Stem definition | Drug id | CAS RN |
---|---|---|
cannabinoid receptors agonists | 5288 | 13956-29-1 |
Dose | Unit | Route |
---|---|---|
0.70 | g | O |
Property | Value | Reference |
---|---|---|
Vd (Volume of distribution) | 6.69 L/kg | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 23.82 hours | Lombardo F, Berellini G, Obach RS |
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
CL (Clearance) | 13.55 mL/min/kg | Lombardo F, Berellini G, Obach RS |
S (Water solubility) | 0.00 mg/mL | Bocci G, Oprea TI, Benet LZ |
Date | Agency | Company | Orphan |
---|---|---|---|
June 25, 2018 | FDA | GW RESEARCH LTD | |
Sept. 19, 2019 | EMA | GW Pharma (International) B.V. |
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 |
---|---|---|---|---|---|---|
Seizure | 184.76 | 21.28 | 130 | 6024 | 132504 | 63350364 |
Multiple-drug resistance | 131.45 | 21.28 | 39 | 6115 | 5131 | 63477737 |
Device related thrombosis | 124.91 | 21.28 | 30 | 6124 | 1755 | 63481113 |
Off label use | 108.18 | 21.28 | 215 | 5939 | 674247 | 62808621 |
Drug resistance | 101.87 | 21.28 | 48 | 6106 | 22885 | 63459983 |
Product administration interrupted | 91.16 | 21.28 | 29 | 6125 | 4807 | 63478061 |
Blood pressure diastolic decreased | 87.15 | 21.28 | 43 | 6111 | 22663 | 63460205 |
Nail disorder | 66.40 | 21.28 | 30 | 6124 | 12985 | 63469883 |
Large intestine polyp | 52.00 | 21.28 | 22 | 6132 | 8135 | 63474733 |
Heart rate irregular | 50.99 | 21.28 | 30 | 6124 | 22391 | 63460477 |
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 |
---|---|---|---|---|---|---|
Seizure | 291.82 | 30.17 | 159 | 3228 | 104698 | 34848846 |
Product administration interrupted | 114.26 | 30.17 | 28 | 3359 | 1787 | 34951757 |
Off label use | 95.09 | 30.17 | 155 | 3232 | 419369 | 34534175 |
Behaviour disorder | 66.75 | 30.17 | 23 | 3364 | 4887 | 34948657 |
Drug interaction | 59.82 | 30.17 | 90 | 3297 | 225856 | 34727688 |
Multiple-drug resistance | 57.74 | 30.17 | 21 | 3366 | 5218 | 34948326 |
Hospitalisation | 44.96 | 30.17 | 40 | 3347 | 56862 | 34896682 |
Drug ineffective | 39.83 | 30.17 | 115 | 3272 | 456636 | 34496908 |
Somnolence | 39.33 | 30.17 | 51 | 3336 | 111065 | 34842479 |
Social avoidant behaviour | 36.25 | 30.17 | 13 | 3374 | 3101 | 34950443 |
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 |
---|---|---|---|---|---|---|
Seizure | 242.76 | 20.46 | 181 | 8085 | 188653 | 79547469 |
Multiple-drug resistance | 131.43 | 20.46 | 45 | 8221 | 8763 | 79727359 |
Off label use | 125.03 | 20.46 | 283 | 7983 | 906932 | 78829190 |
Device related thrombosis | 110.76 | 20.46 | 30 | 8236 | 2653 | 79733469 |
Drug interaction | 107.56 | 20.46 | 170 | 8096 | 415013 | 79321109 |
Product administration interrupted | 91.12 | 20.46 | 28 | 8238 | 3871 | 79732251 |
Behaviour disorder | 85.46 | 20.46 | 30 | 8236 | 6283 | 79729839 |
Blood pressure diastolic decreased | 83.55 | 20.46 | 47 | 8219 | 30169 | 79705953 |
Drug resistance | 73.87 | 20.46 | 49 | 8217 | 42164 | 79693958 |
Drug ineffective | 67.17 | 20.46 | 254 | 8012 | 1080659 | 78655463 |
None
Source | Code | Description |
---|---|---|
ATC | N03AX24 | NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Other antiepileptics |
CHEBI has role | CHEBI:33281 | antibiotics |
CHEBI has role | CHEBI:76924 | plant metabolites |
FDA CS | M0003267 | Cannabinoids |
FDA MoA | N0000182138 | Cytochrome P450 1A2 Inhibitors |
FDA MoA | N0000182139 | Cytochrome P450 2B6 Inhibitors |
FDA MoA | N0000182140 | Cytochrome P450 2C19 Inhibitors |
FDA MoA | N0000185504 | Cytochrome P450 2C9 Inhibitors |
FDA MoA | N0000187062 | Cytochrome P450 2C8 Inhibitors |
FDA MoA | N0000187064 | Cytochrome P450 2B6 Inducers |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Lennox-Gastaut syndrome | indication | 230418006 | |
Severe myoclonic epilepsy in infancy | indication | 230437002 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 9.34 | acidic |
pKa2 | 11.34 | acidic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | 10092525 | June 17, 2035 | USE FOR THE TREATMENT OF DROP SEIZURES IN PATIENTS WITH DRAVET SYNDROME |
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | 10111840 | June 17, 2035 | USE FOR THE TREATMENT OF ATONIC SEIZURES IN PATIENTS WITH DRAVET SYNDROME |
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | 10111840 | June 17, 2035 | USE FOR THE TREATMENT OF ATONIC SEIZURES IN PATIENTS WITH LENNOX-GASTAUT SYNDROME |
