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

Protein Chemical Formula: C₆₅₁₂H₁₀₀₆₀N₁₇₁₂O₂₀₂₀S₄₄
Protein Average Weight: 146100.0 Da

Sequences

Not Available

Synonyms

Afutuzumab
Obinutuzumab

External IDs

GA-101

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Pharmacology

Indication

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

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Used in combination to treat	Refractory follicular lymphoma	Regimen in combination with: Bendamustine (DB06769)	••••••••••••
Used in combination to treat	Previously untreated chronic lymphocytic leukemia	Regimen in combination with: Chlorambucil (DB00291)	••••••••••••

Contraindications & Blackbox Warnings

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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.

Target	Actions	Organism
AB-lymphocyte antigen CD20	antibody regulator	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

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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

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Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">

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.

Drug	Interaction
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Abaloparatide	The risk or severity of adverse effects can be increased when Abaloparatide is combined with Obinutuzumab.
Abatacept	The risk or severity of adverse effects can be increased when Abatacept is combined with Obinutuzumab.
Abciximab	The risk or severity of adverse effects can be increased when Abciximab is combined with Obinutuzumab.
Acebutolol	Acebutolol may increase the hypotensive activities of Obinutuzumab.
Acenocoumarol	The risk or severity of bleeding and hemorrhage can be increased when Acenocoumarol is combined with Obinutuzumab.

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

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Gazyva	Injection, solution, concentrate	1000 mg/40mL	Intravenous	Genentech, Inc.	2013-11-01	Not applicable
Gazyva	Solution	25 mg / mL	Intravenous	Hoffmann La Roche	2014-11-28	Not applicable
Gazyvaro	Injection, solution, concentrate	1000 mg	Intravenous	Roche Registration Gmb H	2020-12-16	Not applicable

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

External Links

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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Advanced Follicular Lymphoma	1
3	Active Not Recruiting	Treatment	B-Cell Chronic Lymphocytic Leukemia	1
3	Active Not Recruiting	Treatment	Chronic Lymphocytic Leukemia	5
3	Active Not Recruiting	Treatment	Chronic Lymphocytic Leukemia / Small Lymphocytic Lymphoma	2
3	Active Not Recruiting	Treatment	Lupus Nephritis	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection
Injection, solution	Intravenous	1000 mg/40ml
Injection, solution, concentrate	Intravenous	1000 mg/40mL
Solution	Intravenous	25 mg / mL
Solution, concentrate	Intravenous	1000 mg
Injection, solution, concentrate	Parenteral	1000 mg
Injection, solution	Intravenous
Solution	Intravenous	1000 mg/40mL
Injection, solution, concentrate	Intravenous	1000 mg
Injection, solution, concentrate	Intravenous; Parenteral	1000 MG

Prices

Not Available

Patents

Not Available

Properties

State

Liquid

Experimental Properties

Property	Value	Source
water solubility	Water soluble	Not Available

Targets

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Details1. B-lymphocyte antigen CD20

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Antibody
Regulator

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

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]
Schnaiter A, Stilgenbauer S: Refractory chronic lymphocytic leukemia--new therapeutic strategies. Oncotarget. 2010 Nov;1(7):472-82. doi: 10.18632/oncotarget.101103. [Article]
Kyriakidis I, Vasileiou E, Rossig C, Roilides E, Groll AH, Tragiannidis A: Invasive Fungal Diseases in Children with Hematological Malignancies Treated with Therapies That Target Cell Surface Antigens: Monoclonal Antibodies, Immune Checkpoint Inhibitors and CAR T-Cell Therapies. J Fungi (Basel). 2021 Mar 5;7(3). pii: jof7030186. doi: 10.3390/jof7030186. [Article]

Drug created at January 05, 2014 20:42 / Updated at June 03, 2022 07:24

Obinutuzumab

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References