Identification

Name
Tositumomab
Accession Number
DB00081  (BTD00085, BIOD00085, DB09557)
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
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 structure
Db00081
Protein chemical formula
C6416H9874N1688O1987S44
Protein average weight
143859.7 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
Not Available
Product Ingredients
IngredientUNIICASInChI Key
Tositumomab I-131K1KT5M40JC192391-48-3Not applicable
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Bexxar TherapyKit; Solution14 mgIntravenousGlaxosmithkline Inc2006-04-102014-07-31Canada
International/Other Brands
Bexxar (Corixa Corp)
Categories
UNII
0343IGH41U
CAS number
208921-02-2

Pharmacology

Indication

For treatment of non-Hodgkin's lymphoma (CD20 positive, follicular)

Structured Indications
Not Available
Pharmacodynamics

Tositumomab 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 action

Binds 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.

TargetActionsOrganism
AB-lymphocyte antigen CD20
antibody
Human
ULow affinity immunoglobulin gamma Fc region receptor III-BNot AvailableHuman
UComplement C1r subcomponentNot AvailableHuman
UComplement C1q subcomponent subunit ANot AvailableHuman
UComplement C1q subcomponent subunit BNot AvailableHuman
UComplement C1q subcomponent subunit CNot AvailableHuman
ULow affinity immunoglobulin gamma Fc region receptor III-ANot AvailableHuman
UHigh affinity immunoglobulin gamma Fc receptor INot AvailableHuman
ULow affinity immunoglobulin gamma Fc region receptor II-aNot AvailableHuman
ULow affinity immunoglobulin gamma Fc region receptor II-bNot AvailableHuman
ULow affinity immunoglobulin gamma Fc region receptor II-cNot AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

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

Route of elimination

Elimination of Iodine-131 occurs by decay and excretion in the urine.

Half life

0.8 hours (mammalian reticulocytes, in vitro)

