- Molecular NameRiluzole
- Synonymriluzole
- Weight234.201
- Drugbank_IDDB00740
- ACS_NO1744-22-5
- Show 2D model
- LogP (experiment)2.784
- LogP (predicted, AB/LogP v2.0)2.66
- pka6.5
- LogD (pH=7, predicted)2.66
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-3.81
- LogSw (predicted, AB/LogsW2.0)0.16
- Sw (mg/ml) (predicted, ACD/Labs)0.04
- No.of HBond Donors2
- No.of HBond Acceptors3
- No.of Rotatable Bonds2
- TPSA76.38
- StatusFDA approved
- AdministrationN/A
- PharmacologyA drug for the treatment of amyotrophic lateral sclerosis (ALS, Lou Gehrig's Disease). A glutamate antagonist (receptors, glutamate) used as an anticonvulsant (anticonvulsants) and to prolong the survival of patients with amyotrophic lateral sclerosis.
- Absorption_value90.0
- Absorption (description)Riluzole is well-absorbed (approximately 90%), with average absolute oral bioavailability of about 60% (CV=30%). A high fat meal decreases absorption, reducing AUC by about 20% and peak blood levels by about 45%.
- Caco_2N/A
- Bioavailability64.0
- Protein binding97.0
- Volume of distribution (VD)3.4 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmRiluzole is extensively metabolized to six major and a number of minor metabolites, which have not all been identified to date. Metabolism is mostly hepatic, consisting of cytochrome P450–dependent hydroxylation and glucuronidation. CYP1A2 is the primary isozyme involved in N-hydroxylation; CYP2D6, CYP2C19, CYP3A4, and CYP2E1 are considered unlikely to contribute significantly to riluzole metabolism in humans.
- Half life14 h
- ExcretionN/A
- Urinary Excretion<1
- Clerance5.5 ml/min/kg
- ToxicityThe most commonly observed AEs associated with the use of RILUTEK more frequently than placebo treated patients, were: asthenia, nausea, dizziness, decreased lung function, diarrhea, abdominal pain, pneumonia, vomiting, vertigo, circumoral paresthesia, anorexia, and somnolence.
- LD50 (rat)N/A
- LD50 (mouse)N/A