Obinutuzumab

Identification

Summary

Obinutuzumab is an antineoplastic CD20 antibody used to treat untreated chronic lymphocytic leukemia in combination with chlorambucil.

Brand Names
Gazyva
Generic Name
Obinutuzumab
DrugBank Accession Number
DB08935
Background

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).

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Protein Structure
Db08935
Protein Chemical Formula
C6512H10060N1712O2020S44
Protein Average Weight
146100.0 Da
Sequences
Not Available
Synonyms
  • Afutuzumab
  • Obinutuzumab
External IDs
  • GA-101

Pharmacology

Indication

Obinutuzumab is used as a combination treatment with chlorambucil to treat patients with untreated chronic lymphocytic leukemia.

Pharmacology
Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
Avoid life-threatening adverse drug events
Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events & improve clinical decision support.
Learn more
Pharmacodynamics

Obinutuzumab is more potent than rituximab in depleting B-cells, antitumor activity, and tumor regression.

Mechanism of action

In 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.

TargetActionsOrganism
AB-lymphocyte antigen CD20
antibody
Humans
Absorption

Obinutuzumab is administered intravenously, so its absorption is 100%.

Volume of distribution

Obinutuzumab has a volume of distribution of about 3.8 L.

Protein binding

Obinutuzumab does not bind to plasma proteins.

Metabolism

Obinutuzumab is not metabolized by the liver.

Route of elimination

The route of elimination of obinutuzumab was not indicated (FDA label).

Half-life

The half life of obinutuzumab is 28.4 days.

Clearance

The clearance of obinutuzumab is 0.09L/day.

Adverse Effects
Adverseeffects
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.
Learn more
Improve decision support & research outcomes with our structured adverse effects data.
Learn more
Toxicity

The 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.

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 Abatacept is combined with Obinutuzumab.
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 bleeding and hemorrhage 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.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Obinutuzumab.
Adenovirus type 7 vaccine liveThe risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Obinutuzumab.
AducanumabThe risk or severity of adverse effects can be increased when Obinutuzumab is combined with Aducanumab.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Obinutuzumab.
AlefaceptThe risk or severity of adverse effects can be increased when Alefacept is combined with Obinutuzumab.
Interactions
Identify potential medication risks
Easily compare up to 40 drugs with our drug interaction checker.
Get severity rating, description, and management advice.
Learn more
Food Interactions
  • Avoid echinacea. Echinacea should be used with caution, if at all, in patients receiving therapeutic immunosuppressants. Monitor for reduced efficacy of the immunosuppressant during concomitant use.

Products

Products2
Drug product information from 10+ global regions
Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.
Access now
Access drug product information from over 10 global regions.
Access now
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
GazyvaSolution25 mg / mLIntravenousHoffmann La Roche2014-11-28Not applicableCanada flag
GazyvaInjection, solution, concentrate1000 mg/40mLIntravenousGenentech, Inc.2013-11-01Not applicableUS flag
GazyvaroInjection, solution, concentrate1000 mgIntravenousRoche Registration Gmb H2020-12-16Not applicableEU flag

Categories

ATC Codes
L01XC15 — Obinutuzumab
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
O43472U9X8
CAS number
949142-50-1

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 References
Not Available
KEGG Drug
D09321
PubChem Substance
347910388
RxNav
974779
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Obinutuzumab
FDA label
Download (484 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentAdvanced Follicular Lymphoma1
3Active Not RecruitingTreatmentB-Cell Chronic Lymphocytic Leukemia (B-CLL)1
3Active Not RecruitingTreatmentChronic Lymphocytic Leukemia (CLL)4
3Active Not RecruitingTreatmentChronic Lymphocytic Leukemia (CLL) / Small Lymphocytic Lymphoma2
3Active Not RecruitingTreatmentNon-Hodgkin's Lymphoma (NHL)1
3CompletedTreatmentChronic Lymphocytic Leukemia (CLL)4
3CompletedTreatmentChronic Lymphocytic Leukemia (CLL) / Lymphoma, Small-Cell1
3CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)1
3Not Yet RecruitingTreatmentChronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma1
3Not Yet RecruitingTreatmentEarly Stage Follicular Lymphoma WHO Grade 1/2 or 3a1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection
Injection, solutionIntravenous1000 mg/40ml
Injection, solution, concentrateIntravenous1000 mg/40mL
SolutionIntravenous25 mg / mL
SolutionIntravenous1000 mg
Injection, solution, concentrateParenteral
Injection, solutionIntravenous
SolutionIntravenous1000 mg/40mL
Injection, solution, concentrateIntravenous1000 mg
Injection, solution, concentrateIntravenous; Parenteral1000 MG
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
water solubilityWater solubleNot Available

Targets

Drugtargets2
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
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. 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. [Article]

Drug created on January 05, 2014 20:42 / Updated on October 24, 2021 16:00