infection / Disorder Related to Renal Transplantation 1 4 Completed Treatment Diabetes Mellitus 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Novartis AG
- Dosage Forms
Form Route Strength Injection, powder, for solution Intravenous 10 mg/2.5mL Injection, powder, for solution Intravenous 10 mg Injection, powder, for solution Intravenous 20 MG Injection, powder, for solution Intravenous 20 mg/5mL Injection, powder, for solution Intravenous; Intravenous bolus 20 MG Powder 20 mg/1vial Powder, for solution Intravenous 20 mg / vial Injection Intravenous Injection, powder, lyophilized, for solution Intravenous Injection, powder, lyophilized, for solution Intravenous 20 mg - Prices
Unit description Cost Unit Simulect 20 mg vial 2471.6USD vial Simulect 10 mg vial 1883.11USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2038279 No 1999-03-09 2011-03-11 Canada
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 61 °C (FAB fragment), 71 °C (whole mAb) Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000) hydrophobicity -0.473 Not Available isoelectric point 8.68 Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antibody
- General Function
- Interleukin-2 receptor activity
- Specific Function
- Receptor for interleukin-2. The receptor is involved in the regulation of immune tolerance by controlling regulatory T cells (TREGs) activity. TREGs suppress the activation and expansion of autorea...
- Gene Name
- IL2RA
- Uniprot ID
- P01589
- Uniprot Name
- Interleukin-2 receptor subunit alpha
- Molecular Weight
- 30818.915 Da
References
- Choy BY, Chan TM, Li FK, Lui SL, Lo WK, Yip T, Tse KC, Lai KN: IL2-receptor antagonist (basiliximab) induction therapy is associated with lower morbidity and mortality in renal transplant recipients. Transplant Proc. 2003 Feb;35(1):195. [Article]
- Kovarik J, Breidenbach T, Gerbeau C, Korn A, Schmidt AG, Nashan B: Disposition and immunodynamics of basiliximab in liver allograft recipients. Clin Pharmacol Ther. 1998 Jul;64(1):66-72. [Article]
- Garcia CD, Bittencourt VB, Tumelero A, Antonello JS, Malheiros D, Garcia VD: Plasmapheresis for recurrent posttransplant focal segmental glomerulosclerosis. Transplant Proc. 2006 Jul-Aug;38(6):1904-5. [Article]
- Berard JL, Velez RL, Freeman RB, Tsunoda SM: A review of interleukin-2 receptor antagonists in solid organ transplantation. Pharmacotherapy. 1999 Oct;19(10):1127-37. [Article]
- Mentre F, Kovarik J, Gerbeau C: Constructing a prediction interval for time to reach a threshold concentration based on a population pharmacokinetic analysis: an application to basiliximab in renal transplantation. J Pharmacokinet Biopharm. 1999 Apr;27(2):213-30. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antibody
- General Function
- Interleukin-2 receptor activity
- Specific Function
- Receptor for interleukin-2. This beta subunit is involved in receptor mediated endocytosis and transduces the mitogenic signals of IL2.
- Gene Name
- IL2RB
- Uniprot ID
- P14784
- Uniprot Name
- Interleukin-2 receptor subunit beta
- Molecular Weight
- 61116.59 Da
References
- Onrust SV, Wiseman LR: Basiliximab. Drugs. 1999 Feb;57(2):207-13; discussion 214. [Article]
- Hausen B, Gummert J, Berry GJ, Christians U, Serkova N, Ikonen T, Hook L, Legay F, Schuler W, Schreier MH, Morris RE: Prevention of acute allograft rejection in nonhuman primate lung transplant recipients: induction with chimeric anti-interleukin-2 receptor monoclonal antibody improves the tolerability and potentiates the immunosuppressive activity of a regimen using low doses of both microemulsion cyclosporine and 40-O-(2-hydroxyethyl)-rapamycin. Transplantation. 2000 Feb 27;69(4):488-96. [Article]
- Schmitz K, Hitzer S, Behrens-Baumann W: [Immune suppression by combination therapy with basiliximab and cyclosporin in high risk keratoplasty. A pilot study]. Ophthalmologe. 2002 Jan;99(1):38-45. [Article]
- Warle MC, Kwekkeboom J, Tilanus HW, Metselaar HJ: Basiliximab interferes with the detection of soluble IL-2 receptor by the Immulite Immunoassay system. J Immunol Methods. 2003 Apr 1;275(1-2):133-6. [Article]
- Emparan C, Laukotter M, Wolters H, Dame C, Heidenreich S, Senninger N: Calcineurin-free protocols with basiliximab induction allow patients included in "old to old" programs achieve standard kidney transplant function. Transplant Proc. 2003 Jun;35(4):1326-7. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Drug created at June 13, 2005 13:24 / Updated at May 22, 2022 04:54