Botulinum toxin type A

Identification

Name
Botulinum toxin type A
Accession Number
DB00083
Description

Purified botulinum toxin from Clostridium botulinum, purified from culture via dialysis and acid precipitation.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Other protein based therapies
Protein Structure
Db00083
Protein Chemical Formula
C6760H10447N1743O2010S32
Protein Average Weight
149322.7 Da
Sequences
>Botulinum Toxin Type A Sequence
MPFVNKQFNYKDPVNGVDIAYIKIPNVGQMQPVKAFKIHNKIWVIPERDTFTNPEEGDLN
PPPEAKQVPVSYYDSTYLSTDNEKDNYLKGVTKLFERIYSTDLGRMLLTSIVRGIPFWGG
STIDTELKVIDTNCINVIQPDGSYRSEELNLVIIGPSADIIQFECKSFGHEVLNLTRNGY
GSTQYIRFSPDFTFGFEESLEVDTNPLLGAGKFATDPAVTLAHELIHAGHRLYGIAINPN
RVFKVNTNAYYEMSGLEVSFEELRTFGGHDAKFIDSLQENEFRLYYYNKFKDIASTLNKA
KSIVGTTASLQYMKNVFKEKYLLSEDTSGKFSVDKLKFDKLYKMLTEIYTEDNFVKFFKV
LNRKTYLNFDKAVFKINIVPKVNYTIYDGFNLRNTNLAANFNGQNTEINNMNFTKLKNFT
GLFEFYKLLCVRGIITSKTKSLDKGYNKALNDLCIKVNNWDLFFSPSEDNFTNDLNKGEE
ITSDTNIEAAEENISLDLIQQYYLTFNFDNEPENISIENLSSDIIGQLELMPNIERFPNG
KKYELDKYTMFHYLRAQEFEHGKSRIALTNSVNEALLNPSRVYTFFSSDYVKKVNKATEA
AMFLGWVEQLVYDFTDETSEVSTTDKIADITIIIPYIGPALNIGNMLYKDDFVGALIFSG
AVILLEFIPEIAIPVLGTFALVSYIANKVLTVQTIDNALSKRNEKWDEVYKYIVTNWLAK
VNTQIDLIRKKMKEALENQAEATKAIINYQYNQYTEEEKNNINFNIDDLSSKLNESINKA
MININKFLNQCSVSYLMNSMIPYGVKRLEDFDASLKDALLKYIYDNRGTLIGQVDRLKDK
VNNTLSTDIPFQLSKYVDNQRLLSTFTEYIKNIINTSILNLRYESNHLIDLSRYASKINI
GSKVNFDPIDKNQIQLFNLESSKIEVILKNAIVYNSMYENFSTSFWIRIPKYFNSISLNN
EYTIINCMENNSGWKVSLNYGEIIWTLQDTQEIKQRVVFKYSQMINISDYINRWIFVTIT
NNRLNNSKIYINGRLIDQKPISNLGNIHASNNIMFKLDGCRDTHRYIWIKYFNLFDKELN
EKEIKDLYDNQSNSGILKDFWGDYLQYDKPYYMLNLYDPNKYVDVNNVGIRGYMYLKGPR
GSVMTTNIYLNSSLYRGTKFIIKKYASGNKDNIVRNNDRVYINVVVKNKEYRLATNASQA
GVEKILSALEIPDVGNLSQVVVMKSKNDQGITNKCKMNLQDNNGNDIGFIGFHQFNNIAK
LVASNWYNRQIERSSRTLGCSWEFIPVDDGWGERPL
Download FASTA Format
Synonyms
  • AbobotulinumtoxinA
  • Botulinum A neurotoxin
  • Botulinum toxin A
  • Botulinum toxin type A
  • BTX-A
  • Evabotulinumtoxina
  • IncobotulinumtoxinA
  • OnabotulinumtoxinA
  • Prabotulinumtoxin A
  • Toxina botulĂ­nica A
  • Toxine botulinique A
External IDs
  • AGN 191622
  • ANT-1207
  • ANT-1401
  • ANT-1403
  • NT 201

Pharmacology

Indication

For the treatment of cervical dystonia in adults to decrease the severity of abnormal head position and neck pain associated with cervical dystonia. Also for the treatment of severe primary axillary hyperhidrosis that is inadequately managed with topical agents and for the treatment of strabismus and blepharospasm associated with dystonia, including benign essential blepharospasm or VII nerve disorders in patients 12 years of age and above. Also used cosmetically to temporarily improve the appearance of moderate-to-severe frown lines between the eyebrows (glabellar lines) as well as for the treatment of excessive underarm sweating.

