==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb

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1420 details
Primary information
ThPP IDTh1070
Therapeutic Peptide/Protein NameBotulinum Toxin Type A
SequenceMPFVNKQFNYKDPVNGVDIAYIKIPNVGQMQPVKAFKIHNKIWVIPERDT view full sequnce in fasta
Functional ClassificationIc
Molecular Weight149322.7
Chemical FormulaC6760H10447N1743O2010S32
Isoelectric Point6.06
Hydrophobicity-0.368
Melting Point (℃)N.A.
Half LifeN.A.
DescriptionPurified botulinum toxin from Clostridium botulinum, purified from culture via dialysis and acid precipitation.
Indication/DiseaseFor 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.
PharmacodynamicsA 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 ActionBotulinum 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.
ToxicityBased 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.
MetabolismN.A.
AbsorptionThe 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 DistributionN.A.
ClearanceN.A.
CategoriesNeuromuscular Blocking Agents, Anti-Wrinkle Agents and Antidystonic Agents
Patents NumberCA2310845
Date of Issue16/05/05
Date of Expiry08/06/18
Drug InteractionN.A.
TargetGrowth hormone receptor
Information of corresponding available drug in the market
Brand NameDysport
CompanyIpsen Pharmaceuticals
Brand DiscriptionDysport (abobotulinumtoxinA), is a purified neurotoxin type A complex produced by fermentation of the bacterium Clostridium botulinum type A, Hall Strain. It is purified from the culture supernatant by a series of precipitation, dialysis, and chromatography steps. The neurotoxin complex is composed of the neurotoxin, hemagglutinin proteins and non-toxin non-hemagglutinin protein.
Prescribed forDysport is indicated for the treatment of Cervical Dystonia and Glabellar Lines
Chemical NameN.A.
FormulationEach vial contains 500 or 300 Units of lyophilized abobotulinumtoxinA, 125 micrograms human serum albumin and 2.5 mg lactose. Dysport may contain trace amounts of cow's milk proteins
Physcial AppearnceDysport is supplied in a single-use, sterile vial for reconstitution
Route of AdministrationIntramuSubcutaneousular Injection
Recommended DosageIn Cervical Dystonia: Initial dose of DYSPORT  is 500 Units given intramuscularly. Re-treatment every 12 to 16 weeks or longer, as necessary, based on return of clinical symptoms with doses administered between 250 and 1000 Units to optimize clinical benefit. In Glabellar Lines: A total dose of 50 Units of DYSPORT , divided in five equal aliquots of 10 Units each, should be administered to affected muscles to achieve clinical effect.
ContraindicationDYSPORT is contraindicated in patients with known hypersensitivity to any botulinum toxin preparation or to any of the components in the formulation.
Side EffectsIn Cervical Dystonia: Most commonly observed adverse reactions (> 5% of patients) are: muscular weakness, dysphagia, dry mouth, injection site discomfort, fatigue, headache, neck pain, musculoskeletal pain, dysphonia, injection site pain, and eye disorders. In Glabellar Lines: The most frequently reported adverse events (≥2%) are nasopharyngitis, headache, injection site pain, injection site reaction, upper respiratory tract infection, eyelid edema, eyelid ptosis, sinusitis and nausea.
Useful Linkhttp://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=195ebbc0-eaac-4015-97fd-3653b815a758 http://www.rxlist.com/dysport-drug.htm
PubMed ID15887434
3-D StructureTh1070 (View) or (Download)