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Identification
NameObinutuzumab
Accession NumberDB08935
TypeBiotech
GroupsApproved
Description

Obinutuzumab is a humanized monoclonal antibody used as a combination treatment with chlorambucil to treat patients with untreated chronic lymphocytic leukemia. It was approved by the FDA in November 2013 and is marketed under the brand name Gazyva. There is a black box warning of fatal Hepatitis B Virus (HBV) reactivation and fatal Progressive Multifocal Leukoencephalopathy (PML).

Protein structureDb08935
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Protein chemical formulaC6512H10060N1712O2020S44
Protein average weight146100.0 Da
SequencesNot Available
Synonyms
Afutuzumab
External Identifiers
  • GA-101
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Gazyvainjection, solution, concentrate1000 mg/40mLintravenousGenentech, Inc.2013-11-01Not applicableUs
Gazyvasolution25 mgintravenousHoffmann La Roche Limited2014-11-28Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIO43472U9X8
CAS number949142-50-1
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
IndicationObinutuzumab is used as a combination treatment with chlorambucil to treat patients with untreated chronic lymphocytic leukemia.
PharmacodynamicsObinutuzumab is more potent than rituximab in depleting B-cells, antitumor activity, and tumor regression.
Mechanism of actionIn contrast to rituximab, which is a classic type I CD20 antibody, obinutuzumab binds to type II CD20 antibodies. This allows obinutuzumab to have a much higher induction of antibody-dependant cytotoxicity and a higher direct cytotoxic effect than the classic CD20 antibodies.
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AbsorptionObinutuzumab is administered intravenously, so its absorption is 100%.
Volume of distribution

Obinutuzumab has a volume of distribution of about 3.8 L.

Protein bindingObinutuzumab does not bind to plasma proteins.
Metabolism

Obinutuzumab is not metabolized by the liver.

Route of eliminationThe route of elimination of obinutuzumab was not indicated (FDA label).
Half lifeThe half life of obinutuzumab is 28.4 days.
Clearance

The clearance of obinutuzumab is 0.09L/day.

ToxicityThe most serious toxicities observed with obinutuzumab are Hepatitis B virus (HBV) reactivation and progressive multifocal leukoencephalopathy (PML). HBV reactivation can occur with all anti-CD20 antibodies and can result in hepatic failure, fulminant hepatitis, and death. PML occurs as a result of JC virus infection and can be fatal as well. Other common but less serious adverse reactions include infusion reactions (pre-treat with glucocorticoids, acetaminophen, and anti-histamine to prevent this), neutropenia, thrombocytopenia, and Tumor Lysis Syndrome (TLS) (pre-treat patients, especially with a high lymphocyte count and/or a high tumor burden, with anti-hyperuricemics and hydration). It is also recommended to NOT administer live virus vaccinations prior to or during obinutuzumab treatment.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Injection, solution, concentrateintravenous1000 mg/40mL
Solutionintravenous25 mg
PricesNot Available
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
water solubilityWater solubleNot Available
References
Synthesis Reference

Robak T: GA-101, a third-generation, humanized and glyco-engineered anti-CD20 mAb for the treatment of B-cell lymphoid malignancies. Curr Opin Investig Drugs. 2009 Jun;10(6):588-96.