Clearance
  • 68.2 mg/hr [patients with NHL]
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Tositumomab.Approved
AcenocoumarolThe risk or severity of adverse effects can be increased when Acenocoumarol is combined with Tositumomab.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Tositumomab.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Tositumomab.Experimental
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Tositumomab.Approved, Vet Approved
AlprostadilThe risk or severity of adverse effects can be increased when Alprostadil is combined with Tositumomab.Approved, Investigational
AnagrelideThe risk or severity of adverse effects can be increased when Anagrelide is combined with Tositumomab.Approved
AncrodThe risk or severity of adverse effects can be increased when Ancrod is combined with Tositumomab.Investigational
AndrographolideThe risk or severity of adverse effects can be increased when Andrographolide is combined with Tositumomab.Investigational
Antithrombin III humanThe risk or severity of adverse effects can be increased when Antithrombin III human is combined with Tositumomab.Approved
ApixabanThe risk or severity of adverse effects can be increased when Apixaban is combined with Tositumomab.Approved
ArdeparinThe risk or severity of adverse effects can be increased when Ardeparin is combined with Tositumomab.Approved, Investigational, Withdrawn
ArgatrobanThe risk or severity of adverse effects can be increased when Argatroban is combined with Tositumomab.Approved, Investigational
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Tositumomab.Approved
BCG vaccineThe therapeutic efficacy of BCG vaccine can be decreased when used in combination with Tositumomab.Investigational
BecaplerminThe risk or severity of adverse effects can be increased when Becaplermin is combined with Tositumomab.Approved, Investigational
BeraprostThe risk or severity of adverse effects can be increased when Beraprost is combined with Tositumomab.Investigational
BevacizumabBevacizumab may increase the cardiotoxic activities of Tositumomab.Approved, Investigational
BivalirudinThe risk or severity of adverse effects can be increased when Bivalirudin is combined with Tositumomab.Approved, Investigational
BuflomedilThe risk or severity of adverse effects can be increased when Buflomedil is combined with Tositumomab.Experimental
ButylphthalideThe risk or severity of adverse effects can be increased when Butylphthalide is combined with Tositumomab.Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Tositumomab.Approved
CangrelorThe risk or severity of adverse effects can be increased when Cangrelor is combined with Tositumomab.Approved
CertoparinThe risk or severity of adverse effects can be increased when Certoparin is combined with Tositumomab.Approved, Investigational
CilostazolThe risk or severity of adverse effects can be increased when Cilostazol is combined with Tositumomab.Approved
Citric AcidThe risk or severity of adverse effects can be increased when Citric Acid is combined with Tositumomab.Approved, Nutraceutical, Vet Approved
ClopidogrelThe risk or severity of adverse effects can be increased when Clopidogrel is combined with Tositumomab.Approved, Nutraceutical
CloricromenThe risk or severity of adverse effects can be increased when Cloricromen is combined with Tositumomab.Experimental
Clostridium tetani toxoid antigen (formaldehyde inactivated)The therapeutic efficacy of Clostridium tetani toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Tositumomab.Approved
ClozapineThe risk or severity of adverse effects can be increased when Tositumomab is combined with Clozapine.Approved
Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)The therapeutic efficacy of Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Tositumomab.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Tositumomab.Approved, Investigational
CymarinCymarin may decrease the cardiotoxic activities of Tositumomab.Experimental
Dabigatran etexilateThe risk or severity of adverse effects can be increased when Dabigatran etexilate is combined with Tositumomab.Approved
DalteparinThe risk or severity of adverse effects can be increased when Dalteparin is combined with Tositumomab.Approved
DanaparoidThe risk or severity of adverse effects can be increased when Danaparoid is combined with Tositumomab.Approved, Withdrawn
DarexabanThe risk or severity of adverse effects can be increased when Darexaban is combined with Tositumomab.Investigational
DefibrotideThe risk or severity of adverse effects can be increased when Defibrotide is combined with Tositumomab.Approved, Investigational
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Tositumomab.Approved
DesirudinThe risk or severity of adverse effects can be increased when Desirudin is combined with Tositumomab.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Tositumomab.Approved
DextranThe risk or severity of adverse effects can be increased when Dextran is combined with Tositumomab.Approved, Vet Approved
Dextran 40The risk or severity of adverse effects can be increased when Dextran 40 is combined with Tositumomab.Approved
Dextran 70The risk or severity of adverse effects can be increased when Dextran 70 is combined with Tositumomab.Approved
Dextran 75The risk or severity of adverse effects can be increased when Dextran 75 is combined with Tositumomab.Approved
DicoumarolThe risk or severity of adverse effects can be increased when Dicoumarol is combined with Tositumomab.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Tositumomab.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Tositumomab.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Tositumomab.Approved
DipyridamoleThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Tositumomab.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Tositumomab.Approved, Investigational
Edetic AcidThe risk or severity of adverse effects can be increased when Edetic Acid is combined with Tositumomab.Approved, Vet Approved
