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Identification
NameTositumomab
Accession NumberDB00081  (BIOD00085, BTD00085)
TypeBiotech
GroupsApproved
Description

Murine IgG2a lambda monoclonal antibody against CD20 antigen (2 heavy chains of 451 residues, 2 lambda chains of 220 residues). It is produced in an antibiotic-free culture of mammalian cells. It can be covalently linked to Iodine 131 (a radioactive isotope of iodine).

Protein structureDb00081
Protein chemical formulaC6416H9874N1688O1987S44
Protein average weight143859.7 Da
Sequences
>Mouse-Human chimeric Anti-CD20 Heavy Chain 1
QAYLQQSGAELVRPGASVKMSCKASGYTFTSYNMHWVKQTPRQGLEWIGAIYPGNGDTSY
NQKFKGKATLTVDKSSSTAYMQLSSLTSEDSAVYFCARVVYYSNSYWYFDVWGTGTTVTV
SGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLY
SLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKAEPKSCDKTHTCPPCPAPELLGGPSV
FLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTY
RVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTK
NQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQG
NVFSCSVMHEALHNHYTQKSLSLSPGK
>Mouse-Human chimeric Anti-CD20 Light Chain 1
QIVLSQSPAILSASPGEKVTMTCRASSSVSYMHWYQQKPGSSPKPWIYAPSNLASGVPAR
FSGSGSGTSYSLTISRVEAEDAATYYCQQWSFNPPTFGAGTKLELKRTVAAPSVFIFPPS
DEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTL
SKADYEKHKVYACEVTHQGLSSPVTKSFNR
>Mouse-Human chimeric Anti-CD20 Heavy Chain 2
QAYLQQSGAELVRPGASVKMSCKASGYTFTSYNMHWVKQTPRQGLEWIGAIYPGNGDTSY
NQKFKGKATLTVDKSSSTAYMQLSSLTSEDSAVYFCARVVYYSNSYWYFDVWGTGTTVTV
SGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLY
SLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKAEPKSCDKTHTCPPCPAPELLGGPSV
FLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTY
RVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTK
NQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQG
NVFSCSVMHEALHNHYTQKSLSLSPGK
>Mouse-Human chimeric Anti-CD20 Light Chain 2
QIVLSQSPAILSASPGEKVTMTCRASSSVSYMHWYQQKPGSSPKPWIYAPSNLASGVPAR
FSGSGSGTSYSLTISRVEAEDAATYYCQQWSFNPPTFGAGTKLELKRTVAAPSVFIFPPS
DEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTL
SKADYEKHKVYACEVTHQGLSSPVTKSFNR
Download FASTA Format
Synonyms
Ig gamma-1 chain C region
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Bexxar Therapysolution; kit14 mgintravenousGlaxosmithkline Inc2006-04-102014-07-31Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International Brands
NameCompany
BexxarCorixa Corp
Brand mixturesNot Available
SaltsNot Available
CategoriesNot Available
CAS number192391-48-3
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor treatment of non-Hodgkin's lymphoma (CD20 positive, follicular)
PharmacodynamicsTositumomab binds to the CD20 antigen, which is predominantly expressed on mature B cells and on >90% of B-cell non-Hodgkin's lympohomas. The antibody leads to selective killing of B-cells.
Mechanism of actionBinds to the CD20 antigen which is found on mature B lymphocytes. The antibody binding appears to induce apoptosis, complement-dependent cytotoxicity and cell death through ionizing radiation.
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

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

Route of eliminationElimination of Iodine-131 occurs by decay and excretion in the urine.
Half life0.8 hours (mammalian reticulocytes, in vitro)
Clearance
  • 68.2 mg/hr [patients with NHL]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Solution; kitintravenous14 mg
Prices
Unit descriptionCostUnit
Bexxar 131 iodine dosimetric180.77USD ml
Bexxar 14 mg/ml dosimetric100.43USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point61 °C (FAB fragment), 71 °C (whole mAb)Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000)
hydrophobicity-0.414Not Available
isoelectric point8.68Not Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesNot Available
AHFS Codes
  • 10:00.00
PDB Entries
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Tositumomab.
AcenocoumarolThe risk or severity of adverse effects can be increased when Acenocoumarol is combined with Tositumomab.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Tositumomab.
AnagrelideThe risk or severity of adverse effects can be increased when Anagrelide is combined with Tositumomab.
ApixabanThe risk or severity of adverse effects can be increased when Apixaban is combined with Tositumomab.
ArgatrobanThe risk or severity of adverse effects can be increased when Argatroban is combined with Tositumomab.
BelimumabThe risk or severity of adverse effects can be increased when Tositumomab is combined with Belimumab.
BivalirudinThe risk or severity of adverse effects can be increased when Bivalirudin is combined with Tositumomab.
CaffeineThe risk or severity of adverse effects can be increased when Caffeine is combined with Tositumomab.
CangrelorThe risk or severity of adverse effects can be increased when Cangrelor is combined with Tositumomab.
CilostazolThe risk or severity of adverse effects can be increased when Cilostazol is combined with Tositumomab.
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Tositumomab.
Citric AcidThe risk or severity of adverse effects can be increased when Citric Acid is combined with Tositumomab.
ClopidogrelThe risk or severity of adverse effects can be increased when Clopidogrel is combined with Tositumomab.
ClozapineThe risk or severity of adverse effects can be increased when Tositumomab is combined with Clozapine.
Dabigatran etexilateThe risk or severity of adverse effects can be increased when Dabigatran etexilate is combined with Tositumomab.
DalteparinThe risk or severity of adverse effects can be increased when Dalteparin is combined with Tositumomab.
DanaparoidThe risk or severity of adverse effects can be increased when Danaparoid is combined with Tositumomab.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Tositumomab.
DesirudinThe risk or severity of adverse effects can be increased when Desirudin is combined with Tositumomab.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Tositumomab.
DiclofenacThe risk or severity of adverse effects can be increased when Diclofenac is combined with Tositumomab.
DicoumarolThe risk or severity of adverse effects can be increased when Dicoumarol is combined with Tositumomab.
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Tositumomab.
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Tositumomab.
DipyridamoleThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Tositumomab.
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Tositumomab.
Edetic AcidThe risk or severity of adverse effects can be increased when Edetic Acid is combined with Tositumomab.
EdoxabanThe risk or severity of adverse effects can be increased when Edoxaban is combined with Tositumomab.
EnoxaparinThe risk or severity of adverse effects can be increased when Enoxaparin is combined with Tositumomab.
EptifibatideThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Tositumomab.
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Tositumomab.
Ethyl biscoumacetateThe risk or severity of adverse effects can be increased when Ethyl biscoumacetate is combined with Tositumomab.
EtodolacThe risk or severity of adverse effects can be increased when Etodolac is combined with Tositumomab.
FenoprofenThe risk or severity of adverse effects can be increased when Fenoprofen is combined with Tositumomab.
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Tositumomab.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Tositumomab.
FlurbiprofenThe risk or severity of adverse effects can be increased when Flurbiprofen is combined with Tositumomab.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Tositumomab.
Fondaparinux sodiumThe risk or severity of adverse effects can be increased when Fondaparinux sodium is combined with Tositumomab.
HeparinThe risk or severity of adverse effects can be increased when Heparin is combined with Tositumomab.
IbuprofenThe risk or severity of adverse effects can be increased when Ibuprofen is combined with Tositumomab.
IndomethacinThe risk or severity of adverse effects can be increased when Indomethacin is combined with Tositumomab.
KetoprofenThe risk or severity of adverse effects can be increased when Ketoprofen is combined with Tositumomab.
KetorolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Tositumomab.
LeflunomideThe risk or severity of adverse effects can be increased when Tositumomab is combined with Leflunomide.
LevomilnacipranThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Tositumomab.
Mefenamic acidThe risk or severity of adverse effects can be increased when Mefenamic acid is combined with Tositumomab.
MeloxicamThe risk or severity of adverse effects can be increased when Meloxicam is combined with Tositumomab.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Tositumomab.
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Tositumomab.
NabumetoneThe risk or severity of adverse effects can be increased when Nabumetone is combined with Tositumomab.
NadroparinThe risk or severity of adverse effects can be increased when Nadroparin is combined with Tositumomab.
NaproxenThe risk or severity of adverse effects can be increased when Naproxen is combined with Tositumomab.
NatalizumabThe risk or severity of adverse effects can be increased when Tositumomab is combined with Natalizumab.
OxaprozinThe risk or severity of adverse effects can be increased when Oxaprozin is combined with Tositumomab.
ParoxetineThe risk or severity of adverse effects can be increased when Paroxetine is combined with Tositumomab.
PhenindioneThe risk or severity of adverse effects can be increased when Phenindione is combined with Tositumomab.
PhenprocoumonThe risk or severity of adverse effects can be increased when Phenprocoumon is combined with Tositumomab.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Tositumomab.
PiroxicamThe risk or severity of adverse effects can be increased when Piroxicam is combined with Tositumomab.
PrasugrelThe risk or severity of adverse effects can be increased when Prasugrel is combined with Tositumomab.
RivaroxabanThe risk or severity of adverse effects can be increased when Rivaroxaban is combined with Tositumomab.
RoflumilastRoflumilast may increase the immunosuppressive activities of Tositumomab.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Tositumomab.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Tositumomab.
SulindacThe risk or severity of adverse effects can be increased when Sulindac is combined with Tositumomab.
SulodexideThe risk or severity of adverse effects can be increased when Sulodexide is combined with Tositumomab.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tositumomab.
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Tiaprofenic acid is combined with Tositumomab.
TicagrelorThe risk or severity of adverse effects can be increased when Ticagrelor is combined with Tositumomab.
TiclopidineThe risk or severity of adverse effects can be increased when Ticlopidine is combined with Tositumomab.
TinzaparinThe risk or severity of adverse effects can be increased when Tinzaparin is combined with Tositumomab.
TirofibanThe risk or severity of adverse effects can be increased when Tirofiban is combined with Tositumomab.
TofacitinibTositumomab may increase the immunosuppressive activities of Tofacitinib.
TolmetinThe risk or severity of adverse effects can be increased when Tolmetin is combined with Tositumomab.
TrastuzumabTrastuzumab may increase the neutropenic activities of Tositumomab.
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Tositumomab.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Tositumomab.
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Tositumomab.
VorapaxarThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Tositumomab.
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Tositumomab.
WarfarinThe risk or severity of adverse effects can be increased when Warfarin is combined with Tositumomab.
Food InteractionsNot Available

