Ibritumomab tiuxetan

Identification

Name
Ibritumomab tiuxetan
Accession Number
DB00078  (BTD00069, BIOD00069)
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Description

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.

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
  • mAb Murine (IGG1) Anti P19437 (CD20_MOUSE)
External IDs
IDEC-129 / IDEC-Y2B8
Product Ingredients
IngredientUNIICASInChI Key
Indium In-111 ibritumomab tiuxetanS9U4ZR2W8VNot AvailableNot applicable
Yttrium y-90 ibritumomab tiuxetanQA846JAV5BNot AvailableNot applicable
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Zevalin1.6 mg/1mLIntravenousAcrotech Biopharma Llc2002-02-19Not applicableUs
ZevalinKit1.6 mg/1mLIntravenousSpectrum Pharmaceuticals, Inc.2002-02-19Not applicableUs
ZevalinKit1.6 mg/1mLIntravenousSpectrum Pharmaceuticals, Inc.2002-02-192009-06-30Us
ZevalinKit1.6 mg/mlIntravenousSpectrum Pharmaceuticals B.V.2004-01-16Not applicableEu
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories
UNII
4Q52C550XK
CAS number
206181-63-7

Pharmacology

Indication

For treatment of non-Hodgkin's lymphoma

Associated Conditions
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
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

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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.

Toxicity
Not Available
Affected organisms
  • Humans and other mammals
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
(R)-warfarinThe risk or severity of adverse effects can be increased when (R)-warfarin is combined with Ibritumomab tiuxetan.
(S)-WarfarinThe risk or severity of adverse effects can be increased when (S)-Warfarin is combined with Ibritumomab tiuxetan.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with 2-Methoxyethanol.
4-hydroxycoumarinThe risk or severity of adverse effects can be increased when 4-hydroxycoumarin is combined with Ibritumomab tiuxetan.
9-(N-methyl-L-isoleucine)-cyclosporin AThe risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
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.
AbetimusThe risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Abetimus.
AbituzumabThe risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Abituzumab.
AbrilumabThe risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Abrilumab.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

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Food Interactions
Not Available

