fasenra
fasenra Uses, Dosage, Side Effects, Food Interaction and all others data.
fasenra is a humanized recombinant monoclonal antibody of the isotype IgG1k immunoglobulin that specifically binds to the alpha chain of the interleukin 5 receptor (IL-5R) expressed on eosinophils and basophils. It inhibits the binding of IL-5 as well as the hetero-oligomerization of the alpha and beta subunits of the IL-5R, thus blocking, signal transduction. Besides, it is an afucosylated IgG which gives it high affinity for the FcγRIIIα receptor in natural killer cells, macrophages and neutrophils. fasenra, FDA approved on November 14, 2017, was developed by MedImmune, the AstraZeneca's global biologic research and development arm.
Eosinophils are the key target of inflammatory respiratory diseases and they undergo apoptosis in absence of IL-5. Therefore, benralizumab action on the IL-5 receptor in basophils and eosinophils produces the apoptosis and its significant reduction in the blood. On the other hand, fasenra binding to natural killer cells FcγRIIIα receptor produces a direct antibody-dependent cell-mediated cytotoxicity. All these effects produce a reduction in eosinophil count in airway mucosa, submucosa, sputum, blood and bone marrow.
| Trade Name | fasenra |
| Availability | Prescription only |
| Generic | Benralizumab |
| Benralizumab Other Names | Benralizumab |
| Related Drugs | Fasenra, Trelegy Ellipta, prednisone, Breo Ellipta, Xopenex, Dulera, Atrovent |
| Weight | 30mg/ml, |
| Type | Solution, Injection, Subcutaneous Solution |
| Formula | C6492H10060N1724O2028S42 |
| Weight | 146054.0 Da |
| Protein binding | There is no reports indicating that Benralizumab binds to plasma proteins. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | Astrazeneca Ab, Astrazeneca Uk Limited |
| Available Country | Saudi Arabia, Australia, Canada, United Kingdom, United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
fasenra is a monoclonal antibody used to treat eosinophilic asthma.
fasenra is indicated as a maintenance treatment of patients 12 years or older with severe asthma and an eosinophilic phenotype. The pathology of severe asthma with eosinophilic phenotype is also denotated as TH2-high phenotype. The patients with this phenotype are characterized by the expression of IL-5 and IL-13, airway hyperresponsiveness, responsiveness to inhaled corticosteroids, high serum IgE and eosinophilia in blood and airway. In the TH2-high phenotype, IL-5 presents a central role as it is responsible for eosinophil differentiation, survival, activation and migration to the lungs.
fasenra is also used to associated treatment for these conditions: Severe Eosinophilic Asthma
How fasenra works
Interleukin-5 (IL-5) induces an eosinophil-mediated inflammatory response by binding to the IL-5 receptor (IL-5R) expressed in eosinophils, basophils and some mast cells. fasenra, unlike IL-5 low-affinity binding, binds with high affinity to the domain I of the α-chain of IL-5R and blocks its signaling and the proliferation of IL-5-dependent cell lines. On the other hand, fasenra is an afucosylated antibody in the CH2 region which gives it a high affinity for the FcγRIIIa on natural killer cells, macrophages and neutrophils. This binding triggers a magnified apoptosis response in eosinophils via antibody-dependent cell-mediated cytotoxicity.
Toxicity
There are not reports of long-term studies regarding tumorgenesis or carcinogenesis. Fertility studies performed in aminal trials showed no adverse histopathological findings.
Food Interaction
No interactions found.fasenra Disease Interaction
Volume of Distribution
Pharmacokinetic reports of fasenra showed a volume of distribution in a range of 52-93ml/kg. For a 70kg individual, the central volume of distribution of fasenra is 3.2 L while the peripheral volume of distribution is reported to be 2.5 L.
Elimination Route
Subcutaneous administration of fasenra presented a dose-proportional pharmacokinetic profile. The administration of 20-200 mg presented an absorption half-life of 3.6 days with a bioavailability of 58%. It is also reported for fasenra a Cmax of 82 mcg/ml and AUC of 775 mcg day/ml.
Half Life
The half-life of fasenra is estimated to be 15-18 days.
Clearance
For a subject weighting 70kg, the typical systemic clearance is 0.29L/day.
Elimination Route
Benraluzimab presents a linear pharmacokinetic without target-receptor mediated clearance. The presence of a dose-proportional pharmacokinetics suggests a rapid depletion of the target and an elimination mainly mediated through the reticuloendothelial system.
Innovators Monograph
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