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | 10137095 | June 17, 2035 | USE FOR THE TREATMENT OF DROP SEIZURES IN PATIENTS WITH LENNOX-GASTAUT SYNDROME |
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | 10137095 | June 17, 2035 | USE IN COMBINATION WITH CLOBAZAM FOR TREATMENT OF DROP SEIZURES IN PATIENTS WITH LENNOX GASTAUT SYNDROME |
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | 10603288 | June 17, 2035 | USE FOR REDUCING CONVULSIVE SEIZURE FREQUENCY IN PATIENTS WITH DRAVET SYNDROME |
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | 10603288 | June 17, 2035 | USE FOR REDUCING CONVULSIVE SEIZURE FREQUENCY IN PATIENTS WITH LENNOX GASTAUT SYNDROME |
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | 10603288 | June 17, 2035 | USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH DRAVET SYNDROME |
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | 10603288 | June 17, 2035 | USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH LENNOX-GASTAUT SYNDROME |
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | 10709671 | June 17, 2035 | USE FOR THE TREATMENT OF FOCAL SEIZURES IN PATIENTS WITH DRAVET SYNDROME |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | July 31, 2023 | NEW PATIENT POPULATION |
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | Sept. 28, 2023 | NEW CHEMICAL ENTITY |
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | Sept. 28, 2025 | INDICATED FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH LENNOX-GASTAUT SYNDROME (LGS) OR DRAVET SYNDROME (DS) IN PATIENTS 2 YEARS OF AGE AND OLDER |
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | July 31, 2027 | TREATMENT OF SEIZURES ASSOCIATED WITH LENNOX-GASTAUT SYNDROME (LGS) OR DRAVET SYNDROME (DS) IN PATIENTS BETWEEN 1 AND 2 YEARS OF AGE |
100MG/ML | EPIDIOLEX | GW RES LTD | N210365 | Sept. 28, 2018 | RX | SOLUTION | ORAL | July 31, 2027 | TREATMENT OF SEIZURES ASSOCIATED WITH TUBEROUS SCLEROSIS COMPLEX (TSC) IN PATIENTS 1 YEAR OF AGE AND OLDER |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Transient receptor potential cation channel subfamily V member 1 | Ion channel | INHIBITOR | IC50 | 5.43 | CHEMBL | SCIENTIFIC LITERATURE | |||
G-protein coupled receptor 55 | GPCR | ANTAGONIST | EC50 | 6.35 | CHEMBL | SCIENTIFIC LITERATURE | |||
D(1A) dopamine receptor | GPCR | Ki | 5.57 | CHEMBL | |||||
5-hydroxytryptamine receptor 1A | GPCR | EC50 | 5.10 | CHEMBL | |||||
5-hydroxytryptamine receptor 2C | GPCR | Ki | 5.96 | CHEMBL | |||||
Alpha-2B adrenergic receptor | GPCR | Ki | 5.50 | CHEMBL | |||||
Alpha-2C adrenergic receptor | GPCR | Ki | 5.43 | CHEMBL | |||||
Kappa-type opioid receptor | GPCR | Ki | 5.64 | CHEMBL | |||||
Delta-type opioid receptor | GPCR | Ki | 5.19 | CHEMBL | |||||
Caspase-1 | Enzyme | Kd | 7.73 | CHEMBL |
ID | Source |
---|---|
P0T | PDB_CHEM_ID |
010751 | NDDF |
10423 | INN_ID |
19GBJ60SN5 | UNII |
2045371 | RXNORM |
20468 | MMSL |
291103 | MMSL |
4036658 | VANDF |
4150 | IUPHAR_LIGAND_ID |
644019 | PUBCHEM_CID |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Epidiolex | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70127-100 | SOLUTION | 100 mg | ORAL | NDA | 32 sections |
Epidiolex | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70127-100 | SOLUTION | 100 mg | ORAL | NDA | 32 sections |
Epidiolex | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70127-100 | SOLUTION | 100 mg | ORAL | NDA | 32 sections |
Kaydia Patch | HUMAN OTC DRUG LABEL | 3 | 75140-002 | PATCH | 0.15 g | TOPICAL | unapproved drug other | 8 sections |
leafPro CBDmed Oil FS QP 20% | HUMAN OTC DRUG LABEL | 1 | 73674-005 | OIL | 20 g | ORAL | unapproved drug other | 15 sections |
leafPro CBDmed Oil FS QP 3% | HUMAN OTC DRUG LABEL | 1 | 73674-001 | OIL | 3 g | ORAL | unapproved drug other | 15 sections |
leafPro CBDmed Oil FS QP 5% | HUMAN OTC DRUG LABEL | 1 | 73674-002 | OIL | 5 g | ORAL | unapproved drug other | 15 sections |
leafPro CBDmed Oil T-FS QD 20% | HUMAN OTC DRUG LABEL | 1 | 73674-024 | OIL | 20 g | ORAL | unapproved drug other | 15 sections |
leafPro CBDmed Oil T-FS QD 3% | HUMAN OTC DRUG LABEL | 1 | 73674-020 | OIL | 3 g | ORAL | unapproved drug other | 15 sections |
leafPro CBDmed Oil T-FS QD 5% | HUMAN OTC DRUG LABEL | 1 | 73674-021 | OIL | 5 g | ORAL | unapproved drug other | 15 sections |