masitinib   Click here for help

GtoPdb Ligand ID: 5656

Synonyms: AB-1010 | AB1010 | Masican® (proposed trade name)
PDB Ligand Immunopharmacology Ligand
Compound class: Synthetic organic
Comment: Using the trade name Masivet, this compound has been used for several years to treat mast cell tumours in dogs [6]. It is a receptor tyrosine kinase (RTK) inhibitor, with inhibitory activity at the cKIT, platelet derived growth factor receptor (PDGFR) and fibroblast growth factor receptor (FGFR) RTKs [4].

SARS-CoV-2: Using X-ray crystallography, masitinib has been shown to bind (non-covalently) into the catalytic site of the SARS-CoV-2 3CL protease (Mpro) [3], which corresponds with detection of in vitro Mpro inhibitory activity. It does not bind to the other viral protease PLpro.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 7
Hydrogen bond donors 2
Rotatable bonds 8
Topological polar surface area 101.63
Molecular weight 498.22
XLogP 3.41
No. Lipinski's rules broken 0
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Canonical SMILES CN1CCN(CC1)Cc1ccc(cc1)C(=O)Nc1ccc(c(c1)Nc1scc(n1)c1cccnc1)C
Isomeric SMILES CN1CCN(CC1)Cc1ccc(cc1)C(=O)Nc1ccc(c(c1)Nc1scc(n1)c1cccnc1)C
InChI InChI=1S/C28H30N6OS/c1-20-5-10-24(16-25(20)31-28-32-26(19-36-28)23-4-3-11-29-17-23)30-27(35)22-8-6-21(7-9-22)18-34-14-12-33(2)13-15-34/h3-11,16-17,19H,12-15,18H2,1-2H3,(H,30,35)(H,31,32)
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Summary of Clinical Use Click here for help
The European Medicines Agency has granted masitinib orphan designation as a treatment for pancreatic cancer, amyotrophic lateral sclerosis (ALS, a.k.a. motor neurone disease, MND) and mastocytosis. It has been evaluated in clinical trials for a number of inflammatory conditions, solid tumours, multiple myeloma, ALS and Alzheimer's disease. Click here to link to's complete listing of masitinib trials (note that many of these are not active or have been terminated). In June 2021, a Phase 3 study testing the safety and effectiveness of masitinib as an add-on treatment to riluzole for ALS was announced by AB Science.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT02588677 Masitinib in Combination With Riluzole for the Treatment of Patients Suffering From Amyotrophic Lateral Sclerosis (ALS) Phase 2/Phase 3 Interventional AB Science
NCT03127267 Efficacy and Safety of Masitinib Versus Placebo in the Treatment of ALS Patients Phase 3 Interventional AB Science