EdoxabanThe risk or severity of adverse effects can be increased when Edoxaban is combined with Tositumomab.Approved
EnoxaparinThe risk or severity of adverse effects can be increased when Enoxaparin is combined with Tositumomab.Approved
EpinastineThe risk or severity of adverse effects can be increased when Epinastine is combined with Tositumomab.Approved, Investigational
EplivanserinThe risk or severity of adverse effects can be increased when Eplivanserin is combined with Tositumomab.Investigational
eplivanserineThe risk or severity of adverse effects can be increased when eplivanserine is combined with Tositumomab.Investigational
EpoprostenolThe risk or severity of adverse effects can be increased when Epoprostenol is combined with Tositumomab.Approved
EptifibatideThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Tositumomab.Approved, Investigational
Ethyl biscoumacetateThe risk or severity of adverse effects can be increased when Ethyl biscoumacetate is combined with Tositumomab.Withdrawn
Ferulic acidThe risk or severity of adverse effects can be increased when Ferulic acid is combined with Tositumomab.Experimental
FingolimodTositumomab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FluindioneThe risk or severity of adverse effects can be increased when Fluindione is combined with Tositumomab.Investigational
FondaparinuxThe risk or severity of adverse effects can be increased when Fondaparinux is combined with Tositumomab.Investigational
Fondaparinux sodiumThe risk or severity of adverse effects can be increased when Fondaparinux sodium is combined with Tositumomab.Approved, Investigational
G17DTThe therapeutic efficacy of G17DT can be decreased when used in combination with Tositumomab.Investigational
GabexateThe risk or severity of adverse effects can be increased when Gabexate is combined with Tositumomab.Investigational
GI-5005The therapeutic efficacy of GI-5005 can be decreased when used in combination with Tositumomab.Investigational
GitoformateGitoformate may decrease the cardiotoxic activities of Tositumomab.Experimental
HeparinThe risk or severity of adverse effects can be increased when Heparin is combined with Tositumomab.Approved, Investigational
Hepatitis A VaccineThe therapeutic efficacy of Hepatitis A Vaccine can be decreased when used in combination with Tositumomab.Approved
Hepatitis B Vaccine (Recombinant)The therapeutic efficacy of Hepatitis B Vaccine (Recombinant) can be decreased when used in combination with Tositumomab.Approved, Withdrawn
HydroxytyrosolThe risk or severity of adverse effects can be increased when Hydroxytyrosol is combined with Tositumomab.Investigational
IbudilastThe risk or severity of adverse effects can be increased when Ibudilast is combined with Tositumomab.Approved, Investigational
Icosapent ethylThe risk or severity of adverse effects can be increased when Icosapent ethyl is combined with Tositumomab.Approved, Nutraceutical
IdraparinuxThe risk or severity of adverse effects can be increased when Idraparinux is combined with Tositumomab.Investigational
IfenprodilThe risk or severity of adverse effects can be increased when Ifenprodil is combined with Tositumomab.Approved, Investigational, Withdrawn
IfetrobanThe risk or severity of adverse effects can be increased when Ifetroban is combined with Tositumomab.Investigational
IloprostThe risk or severity of adverse effects can be increased when Iloprost is combined with Tositumomab.Approved, Investigational
IndobufenThe risk or severity of adverse effects can be increased when Indobufen is combined with Tositumomab.Investigational
INGN 201The therapeutic efficacy of INGN 201 can be decreased when used in combination with Tositumomab.Investigational
INGN 225The therapeutic efficacy of INGN 225 can be decreased when used in combination with Tositumomab.Investigational
KetanserinThe risk or severity of adverse effects can be increased when Ketanserin is combined with Tositumomab.Investigational
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Tositumomab.Experimental
LeflunomideThe risk or severity of adverse effects can be increased when Tositumomab is combined with Leflunomide.Approved, Investigational
LepirudinThe risk or severity of adverse effects can be increased when Lepirudin is combined with Tositumomab.Approved
LetaxabanThe risk or severity of adverse effects can be increased when Letaxaban is combined with Tositumomab.Investigational
LinsidomineThe risk or severity of adverse effects can be increased when Linsidomine is combined with Tositumomab.Experimental
MelagatranThe risk or severity of adverse effects can be increased when Melagatran is combined with Tositumomab.Experimental
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Tositumomab.Investigational, Withdrawn
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Tositumomab.Experimental
MilrinoneThe risk or severity of adverse effects can be increased when Milrinone is combined with Tositumomab.Approved
NadroparinThe risk or severity of adverse effects can be increased when Nadroparin is combined with Tositumomab.Approved
NafamostatThe risk or severity of adverse effects can be increased when Nafamostat is combined with Tositumomab.Approved, Investigational
NaftopidilThe risk or severity of adverse effects can be increased when Naftopidil is combined with Tositumomab.Investigational
NatalizumabThe risk or severity of adverse effects can be increased when Tositumomab is combined with Natalizumab.Approved, Investigational
NimesulideThe risk or severity of adverse effects can be increased when Nimesulide is combined with Tositumomab.Approved, Investigational, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Nitroaspirin is combined with Tositumomab.Investigational
OleandrinOleandrin may decrease the cardiotoxic activities of Tositumomab.Experimental, Investigational
OtamixabanThe risk or severity of adverse effects can be increased when Otamixaban is combined with Tositumomab.Investigational
