Riluzole

Benzothiazole — NERVOUS SYSTEM

Key facts

Riluzole is an ofp drug in the Benzothiazole class catalogued in DrugCentral. It was first approved by the FDA in 1995. DrugCentral lists 12 molecular targets, including SLC6A2, KCNN4 and PTR1. Recorded indications include Amyotrophic lateral sclerosis.

• Approval status: ofp (first approved 1995 by the FDA).
• Drug class: Benzothiazole.
• Molecular targets: SLC6A2, KCNN4, PTR1 and TRPC5 (12 listed in DrugCentral).
• Indications: Amyotrophic lateral sclerosis.
• ATC code: N07XX02 (Other nervous system drugs).
• Molecular formula: C8H5F3N2OS; molecular weight 234.20 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Amyotrophic lateral sclerosis

Contraindications (8)

• Alcoholism
• Drug-induced hepatitis
• Fever greater than 100.4 Fahrenheit
• Hyperbilirubinemia
• Interstitial pneumonia
• Jaundice
• Liver function tests abnormal
• Neutropenic disorder

Mechanism & targets

• Established pharmacologic class: Benzothiazole

Molecular targets (12)

Target	Gene	Action	Activity
Sodium-dependent noradrenaline transporter	SLC6A2	unknown	Ki 5.76
Intermediate conductance calcium-activated potassium channel protein 4	KCNN4	activator	IC50 5.70
Pteridine reductase 1	PTR1	unknown	Ki 5.40
Short transient receptor potential channel 5	TRPC5	activator	EC50 5.04
Small conductance calcium-activated potassium channel protein 3	KCNN3	activator	EC50 4.90
Small conductance calcium-activated potassium channel protein 2	Kcnn2	activator	EC50 4.89
Small conductance calcium-activated potassium channel protein 1	KCNN1	activator	EC50 4.68
Sodium channel protein type 9 subunit alpha	SCN9A	unknown	IC50 4.39
Potassium voltage-gated channel subfamily H member 2	KCNH2	blocker	IC50 4.30
Sodium channel protein type 4 subunit alpha	SCN4A	unknown	IC50 4.29
Glutamate receptor ionotropic, NMDA 3A	GRIN3A	unknown	—
Sodium channel protein type 5 subunit alpha	SCN5A	blocker	—

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1995-12-12	FDA	—	COVIS PHARMA SARL	Yes

ATC classification

ATC code	Therapeutic hierarchy
N07XX02	NERVOUS SYSTEM › OTHER NERVOUS SYSTEM DRUGS › OTHER NERVOUS SYSTEM DRUGS › Other nervous system drugs

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Amyotrophic lateral sclerosis	270.4
Death	251.4
Pancreatitis acute	88.4
Motor neurone disease	87.5
Disease progression	61.8
Portal vein thrombosis	59.0
Respiratory failure	55.5
Interstitial lung disease	53.6
Gastrostomy	50.9
Pancreatitis relapsing	40.1
Pseudocyst	39.2
Inappropriate antidiuretic hormone secretion	39.0

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Riluzole is on its molecule page.

• Molecular formula: C₈H₅F₃N₂OS
• Molecular weight: 234.20 g/mol
• CAS number: 1744-22-5
• InChIKey: FTALBRSUTCGOEG-UHFFFAOYSA-N
• PubChem CID: 5070

NC1=NC2=C(S1)C=C(OC(F)(F)F)C=C2

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Riluzole used for?

DrugCentral lists the following indications for Riluzole: Amyotrophic lateral sclerosis.

How does Riluzole work?

Its molecular targets in DrugCentral include SLC6A2, KCNN4 (activator), PTR1 and TRPC5 (activator).

When was Riluzole first approved?

Riluzole was first approved by the FDA in 1995.

What drug class does Riluzole belong to?

Riluzole is in the Benzothiazole class.

What is the chemical formula of Riluzole?

Riluzole has the molecular formula C8H5F3N2OS and a molecular weight of 234.20 g/mol.

Sources

• DrugCentral drug card 2382 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL744 — compound record and bioactivity
• PubChem CID 5070 — chemical identifiers
• DrugBank DB00740 — drug record
• FDA UNII 7LJ087RS6F — substance identity
• DailyMed: FDA labels for Riluzole — current prescribing information (label search)
• UniProt P23975 (SLC6A2) — target protein
• UniProt O15554 (KCNN4) — target protein
• UniProt Q9UL62 (TRPC5) — target protein
• UniProt Q9UGI6 (KCNN3) — target protein
• UniProt Q92952 (KCNN1) — target protein
• UniProt Q15858 (SCN9A) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.