Fostamatinib
Fostamatinib Uses, Dosage, Side Effects, Food Interaction and all others data.
Fostamatinib has been investigated for the treatment and basic science of Rheumatoid Arthritis and Immune Thrombocytopenic Purpura (ITP). It was approved on April 17, 2018, under the trade name Tavalisse for use in ITP . Fostamatinib has also been granted orphan drug status by the FDA .
Recently, fostamatinib has been identified as a potential therapeutic for controlling acute respiratory distress syndrome (ARDS) in patients with severe COVID-19 through its ability to modulate the SYK kinase.
The active metabolite of fostamatinib, R406, inhibits signal transduction by Fcγ receptors involved in the antibody-mediated destruction of platelets by immune cells in chronic ITP . This results in increased platelet counts in this population.
| Trade Name | Fostamatinib |
| Availability | Prescription only |
| Generic | Fostamatinib |
| Fostamatinib Other Names | Fostamatinib |
| Related Drugs | Tavalisse, Promacta, prednisone, dexamethasone, triamcinolone, Decadron, Nplate |
| Weight | 100mg, 150mg |
| Type | Oral tablet |
| Formula | C23H26FN6O9P |
| Weight | Average: 580.4595 Monoisotopic: 580.148291177 |
| Protein binding | R406 is 98.3% bound to plasma proteins . |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Fostamatinib is a spleen tyrosine kinase inhibitor used to treat chronic immune thrombocytopenia after attempting one other treatment.
Fostamatinib is indicated for use in the treatment of chronic immune thrombocytopenia (ITP) in patients who have had insufficient response to previous therapy .
Fostamatinib is also used to associated treatment for these conditions: Chronic immune thrombocytopenia
Toxicity
Neither fostamatinib or R406 were found to be carcinogenic or mutagenic . Fostamatinib can cause embryo-fetal mortality or developmental abnormalities at exposures of 0.3-10 times the maximum recommended human dose.
Serious adverse effects include hypertension, neutropenia, diarrhea, and hepatotoxicity
Food Interaction
- Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of fostamatinib.
- Take with or without food.
Fostamatinib Hypertension interaction
[Moderate] The use of fostamatinib may cause hypertension.
It is recommended to monitor blood pressure every 2 weeks until stable, then monthly and to adjust or initiate antihypertensive therapy to ensure maintenance of blood pressure control during treatment.
If increased blood pressure persists despite appropriate therapy, therapy interruption, reduction or discontinuation may be necessary.
Caution should be exercised when using this agent in patients with pre-existing hypertension as they may be more susceptible to the hypertensive effects of fostamatinib.
Fostamatinib Disease Interaction
Moderate: diarrhea, hepatotoxicity, hypertension, neutropenia
Volume of Distribution
R406 has an apparent oral volume of distribution of approximately 400 L .
Elimination Route
Fostmatinib is the methylene phosphate prodrug of R406, the active metabolite . It is extensively hydrolyzed by intestinal alkaline phosphatase. Only negligible amounts of fostamatinib enter systemic circulation .
R406 has an absolute bioavailability of 55% and reaches peak plasma concentrations in approximately 1.5 h . Administration with a high calorie, high fat meal increases exposure by 23% and the maximum plasma concentration by 15%. This may lengthen time to peak plasma concentration to approximately 3 h . Exposure to R406 is known to be dose proportional up to 200 mg twice daily . R406 accumulates 2-3 fold with twice daily dosing at 100-160 mg.
Half Life
R406 has a half-life of elimination of approximately 15 h .
Clearance
R406 has an apparent oral clearance of approximately 300 mL/min .
Elimination Route
About 80% of R406 is excreted in the feces, primarily as the O-glucuronide conjugate and the O-desmethyl metabolite produced by gut bacteria . The remaining 20% is excreted in the urine as the N-glucuronide conjugate.
Innovators Monograph
You find simplified version here Fostamatinib
