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
- 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 botulínica 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
- Blepharospasm
- Cervical Dystonia
- Chronic Migraine
- Equinus deformity of foot, acquired
- Lower Limb Spasticity
- Sialorrhea
- Strabismus
- Upper Limb Spasticity
- Urinary Bladder, Overactive
- Urinary Incontinence (UI)
- Detrusor overactivity, neurologic conditions
- Hypertonicity disorders of the 7th nerve
- Severe axillary hyperhidrosis
- Associated Therapies
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- 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.
Target Actions Organism ASynaptosomal-associated protein 25 inhibitorHumans URho-related GTP-binding protein RhoB Not Available Humans - 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.
Learn More- 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.
Drug Interaction Unlock Additional DataAcetazolamide The risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Acetazolamide. Acetophenazine The risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Acetophenazine. Aclidinium The risk or severity of adverse effects can be increased when Aclidinium is combined with Botulinum toxin type A. Agomelatine The risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Agomelatine. Alfentanil The risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Alfentanil. Alimemazine The risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Alimemazine. Almotriptan The risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Almotriptan. Alosetron The risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Alosetron. Alprazolam The risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Alprazolam. Alverine The risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Alverine. Additional Data Available- Extended DescriptionExtended DescriptionAvailable for Purchase
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - SeveritySeverityAvailable for Purchase
A severity rating for each drug interaction, from minor to major.
Learn more - Evidence LevelEvidence LevelAvailable for Purchase
A rating for the strength of the evidence supporting each drug interaction.
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An effect category for each drug interaction. Know how this interaction affects the subject drug.
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- Food Interactions
- Not Available
Products
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataBotox Injection, powder, lyophilized, for solution 200 [USP'U]/1 Intradermal; Intramuscular Allergan, Inc. 2010-01-11 Not applicable US 
Botox Powder, for solution 100 unit Intramuscular Allergan 1992-12-31 Not applicable Canada 
Botox Injection, powder, lyophilized, for solution 100 [USP'U]/1 Intradermal; Intramuscular Allergan, Inc. 1989-12-15 Not applicable US BOTOX Cosmetic Injection, powder, lyophilized, for solution 50 [USP'U]/1 Intramuscular Allergan, Inc. 2008-07-15 Not applicable US BOTOX Cosmetic Powder, for solution 100 unit Intramuscular Allergan 2001-05-07 Not applicable Canada BOTOX Cosmetic Injection, powder, lyophilized, for solution 100 [USP'U]/1 Intramuscular Allergan, Inc. 2008-05-20 Not applicable US Dysport Injection, powder, lyophilized, for solution 500 U/1 Intramuscular Ipsen Biopharmaceuticals, Inc. 2009-11-02 Not applicable US Dysport Injection, powder, lyophilized, for solution 300 [USP'U]/1 Intramuscular Medicis Pharmaceutical Corporation 2009-05-25 2015-03-31 US Dysport Injection, powder, lyophilized, for solution 300 U/1 Intramuscular Galderma Laboratories, L.P. 2009-11-02 Not applicable US Dysport Injection, powder, lyophilized, for solution 300 U/1 Intramuscular Ipsen Biopharmaceuticals, Inc. 2009-11-02 Not applicable US Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable 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
- Acetylcholine Release Inhibitors
- Agents that produce neuromuscular block (indirect)
- Amino Acids, Peptides, and Proteins
- Bacterial Proteins
- Bacterial Toxins
- Biological Factors
- Botulinum Toxins
- Botulinum Toxins, Type A
- Botulinum Toxins, Type A, antagonists & inhibitors
- Central Nervous System Depressants
- Cholinergic Agents
- Endopeptidases
- Enzymes
- Enzymes and Coenzymes
- Ganglion Blockers
- Hydrolases
- Membrane Transport Modulators
- Metalloendopeptidases
- Metalloproteases
- Muscle Relaxants
- Muscle Relaxants, Peripherally Acting Agents
- Musculo-Skeletal System
- Neuromuscular Agents
- Neurotoxins
- Neurotransmitter Agents
- Noxae
- Other Miscellaneous Therapeutic Agents
- Peptide Hydrolases
- Peripheral Nervous System Agents
- Proteins
- Toxic Actions
- Toxins, Biological
- 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
- Montecucco C, Molgo J: Botulinal neurotoxins: revival of an old killer. Curr Opin Pharmacol. 2005 Jun;5(3):274-9. [PubMed:15907915]
- 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]
- Shukla HD, Sharma SK: Clostridium botulinum: a bug with beauty and weapon. Crit Rev Microbiol. 2005;31(1):11-8. [PubMed:15839401]
- 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]
- Schurch B, Corcos J: Botulinum toxin injections for paediatric incontinence. Curr Opin Urol. 2005 Jul;15(4):264-7. [PubMed:15928517]
- External Links
- UniProt
- P10845
- Genbank
- X52066
- KEGG Drug
- D00783
- KEGG Compound
- C07946
- PubChem Substance
- 46505347
- 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
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Glabellar Frown Lines 1 4 Active Not Recruiting Treatment Mixed Urinary Incontinence / Stress Urinary Incontinence (SUI) / Urgency Incontinence 1 4 Active Not Recruiting Treatment Painful Intercourse / Pelvic Floor Dysfunctions / Pelvic Pain 1 4 Active Not Recruiting Treatment Spinal Cord Injuries (SCI) / Urinary Bladder, Overactive 1 4 Active Not Recruiting Treatment Synkinesis 1 4 Completed Basic Science Healthy Volunteers 1 4 Completed Other Forehead Rhytides / Forehead Wrinkles 1 4 Completed Other Glabellar Frown Lines 1 4 Completed Other Skin Wrinklings 1 4 Completed Prevention Autonomic Dysreflexia 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Allergan Inc.