Associated Conditions
Associated Therapies
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

A 150 kDa neurotoxic protein produced from fermentation of Hall strain Clostridium botulinum type A grown in a medium containing casein hydrolysate, glucose and yeast extract. It is purified from the culture solution by dialysis and a series of acid precipitations to a complex consisting of the neurotoxin, and several accessory proteins. Botulinum Toxin Type A is not expected to be present in the peripheral blood at measurable levels following IM or intradermal injection at the recommended doses. The recommended quantities of neurotoxin administered at each treatment session are not expected to result in systemic, overt distant clinical effects, i.e. muscle weakness, in patients without other neuromuscular dysfunction. However, sub-clinical systemic effects have been shown by single-fiber electromyography after IM doses of botulinum toxins appropriate to produce clinically observable local muscle weakness.

Mechanism of action

Botulinum Toxin Type A blocks neuromuscular transmission by binding to acceptor sites on motor or sympathetic nerve terminals, entering the nerve terminals, and inhibiting the release of acetylcholine. This inhibition occurs as the neurotoxin cleaves SNAP-25, a protein integral to the successful docking and release of acetylcholine from vesicles situated within nerve endings.

TargetActionsOrganism
ASynaptosomal-associated protein 25
inhibitor
Humans
URho-related GTP-binding protein RhoBNot AvailableHumans
Absorption

The chemical complexity of Botulinum Toxin Type A combined with its extreme potency limits the opportunity to study its pharmacokinetic profile in humans. Therefore, no human pharmacokinetic studies have been performed. Botulinum Toxin Type A is injected directly into the target organ, a skeletal muscle. Thus, bioavailability of the intravenous or oral route is not of clinical relevance.

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
Learn about our commercial Adverse Effects data.
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Toxicity

Based on toxicological studies, it has been estimated that the human LD50 by injection is approximately 2800 Units, equivalent to 28 individual vials of BOTOX (Botulinum Toxin Type A) Purified Neurotoxin Complex (100 Units) for a 70 kg adult. When injected intramuscularly, Botulinum Toxin Type A has been shown to be teratogenic or to have embryocidal effects in some animal species.

Affected organisms
  • Humans and other mammals
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
AcetazolamideThe risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Acetazolamide.
AcetophenazineThe risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Acetophenazine.
AclidiniumThe risk or severity of adverse effects can be increased when Aclidinium is combined with Botulinum toxin type A.
AgomelatineThe risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Agomelatine.
AlfentanilThe risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Alfentanil.
AlimemazineThe risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Alimemazine.
AlmotriptanThe risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Almotriptan.
AlosetronThe risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Alosetron.
AlprazolamThe risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Alprazolam.
AlverineThe risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Alverine.
Additional Data Available
  • Extended Description
    Extended Description
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  • Severity
    Severity
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    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level
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    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action
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Food Interactions
Not Available

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BotoxInjection, powder, lyophilized, for solution100 [USP'U]/1Intradermal; IntramuscularAllergan, Inc.1989-12-15Not applicableUS flag
BotoxInjection, powder, lyophilized, for solution200 [USP'U]/1Intradermal; IntramuscularAllergan, Inc.2010-01-11Not applicableUS flag
BotoxPowder, for solution100 unitIntramuscularAllergan1992-12-31Not applicableCanada flag
BOTOX CosmeticPowder, for solution100 unitIntramuscularAllergan2001-05-07Not applicableCanada flag
BOTOX CosmeticInjection, powder, lyophilized, for solution100 [USP'U]/1IntramuscularAllergan, Inc.2008-05-20Not applicableUS flag
BOTOX CosmeticInjection, powder, lyophilized, for solution50 [USP'U]/1IntramuscularAllergan, Inc.2008-07-15Not applicableUS flag
DysportInjection, powder, lyophilized, for solution300 [USP'U]/1IntramuscularMedicis Pharmaceutical Corporation2009-05-252015-03-31US flag
DysportInjection, powder, lyophilized, for solution300 U/1IntramuscularGalderma Laboratories, L.P.2009-11-02Not applicableUS flag
DysportInjection, powder, lyophilized, for solution300 U/1IntramuscularIpsen Biopharmaceuticals, Inc.2009-11-02Not applicableUS flag
DysportInjection, powder, lyophilized, for solution500 U/1IntramuscularIpsen Biopharmaceuticals, Inc.2009-11-02Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code
    Available for Purchase

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

ATC Codes
M03AX01 — Botulinum toxin
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

Chemical Identifiers

UNII
E211KPY694
CAS number
93384-43-1

References

General References
  1. Montecucco C, Molgo J: Botulinal neurotoxins: revival of an old killer. Curr Opin Pharmacol. 2005 Jun;5(3):274-9. [PubMed:15907915]
  2. Brin MF, Lew MF, Adler CH, Comella CL, Factor SA, Jankovic J, O'Brien C, Murray JJ, Wallace JD, Willmer-Hulme A, Koller M: Safety and efficacy of NeuroBloc (botulinum toxin type B) in type A-resistant cervical dystonia. Neurology. 1999 Oct 22;53(7):1431-8. [PubMed:10534247]
  3. Shukla HD, Sharma SK: Clostridium botulinum: a bug with beauty and weapon. Crit Rev Microbiol. 2005;31(1):11-8. [PubMed:15839401]
  4. Eisenach JH, Atkinson JL, Fealey RD: Hyperhidrosis: evolving therapies for a well-established phenomenon. Mayo Clin Proc. 2005 May;80(5):657-66. [PubMed:15887434]
  5. Schurch B, Corcos J: Botulinum toxin injections for paediatric incontinence. Curr Opin Urol. 2005 Jul;15(4):264-7. [PubMed:15928517]
UniProt
P10845
Genbank
X52066
KEGG Drug
D00783
KEGG Compound
C07946
PubChem Substance
46505347
RxNav
1000104
Therapeutic Targets Database
DAP001298
PharmGKB
PA164754825
RxList
RxList Drug Page
Wikipedia
Botulinum_toxin
AHFS Codes
  • 92:92.00 — Other Miscellaneous Therapeutic Agents
FDA label
Download (115 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentFacial Rhytides, Skin Folds, Loss of Volume and Skin Quality1
4Active Not RecruitingTreatmentGlabellar Frown Lines1
4Active Not RecruitingTreatmentMixed Urinary Incontinence / Stress Urinary Incontinence (SUI) / Urgency Incontinence1
4Active Not RecruitingTreatmentPainful Intercourse / Pelvic Floor Dysfunctions / Pelvic Pain1
4Active Not RecruitingTreatmentSpinal Cord Injuries (SCI) / Urinary Bladder, Overactive1
4CompletedNot AvailableHealthy Subjects, Only With Wrinkles on Forehead1
4CompletedBasic ScienceHealthy Volunteers1
4CompletedOtherForehead Rhytides / Forehead Wrinkles1
4CompletedOtherGlabellar Frown Lines1
4CompletedPreventionAutonomic Dysreflexia1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Allergan Inc.
  • Tercica Inc.
Dosage Forms
FormRouteStrength
Injection, powder, for solutionParenteral100 U
Injection, powder, for solutionParenteral200 U
Injection, powder, lyophilized, for solutionIntradermal; Intramuscular100 [USP'U]/1
Injection, powder, lyophilized, for solutionIntradermal; Intramuscular200 [USP'U]/1
Powder, for solutionIntramuscular100 unit
InjectionIntramuscular100 U
Injection, powder, for solutionIntradermal; Intramuscular200 U
Injection, powder, for solution100 iu
Injection, powder, for solution300 iu
Injection, powder, for solution500 iu
Injection, powder, for solutionIntramuscular; Subcutaneous300 U
Injection, powder, for solutionIntramuscular; Subcutaneous500 UI
Injection, powder, lyophilized, for solutionIntramuscular300 U/1
Injection, powder, lyophilized, for solutionIntramuscular300 [USP'U]/1
Injection, powder, lyophilized, for solutionIntramuscular500 U/1
Injection, powder, lyophilized, for solutionIntramuscular; Subcutaneous300 U
Injection, solutionIntramuscular500 U
Injection, powder, lyophilized, for solutionIntramuscular; Subcutaneous500 U
Injection, powder, for solution200 iu
Injection, powder, for solution50 iu
PowderIntramuscular100 [USP'U]/1
Injection, powder, lyophilized, for solutionIntramuscular200 IU
Injection, powder, for solutionIntramuscular100 U
Injection, powder, lyophilized, for solutionIntramuscular; Subcutaneous50 U
Injection, powder, for solutionParenteral50 U
Injection, powder, lyophilized, for solutionIntramuscular100 [USP'U]/1
Injection, powder, lyophilized, for solutionIntramuscular200 [USP'U]/1
Injection, powder, lyophilized, for solutionIntramuscular50 [USP'U]/1
Powder, for solutionIntramuscular50 unit
Powder, for solutionIntramuscular
Injection, powder, lyophilized, for solutionIntramuscular100 U
Injection, powder, lyophilized, for solutionIntramuscular50 U
Prices
Unit descriptionCostUnit
Botox 200 unit vial1260.0USD vial
Dysport 500 unit vial852.0USD vial
Botox 100 unit655.2USD vial
Botox 100 unit vial630.0USD vial
Botox cosmetic 100 unit vial630.0USD vial
Botox cosmetic 50 unit vial346.8USD vial
Botox (100 - 200 unit/Vial)3.74USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA2280565No2005-11-152019-08-20Canada flag
CA2310845No2001-05-152014-06-07Canada flag
Additional Data Available
  • Filed On
    Filed On
    Available for Purchase