General ReferencesNot Available
External Links
ATC CodesL01XC15
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (484 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Obinutuzumab.
AcebutololAcebutolol may increase the hypotensive activities of Obinutuzumab.
AcenocoumarolThe risk or severity of adverse effects can be increased when Acenocoumarol is combined with Obinutuzumab.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Obinutuzumab.
AliskirenAliskiren may increase the hypotensive activities of Obinutuzumab.
AmilorideAmiloride may increase the hypotensive activities of Obinutuzumab.
AmlodipineAmlodipine may increase the hypotensive activities of Obinutuzumab.
AnagrelideThe risk or severity of adverse effects can be increased when Anagrelide is combined with Obinutuzumab.
ApixabanThe risk or severity of adverse effects can be increased when Apixaban is combined with Obinutuzumab.
ArgatrobanThe risk or severity of adverse effects can be increased when Argatroban is combined with Obinutuzumab.
AtenololAtenolol may increase the hypotensive activities of Obinutuzumab.
Azilsartan medoxomilAzilsartan medoxomil may increase the hypotensive activities of Obinutuzumab.
BelimumabThe risk or severity of adverse effects can be increased when Obinutuzumab is combined with Belimumab.
BenazeprilBenazepril may increase the hypotensive activities of Obinutuzumab.
BetaxololBetaxolol may increase the hypotensive activities of Obinutuzumab.
BisoprololBisoprolol may increase the hypotensive activities of Obinutuzumab.
BivalirudinThe risk or severity of adverse effects can be increased when Bivalirudin is combined with Obinutuzumab.
BumetanideBumetanide may increase the hypotensive activities of Obinutuzumab.
CandesartanCandesartan may increase the hypotensive activities of Obinutuzumab.
CangrelorThe risk or severity of adverse effects can be increased when Cangrelor is combined with Obinutuzumab.
CaptoprilCaptopril may increase the hypotensive activities of Obinutuzumab.
CarvedilolCarvedilol may increase the hypotensive activities of Obinutuzumab.
ChlorothiazideChlorothiazide may increase the hypotensive activities of Obinutuzumab.
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Obinutuzumab.
CilazaprilCilazapril may increase the hypotensive activities of Obinutuzumab.
CilostazolThe risk or severity of adverse effects can be increased when Cilostazol is combined with Obinutuzumab.
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Obinutuzumab.
Citric AcidThe risk or severity of adverse effects can be increased when Citric Acid is combined with Obinutuzumab.
ClevidipineClevidipine may increase the hypotensive activities of Obinutuzumab.
ClonidineClonidine may increase the hypotensive activities of Obinutuzumab.
ClopidogrelThe risk or severity of adverse effects can be increased when Clopidogrel is combined with Obinutuzumab.
ClozapineThe risk or severity of adverse effects can be increased when Obinutuzumab is combined with Clozapine.
Dabigatran etexilateThe risk or severity of adverse effects can be increased when Dabigatran etexilate is combined with Obinutuzumab.
DalteparinThe risk or severity of adverse effects can be increased when Dalteparin is combined with Obinutuzumab.
DanaparoidThe risk or severity of adverse effects can be increased when Danaparoid is combined with Obinutuzumab.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Obinutuzumab.
DesirudinThe risk or severity of adverse effects can be increased when Desirudin is combined with Obinutuzumab.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Obinutuzumab.
DiclofenacThe risk or severity of adverse effects can be increased when Diclofenac is combined with Obinutuzumab.
DicoumarolThe risk or severity of adverse effects can be increased when Dicoumarol is combined with Obinutuzumab.
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Obinutuzumab.
DiltiazemDiltiazem may increase the hypotensive activities of Obinutuzumab.
DipyridamoleThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Obinutuzumab.
DoxazosinDoxazosin may increase the hypotensive activities of Obinutuzumab.
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Obinutuzumab.
Edetic AcidThe risk or severity of adverse effects can be increased when Edetic Acid is combined with Obinutuzumab.
EdoxabanThe risk or severity of adverse effects can be increased when Edoxaban is combined with Obinutuzumab.
EnalaprilEnalapril may increase the hypotensive activities of Obinutuzumab.
EnalaprilatEnalaprilat may increase the hypotensive activities of Obinutuzumab.
EnoxaparinThe risk or severity of adverse effects can be increased when Enoxaparin is combined with Obinutuzumab.
EplerenoneEplerenone may increase the hypotensive activities of Obinutuzumab.
EprosartanEprosartan may increase the hypotensive activities of Obinutuzumab.
EptifibatideThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Obinutuzumab.
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Obinutuzumab.
EsmololEsmolol may increase the hypotensive activities of Obinutuzumab.
Etacrynic acidEthacrynic acid may increase the hypotensive activities of Obinutuzumab.
Ethyl biscoumacetateThe risk or severity of adverse effects can be increased when Ethyl biscoumacetate is combined with Obinutuzumab.
EtodolacThe risk or severity of adverse effects can be increased when Etodolac is combined with Obinutuzumab.
FelodipineFelodipine may increase the hypotensive activities of Obinutuzumab.
FenoprofenThe risk or severity of adverse effects can be increased when Fenoprofen is combined with Obinutuzumab.
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Obinutuzumab.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Obinutuzumab.
FlurbiprofenThe risk or severity of adverse effects can be increased when Flurbiprofen is combined with Obinutuzumab.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Obinutuzumab.
Fondaparinux sodiumThe risk or severity of adverse effects can be increased when Fondaparinux sodium is combined with Obinutuzumab.
FosinoprilFosinopril may increase the hypotensive activities of Obinutuzumab.
FurosemideFurosemide may increase the hypotensive activities of Obinutuzumab.
GuanfacineGuanfacine may increase the hypotensive activities of Obinutuzumab.
HeparinThe risk or severity of adverse effects can be increased when Heparin is combined with Obinutuzumab.
HydralazineHydralazine may increase the hypotensive activities of Obinutuzumab.
HydrochlorothiazideHydrochlorothiazide may increase the hypotensive activities of Obinutuzumab.
IbuprofenThe risk or severity of adverse effects can be increased when Ibuprofen is combined with Obinutuzumab.
IndapamideIndapamide may increase the hypotensive activities of Obinutuzumab.
IndomethacinThe risk or severity of adverse effects can be increased when Indomethacin is combined with Obinutuzumab.
IrbesartanIrbesartan may increase the hypotensive activities of Obinutuzumab.
IsradipineIsradipine may increase the hypotensive activities of Obinutuzumab.
KetoprofenThe risk or severity of adverse effects can be increased when Ketoprofen is combined with Obinutuzumab.
KetorolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Obinutuzumab.
LabetalolLabetalol may increase the hypotensive activities of Obinutuzumab.
LeflunomideThe risk or severity of adverse effects can be increased when Obinutuzumab is combined with Leflunomide.
LevomilnacipranThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Obinutuzumab.
LisinoprilLisinopril may increase the hypotensive activities of Obinutuzumab.
LosartanLosartan may increase the hypotensive activities of Obinutuzumab.
MannitolMannitol may increase the hypotensive activities of Obinutuzumab.
MecamylamineMecamylamine may increase the hypotensive activities of Obinutuzumab.
Mefenamic acidThe risk or severity of adverse effects can be increased when Mefenamic acid is combined with Obinutuzumab.
MeloxicamThe risk or severity of adverse effects can be increased when Meloxicam is combined with Obinutuzumab.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Obinutuzumab.
MethyclothiazideMethyclothiazide may increase the hypotensive activities of Obinutuzumab.
MethyldopaMethyldopa may increase the hypotensive activities of Obinutuzumab.
MetolazoneMetolazone may increase the hypotensive activities of Obinutuzumab.
MetoprololMetoprolol may increase the hypotensive activities of Obinutuzumab.
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Obinutuzumab.
MinoxidilMinoxidil may increase the hypotensive activities of Obinutuzumab.
MoexiprilMoexipril may increase the hypotensive activities of Obinutuzumab.
MoxonidineMoxonidine may increase the hypotensive activities of Obinutuzumab.
NabumetoneThe risk or severity of adverse effects can be increased when Nabumetone is combined with Obinutuzumab.
NadololNadolol may increase the hypotensive activities of Obinutuzumab.
NadroparinThe risk or severity of adverse effects can be increased when Nadroparin is combined with Obinutuzumab.
NaproxenThe risk or severity of adverse effects can be increased when Naproxen is combined with Obinutuzumab.
NatalizumabThe risk or severity of adverse effects can be increased when Obinutuzumab is combined with Natalizumab.
NebivololNebivolol may increase the hypotensive activities of Obinutuzumab.
NicardipineNicardipine may increase the hypotensive activities of Obinutuzumab.
NifedipineNifedipine may increase the hypotensive activities of Obinutuzumab.
NimodipineNimodipine may increase the hypotensive activities of Obinutuzumab.
NisoldipineNisoldipine may increase the hypotensive activities of Obinutuzumab.
NitroprussideNitroprusside may increase the hypotensive activities of Obinutuzumab.
