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riluzole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2382 | 1744-22-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
The etiology and pathogenesis of amyotrophic lateral sclerosis (ALS) are not known, although a number of hypotheses have been advanced. One hypothesis is that motor neurons, made vulnerable through either genetic predisposition or environmental factors, are injured by glutamate. In some cases of familial ALS the enzyme superoxide dismutase has been found to be defective. The mode of action of riluzole is unknown. Its pharmacological properties include the following, some of which may be related to its effect: 1) an inhibitory effect on glutamate release, 2) inactivation of voltage-dependent sodium channels, and 3) ability to interfere with intracellular events that follow transmitter binding at excitatory amino acid receptors. Riluzole has also been shown, in a single study, to delay median time to death in a transgenic mouse model of ALS. These mice express human superoxide dismutase bearing one of the mutations found in one of the familial forms of human ALS. It is also neuroprotective in various in vivo experimental models of neuronal injury involving excitotoxic mechanisms. In in vitro tests, riluzole protected cultured rat motor neurons from the excitotoxic effects of glutamic acid and prevented the death of cortical neurons induced by anoxia. Due to its blockade of glutamatergic neurotransmission, riluzole also exhibits myorelaxant, sedative, and anticonvulsant properties.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 2 % | Benet LZ, Broccatelli F, Oprea TI |
| BA (Bioavailability) | 64 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 3.50 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 11.30 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.04 % | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.348 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.526 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 71.121 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 12.706 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 7.010 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 9.110 | % | High | 1 |
| herg | hERG pIC50 | 4.508 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 9.290 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 26.002 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 4.120 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ALK,AURKA,AXL,BRAF,CAMK2B,CAMK2D,CDK1,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,ITK,JAK1,MAP3K1,MAP3K10,MAP3K21,MAPK10,MAPK7,MARK4,MET,MTOR,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,SIK2,SIK3,STK33,TTK,ULK1 | 40 | |||
| kinase-selectivity-class | DYRK1B,EIF2AK3,GRK2,MAPK7,PDK4 | 5 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.918 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 24.378 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 6.050 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.372 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | High | 1 | |
| pppb | Pig plasma protein binding (% unbound) | 4.440 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 12.162 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 40.060 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 6.950 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 101.158 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 12, 1995 | FDA | COVIS PHARMA SARL |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Amyotrophic lateral sclerosis | 120.74 | 36.07 | 19 | 808 | 1329 | 90626291 |
| Death | 120.05 | 36.07 | 65 | 762 | 456486 | 90171134 |
| Depersonalisation/derealisation disorder | 36.11 | 36.07 | 7 | 820 | 1625 | 90625995 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Amyotrophic lateral sclerosis | 131.70 | 31.25 | 23 | 1047 | 1089 | 42619176 |
| Death | 77.27 | 31.25 | 75 | 995 | 471110 | 42149155 |
| Pancreatitis acute | 67.78 | 31.25 | 27 | 1043 | 33537 | 42586728 |
| Portal vein thrombosis | 58.39 | 31.25 | 15 | 1055 | 4534 | 42615731 |
| Pancreatitis relapsing | 49.89 | 31.25 | 9 | 1061 | 510 | 42619755 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Amyotrophic lateral sclerosis | 175.59 | 29.39 | 30 | 1663 | 2061 | 110585545 |
| Pancreatitis acute | 82.69 | 29.39 | 32 | 1661 | 60242 | 110527364 |
| Death | 81.02 | 29.39 | 74 | 1619 | 698795 | 109888811 |
| Portal vein thrombosis | 59.17 | 29.39 | 15 | 1678 | 7043 | 110580563 |
| Gastrostomy | 50.49 | 29.39 | 10 | 1683 | 1540 | 110586066 |
| Pancreatitis relapsing | 44.60 | 29.39 | 9 | 1684 | 1523 | 110586083 |
| Respiratory failure | 42 | 29.39 | 31 | 1662 | 215301 | 110372305 |
| Interstitial lung disease | 36.37 | 29.39 | 24 | 1669 | 139310 | 110448296 |
| Inappropriate antidiuretic hormone secretion | 36.06 | 29.39 | 15 | 1678 | 33836 | 110553770 |
| Pseudocyst | 35.84 | 29.39 | 6 | 1687 | 362 | 110587244 |
| Motor neurone disease | 31.79 | 29.39 | 6 | 1687 | 718 | 110586888 |
| Dysphoria | 31.77 | 29.39 | 9 | 1684 | 6419 | 110581187 |
| Depersonalisation/derealisation disorder | 30.47 | 29.39 | 7 | 1686 | 2174 | 110585432 |
| Disease progression | 30.30 | 29.39 | 27 | 1666 | 244007 | 110343599 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N07XX02 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS OTHER NERVOUS SYSTEM DRUGS Other nervous system drugs |
| FDA CS | M0483511 | Benzothiazoles |
| FDA EPC | N0000175740 | Benzothiazole |
| CHEBI has role | CHEBI:35469 | antidepressant |
| CHEBI has role | CHEBI:35476 | antipsychotic agent |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:35705 | immunosuppressive agent |
| CHEBI has role | CHEBI:38070 | anti-arrhythmia drug |
| MeSH PA | D000927 | Anticonvulsants |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018691 | Excitatory Amino Acid Antagonists |
| MeSH PA | D018696 | Neuroprotective Agents |
| MeSH PA | D020011 | Protective Agents |
Related Drugs by ATC class:
N07XX Other nervous system drugs 23 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Amyotrophic lateral sclerosis | indication | 86044005 | DOID:332 |
| Alcoholism | contraindication | 7200002 | |
| Hyperbilirubinemia | contraindication | 14783006 | DOID:2741 |
| Jaundice | contraindication | 18165001 | |
| Interstitial pneumonia | contraindication | 64667001 | |
| Liver function tests abnormal | contraindication | 166603001 | |
| Drug-induced hepatitis | contraindication | 235876009 | |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Fever greater than 100.4 Fahrenheit | contraindication | 426000000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.47 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 50MG/10ML | TIGLUTIK KIT | ITALFARMACO SA | N209080 | Sept. 5, 2018 | RX | SUSPENSION | ORAL | 8765150 | March 12, 2029 | A METHOD OF TREATING AMYOTROPHIC LATERAL SCLEROSIS IN A PATIENT IN NEED OF SUCH TREATMENT, SAID METHOD COMPRISING ADMINISTERING TO SAID PATIENT AN EFFECTIVE AMOUNT OF A SUSPENSION ACCORDING TO CLAIM 1 |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sodium channel protein type 5 subunit alpha | Ion channel | BLOCKER | WOMBAT-PK | CHEMBL | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | BLOCKER | IC50 | 4.30 | IUPHAR | ||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 5.77 | DRUG MATRIX | |||||
| Sodium channel protein type 4 subunit alpha | Ion channel | IC50 | 4.29 | CHEMBL | |||||
| Sodium channel protein type 9 subunit alpha | Ion channel | IC50 | 4.39 | CHEMBL | |||||
| Intermediate conductance calcium-activated potassium channel protein 4 | Ion channel | ACTIVATOR | IC50 | 5.70 | IUPHAR | ||||
| Glutamate receptor ionotropic, NMDA 3A | Ion channel | WOMBAT-PK | |||||||
| Small conductance calcium-activated potassium channel protein 3 | Ion channel | ACTIVATOR | EC50 | 4.90 | IUPHAR | ||||
| Small conductance calcium-activated potassium channel protein 1 | Ion channel | ACTIVATOR | EC50 | 4.68 | IUPHAR | ||||
| Short transient receptor potential channel 5 | Ion channel | ACTIVATOR | EC50 | 5.04 | IUPHAR | ||||
| Pteridine reductase 1 | Enzyme | Ki | 5.40 | CHEMBL | |||||
| Small conductance calcium-activated potassium channel protein 2 | Ion channel | ACTIVATOR | EC50 | 4.89 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4020941 | VUID |
| N0000148421 | NUI |
| D00775 | KEGG_DRUG |
| 4020941 | VANDF |
| C0073379 | UMLSCUI |
| CHEBI:8863 | CHEBI |
| 657 | PDB_CHEM_ID |
| CHEMBL744 | ChEMBL_ID |
| DB00740 | DRUGBANK_ID |
| D019782 | MESH_DESCRIPTOR_UI |
| 5070 | PUBCHEM_CID |
| 2326 | IUPHAR_LIGAND_ID |
| 5912 | INN_ID |
| 7LJ087RS6F | UNII |
| 196501 | RXNORM |
| 162294 | MMSL |
| 5067 | MMSL |
| 5425 | MMSL |
| d03869 | MMSL |
| 005183 | NDDF |
| 109141001 | SNOMEDCT_US |
| 386980005 | SNOMEDCT_US |
| 7LJ087RS6F | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Riluzole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-775 | TABLET, FILM COATED | 50 mg | ORAL | ANDA | 26 sections |
| Riluzole | Human Prescription Drug Label | 1 | 62756-538 | TABLET, FILM COATED | 50 mg | ORAL | ANDA | 26 sections |
| Riluzole | Human Prescription Drug Label | 1 | 67877-286 | TABLET | 50 mg | ORAL | ANDA | 27 sections |
| riluzole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68462-381 | TABLET, FILM COATED | 50 mg | ORAL | ANDA | 26 sections |
| RILUZOLE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69076-200 | TABLET, FILM COATED | 50 mg | ORAL | ANDA | 18 sections |
| TIGLUTIK | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70726-0303 | LIQUID | 50 mg | ORAL | NDA | 31 sections |
| Teglutik | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70726-0304 | LIQUID | 5 mg | ORAL | Unapproved drug for use in drug shortage | 2 sections |
| Teglutik | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70726-0305 | LIQUID | 5 mg | ORAL | Unapproved drug for use in drug shortage | 2 sections |
| Teglutik | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70726-0306 | LIQUID | 5 mg | ORAL | Unapproved drug for use in drug shortage | 2 sections |