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Identification

Summary

Ublituximab is a low-fucose monoclonal anti-CD20 antibody with enhanced ADCC being investigated for use in leukemia, lymphoma, and autoimmune conditions such as multiple sclerosis.

Generic Name
Ublituximab
DrugBank Accession Number
DB11850
Background

CD20, an antigen expressed by various B and T cells, is an attractive therapeutic target in various cancers and autoimmune conditions.1,2,3 Monoclonal antibodies for B cell depletion rely on their binding affinity and ability to clear bound cells through mechanisms such as antibody-dependent cellular cytotoxicity (ADCC), mediated by interactions between an antibody and Fcγ receptors on natural killer cells or macrophages.4 Ublituximab is a chimeric anti-CD20 IgG1κ antibody produced in the rat YB2/0 cell line to target a unique epitope and enhance ADCC compared to other approved anti-CD20 antibodies such as rituximab, ofatumumab, obinutuzumab, and ocrelizumab.4,5,7

Ublituximab was initially developed by LFB Group but was licensed to TG Therapeutics in 2012. It is being investigated for use in numerous B cell-dependent conditions, including chronic lymphocytic leukemia, non-Hodgkin's lymphoma, and relapsing multiple sclerosis7

Type
Biotech
Groups
Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • Ublituximab

Pharmacology

Indication

Not Available

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

B cell dysregulation underlies the pathogenesis of various cancers and autoimmune conditions such as multiple sclerosis, neuromyelitis optica spectrum disease, and myelin oligodendrocyte glycoprotein IgG-associated disease.1,2,3 CD20 is an antigen expressed on pre-B cells, immature/mature B cells, memory B cells, and a subpopulation of CD3-positive T cells.2 Anti-CD20 antibodies can therefore induce B cell depletion through direct cell death, induction of complement pathways, and Fc-gamma receptor (FcγR)-mediated phagocytosis (antibody-dependent cellular cytotoxicity, ADCC).4

Although several anti-CD20 antibodies have been developed, therapy has been hampered by low CD20 expression by malignant cells in diseases such as B cell chronic lymphocytic leukemia and suboptimal antibody-dependent cytotoxicity.5 Ublituximab binds to an epitope on CD20 distinct from that bound by other approved antibodies such as rituximab, ofatumumab, obinutuzumab, and ocrelizumab, with a similar binding constant to rituximab.4,5 Uniquely, ublituximab is produced in the rat YB2/0 cell line such that it has a low fucose content (24% compared to 93% for rituximab), improving its interaction with FcγR, especially FcγRIIIA (CD16) expressed by natural killer cells and macrophages.4,5 This difference grants ublituximab enhanced ADCC, including for low CD20-expressing malignant cells.5,6

TargetActionsOrganism
AB-lymphocyte antigen CD20
binder
antibody
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

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
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Ublituximab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Ublituximab.
AducanumabThe risk or severity of adverse effects can be increased when Ublituximab is combined with Aducanumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Ublituximab.
AlirocumabThe risk or severity of adverse effects can be increased when Alirocumab is combined with Ublituximab.
AmivantamabThe risk or severity of adverse effects can be increased when Ublituximab is combined with Amivantamab.
AnifrolumabThe risk or severity of adverse effects can be increased when Ublituximab is combined with Anifrolumab.
AnsuvimabThe risk or severity of adverse effects can be increased when Ublituximab is combined with Ansuvimab.
Anthrax immune globulin humanThe risk or severity of adverse effects can be increased when Anthrax immune globulin human is combined with Ublituximab.
Antilymphocyte immunoglobulin (horse)The risk or severity of adverse effects can be increased when Antilymphocyte immunoglobulin (horse) is combined with Ublituximab.
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Food Interactions
Not Available