OlmesartanOlmesartan may increase the hypotensive activities of Obinutuzumab.
OxaprozinThe risk or severity of adverse effects can be increased when Oxaprozin is combined with Obinutuzumab.
ParoxetineThe risk or severity of adverse effects can be increased when Paroxetine is combined with Obinutuzumab.
PenbutololPenbutolol may increase the hypotensive activities of Obinutuzumab.
PerindoprilPerindopril may increase the hypotensive activities of Obinutuzumab.
PhenindioneThe risk or severity of adverse effects can be increased when Phenindione is combined with Obinutuzumab.
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Obinutuzumab.
PhenprocoumonThe risk or severity of adverse effects can be increased when Phenprocoumon is combined with Obinutuzumab.
PhentolaminePhentolamine may increase the hypotensive activities of Obinutuzumab.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Obinutuzumab.
PindololPindolol may increase the hypotensive activities of Obinutuzumab.
PiroxicamThe risk or severity of adverse effects can be increased when Piroxicam is combined with Obinutuzumab.
PrasugrelThe risk or severity of adverse effects can be increased when Prasugrel is combined with Obinutuzumab.
PrazosinPrazosin may increase the hypotensive activities of Obinutuzumab.
PropranololPropranolol may increase the hypotensive activities of Obinutuzumab.
QuinaprilQuinapril may increase the hypotensive activities of Obinutuzumab.
RamiprilRamipril may increase the hypotensive activities of Obinutuzumab.
ReserpineReserpine may increase the hypotensive activities of Obinutuzumab.
RivaroxabanThe risk or severity of adverse effects can be increased when Rivaroxaban is combined with Obinutuzumab.
RoflumilastRoflumilast may increase the immunosuppressive activities of Obinutuzumab.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Obinutuzumab.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Obinutuzumab.
SotalolSotalol may increase the hypotensive activities of Obinutuzumab.
SpironolactoneSpironolactone may increase the hypotensive activities of Obinutuzumab.
SulindacThe risk or severity of adverse effects can be increased when Sulindac is combined with Obinutuzumab.
SulodexideThe risk or severity of adverse effects can be increased when Sulodexide is combined with Obinutuzumab.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Obinutuzumab.
TelmisartanTelmisartan may increase the hypotensive activities of Obinutuzumab.
TerazosinTerazosin may increase the hypotensive activities of Obinutuzumab.
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Tiaprofenic acid is combined with Obinutuzumab.
TicagrelorThe risk or severity of adverse effects can be increased when Ticagrelor is combined with Obinutuzumab.
TiclopidineThe risk or severity of adverse effects can be increased when Ticlopidine is combined with Obinutuzumab.
TimololTimolol may increase the hypotensive activities of Obinutuzumab.
TinzaparinThe risk or severity of adverse effects can be increased when Tinzaparin is combined with Obinutuzumab.
TirofibanThe risk or severity of adverse effects can be increased when Tirofiban is combined with Obinutuzumab.
TofacitinibObinutuzumab may increase the immunosuppressive activities of Tofacitinib.
TolmetinThe risk or severity of adverse effects can be increased when Tolmetin is combined with Obinutuzumab.
TorasemideTorasemide may increase the hypotensive activities of Obinutuzumab.
TrandolaprilTrandolapril may increase the hypotensive activities of Obinutuzumab.
TrastuzumabTrastuzumab may increase the neutropenic activities of Obinutuzumab.
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Obinutuzumab.
TriamtereneTriamterene may increase the hypotensive activities of Obinutuzumab.
ValsartanValsartan may increase the hypotensive activities of Obinutuzumab.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Obinutuzumab.
VerapamilVerapamil may increase the hypotensive activities of Obinutuzumab.
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Obinutuzumab.
VorapaxarThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Obinutuzumab.
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Obinutuzumab.
WarfarinThe risk or severity of adverse effects can be increased when Warfarin is combined with Obinutuzumab.
Food Interactions
  • Echinacea: diminished therapeutic effect of immunosuppressants

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
Molecular Weight:
33076.99 Da
References
  1. Robak T: GA-101, a third-generation, humanized and glyco-engineered anti-CD20 mAb for the treatment of B-cell lymphoid malignancies. Curr Opin Investig Drugs. 2009 Jun;10(6):588-96. [PubMed:19513948 ]
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Drug created on January 05, 2014 13:42 / Updated on March 14, 2016 10:05