Ibritumomab tiuxetan

Identification

Summary

Ibritumomab tiuxetan is a monoclonal anti-CD20 antibody used to treat B-cell non-Hodgkin's lymphoma via a conjugated radioactive isotope.

Brand Names
Zevalin
Generic Name
Ibritumomab tiuxetan
DrugBank Accession Number
DB00078
Background

Indium or yttrium conjugated murine IgG1 kappa monoclonal antibody directed against the CD20 antigen, which is found on the surface of normal and malignant B lymphocytes. Ibritumomab is produced in Chinese hamster ovary cells and is composed of two murine gamma 1 heavy chains of 445 amino acids each and two kappa light chains of 213 amino acids each.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Protein Structure
Db00078
Protein Chemical Formula
C6382H9830N1672O1979S54
Protein Average Weight
143375.5 Da
Sequences
>Ibritumomab tiuxetan heavy chain
QAYLQQSGAELVRPGASVKMSCKASGYTFTSYNMHWVKQTPRQGLEWIGAIYPGNGDTSY
NQKFKGKATLTVDKSSSTAYMQLSSLTSEDSAVYFCARVVYYSNSYWYFDVWGTGTTVTV
SAPSVYPLAPVCGDTTGSSVTLGCLVKGYFPEPVTLTWNSGSLSSGVHTFPAVLQSDLYT
LSSSVTVTSSTWPSQSITCNVAHPASSTKVDKKIEPRGPTIKPCPPCKCPAPNLLGGPSV
FIFPPKIKDVLMISLSPIVTCVVVDVSEDDPDVQISWFVNNVEVHTAQTQTHREDYNSTL
RVVSALPIQHQDWMSGKEFKCKVNNKDLPAPIERTISKPKGSVRAPQVYVLPPPEEEMTK
KQVTLTCMVTDFMPEDIYVEWTNNGKTELNYKNTEPVLDSDGSYFMYSKLRVEKKNWVER
NSYSCSVVHEGLHNHHTTKSFSR
>Ibritumomab tiuxetan light chain
QIVLSQSPAILSASPGEKVTMTCRASSSVSYMHWYQQKPGSSPKPWIYAPSNLASGVPAR
FSGSGSGTSYSLTISRVEAEDAATYYCQQWSFNPPTFGAGTKLELKRADAAPTVFIFPPS
DEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTL
SKADYEKHKVYACEVTHQGLSSPVTKSFN
Download FASTA Format
Synonyms
  • Ibritumomab
  • Ibritumomab tiuxetan
  • mAb Murine (IGG1) Anti P19437 (CD20_MOUSE)
External IDs
  • IDEC-129
  • IDEC-Y2B8

Pharmacology

Indication

For treatment of non-Hodgkin's lymphoma

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Ibritumomab is a murine monoclonal antibody against CD20 that has been radiolabeled with yttrium-90.

Mechanism of action

The Fab segment of the antibody targets the CD20 epitope on B-cells, allowing the radioactive yttrium to destroy the cell via production of beta particles.

TargetActionsOrganism
AB-lymphocyte antigen CD20
antibody
Humans
Absorption

Not Available

Volume of distribution

Binding observed on lymphoid cells of the bone marrow, lymph node, thymus, red and white pulp of the spleen, lymphoid follicles of the tonsil, and lymphoid nodules of other organs (e.g., large and small intestines)

Protein binding

Not Available

Metabolism

Most likely removed by opsonization via the reticuloendothelial system when bound to B cells, or by human antimurine antibody production

Route of elimination

Not Available

Half-life

0.8 hours (mammalian reticulocytes, in vitro)

Clearance

Approximately 7.2% of injected dose of yttrium Y 90 ibritumomab tiuxetan is excreted in urine within 7 days.

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 Ibritumomab tiuxetan is combined with Abatacept.
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Ibritumomab tiuxetan.
AcenocoumarolThe risk or severity of adverse effects can be increased when Acenocoumarol is combined with Ibritumomab tiuxetan.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Ibritumomab tiuxetan.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Ibritumomab tiuxetan.
Adenovirus type 7 vaccine liveThe risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Ibritumomab tiuxetan.
AducanumabThe risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Aducanumab.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Ibritumomab tiuxetan.
AlefaceptThe risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Alefacept.
AlemtuzumabThe risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Alemtuzumab.
Interactions
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Food Interactions
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Individuals taking these herbs/supplements while taking ibritumomab tiuxetan should be monitored for thrombocytopenia more frequently. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Products