Categories

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
Not Available

Chemical Identifiers

UNII
U59UGK3IPC
CAS number
1174014-05-1

References

General References
  1. Babiker HM, Glode AE, Cooke LS, Mahadevan D: Ublituximab for the treatment of CD20 positive B-cell malignancies. Expert Opin Investig Drugs. 2018 Apr;27(4):407-412. doi: 10.1080/13543784.2018.1459560. Epub 2018 Apr 3. [Article]
  2. Graf J, Mares J, Barnett M, Aktas O, Albrecht P, Zamvil SS, Hartung HP: Targeting B Cells to Modify MS, NMOSD, and MOGAD: Part 1. Neurol Neuroimmunol Neuroinflamm. 2020 Dec 16;8(1). pii: 8/1/e918. doi: 10.1212/NXI.0000000000000918. Print 2021 Jan. [Article]
  3. Graf J, Mares J, Barnett M, Aktas O, Albrecht P, Zamvil SS, Hartung HP: Targeting B cells to modify MS, NMOSD, and MOGAD: Part 2. Neurol Neuroimmunol Neuroinflamm. 2020 Dec 16;8(1). pii: 8/1/e919. doi: 10.1212/NXI.0000000000000919. Print 2021 Jan. [Article]
  4. Fox E, Lovett-Racke AE, Gormley M, Liu Y, Petracca M, Cocozza S, Shubin R, Wray S, Weiss MS, Bosco JA, Power SA, Mok K, Inglese M: A phase 2 multicenter study of ublituximab, a novel glycoengineered anti-CD20 monoclonal antibody, in patients with relapsing forms of multiple sclerosis. Mult Scler. 2021 Mar;27(3):420-429. doi: 10.1177/1352458520918375. Epub 2020 Apr 30. [Article]
  5. de Romeuf C, Dutertre CA, Le Garff-Tavernier M, Fournier N, Gaucher C, Glacet A, Jorieux S, Bihoreau N, Behrens CK, Beliard R, Vieillard V, Cazin B, Bourel D, Prost JF, Teillaud JL, Merle-Beral H: Chronic lymphocytic leukaemia cells are efficiently killed by an anti-CD20 monoclonal antibody selected for improved engagement of FcgammaRIIIA/CD16. Br J Haematol. 2008 Mar;140(6):635-43. doi: 10.1111/j.1365-2141.2007.06974.x. [Article]
  6. Le Garff-Tavernier M, Herbi L, de Romeuf C, Nguyen-Khac F, Davi F, Grelier A, Boudjoghra M, Maloum K, Choquet S, Urbain R, Vieillard V, Merle-Beral H: Antibody-dependent cellular cytotoxicity of the optimized anti-CD20 monoclonal antibody ublituximab on chronic lymphocytic leukemia cells with the 17p deletion. Leukemia. 2014 Jan;28(1):230-3. doi: 10.1038/leu.2013.240. Epub 2013 Aug 20. [Article]
  7. Kaplon H, Reichert JM: Antibodies to watch in 2021. MAbs. 2021 Jan-Dec;13(1):1860476. doi: 10.1080/19420862.2020.1860476. [Article]
PubChem Substance
347911248
Wikipedia
Ublituximab

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3Active Not RecruitingTreatmentChronic Lymphocytic Leukemia (CLL)1
3CompletedTreatmentChronic Lymphocytic Leukemia (CLL)1
3CompletedTreatmentMultiple Sclerosis, Relapsing Forms of Multiple Sclerosis2
3Enrolling by InvitationTreatmentMultiple Sclerosis, Relapsing Forms of Multiple Sclerosis1
2Active Not RecruitingTreatmentChronic Lymphocytic Leukemia (CLL)1
2Active Not RecruitingTreatmentChronic Lymphocytic Leukemia (CLL) / Chronic Lymphocytic Leukemia (CLL) - Refractory / Relapsed Chronic Lymphocytic Leukemia / Small Lymphocytic Lymphoma1
2Active Not RecruitingTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
2CompletedTreatmentMultiple Sclerosis1
2RecruitingTreatmentChronic Lymphocytic Leukemia (CLL) / Chronic Lymphocytic Leukemia or Small Lymphocytic Leukemia (CLL or SLL) / CLL Progression1
2SuspendedTreatmentFollicular Lymphoma ( FL) / Marginal Zone Lymphoma (MZL)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binder
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. Fox E, Lovett-Racke AE, Gormley M, Liu Y, Petracca M, Cocozza S, Shubin R, Wray S, Weiss MS, Bosco JA, Power SA, Mok K, Inglese M: A phase 2 multicenter study of ublituximab, a novel glycoengineered anti-CD20 monoclonal antibody, in patients with relapsing forms of multiple sclerosis. Mult Scler. 2021 Mar;27(3):420-429. doi: 10.1177/1352458520918375. Epub 2020 Apr 30. [Article]
  2. de Romeuf C, Dutertre CA, Le Garff-Tavernier M, Fournier N, Gaucher C, Glacet A, Jorieux S, Bihoreau N, Behrens CK, Beliard R, Vieillard V, Cazin B, Bourel D, Prost JF, Teillaud JL, Merle-Beral H: Chronic lymphocytic leukaemia cells are efficiently killed by an anti-CD20 monoclonal antibody selected for improved engagement of FcgammaRIIIA/CD16. Br J Haematol. 2008 Mar;140(6):635-43. doi: 10.1111/j.1365-2141.2007.06974.x. [Article]
  3. Le Garff-Tavernier M, Herbi L, de Romeuf C, Nguyen-Khac F, Davi F, Grelier A, Boudjoghra M, Maloum K, Choquet S, Urbain R, Vieillard V, Merle-Beral H: Antibody-dependent cellular cytotoxicity of the optimized anti-CD20 monoclonal antibody ublituximab on chronic lymphocytic leukemia cells with the 17p deletion. Leukemia. 2014 Jan;28(1):230-3. doi: 10.1038/leu.2013.240. Epub 2013 Aug 20. [Article]

Drug created at October 20, 2016 20:53 / Updated at January 12, 2022 01:43