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Conestat alfa | CAS No: 80295-38-1 | GMP-certified suppliers
A medication that treats acute hereditary angioedema attacks in adults by replacing deficient C1 esterase inhibitor to regulate complement and contact system pathways.
Therapeutic categories
Primary indications
- For the treatment of acute attacks of hereditary angioedema (HAE) due to C1 esterase inhibitor deficiency in adults
Product Snapshot
- Conestat alfa is formulated as an injectable powder and solution for intravenous administration
- It is indicated for the treatment of acute attacks of hereditary angioedema (HAE) related to C1 esterase inhibitor deficiency in adults
- The product is approved or investigational in key regulatory markets including the European Union and the United States
Clinical Overview
Clinically, conestat alfa is indicated for the treatment of acute attacks of hereditary angioedema (HAE) due to C1 esterase inhibitor deficiency in adults. HAE is characterized by episodic swelling caused by increased vascular permeability linked to uncontrolled activation of plasma kallikrein and resultant bradykinin overproduction. The deficiency in C1 esterase inhibitor leads to unregulated cleavage of complement components C4 and C2, further amplifying the complement cascade and contributing to symptomatology.
Mechanistically, conestat alfa replaces the deficient endogenous inhibitor, restoring regulation across the complement, contact, coagulation, and fibrinolytic systems. In addition to inhibiting proteases in the complement and contact pathways, it also modulates thrombin activity in coagulation and tissue plasminogen activator (tPA) and plasmin in fibrinolysis. This multifaceted protease inhibition stabilizes vascular permeability and reverses acute HAE attacks.
Pharmacodynamically, administration of 50 U/kg intravenously elevates plasma C1INH activity levels above 0.7 U/mL, which is considered the lower limit of normal in HAE patients. This repletion correlates with clinical resolution of angioedema symptoms.
Safety considerations include hypersensitivity reactions to rabbit proteins due to the transgenic source of the recombinant protein. Immunogenicity and potential for allergic responses should be monitored during treatment.
Conestat alfa is marketed under the trade name Ruconest, approved by the US Food and Drug Administration for acute HAE attack management in adults. It is classified among serine protease inhibitors and complement system proteins used specifically for hereditary angioedema therapy.
From an API sourcing perspective, quality assurance should prioritize consistency in glycosylation patterns and control of host-derived impurities, given the recombinant origin in a transgenic animal system. Compliance with regulatory standards for biologics and traceability of transgenic sources are essential for ensuring reproducible clinical performance.
Identification & chemistry
| Generic name | Conestat alfa |
|---|---|
| Molecule type | Biotech |
| CAS | 80295-38-1 |
| UNII | 5QS67N4551 |
| DrugBank ID | DB09228 |
Pharmacology
| Summary | This drug acts as a replacement C1 esterase inhibitor, targeting key proteases involved in the complement and contact system pathways, including activated C1s, kallikrein, and factor XIIa. By restoring inhibition of these enzymes, it modulates complement activation, coagulation, and fibrinolytic processes, reducing excessive bradykinin production that leads to vascular leakage. Its primary therapeutic intent is to manage acute attacks of hereditary angioedema associated with C1 inhibitor deficiency. |
|---|---|
| Mechanism of action | The primary function of endogenous C1INH is to regulate the activation of the complement and contact system pathways. It does this through inhibition of several target proteases within these pathways including activated C1s, kallikrein, factor XIIa and factor XIa. C1 esterase inhibitor has also been shown to inhibit the action of thrombin within the coagulation pathway, and tPA and plasmin within the fibrinolytic pathway. Deficiency of C1-inhibitor allows increased plasma kallikrein activation and subsequent production of bradykinin. Additionally, C4 and C2 cleavage is no longer inhibited allowing auto-activation of the complement system. Down-stream effects of the lack of enzyme inhibition by C1 esterase inhibitor results in swelling due to leakage of fluid from blood vessels into connective tissue and consequently the presentation of hereditary angioedema (HAE). Replacement of C1 esterase inhibitor results in a reversal of these effects. |
| Pharmacodynamics | A dose of 50 U/kg of Ruconest increases plasma C1INH activity levels to greater than 0.7 U/mL (the lower limit of normal) in HAE patients. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Complement C1r subcomponent | Humans | inhibitor |
| Complement C1s subcomponent | Humans | inhibitor |
| Plasma kallikrein | Humans | inhibitor |
ADME / PK
| 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. |
|---|---|
| Route of elimination | Elimination half-life was approximately 2.5 hours. |
| Clearance | Clearance was found to be 1207 ± 414 mL/hr following administration of 50 U/kg. |
Formulation & handling
- Conestat alfa is a biotech-derived peptide formulated for parenteral and intravenous administration, requiring sterile preparation.