    The date on which a patent was filed with the relevant government.

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Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilitySolubleNot Available
hydrophobicity-0.368Not Available
isoelectric point6.06Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
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. Zhou JY, Wang ZF, Ren XM, Tang MZ, Shi YL: Antagonism of botulinum toxin type A-induced cleavage of SNAP-25 in rat cerebral synaptosome by toosendanin. FEBS Lett. 2003 Dec 4;555(2):375-9. [PubMed:14644446]
  2. Flynn TC: Myobloc. Dermatol Clin. 2004 Apr;22(2):207-11, vii. [PubMed:15222581]
  3. Okada M, Yoshida S, Zhu G, Kaneko S: [Methodological consideration in studying the exocytosis mechanisms using microdialysis]. Nihon Shinkei Seishin Yakurigaku Zasshi. 2004 Aug;24(4):165-70. [PubMed:15484814]
  4. Frassoni C, Inverardi F, Coco S, Ortino B, Grumelli C, Pozzi D, Verderio C, Matteoli M: Analysis of SNAP-25 immunoreactivity in hippocampal inhibitory neurons during development in culture and in situ. Neuroscience. 2005;131(4):813-23. [PubMed:15749336]
  5. Straughan D: Progress in applying the Three Rs to the potency testing of Botulinum toxin type A. Altern Lab Anim. 2006 Jun;34(3):305-13. [PubMed:16831062]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Gtpase activity
Specific Function
Mediates apoptosis in neoplastically transformed cells after DNA damage. Not essential for development but affects cell adhesion and growth factor signaling in transformed cells. Plays a negative r...
Gene Name
RHOB
Uniprot ID
P62745
Uniprot Name
Rho-related GTP-binding protein RhoB
Molecular Weight
22123.185 Da
References
  1. Ishida H, Zhang X, Erickson K, Ray P: Botulinum toxin type A targets RhoB to inhibit lysophosphatidic acid-stimulated actin reorganization and acetylcholine release in nerve growth factor-treated PC12 cells. J Pharmacol Exp Ther. 2004 Sep;310(3):881-9. Epub 2004 May 12. [PubMed:15140914]

Drug created on June 13, 2005 07:24 / Updated on November 23, 2020 09:08

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