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| Primary information |
|---|
| ID | 10750 |
| Therapeutic ID | Th1173 |
| Protein Name | Conestat alfa |
| Sequence | NA
|
| Molecular Weight | 67000 |
| 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 | The common adverse reactions (= 2%) reported in clinical trials were headache, nausea, and diarrhea. Serious arterial and venous thromboembolic (TE) events have been reported at the recommended dose of plasma derived C1 esterase inhibitor products in patients with risk factors. Risk factors may include the presence of an indwelling venous catheter/access device, prior history of thrombosis, underlying atherosclerosis, use of oral contraceptives or certain androgens, morbid obesity, and immobility. Monitor patients with known risk factors for TE events during and after administration. |
| Metabolism | NA |
| Absorption | Mean Cmax was found to be 1.2 U/mL and Tmax was 0.31 ± 0.10 hr following administration of 50 U/kg. |
| NA |
| Clearance | Clearance was found to be 1207 ± 414 mL/hr following administration of 50 U/kg. |
| Categories | NA |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | Complement C1r subcomponent,Complement C1s subcomponent,Plasma kallikrein,Coagulation factor XII,Prothrombin,Coagulation factor XI,Tissue-type plasminogen activator |
| Brand Name | Ruconest |
| Company | Pharming; Santarus, Inc. |
| Brand Description | Pharming; Santarus, Inc. |
| 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 |
| Physical Appearance | 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 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |