ibudilast   Click here for help

GtoPdb Ligand ID: 7399

Synonyms: AV-411 | KC-404 | Ketas® | MN-166
Approved drug PDB Ligand Immunopharmacology Ligand
ibudilast is an approved drug
Compound class: Synthetic organic
Comment: Ibudilast is a phosphodiesterase (PDE) inhibitor antiinflammatory drug. See the Biological activity tab for affinity data across a range of PDE isozymes.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 2
Hydrogen bond donors 0
Rotatable bonds 3
Topological polar surface area 34.37
Molecular weight 230.14
XLogP 2.65
No. Lipinski's rules broken 0
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Canonical SMILES CC(C(=O)c1c(nn2c1cccc2)C(C)C)C
Isomeric SMILES CC(C(=O)c1c(nn2c1cccc2)C(C)C)C
InChI InChI=1S/C14H18N2O/c1-9(2)13-12(14(17)10(3)4)11-7-5-6-8-16(11)15-13/h5-10H,1-4H3
No information available.
Summary of Clinical Use Click here for help
Ibudilast is an anti-inflammatory and neuroprotective drug. It prolongs time-to-first relapse and attenuates brain volume shrinkage in patients with relapsing-remitting (RR) and/or secondary progressive (SP) multiple sclerosis (MS). Phase 2 evidence of ibudilast-related reduction in brain shrinkage in MS patients with progressive disease was published in August 2018 [3]. However, there is no information regarding full approval for clinical use of this drug on the US FDA or European Medicines Agency websites. Individual national agencies may have granted marketing authorisation. The EMA has authorised use (in 2016) of ibudilast as an orphan drug for the treatment of amyotrophic lateral sclerosis.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Mechanism of action is complex, involving PDE inhibition, NO inhibition, and reduction in reactive oxygen species (neuroprotective action).