OuabainOuabain may decrease the cardiotoxic activities of Tositumomab.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Tositumomab.Approved, Vet Approved
Pentaerythritol TetranitrateThe risk or severity of adverse effects can be increased when Pentaerythritol Tetranitrate is combined with Tositumomab.Approved
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Tositumomab.Approved
PentoxifyllineThe risk or severity of adverse effects can be increased when Pentoxifylline is combined with Tositumomab.Approved, Investigational
PeruvosidePeruvoside may decrease the cardiotoxic activities of Tositumomab.Experimental
PhenindioneThe risk or severity of adverse effects can be increased when Phenindione is combined with Tositumomab.Approved, Investigational
PhenprocoumonThe risk or severity of adverse effects can be increased when Phenprocoumon is combined with Tositumomab.Approved, Investigational
PicotamideThe risk or severity of adverse effects can be increased when Picotamide is combined with Tositumomab.Experimental
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Tositumomab.Approved, Investigational
PrasugrelThe risk or severity of adverse effects can be increased when Prasugrel is combined with Tositumomab.Approved
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Tositumomab.Experimental
Protein CThe risk or severity of adverse effects can be increased when Protein C is combined with Tositumomab.Approved
Protein S humanThe risk or severity of adverse effects can be increased when Protein S human is combined with Tositumomab.Approved
ProtocatechualdehydeThe risk or severity of adverse effects can be increased when Protocatechualdehyde is combined with Tositumomab.Approved
Rabies virus inactivated antigen, AThe therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Tositumomab.Approved
RamatrobanThe risk or severity of adverse effects can be increased when Ramatroban is combined with Tositumomab.Investigational
ResveratrolThe risk or severity of adverse effects can be increased when Resveratrol is combined with Tositumomab.Approved, Experimental, Investigational
ReviparinThe risk or severity of adverse effects can be increased when Reviparin is combined with Tositumomab.Approved, Investigational
RidogrelThe risk or severity of adverse effects can be increased when Ridogrel is combined with Tositumomab.Approved
RindopepimutThe therapeutic efficacy of Rindopepimut can be decreased when used in combination with Tositumomab.Investigational
RivaroxabanThe risk or severity of adverse effects can be increased when Rivaroxaban is combined with Tositumomab.Approved
RoflumilastRoflumilast may increase the immunosuppressive activities of Tositumomab.Approved
Rotavirus VaccineThe therapeutic efficacy of Rotavirus Vaccine can be decreased when used in combination with Tositumomab.Approved
Rubella virus vaccineThe therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Tositumomab.Approved
Salmonella typhi ty21a live antigenThe therapeutic efficacy of Salmonella typhi ty21a live antigen can be decreased when used in combination with Tositumomab.Approved
SarpogrelateThe risk or severity of adverse effects can be increased when Sarpogrelate is combined with Tositumomab.Investigational
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Tositumomab.Approved, Vet Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Tositumomab.Approved
SRP 299The therapeutic efficacy of SRP 299 can be decreased when used in combination with Tositumomab.Investigational
SRT501The risk or severity of adverse effects can be increased when SRT501 is combined with Tositumomab.Investigational
SulodexideThe risk or severity of adverse effects can be increased when Sulodexide is combined with Tositumomab.Approved, Investigational
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tositumomab.Approved, Investigational
TecemotideThe therapeutic efficacy of Tecemotide can be decreased when used in combination with Tositumomab.Investigational
TesmilifeneThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Tositumomab.Investigational
TG4010The therapeutic efficacy of TG4010 can be decreased when used in combination with Tositumomab.Investigational
TicagrelorThe risk or severity of adverse effects can be increased when Ticagrelor is combined with Tositumomab.Approved
TiclopidineThe risk or severity of adverse effects can be increased when Ticlopidine is combined with Tositumomab.Approved
TirofibanThe risk or severity of adverse effects can be increased when Tirofiban is combined with Tositumomab.Approved
TofacitinibTositumomab may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TranilastThe risk or severity of adverse effects can be increased when Tranilast is combined with Tositumomab.Approved, Investigational
TrapidilThe risk or severity of adverse effects can be increased when Trapidil is combined with Tositumomab.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Tositumomab.Approved, Investigational
TrastuzumabTrastuzumab may increase the neutropenic activities of Tositumomab.Approved, Investigational
TriflusalThe risk or severity of adverse effects can be increased when Triflusal is combined with Tositumomab.Approved, Investigational
TroxerutinThe risk or severity of adverse effects can be increased when Troxerutin is combined with Tositumomab.Investigational
VorapaxarThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Tositumomab.Approved
WarfarinThe risk or severity of adverse effects can be increased when Warfarin is combined with Tositumomab.Approved
XimelagatranThe risk or severity of adverse effects can be increased when Ximelagatran is combined with Tositumomab.Approved, Investigational, Withdrawn
Yellow fever vaccineThe therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Tositumomab.Approved
Zoster vaccineThe therapeutic efficacy of Zoster vaccine can be decreased when used in combination with Tositumomab.Approved
Food Interactions
Not Available

