Fostamatinib

Fostamatinib
Clinical data
Trade namesTavalisse, Tavlesse
Other namesFostamatinib disodium hexahydrate, tamatinib fosdium, R-788, NSC-745942, R-935788
AHFS/Drugs.comMonograph
MedlinePlusa618025
License data
Pregnancy
category
  • Not recommended
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability55% (tamatinib metabolite)
Protein binding98% (tamatinib metabolite)
MetabolismGut (ALP to tamatinib)
Liver (tamatinib metabolite by CYP3A4, UGT1A9)
Elimination half-life15 hours
Excretionfaecal (80%), urine (20%)
Identifiers
  • [6-({5-Fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl}amino)-2,2-dimethyl-3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl]methyl dihydrogen phosphate
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.125.771 Edit this at Wikidata
Chemical and physical data
FormulaC23H26FN6O9P
Molar mass580.466 g·mol−1
3D model (JSmol)
  • Fc1cnc(nc1Nc2nc3N(C(=O)C(Oc3cc2)(C)C)COP(=O)(O)O)Nc4cc(OC)c(OC)c(OC)c4
  • InChI=1S/C23H26FN6O9P/c1-23(2)21(31)30(11-38-40(32,33)34)20-14(39-23)6-7-17(28-20)27-19-13(24)10-25-22(29-19)26-12-8-15(35-3)18(37-5)16(9-12)36-4/h6-10H,11H2,1-5H3,(H2,32,33,34)(H2,25,26,27,28,29) checkY

Fostamatinib, sold under the brand names Tavalisse and Tavlesse, is a tyrosine kinase inhibitor medication for the treatment of chronic immune thrombocytopenia (ITP).[2][3] The drug is administered by mouth.[2][3]

Fostamatinib blocks the activity of the enzyme spleen tyrosine kinase (SYK).[3] This enzyme is involved in stimulating parts of the immune system.[3] By blocking SYK's activity, fostamatinib reduces the immune system's destruction of platelets, so allowing the platelet count to rise, which reduces the likelihood of excessive bleeding.[3]

The most commonly reported side effects are diarrhea, high blood pressure, nausea, respiratory infection, dizziness, increased liver enzymes, rash, abdominal pain, fatigue, chest pain and decreased white blood cell count.[4][3]

The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.[5]

  1. ^ "Summary Basis of Decision (SBD) for Tavalisse". Health Canada. 23 October 2014. Retrieved 29 May 2022.
  2. ^ a b c "Tavalisse- fostamatinib tablet". DailyMed. 10 May 2018. Retrieved 5 May 2020.
  3. ^ a b c d e f g "Tavlesse EPAR". European Medicines Agency (EMA). 12 November 2019. Retrieved 26 March 2020. Public Domain This article incorporates text from this source, which is in the public domain.
  4. ^ Cite error: The named reference Tavalisse snapshot was invoked but never defined (see the help page).
  5. ^ New Drug Therapy Approvals 2018 (PDF). U.S. Food and Drug Administration (FDA) (Report). January 2019. Retrieved 16 September 2020.