Identification

Summary

Letibotulinumtoxina is a purified type A botulinum neurotoxin protein complex used to improve the appearance of glabellar lines.

Generic Name
Letibotulinumtoxina
DrugBank Accession Number
DB16820
Background

The aesthetic utility of botulinum toxin was discovered incidentally following its initial use in the treatment of facial spasmodic disorders in the early 1970s.1 The first aesthetic use of botulinum toxin was reported in 1989, when onabotulinumtoxinA (Botox) was used as a treatment for facial asymmetry resulting from iatrogenic facial nerve damage.1 It was subsequently approved by the FDA in 1992 for use in aesthetic procedures and has since become one of the most popular cosmetic procedures worldwide.1

Letibotulinumtoxina is a type A botulinum neurotoxin produced from fermentation of Clostridium botulinum strain CBFC26.2 It is a 900 kDa multimeric complex comprising a 150 kDa toxin, a 130 kDa non-toxic non-haemagglutinating protein, and various other haemagglutinins.2 Letibotulinumtoxina has been a market-leading cosmetic product in South Korea for a number of years and was more recently approved in the European Union.3 It was approved for use in Canada in June 2022 for the treatment of glabellar lines.2,3

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Other protein based therapies
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • BoNT/A-DS
  • Letibotulinumtoxina

Pharmacology

Indication

Letibotulinumtoxina is indicated for the temporary improvement of the appearance of moderate-to-severe glabellar lines associated with corrugator and/or procerus muscle activity in adult patients ≤65 years of age.2

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

The intramuscular injection of botulinum neurotoxin results in a dose-related muscle weakness resulting from the irreversible blockade of acetylcholine release from pre-synaptic vesicles.2

Mechanism of action

Letibotulinumtoxina, like other botulinum toxins, exerts its therapeutic effects via action directly on motor neurons.4 The toxin heavy chain mediates binding to surface receptors on nerve endings, after which the toxin is internalized via receptor-mediated endocytosis.2 The toxin light chain is subsequently translocated into the cytosol where it cleaves SNAP25,2,4 a cytosolic protein that forms a portion of the SNARE complex involved in vesicle fusion prior to exocytosis. The cleavage of SNAP25 prevents the formation of the SNARE complex, which subsequently prevents the exocytosis of acetylcholine into the neuromuscular junction, thereby inducing flaccid paralysis of the affected muscle(s).2

TargetActionsOrganism
ASynaptosomal-associated protein 25
cleavage
Humans
Absorption

Pharmacokinetic studies of letibotulinumtoxina are not feasible due to an extremely high affinity for its pre-synaptic cholinergic binding sites - as affinity is in the picomolar range, no detectable amount of toxin appears in the blood following administration.2

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

As with other exogenously administered proteins, letibotulinumtoxina is expected to undergo non-specific enzymatic degradation to smaller peptides and amino acids.2

Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Overdosage of letibotulinumtoxina is likely to result in excessive neuromuscular weakness with a variety of associated symptoms. Patients should be monitored closely in the event of an overdose, and may require respiratory support if respiratory paralysis occurs.2

Symptoms of overdosage are not likely to be present immediately following injection, and patients should be medically supervised for several weeks for signs and symptoms of excessive muscle weakness or paralysis.2

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
AcetyldigitoxinThe risk or severity of Cardiac Arrhythmia can be increased when Letibotulinumtoxina is combined with Acetyldigitoxin.
AtracuriumThe risk or severity of neuromuscular blockade can be increased when Atracurium is combined with Letibotulinumtoxina.
Atracurium besylateThe risk or severity of neuromuscular blockade can be increased when Atracurium besylate is combined with Letibotulinumtoxina.
BaclofenThe therapeutic efficacy of Letibotulinumtoxina can be increased when used in combination with Baclofen.
Beclomethasone dipropionateThe risk or severity of myopathy and weakness can be increased when Letibotulinumtoxina is combined with Beclomethasone dipropionate.
BetamethasoneThe risk or severity of myopathy and weakness can be increased when Letibotulinumtoxina is combined with Betamethasone.
Betamethasone phosphateThe risk or severity of myopathy and weakness can be increased when Letibotulinumtoxina is combined with Betamethasone phosphate.
Botulinum toxin type AThe risk or severity of neuromuscular blockade can be increased when Botulinum toxin type A is combined with Letibotulinumtoxina.
Botulinum toxin type BThe therapeutic efficacy of Letibotulinumtoxina can be increased when used in combination with Botulinum toxin type B.
BudesonideThe risk or severity of myopathy and weakness can be increased when Letibotulinumtoxina is combined with Budesonide.
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Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
LetyboPowder, for solution50 unit / vialIntramuscularCroma Aesthetics Canada, Ltd.Not applicableNot applicableCanada flag
LetyboPowder, for solution100 unit / vialIntramuscularCroma Aesthetics Canada, Ltd.Not applicableNot applicableCanada flag

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
  • Humans and other mammals

Chemical Identifiers

UNII
W5O50S8A59
CAS number
1800016-51-6

References

General References
  1. Gart MS, Gutowski KA: Overview of Botulinum Toxins for Aesthetic Uses. Clin Plast Surg. 2016 Jul;43(3):459-71. doi: 10.1016/j.cps.2016.03.003. Epub 2016 May 4. [Article]
  2. Health Canada Product Monograph: Letybo (letibotulinumtoxina) powder for solution for intramuscular injection [Link]
  3. BusinessWire: Croma Aesthetics Canada Ltd. Receives Canadian Market Authorization for Letybo (LetibotulinumtoxinA for Injection) for the Treatment of Glabellar Lines [Link]
  4. Botox Medical: BOTOX Mechanism of Action [Link]
Not Available

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Powder, for solutionIntramuscular100 unit / vial
Powder, for solutionIntramuscular50 unit / vial
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Cleavage
General Function
Syntaxin-1 binding
Specific Function
t-SNARE involved in the molecular regulation of neurotransmitter release. May play an important role in the synaptic function of specific neuronal systems. Associates with proteins involved in vesi...
Gene Name
SNAP25
Uniprot ID
P60880
Uniprot Name
Synaptosomal-associated protein 25
Molecular Weight
23314.905 Da
References
  1. Health Canada Product Monograph: Letybo (letibotulinumtoxina) powder for solution for intramuscular injection [Link]

Drug created at July 04, 2022 18:22 / Updated at July 06, 2022 18:42