References

General References
Not Available
External Links
UniProt
P01857
Genbank
J00228
PubChem Substance
46506662
ChEMBL
CHEMBL1201604
Therapeutic Targets Database
DAP000384
PharmGKB
PA164748364
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Tositumomab
ATC Codes
V10XA53 — Tositumomab/iodine (131i) tositumomab

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentFollicular Lymphoma (FL)1
1CompletedTreatmentLymphoma, B-Cell / Non-Hodgkin's Lymphoma (NHL)1
1CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)2
1Unknown StatusTreatmentChronic Lymphocytic Leukaemia (CLL)1
1Unknown StatusTreatmentNon-Hodgkin's Lymphoma (NHL)2
1, 2CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)1
2Active Not RecruitingTreatmentLymphoma, B-Cell1
2Active Not RecruitingTreatmentMalignant Lymphomas1
2Active Not RecruitingTreatmentMultiple Myeloma (MM)1
2CompletedTreatmentFollicular Lymphoma (FL)1
2CompletedTreatmentLymphoid Leukemia in Remission / Stage I Chronic Lymphocytic Leukemia / Stage II Chronic Lymphocytic Leukemia / Stage III Chronic Lymphocytic Leukemia / Stage III Small Lymphocytic Lymphoma / Stage IV Chronic Lymphocytic Leukemia / Stage IV Small Lymphocytic Lymphoma1
2CompletedTreatmentLymphoma, Mantle-Cell1
2CompletedTreatmentMalignant Lymphomas1
2CompletedTreatmentMantle Cell Lymphoma (MCL)1
2CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)9
2TerminatedTreatmentFollicular Lymphoma (FL)1
2TerminatedTreatmentFollicular Lymphoma (FL) / Non-Hodgkin's Lymphoma (NHL)1
2TerminatedTreatmentNon-Hodgkin's Lymphoma (NHL)1
2Unknown StatusTreatmentNon-Hodgkin's Lymphoma (NHL)1
3CompletedTreatmentLymphoma, B-Cell / Lymphoma, Large-Cell, Immunoblastic / Non-Hodgkin's Lymphoma (NHL)1
3CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)1
3WithdrawnTreatmentFollicular Lymphoma (FL) / Lymphoma, Large-Cell, Follicular / Lymphoma, Small Cleaved-Cell, Follicular / Non-Hodgkin's Lymphoma (NHL)1
Not AvailableUnknown StatusTreatmentNon-Hodgkin's Lymphoma (NHL)2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
Kit; solutionIntravenous14 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.
Patents
Not Available