- The API is supplied as a powder for reconstitution or as a liquid solution, indicating sensitivity to moisture and necessitating appropriate storage conditions.
- Due to its protein nature, conestat alfa should be handled under controlled temperature to maintain stability and biological activity.
Regulatory status
| Lifecycle | The API is currently marketed in both the EU and US, with patent protection having expired in the EU and pending expiration in the US within the next 12 months. This positioning indicates a mature market in the EU and an approaching shift toward increased generic competition in the US. |
|---|
| Markets | EU, US |
|---|
Supply Chain
| Supply chain summary | Conestat alfa is produced by a limited number of originator companies, with its branded product Ruconest marketed primarily in the EU and US regions. The presence in major markets suggests established supply channels, while patent expiry status is not specified, indicating either existing or impending generic competition. |
|---|
Safety
| 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. |
|---|
- May cause headache, nausea, and diarrhea in ≥ 2% of subjects during clinical use
- Associated with risk of arterial and venous thromboembolic events, particularly in patients with predisposing risk factors
- Use caution and monitor for thromboembolic complications in the presence of indwelling venous catheters, history of thrombosis, or related risk conditions
Conestat alfa is a type of Hemostatics
Hemostatics, a subcategory of pharmaceutical active pharmaceutical ingredients (APIs), play a crucial role in promoting hemostasis, the process of blood clotting, to control bleeding. These essential medical substances are widely used in surgical procedures, trauma cases, and various medical conditions where excessive bleeding is a concern.
Hemostatics function by either promoting the aggregation of platelets or enhancing the coagulation cascade, thus facilitating clot formation and preventing blood loss. Several types of hemostatic agents are available, including topical agents, injectable agents, and absorbable sponges.
Topical hemostatic agents are commonly used in minor surgeries and dental procedures. These agents, such as oxidized regenerated cellulose and gelatin-based products, are applied directly to the bleeding site to induce clot formation and achieve hemostasis.
Injectable hemostatics, on the other hand, are administered intravenously or intramuscularly and work systemically to promote blood clotting. Examples of injectable hemostatics include recombinant factor VIIa and fibrinogen concentrates, which are employed in cases of severe bleeding or hemophilia.
Absorbable sponges, often made of gelatin or collagen, are frequently used in surgical procedures to control bleeding. These sponges absorb blood, swell, and create a physical barrier that supports clot formation.
Hemostatics have revolutionized medical practices by reducing blood loss during surgeries, improving patient outcomes, and minimizing the need for blood transfusions. They have become indispensable tools in various medical specialties, including cardiovascular surgery, orthopedics, and trauma care.
In conclusion, hemostatics are vital pharmaceutical APIs that promote hemostasis and prevent excessive bleeding. Their application in medical procedures ensures efficient clot formation and enhances patient safety.
Conestat alfa (Hemostatics), classified under Central Nervous System Agents
Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.
CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.
The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.
Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.
Conestat alfa API manufacturers & distributors
Compare qualified Conestat alfa API suppliers worldwide. We currently have 1 companies offering Conestat alfa API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Sanofi | Producer | France | France | CoA, GMP | 93 products |
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