Targets

1. B-lymphocyte antigen CD20

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: antibody

Components

Name UniProt ID Details
B-lymphocyte antigen CD20 P11836 Details

References:

  1. 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
  2. Dillman RO: Monoclonal antibody therapy for lymphoma: an update. Cancer Pract. 2001 Mar-Apr;9(2):71-80. Pubmed
  3. Iodine-131 Tositumomab: (131)I-anti-B1 antibody, (131)I-tositumomab, anti-CD20 murine monoclonal antibody-I-131, B1, Bexxar, (131)I-anti-B1 antibody, iodine-131 tositumomab, iodine-131 anti-B1 antibody, tositumomab. BioDrugs. 2003;17(4):290-5. Pubmed
  4. Friedberg JW, Fisher RI: Iodine-131 tositumomab (Bexxar): radioimmunoconjugate therapy for indolent and transformed B-cell non-Hodgkin’s lymphoma. Expert Rev Anticancer Ther. 2004 Feb;4(1):18-26. Pubmed
  5. Silverman DH, Delpassand ES, Torabi F, Goy A, McLaughlin P, Murray JL: Radiolabeled antibody therapy in non-Hodgkins lymphoma: radiation protection, isotope comparisons and quality of life issues. Cancer Treat Rev. 2004 Apr;30(2):165-72. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  7. Beeson C, Butrynski JE, Hart MJ, Nourigat C, Matthews DC, Press OW, Senter PD, Bernstein ID: Conditionally cleavable radioimmunoconjugates: a novel approach for the release of radioisotopes from radioimmunoconjugates. Bioconjug Chem. 2003 Sep-Oct;14(5):927-33. Pubmed

2. Low affinity immunoglobulin gamma Fc region receptor III-B

Kind: Protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Low affinity immunoglobulin gamma Fc region receptor III-B O75015 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

3. Complement C1r subcomponent

Kind: Protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Complement C1r subcomponent P00736 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

4. Complement C1q subcomponent subunit A

Kind: Protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Complement C1q subcomponent subunit A P02745 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

5. Complement C1q subcomponent subunit B

Kind: Protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Complement C1q subcomponent subunit B P02746 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

6. Complement C1q subcomponent subunit C

Kind: Protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Complement C1q subcomponent subunit C P02747 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

7. Low affinity immunoglobulin gamma Fc region receptor III-A

Kind: Protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Low affinity immunoglobulin gamma Fc region receptor III-A P08637 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

8. High affinity immunoglobulin gamma Fc receptor I

Kind: Protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
High affinity immunoglobulin gamma Fc receptor I P12314 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

9. Low affinity immunoglobulin gamma Fc region receptor II-a

Kind: Protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Low affinity immunoglobulin gamma Fc region receptor II-a P12318 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

10. Low affinity immunoglobulin gamma Fc region receptor II-b

Kind: Protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Low affinity immunoglobulin gamma Fc region receptor II-b P31994 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

11. Low affinity immunoglobulin gamma Fc region receptor II-c

Kind: Protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Low affinity immunoglobulin gamma Fc region receptor II-c P31995 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

Comments
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Drug created on June 13, 2005 07:24 / Updated on September 29, 2010 14:34