Stem definition | Drug id | CAS RN |
---|---|---|
2382 | 1744-22-5 |
Dose | Unit | Route |
---|---|---|
0.10 | g | O |
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 |
Date | Agency | Company | Orphan |
---|---|---|---|
Dec. 12, 1995 | FDA | COVIS PHARMA SARL |
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 | 82.98 | 38.18 | 14 | 645 | 1053 | 50603412 |
Death | 81.83 | 38.18 | 51 | 608 | 325328 | 50279137 |
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 | 80.84 | 33.07 | 15 | 830 | 876 | 29572806 |
Death | 65.90 | 33.07 | 63 | 782 | 342021 | 29231661 |
Portal vein thrombosis | 56.18 | 33.07 | 14 | 831 | 3295 | 29570387 |
Pancreatitis acute | 38.16 | 33.07 | 17 | 828 | 24368 | 29549314 |
Pancreatitis relapsing | 37.38 | 33.07 | 7 | 838 | 428 | 29573254 |
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 | 126.40 | 28.75 | 23 | 1348 | 1627 | 64495734 |
Portal vein thrombosis | 54.53 | 28.75 | 14 | 1357 | 4977 | 64492384 |
Death | 51.81 | 28.75 | 57 | 1314 | 482648 | 64014713 |
Interstitial lung disease | 49.79 | 28.75 | 29 | 1342 | 97703 | 64399658 |
Pancreatitis acute | 42.83 | 28.75 | 20 | 1351 | 42835 | 64454526 |
Inappropriate antidiuretic hormone secretion | 40.88 | 28.75 | 16 | 1355 | 22273 | 64475088 |
Pancreatitis relapsing | 34.53 | 28.75 | 7 | 1364 | 871 | 64496490 |
Dysphoria | 32.25 | 28.75 | 9 | 1362 | 4379 | 64492982 |
Depersonalisation/derealisation disorder | 30.17 | 28.75 | 7 | 1364 | 1633 | 64495728 |
Disease progression | 28.99 | 28.75 | 24 | 1347 | 141656 | 64355705 |
None
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 |
MeSH PA | D000927 | Anticonvulsants |
MeSH PA | D002491 | Central Nervous System Agents |
MeSH PA | D018691 | Excitatory Amino Acid Antagonists |
MeSH PA | D018696 | Neuroprotective Agents |
MeSH PA | D018377 | Neurotransmitter Agents |
MeSH PA | D020011 | Protective Agents |
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 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 3.47 | Basic |
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 SPA | 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 |
None
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 | |||||
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 |
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 |
5912 | INN_ID |
2326 | IUPHAR_LIGAND_ID |
7LJ087RS6F | UNII |
196501 | RXNORM |
162294 | MMSL |
5067 | MMSL |
5425 | MMSL |
d03869 | MMSL |
005183 | NDDF |
109141001 | SNOMEDCT_US |
386980005 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Riluzole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-4145 | TABLET, FILM COATED | 50 mg | ORAL | ANDA | 27 sections |
EXSERVAN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10094-350 | FILM | 50 mg | ORAL | NDA | 29 sections |
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 | 64980-191 | TABLET, FILM COATED | 50 mg | ORAL | NDA AUTHORIZED GENERIC | 17 sections |
Riluzole | Human Prescription Drug Label | 1 | 67877-286 | TABLET | 50 mg | ORAL | ANDA | 26 sections |
Riluzole | Human Prescription Drug Label | 1 | 67877-286 | TABLET | 50 mg | ORAL | ANDA | 26 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 | 26 sections |
Exservan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70510-2201 | FILM | 50 mg | ORAL | NDA | 30 sections |
Rilutek | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70515-700 | TABLET | 50 mg | ORAL | NDA | 27 sections |
TIGLUTIK | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70726-0303 | LIQUID | 50 mg | ORAL | NDA | 31 sections |