This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Summary

Ligelizumab is an IgE-directed monoclonal antibody under investigation for the treatment of chronic spontaneous urticaria (CSU).

Generic Name
Ligelizumab
DrugBank Accession Number
DB11856
Background

Ligelizumab is a humanized IgG1k monoclonal antibody targeted against immunoglobulin E (IgE). Similar in mechanism to omalizumab, another IgE-directed monoclonal antibody, ligelizumab has a distinct binding epitope as compared to its peer (with a small degree of overlap) which appears to confer a greater affinity for free serum IgE and an altered sensitivity to IgE conformation.2

Ligelizumab is currently under investigation for the treatment of chronic spontaneous urticaria (CSU), an autoimmune-driven inflammatory condition. While the precise pathogenesis of CSU is not entirely clear, autoantibodies against IgE receptors, and sometimes against IgE itself, are thought to exist in 30-40% of patients,3,4 and the efficacy anti-IgE antibody therapy in the treatment of CSU has been previously established with omalizumab. Initial trials of ligelizumab suggest a greater efficacy over its predecessor for the treatment of CSU.4

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
  • Ligelizumab
External IDs
  • QGE031

Pharmacology

Indication

Not Available

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

Immunoglobulin E (IgE) is a key driver of hypersensitivity reactions, and has thus become an attractive target in the treatment of immune-mediated hypersensitivity disorders. Immediate hypersensitivity reactions are due to IgE binding with FcεRI, which activates allergic effector cells that undergo degranulation to release vasoactive and pro-inflammatory mediators.2 IgE also binds to CD23/FcεRII, which appears responsible for antigen presentation, antigen transport across airway/epithelial barriers, and the regulation of IgE synthesis.2

Ligelizumab is a monoclonal antibody directed at IgE, binding specifically to an epitope in the IgE Cε3 domain.2 It neutralizes serum IgE and also appears to inhibit the production of IgE via inhibition of IgE-FcεRI binding activity and, to a lesser extent, IgE binding to CD23.

TargetActionsOrganism
AImmunoglobulin heavy constant epsilon
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 Ligelizumab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Ligelizumab.
AducanumabThe risk or severity of adverse effects can be increased when Ligelizumab is combined with Aducanumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Ligelizumab.
AlirocumabThe risk or severity of adverse effects can be increased when Alirocumab is combined with Ligelizumab.
AmivantamabThe risk or severity of adverse effects can be increased when Ligelizumab is combined with Amivantamab.
AnifrolumabThe risk or severity of adverse effects can be increased when Ligelizumab is combined with Anifrolumab.
AnsuvimabThe risk or severity of adverse effects can be increased when Ligelizumab 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 Ligelizumab.
Antilymphocyte immunoglobulin (horse)The risk or severity of adverse effects can be increased when Antilymphocyte immunoglobulin (horse) is combined with Ligelizumab.
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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
L8LE0L691T
CAS number
1322627-61-1

References

General References
  1. Kaplon H, Reichert JM: Antibodies to watch in 2021. MAbs. 2021 Jan-Dec;13(1):1860476. doi: 10.1080/19420862.2020.1860476. [Article]
  2. Gasser P, Tarchevskaya SS, Guntern P, Brigger D, Ruppli R, Zbaren N, Kleinboelting S, Heusser C, Jardetzky TS, Eggel A: The mechanistic and functional profile of the therapeutic anti-IgE antibody ligelizumab differs from omalizumab. Nat Commun. 2020 Jan 8;11(1):165. doi: 10.1038/s41467-019-13815-w. [Article]
  3. Saini SS, Kaplan AP: Chronic Spontaneous Urticaria: The Devil's Itch. J Allergy Clin Immunol Pract. 2018 Jul - Aug;6(4):1097-1106. doi: 10.1016/j.jaip.2018.04.013. [Article]
  4. Maurer M, Gimenez-Arnau AM, Sussman G, Metz M, Baker DR, Bauer A, Bernstein JA, Brehler R, Chu CY, Chung WH, Danilycheva I, Grattan C, Hebert J, Katelaris C, Makris M, Meshkova R, Savic S, Sinclair R, Sitz K, Staubach P, Wedi B, Loffler J, Barve A, Kobayashi K, Hua E, Severin T, Janocha R: Ligelizumab for Chronic Spontaneous Urticaria. N Engl J Med. 2019 Oct 3;381(14):1321-1332. doi: 10.1056/NEJMoa1900408. [Article]
PubChem Substance
347911250
Wikipedia
Ligelizumab

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3Active Not RecruitingTreatmentChronic Spontaneous Urticaria1
3CompletedTreatmentChronic Spontaneous Urticaria3
3RecruitingTreatmentChronic Inducible Urticaria1
3RecruitingTreatmentPeanut Allergies1
2CompletedTreatmentAsthma1
2CompletedTreatmentAtopic Dermatitis1
2CompletedTreatmentChronic Spontaneous Urticaria3
2TerminatedTreatmentAsthma2
2TerminatedTreatmentBullous Pemphigoid (BP)1
2WithdrawnTreatmentPeanut Allergies1

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
Antibody
Curator comments
Ligelizumab targets a distinct epitope in the IgE Cε3 domain.
General Function
Constant region of immunoglobulin heavy chains. Immunoglobulins, also known as antibodies, are membrane-bound or secreted glycoproteins produced by B lymphocytes. In the recognition phase of humoral immunity, the membrane-bound immunoglobulins serve as receptors which, upon binding of a specific antigen, trigger the clonal expansion and differentiation of B lymphocytes into immunoglobulins-secreting plasma cells. Secreted immunoglobulins mediate the effector phase of humoral immunity, which results in the elimination of bound antigens (PubMed:22158414, PubMed:20176268). The antigen binding site is formed by the variable domain of one heavy chain, together with that of its associated light chain. Thus, each immunoglobulin has two antigen binding sites with remarkable affinity for a particular antigen. The variable domains are assembled by a process called V-(D)-J rearrangement and can then be subjected to somatic hypermutations which, after exposure to antigen and selection, allow affinity maturation for a particular antigen (PubMed:17576170, PubMed:20176268).
Specific Function
Antigen binding
Gene Name
IGHE
Uniprot ID
P01854
Uniprot Name
Immunoglobulin heavy constant epsilon
Molecular Weight
47018.665 Da
References
  1. Kaplon H, Reichert JM: Antibodies to watch in 2021. MAbs. 2021 Jan-Dec;13(1):1860476. doi: 10.1080/19420862.2020.1860476. [Article]
  2. Gasser P, Tarchevskaya SS, Guntern P, Brigger D, Ruppli R, Zbaren N, Kleinboelting S, Heusser C, Jardetzky TS, Eggel A: The mechanistic and functional profile of the therapeutic anti-IgE antibody ligelizumab differs from omalizumab. Nat Commun. 2020 Jan 8;11(1):165. doi: 10.1038/s41467-019-13815-w. [Article]

Drug created at October 20, 2016 20:54 / Updated at November 25, 2021 07:24