References

General References
  1. Link [Link]
External Links
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
ATC Codes
V10XX02 — Ibritumomab tiuxetan (90y)
FDA label
Download (102 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentBlood and Marrow Transplant (BMT) / Non-Hodgkin's Lymphoma (NHL)1
1CompletedTreatmentMalignant Lymphomas1
1CompletedTreatmentMultiple Myeloma and Plasma Cell Neoplasm1
1, 2CompletedTreatmentLeukemias / Malignant Lymphomas1
1, 2CompletedTreatmentLymphoma, B-Cell1
1, 2CompletedTreatmentMalignant Lymphomas1
1, 2CompletedTreatmentPost Transplant Lymphoproliferative Disorder / Recurrent Adult Burkitt Lymphoma / Recurrent Adult Diffuse Large Cell Lymphoma / Stage III Adult Burkitt Lymphoma / Stage III Adult Diffuse Large Cell Lymphoma / Stage IV Adult Burkitt Lymphoma / Stage IV Adult Diffuse Large Cell Lymphoma / Waldenström's Macroglobulinemia (WM)1
1, 2TerminatedTreatmentExtranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue / Nodal marginal zone B-cell lymphomas / Recurrent Grade 1 Follicular Lymphoma / Recurrent Grade 2 Follicular Lymphoma / Recurrent Grade 3 Follicular Lymphoma / Recurrent Marginal Zone Lymphoma / Recurrent Small Lymphocytic Lymphoma / Splenic Marginal Zone Lymphoma / Waldenström's Macroglobulinemia (WM)1
1, 2TerminatedTreatmentMalignant Lymphomas1
1, 2TerminatedTreatmentNon-Hodgkin's Lymphoma (NHL)1
1, 2Unknown StatusTreatmentNon-Hodgkin's Lymphoma (NHL)1
2Active Not RecruitingTreatmentMalignant Lymphomas2
2CompletedTreatmentCD20+ Aggressive Non-Hodgkin's Lymphoma / Primary Non-Hodgkin-Lymphoma / Refractory Non-Hodgkin's lymphoma1
2CompletedTreatmentDiffuse Large Cell Lymphoma / Malignant Lymphomas1
2CompletedTreatmentFollicular Lymphoma (FL)3
2CompletedTreatmentLeukemias / Malignant Lymphomas1
2CompletedTreatmentLymphoma, B-Cell1
2CompletedTreatmentLymphoma, B-Cell / Lymphoma, Low-Grade / Non-Hodgkin's Lymphoma (NHL)1
2CompletedTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL)3
2CompletedTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL) / Mantle Cell Lymphoma (MCL)1
2CompletedTreatmentLymphoma, Large Cell, Diffuse1
2CompletedTreatmentMalignant Lymphomas5
2CompletedTreatmentMantle Cell Lymphoma (MCL)4
2CompletedTreatmentMarginal Zone Lymphoma (MZL)1
2CompletedTreatmentMultiple Myeloma (MM)1
2CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)5
2RecruitingTreatmentRefractory Non-Hodgkin's lymphoma / Relapsed Non Hodgkin Lymphoma1
2TerminatedTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL)1
2TerminatedTreatmentMalignant Lymphomas2
2TerminatedTreatmentMantle Cell Lymphoma (MCL)1
2TerminatedTreatmentNon-Hodgkin's Lymphoma (NHL)3
2TerminatedTreatmentPrimary Central Nervous System Non-Hodgkin Lymphoma1
2Unknown StatusTreatmentFollicular Lymphoma (FL)2
2Unknown StatusTreatmentNon-Hodgkin's Lymphoma (NHL)1
2WithdrawnTreatmentAdult Non-Hodgkin's Lymphoma / Anaplastic Large Cell Lymphoma / Anaplastic Large-Cell Lymphoma / Lymphoma, AIDS Related1
2WithdrawnTreatmentMalignant Lymphomas1
3Active Not RecruitingTreatmentFollicular Non-Hodgkin's Lymphoma1
3CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)2
3TerminatedTreatmentFollicle Center Lymphoma / Lymphoma, Large B-Cell, Diffuse (DLBCL)1
3TerminatedTreatmentFollicular Lymphoma (FL)2
3TerminatedTreatmentNon-Hodgkin's Lymphoma (NHL)1
3Unknown StatusTreatmentLymphoma, Large Cell, Diffuse1
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
4CompletedTreatmentLymphoma, Low-Grade / Non-Hodgkin's Lymphoma (NHL)1
Not AvailableCompletedNot AvailableFollicular Lymphoma (FL) / Non-Hodgkin's Lymphoma (NHL)1
Not AvailableCompletedNot AvailableNon-Hodgkin's Lymphoma (NHL)1
Not AvailableCompletedTreatmentMalignant Lymphomas / Non-Hodgkin's Lymphoma (NHL)1
Not AvailableRecruitingNot AvailableNon-Hodgkin's Lymphoma (NHL)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Spectrum Pharmaceuticals
Dosage forms
FormRouteStrength
KitIntravenous1.6 mg/1mL
KitIntravenous1.6 mg/ml
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)
CA2149329No2008-07-152013-11-12Canada
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

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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

Taxonomy

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

Targets

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. [PubMed:10541376]
  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. [PubMed:11418316]
  3. Dillman RO: Monoclonal antibody therapy for lymphoma: an update. Cancer Pract. 2001 Mar-Apr;9(2):71-80. [PubMed:11879282]
  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. [PubMed:12011122]
  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. [PubMed:15045033]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  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. [PubMed:20113680]

Drug created on June 13, 2005 07:24 / Updated on May 26, 2020 02:54

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