fostamatinib

Ligand id: 7796

Name: fostamatinib

Structure and Physico-chemical Properties

2D Structure
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Calculated Physico-chemical Properties
Hydrogen bond acceptors 11
Hydrogen bond donors 4
Rotatable bonds 10
Topological polar surface area 196.53
Molecular weight 580.15
XLogP 1.06
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Fostamatinib (as the disodium hexahydrate salt) received FDA approval for the treatment of chronic immune thrombocytopenia (ITP) [5] in April 2018, in particular for the treatment of patients with an inadequete response to previous treatment.
Fostamatinib has completed Phase 3 clinical trials for rheumatoid arthritis [3] (NCT01197534 & NCT01197755), and Phase 2 for a range of solid tumours (NCT00923481).
Mechanism Of Action and Pharmacodynamic Effects
The active moeity, tamatinib inhibits Syk kinase-mediated IgE- and IgG-mediated activation of Fc gamma receptor signaling, resulting in inhibition of the activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage [1,4].