- Guide to PHARMACOLOGY
Synonyms: Rilutek® | RP-54274 | Tiglutik® (thickened oral suspension)
riluzole is an approved drug (FDA (1995), EMA (1996))
Compound class: Synthetic organic
Comment: Marketed formulations may contain riluzole hydrochloride (PubChem CID 6419992).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|No information available.|
|Summary of Clinical Use|
|Used in the treatment of amyotrophic lateral sclerosis (ALS, a.k.a. motor neurone disease or MND).
Riluzole, along with amiloride and fluoxetine are repurposing candidates as potential therapeutics for secondary progressive multiple sclerosis (SPMS or late MS), having already been shown to provide neuroprotective benefit [2,6-8]. A Phase 2 clinical trial in secondary progressive MS (NCT01910259, MS-SMART trial) is ongoing (Jan 2018).
|Mechanism Of Action and Pharmacodynamic Effects|
|The mechanism of action of riluzole is complex, and appears to include inhibition of glutamate release, inactivation of voltage-dependent sodium channels and interference with intracellular events that follow transmitter binding at excitatory amino acid receptors. Due to the complex nature of this drug's MMOA, we do not tag a primary drug target.|
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT01910259||MS-SMART: Multiple Sclerosis-Secondary Progressive Multi-Arm Randomisation Trial||Phase 2 Interventional||University College, London|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)