Riluzole (Rilutek, Tiglutik)

Other Medications · Approved since 1995

US Off-label EU EMA Approved ES Hospital use off-label in CRC Oral 4 Clinical Trials
Glutamate receptors voltage-gated sodium channels

Description

Riluzole is a glutamate release inhibitor and sodium channel blocker originally developed for amyotrophic lateral sclerosis (ALS) that is being repurposed in colorectal cancer as a neuroprotective agent. In CRC treatment, riluzole is primarily used off-label to prevent oxaliplatin-induced peripheral neuropathy, a dose-limiting side effect of FOLFOX-based chemotherapy regimens. The drug has also been explored for managing cancer-related cognitive impairment and as a combination agent with standard CRC therapies like mFOLFOX6 and bevacizumab.

Mechanism of Action

Riluzole inhibits glutamate release from presynaptic nerve terminals and blocks voltage-gated sodium channels, reducing neuronal excitotoxicity. By modulating glutamate neurotransmission and protecting against oxidative stress-induced neuronal damage, riluzole may help preserve nerve function during neurotoxic chemotherapy treatments.

Molecular Targets

Side Effects

Nausea Fatigue Dizziness Decreased lung function Abdominal pain Diarrhea Loss of appetite Vertigo

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT07447050 Phase 2
Recruiting
Riluzole For Preventing Cognitive Dysfunction in Ca Pts Receiving Chemo (REFOCUS): Pilot Trial
United States
NCT06580002 Phase 2
Recruiting
Repurposing Riluzole for Cancer-Related Cognitive Impairment: A Pilot Trial
United States
NCT04761614 Phase 1
Archived
Riluzole in Combination With mFOLFOX6 and Bevacizumab in Treating Patients With Metastatic Colorectal Cancer
United States
NCT03722680 Phase 2
Suspended
Effectiveness Assessment of Riluzole in the Prevention of Oxaliplatin-induced Peripheral Neuropathy.
France