NAV

Obinutuzumab

Identification

Summary

Obinutuzumabis 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

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
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

obinutuzumab的半衰期是28.4天。

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
Pharmacogenomic Effects/ADRsBrowse all" title="" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug InteractionsLearn More" title="" 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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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.
Acetylsalicylic acid The risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Obinutuzumab.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Obinutuzumab.
Adenovirus type 7 vaccine live The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Obinutuzumab.
Aducanumab The risk or severity of adverse effects can be increased when Obinutuzumab is combined with Aducanumab.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Obinutuzumab.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Obinutuzumab.
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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 Region Image
Gazyva Solution 25 mg / mL Intravenous Hoffmann La Roche 2014-11-28 Not applicable Canada flag
Gazyva Injection, solution, concentrate 1000 mg/40mL Intravenous Genentech, Inc. 2013-11-01 Not applicable US flag
Gazyvaro Injection, solution, concentrate 1000 mg Intravenous Roche Registration Gmb H 2020-12-16 Not applicable EU flag

Categories

ATC Codes
L01FA03 — Obinutuzumab
Drug Categories
Chemical TaxonomyProvided byClassyfire
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 TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count
4 Active Not Recruiting Treatment Advanced Follicular Lymphoma 1
3 Active Not Recruiting Treatment B-Cell Chronic Lymphocytic Leukemia (B-CLL) 1
3 Active Not Recruiting Treatment Chronic Lymphocytic Leukemia (CLL) 4
3 Active Not Recruiting Treatment Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma 3
3 Completed Treatment Chronic Lymphocytic Leukemia (CLL) 4
3 Completed Treatment Chronic Lymphocytic Leukemia (CLL)/Lymphoma, Small-Cell 1
3 Completed Treatment Non-Hodgkin's Lymphoma (NHL) 2
3 Not Yet Recruiting Treatment Chronic Lymphocytic Leukemia or Small Lymphocytic Leukemia (CLL or SLL) 1
3 Recruiting Treatment Chronic Lymphocytic Leukemia (CLL) 4
3 Recruiting Treatment Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma 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 Intravenous 1000 mg
Injection, solution, concentrate Parenteral
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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Details 1.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
分子量
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]
  2. Schnaiter A, Stilgenbauer S: Refractory chronic lymphocytic leukemia--new therapeutic strategies. Oncotarget. 2010 Nov;1(7):472-82. doi: 10.18632/oncotarget.101103. [Article]
  3. 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