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-0.414Not Available
isoelectric point8.68Not 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
Human
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. 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]
  2. Dillman RO: Monoclonal antibody therapy for lymphoma: an update. Cancer Pract. 2001 Mar-Apr;9(2):71-80. [PubMed:11879282]
  3. Authors unspecified: 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:12899647]
  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:14748653]
  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:15023434]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  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:13129395]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Not Available
Specific Function
Receptor for the Fc region of immunoglobulins gamma. Low affinity receptor. Binds complexed or aggregated IgG and also monomeric IgG. Contrary to III-A, is not capable to mediate antibody-dependent...
Gene Name
FCGR3B
Uniprot ID
O75015
Uniprot Name
Low affinity immunoglobulin gamma Fc region receptor III-B
Molecular Weight
26215.64 Da
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:17139284]
  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:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Serine-type peptidase activity
Specific Function
C1r B chain is a serine protease that combines with C1q and C1s to form C1, the first component of the classical pathway of the complement system.
Gene Name
C1R
Uniprot ID
P00736
Uniprot Name
Complement C1r subcomponent
Molecular Weight
80118.04 Da
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:17139284]
  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:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Not Available
Specific Function
C1q associates with the proenzymes C1r and C1s to yield C1, the first component of the serum complement system. The collagen-like regions of C1q interact with the Ca(2+)-dependent C1r(2)C1s(2) proe...
Gene Name
C1QA
Uniprot ID
P02745
Uniprot Name
Complement C1q subcomponent subunit A
Molecular Weight
26016.47 Da
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:17139284]
  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:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Not Available
Specific Function
C1q associates with the proenzymes C1r and C1s to yield C1, the first component of the serum complement system. The collagen-like regions of C1q interact with the Ca(2+)-dependent C1r(2)C1s(2) proe...
Gene Name
C1QB
Uniprot ID
P02746
Uniprot Name
Complement C1q subcomponent subunit B
Molecular Weight
26721.62 Da
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:17139284]
  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:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Not Available
Specific Function
C1q associates with the proenzymes C1r and C1s to yield C1, the first component of the serum complement system. The collagen-like regions of C1q interact with the Ca(2+)-dependent C1r(2)C1s(2) proe...
Gene Name
C1QC
Uniprot ID
P02747
Uniprot Name
Complement C1q subcomponent subunit C
Molecular Weight
25773.56 Da
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:17139284]
  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:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Not Available
Specific Function
Receptor for the Fc region of IgG. Binds complexed or aggregated IgG and also monomeric IgG. Mediates antibody-dependent cellular cytotoxicity (ADCC) and other antibody-dependent responses, such as...
Gene Name
FCGR3A
Uniprot ID
P08637
Uniprot Name
Low affinity immunoglobulin gamma Fc region receptor III-A
Molecular Weight
29088.895 Da
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:17139284]
  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:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Receptor signaling protein activity
Specific Function
High affinity receptor for the Fc region of immunoglobulins gamma. Functions in both innate and adaptive immune responses.
Gene Name
FCGR1A
Uniprot ID
P12314
Uniprot Name
High affinity immunoglobulin gamma Fc receptor I
Molecular Weight
42631.525 Da
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:17139284]
  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:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Not Available
Specific Function
Binds to the Fc region of immunoglobulins gamma. Low affinity receptor. By binding to IgG it initiates cellular responses against pathogens and soluble antigens. Promotes phagocytosis of opsonized ...
Gene Name
FCGR2A
Uniprot ID
P12318
Uniprot Name
Low affinity immunoglobulin gamma Fc region receptor II-a
Molecular Weight
35000.42 Da
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:17139284]
  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:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Not Available
Specific Function
Receptor for the Fc region of complexed or aggregated immunoglobulins gamma. Low affinity receptor. Involved in a variety of effector and regulatory functions such as phagocytosis of immune complex...
Gene Name
FCGR2B
Uniprot ID
P31994
Uniprot Name
Low affinity immunoglobulin gamma Fc region receptor II-b
Molecular Weight
34043.355 Da
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:17139284]
  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:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Transmembrane signaling receptor activity
Specific Function
Receptor for the Fc region of complexed immunoglobulins gamma. Low affinity receptor. Involved in a variety of effector and regulatory functions such as phagocytosis of immune complexes and modulat...
Gene Name
FCGR2C
Uniprot ID
P31995
Uniprot Name
Low affinity immunoglobulin gamma Fc region receptor II-c
Molecular Weight
35577.96 Da
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:17139284]
  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:17016423]

Drug created on June 13, 2005 07:24 / Updated on November 06, 2017 06:43