A database of FDA approved therapeutic peptides and proteins
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1722 details |
Primary information | |
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ThPP ID | Th1173 |
Therapeutic Peptide/Protein Name | Conestat alfa |
Sequence | NA view full sequnce in fasta |
Functional Classification | Ia |
Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting Point (℃) | NA |
Half Life | 2.4 to 2.7 hours |
Description | Conestat 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/Disease | For the treatment of acute attacks of hereditary angioedema (HAE) due to C1 esterase inhibitor deficiency in adults. |
Pharmacodynamics | The 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 Action | C1INH 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. |
Toxicity | In 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. |
Metabolism | NA |
Absorption | AUC of 3.3 ± 1.0 for 50 IU/KG to 10.6 ± 2.5 (IU x hr/mL) for 100 IU/KG |
Volume of Distribution | NA |
Clearance | 1207±414 for 50IU/KG and 781± 147 for 100 IU/KG |
Categories | NA |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | NA |
Information of corresponding available drug in the market | |
Brand Name | Ruconest |
Company | Pharming; Santarus, Inc. |
Brand Discription | RUCONEST 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 for | RUCONEST is a C1 esterase inhibitor [recombinant] indicated for the treatment of acute attacks in adult and adolescent patients with hereditary angioedema (HAE). |
Chemical Name | NA |
Formulation | 2100 U/1 |
Physcial Appearnce | powder for solution |
Route of Administration | IV |
Recommended Dosage | IV 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. |
Contraindication | RUCONEST 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 Effects | The 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 Link | http://www.rxlist.com/ruconest-drug/clinical-pharmacology.htm |
PubMed ID | 25673959 |
3-D Structure | N.A. |