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

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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Drug Discovery

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Associated Conditions

• Kidney Transplant Rejection

Contraindications & Blackbox Warnings

Contraindications & Blackbox Warnings

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Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects

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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.

Target	Actions	Organism
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

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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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Abatacept	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.
Altretamine	The risk or severity of adverse effects can be increased when Basiliximab is combined with Altretamine.

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Food Interactions

No interactions found.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Simulect	Injection, powder, for solution	10 mg	Intravenous	Novartis Europharm Limited	2016-09-08	Not applicable
Simulect	Injection, powder, for solution	10 mg/2.5mL	Intravenous	Novartis Pharmaceuticals Corporation	1998-05-12	Not applicable
Simulect	Injection, powder, for solution	20 mg	Intravenous	Novartis Europharm Limited	2016-09-08	Not applicable
Simulect	Injection, powder, for solution	20 mg/5mL	Intravenous	Novartis Pharmaceuticals Corporation	1998-05-12	Not applicable
Simulect	Powder, for solution	20 mg / vial	Intravenous	Novartis	2000-10-23	Not applicable

Categories

ATC Codes

L04AC02 — Basiliximab

• L04AC — Interleukin inhibitors
• L04A — IMMUNOSUPPRESSANTS
• L04 — IMMUNOSUPPRESSANTS
• L — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

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

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

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	Transplantation, Liver	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
Injection, powder, for solution	Intravenous	10 mg/2.5mL
Injection, powder, for solution	Intravenous	20 MG
Injection, powder, for solution	Intravenous	20 mg/5mL
Injection, powder, for solution	Intravenous; Intravenous bolus
Powder		20 mg/1vial
Powder, for solution	Intravenous	20 mg / vial
Injection, powder, lyophilized, for solution	Intravenous	20 mg
Injection	Intravenous
Injection, powder, lyophilized, for solution	Intravenous

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

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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Details1. Interleukin-2 receptor subunit alpha

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]

Details2. Interleukin-2 receptor subunit beta

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]

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Drug created on June 13, 2005 13:24 / Updated on July 23, 2021 16:03