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
Fostamatinib
Fostamatinib

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

*** Taking medicines without doctor's advice can cause long-term problems.
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