==== 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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1722 details
Primary information
ThPP IDTh1173
Therapeutic Peptide/Protein NameConestat alfa
SequenceNA view full sequnce in fasta
Functional ClassificationIa
Molecular WeightNA
Chemical FormulaNA
Isoelectric PointNA
HydrophobicityNA
Melting Point (℃)NA
Half Life2.4 to 2.7 hours
DescriptionConestat alfa is a recombinant, human C1-inhibitor (rhC1INH), for the treatment of acute attacks of hereditary angioedema (HAE) due to C1 esterase inhibitor deficiency in adults. Conestat alfa was approved in October 2010 in all 27 EU member states plus Norway, Iceland and Liechtenstein.
Indication/DiseaseFor the treatment of acute attacks of hereditary angioedema (HAE) due to C1 esterase inhibitor deficiency in adults.
PharmacodynamicsThe complement component (protein) C4 is a substrate for activated C1. Patients with HAE have low levels of C4 in the circulation; RUCONEST shows a dose-dependent restoration of complement homeostasis of C4 in HAE patients. A dose of 50 IU/kg of RUCONEST increases plasma C1INH activity levels to greater than 0.7 IU/mL (the lower limit of normal) in HAE patients.
Mechanism of ActionC1INH exerts its inhibitory effect by irreversibly binding several proteases (target proteases) of the contact and complement systems. The effect of RUCONEST on the following target proteases was assessed in vitro: activated C1s, kallikrein, factor XIIa and factor XIa. Inhibition kinetics were found to be comparable with those observed for plasma-derived human C1INH.
ToxicityIn a 14-day monkey toxicology study of intravenous doses up to 2000 IU/kg twice daily, increases in AST and ALP were observed at doses of 500 IU/kg and higher.
MetabolismNA
AbsorptionAUC of 3.3 ± 1.0 for 50 IU/KG to 10.6 ± 2.5 (IU x hr/mL) for 100 IU/KG
Volume of DistributionNA
Clearance1207±414 for 50IU/KG and 781± 147 for 100 IU/KG
CategoriesNA
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetNA
Information of corresponding available drug in the market
Brand NameRuconest
CompanyPharming; Santarus, Inc.
Brand DiscriptionRUCONEST is a recombinant analogue of human complement component 1 esterase inhibitor for intravenous injection. RUCONEST is purified from the milk of transgenic rabbits, and supplied as a sterile, preservative-free, white/off-white lyophilized powder for reconstitution for injection.
Prescribed forRUCONEST is a C1 esterase inhibitor [recombinant] indicated for the treatment of acute attacks in adult and adolescent patients with hereditary angioedema (HAE).
Chemical NameNA
Formulation2100 U/1
Physcial Appearncepowder for solution
Route of AdministrationIV
Recommended DosageIV Injection; The recommended dose of RUCONEST is 50 IU per kg with a maximum of 4200 IU to be administered as a slow intravenous injection over approximately 5 minutes.
ContraindicationRUCONEST is contraindicated in patients with a history of allergy to rabbits or rabbit-derived products. RUCONEST is contraindicated in patients with a history of life-threatening immediate hypersensitivity reactions to C1 esterase inhibitor preparations, including anaphylaxis.
Side EffectsThe serious adverse reaction in clinical studies of RUCONEST was anaphylaxis. The most common adverse reactions ( ≥ 2%) reported in all clinical trials were headache, nausea, and diarrhea.
Useful Linkhttp://www.rxlist.com/ruconest-drug/clinical-pharmacology.htm
PubMed ID25673959
3-D StructureN.A.