- Tercica Inc.
- Dosage Forms
Form Route Strength Injection, powder, for solution Intramuscular 125 U Injection, powder, for solution Intramuscular 125 SU Injection, powder, for solution Parenteral 100 U Injection, powder, for solution Parenteral 200 U Injection, powder, lyophilized, for solution Intradermal; Intramuscular 100 [USP'U]/1 Injection, powder, lyophilized, for solution Intradermal; Intramuscular 200 [USP'U]/1 Powder, for solution Intramuscular 100 unit Injection, powder, for solution Intramuscular 100 U Injection Intramuscular 100 U Injection, powder, for solution Intradermal; Intramuscular 200 U Injection, powder, for solution 100 iu Injection, powder, for solution 300 iu Injection, powder, for solution 500 iu Injection, powder, for solution Intramuscular; Subcutaneous 300 U Injection, powder, for solution Intramuscular; Subcutaneous 500 UI Injection, powder, lyophilized, for solution Intramuscular 300 U/1 Injection, powder, lyophilized, for solution Intramuscular 300 [USP'U]/1 Injection, powder, lyophilized, for solution Intramuscular 500 U/1 Injection, powder, lyophilized, for solution Intramuscular; Subcutaneous 300 U Injection, solution Intramuscular 500 U Injection, powder, for solution 500 U Injection, powder, lyophilized, for solution Intramuscular; Subcutaneous 500 U Injection, powder, for solution 200 iu Injection, powder, for solution 50 iu Powder Intramuscular 100 [USP'U]/1 Injection, powder, for solution Intramuscular 200 U Injection, powder, for solution Intramuscular 50 U Injection, powder, lyophilized, for solution Intramuscular; Subcutaneous 100 IU Injection, powder, lyophilized, for solution Intramuscular 200 IU Injection, powder, lyophilized, for solution Intramuscular; Subcutaneous 50 U Injection, powder, for solution Parenteral 4 AU/ 0.1 ml Injection, powder, for solution Parenteral 4 AU/0.1ml Injection, powder, for solution Parenteral 50 U Injection, powder, lyophilized, for solution Intramuscular 100 [USP'U]/1 Injection, powder, lyophilized, for solution Intramuscular 200 [USP'U]/1 Injection, powder, lyophilized, for solution Intramuscular 50 [USP'U]/1 Powder, for solution Intramuscular 50 unit Powder, for solution Intramuscular Injection, powder, for solution 100 LD50 Units Injection, powder, for solution 50 LD50 Units Injection, powder, lyophilized, for solution Intramuscular 100 U Injection, powder, lyophilized, for solution Intramuscular 50 U - Prices
Unit description Cost Unit Botox 200 unit vial 1260.0USD vial Dysport 500 unit vial 852.0USD vial Botox 100 unit 655.2USD vial Botox 100 unit vial 630.0USD vial Botox cosmetic 100 unit vial 630.0USD vial Botox cosmetic 50 unit vial 346.8USD 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 Number Pediatric Extension Approved Expires (estimated) Region Unlock Additional DataCA2280565 No 2005-11-15 2019-08-20 Canada CA2310845 No 2001-05-15 2014-06-07 Canada Additional Data Available- Filed OnFiled OnAvailable for Purchase
The date on which a patent was filed with the relevant government.
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Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Soluble Not Available hydrophobicity -0.368 Not Available isoelectric point 6.06 Not 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
- 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]
- Flynn TC: Myobloc. Dermatol Clin. 2004 Apr;22(2):207-11, vii. [PubMed:15222581]
- 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]
- 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]
- 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]
- 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
- 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 January 25, 2021 22:38