Products2
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Product Ingredients
IngredientUNIICASInChI Key
Indium In-111 ibritumomab tiuxetanS9U4ZR2W8VNot AvailableNot applicable
Yttrium y-90 ibritumomab tiuxetanQA846JAV5BNot AvailableNot applicable
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ZevalinKit1.6 mg/mlIntravenousCeft Biopharma S.R.O.2016-09-08Not applicableEU flag
ZevalinKit1.6 mg/1mLIntravenousSpectrum Pharmaceuticals, Inc.2002-02-192009-06-30US flag
ZevalinKit1.6 mg/1mLIntravenousAcrotech Biopharma Llc2002-02-19Not applicableUS flag
ZevalinKit1.6 mg/1mLIntravenousSpectrum Pharmaceuticals, Inc.2002-02-19Not applicableUS flag

Categories

ATC Codes
V10XX02 — Ibritumomab tiuxetan (90y)
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
4Q52C550XK
CAS number
206181-63-7

References

General References
  1. Link [Link]
UniProt
P01865
Genbank
J00470
PubChem Substance
46506112
RxNav
262323
Therapeutic Targets Database
DAP000383
PharmGKB
PA164781375
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Ibritumomab_tiuxetan
FDA label
Download (102 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentLow Grade Lymphoma / Non-Hodgkin's Lymphoma (NHL)1
3Active Not RecruitingTreatmentNon-Hodgkin's Lymphoma, Lymphoma, Follicular1
3CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)2
3TerminatedTreatmentDiffuse Large B-Cell Lymphoma (DLBCL) / Follicle Center Lymphoma1
3TerminatedTreatmentFollicular Lymphoma ( FL)2
3TerminatedTreatmentNon-Hodgkin's Lymphoma (NHL)1
3Unknown StatusTreatmentDiffuse Large Cell Diffuse Lymphoma1
3Unknown StatusTreatmentNon-Hodgkin's Lymphoma (NHL)1
3WithdrawnTreatmentFollicular Lymphoma ( FL) / Lymphoma, Large-Cell, Follicular / Lymphoma, Small Cleaved-Cell, Follicular / Non-Hodgkin's Lymphoma (NHL)1
2Active Not RecruitingTreatmentMalignant Lymphomas1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Spectrum Pharmaceuticals
Dosage Forms
FormRouteStrength
InjectionIntravenous; Parenteral1.6 MG/ML
KitIntravenous1.6 mg/ml
KitIntravenous1.6 mg/1mL
SolutionIntravenous3.2 mg
Prices
Unit descriptionCostUnit
Zevalin y-90 kit37800.0USD kit
Zevalin in-111 kit4200.0USD kit
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA2149329No2008-07-152013-11-12Canada 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-0.359Not Available
isoelectric point7.91Not Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antibody
General Function
Mhc class ii protein complex binding
Specific Function
This protein may be involved in the regulation of B-cell activation and proliferation.
Gene Name
MS4A1
Uniprot ID
P11836
Uniprot Name
B-lymphocyte antigen CD20
Molecular Weight
33076.99 Da
References
  1. Wiseman GA, White CA, Witzig TE, Gordon LI, Emmanouilides C, Raubitschek A, Janakiraman N, Gutheil J, Schilder RJ, Spies S, Silverman DH, Grillo-Lopez AJ: Radioimmunotherapy of relapsed non-Hodgkin's lymphoma with zevalin, a 90Y-labeled anti-CD20 monoclonal antibody. Clin Cancer Res. 1999 Oct;5(10 Suppl):3281s-3286s. [Article]
  2. Goldenberg DM: The role of radiolabeled antibodies in the treatment of non-Hodgkin's lymphoma: the coming of age of radioimmunotherapy. Crit Rev Oncol Hematol. 2001 Jul-Aug;39(1-2):195-201. [Article]
  3. Dillman RO: Monoclonal antibody therapy for lymphoma: an update. Cancer Pract. 2001 Mar-Apr;9(2):71-80. [Article]
  4. Witzig TE, Gordon LI, Cabanillas F, Czuczman MS, Emmanouilides C, Joyce R, Pohlman BL, Bartlett NL, Wiseman GA, Padre N, Grillo-Lopez AJ, Multani P, White CA: Randomized controlled trial of yttrium-90-labeled ibritumomab tiuxetan radioimmunotherapy versus rituximab immunotherapy for patients with relapsed or refractory low-grade, follicular, or transformed B-cell non-Hodgkin's lymphoma. J Clin Oncol. 2002 May 15;20(10):2453-63. [Article]
  5. Witzig TE: Yttrium-90-ibritumomab tiuxetan radioimmunotherapy: a new treatment approach for B-cell non-Hodgkin's lymphoma. Drugs Today (Barc). 2004 Feb;40(2):111-9. [Article]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  7. Goldsmith SJ: Radioimmunotherapy of lymphoma: Bexxar and Zevalin. Semin Nucl Med. 2010 Mar;40(2):122-35. doi: 10.1053/j.semnuclmed.2009.11.002. [Article]

Drug created on June 13, 2005 13:24 / Updated on August 07, 2021 00:17