Basiliximab

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
Db00074
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

Pharmacology
Reduce drug development failure rates
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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.

TargetActionsOrganism
AInterleukin-2 receptor subunit alpha
antibody
Humans
UInterleukin-2 receptor subunit beta
antibody
Humans
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
Adverseeffects
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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.
DrugInteraction
AbataceptThe risk or severity of adverse effects can be increased when Basiliximab is combined with Abatacept.
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Basiliximab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Basiliximab.
Adenovirus type 7 vaccine liveThe risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Basiliximab.
AducanumabThe risk or severity of adverse effects can be increased when Basiliximab is combined with Aducanumab.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Basiliximab.
AlefaceptThe risk or severity of adverse effects can be increased when Basiliximab is combined with Alefacept.
AlemtuzumabThe risk or severity of adverse effects can be increased when Basiliximab is combined with Alemtuzumab.
AlirocumabThe risk or severity of adverse effects can be increased when Basiliximab is combined with Alirocumab.
Allogeneic processed thymus tissueThe therapeutic efficacy of Allogeneic processed thymus tissue can be decreased when used in combination with Basiliximab.
Interactions
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Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
SimulectInjection, powder, for solution20 mg/5mLIntravenousNovartis Pharmaceuticals Corporation1998-05-12Not applicableUS flag
SimulectInjection, powder, for solution10 mgIntravenousNovartis Europharm Limited2016-09-08Not applicableEU flag
SimulectInjection, powder, for solution10 mg/2.5mLIntravenousNovartis Pharmaceuticals Corporation1998-05-12Not applicableUS flag
SimulectInjection, powder, for solution20 mgIntravenousNovartis Europharm Limited2016-09-08Not applicableEU flag
SimulectPowder, for solution20 mg / vialIntravenousNovartis2000-10-23Not applicableCanada flag

Categories

ATC Codes
L04AC02 — Basiliximab
Drug Categories
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
UniProt
P01857
Genbank
J00228
PubChem Substance
46505169
RxNav
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
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentKidney Transplantation1
4CompletedPreventionAdverse Side Effects / Kidney Transplantation1
4CompletedPreventionDisorder Related to Renal Transplantation1
4CompletedPreventionKidney Transplantation3
4CompletedPreventionTransplantation, Liver1
4CompletedTreatmentChronic Kidney Disease (CKD) / End Stage Renal Disease (ESRD) / Hemodialysis Treatment / Kidney Transplantation / Renal Replacement Therapies1
4CompletedTreatmentChronic Renal Diseases1
4CompletedTreatmentCirrhosis of the Liver / Liver Transplant Disorder1
4CompletedTreatmentCytomegalovirus (CMV) Infection / Disorder Related to Renal Transplantation1
4CompletedTreatmentDiabetes Mellitus1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Novartis AG
Dosage Forms
FormRouteStrength
Injection, powder, for solutionIntravenous10 mg
Injection, powder, for solutionIntravenous10 mg/2.5mL
Injection, powder, for solutionIntravenous20 MG
Injection, powder, for solutionIntravenous20 mg/5mL
Injection, powder, for solutionIntravenous; Intravenous bolus20 MG
Powder20 mg/1vial
Powder, for solutionIntravenous20 mg / vial
Injection, powder, lyophilized, for solutionIntravenous20 mg
InjectionIntravenous
Injection, powder, lyophilized, for solutionIntravenous
Prices
Unit descriptionCostUnit
Simulect 20 mg vial2471.6USD vial
Simulect 10 mg vial1883.11USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA2038279No1999-03-092011-03-11Canada flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)61 °C (FAB fragment), 71 °C (whole mAb)Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000)
hydrophobicity-0.473Not Available
isoelectric point8.68Not Available

Targets

Drugtargets2
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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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. 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
  1. Onrust SV, Wiseman LR: Basiliximab. Drugs. 1999 Feb;57(2):207-13; discussion 214. [Article]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Drug created on June 13, 2005 13:24 / Updated on October 22, 2021 23:18