cannabidiol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
cannabinoid receptors agonists 5288 13956-29-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cannabidiol
  • GWP42003-P
  • epidiolex
The precise mechanisms by which cannabidiol exerts its anticonvulsant effect in humans are unknown. Cannabidiol does not appear to exert its anticonvulsant effects through interaction with cannabinoid receptors.
  • Molecular weight: 314.47
  • Formula: C21H30O2
  • CLOGP: 6.94
  • LIPINSKI: None
  • HAC: 2
  • HDO: 2
  • TPSA: 40.46
  • ALOGS: -4.40
  • ROTB: 6
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.70 g O

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 6.69 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 13.55 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 23.82 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 0.00 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 5.152 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.023 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 8.128 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 48.084 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 0.060 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 0.230 % High 1
herg hERG pIC50 5.195 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 128.825 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 58.614 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 0.250 % High 1
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AURKB,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK2,CDK4,CDK5,CDK9,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IKBKB,ITK,JAK1,JAK2,JAK3,KDR,KIT,MAP2K6,MAP3K1,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MAPKAPK5,MARK4,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2,ZAP70 76
kinase-selectivity-class AXL,EIF2AK3,EPHB4,GRK2,STK33,TEK 6
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.222 High 1
mh-clint Mouse hepatocyte intrinsic clearance 281.838 High 1
mppb Mouse plasma protein binding (% unbound) 0.270 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.375 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 0.330 % High 1
rh-clint Rat hepatocyte intrinsic clearance 273.527 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 0.720 % High 1
rppb Rat plasma protein binding (% unbound) 0.210 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 12.531 uM High 1

Approvals:

DateAgencyCompanyOrphan
June 25, 2018 FDA GW RESEARCH LTD
Sept. 19, 2019 EMA GW Pharma (International) B.V.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Seizure 581.13 19.62 296 9431 152333 90466387
Product administration interrupted 212.42 19.62 71 9656 12421 90606299
Hospitalisation 201.81 19.62 141 9586 127959 90490761
Off label use 197.41 19.62 390 9337 1101862 89516858
Multiple-drug resistance 184.76 19.62 57 9670 7719 90611001
Device related thrombosis 122.02 19.62 31 9696 2062 90616658
Drug resistance 109.37 19.62 57 9670 30392 90588328
Blood pressure diastolic decreased 95.72 19.62 50 9677 26776 90591944
Drug ineffective 73.29 19.62 317 9410 1383981 89234739
Tonic convulsion 69.05 19.62 19 9708 1719 90617001
Petit mal epilepsy 67.97 19.62 24 9703 4934 90613786
Drug interaction 53.89 19.62 102 9625 276351 90342369
Status epilepticus 52.92 19.62 30 9697 18844 90599876
Heart rate irregular 50.92 19.62 32 9695 24236 90594484
Bone loss 48.24 19.62 17 9710 3475 90615245
Large intestine polyp 46.87 19.62 22 9705 9364 90609356
Emergency care 43.52 19.62 13 9714 1576 90617144
Cystic fibrosis 42.56 19.62 16 9711 3925 90614795
Product preparation issue 42.52 19.62 14 9713 2332 90616388
Therapeutic product effective for unapproved indication 42.35 19.62 8 9719 130 90618590
Breast cancer metastatic 42.28 19.62 24 9703 15108 90603612
Somnolence 40.53 19.62 77 9650 209007 90409713
Generalised tonic-clonic seizure 40.43 19.62 32 9695 34871 90583849
Sinus headache 38.06 19.62 17 9710 6459 90612261
Atonic seizures 37.47 19.62 10 9717 806 90617914
Therapeutic product ineffective for unapproved indication 36.13 19.62 8 9719 293 90618427
Metastases to bone 35.29 19.62 26 9701 25479 90593241
Psychomotor hyperactivity 34.94 19.62 20 9707 12793 90605927
Electroencephalogram 32.56 19.62 4 9723 0 90618720
Body temperature decreased 32.33 19.62 24 9703 23792 90594928
Feeling jittery 31.57 19.62 20 9707 15351 90603369
Drug level increased 31.18 19.62 25 9702 27737 90590983
Agitation 30.80 19.62 37 9690 67061 90551659
Change in seizure presentation 30.75 19.62 8 9719 584 90618136
Metastases to liver 30.37 19.62 25 9702 28782 90589938
Death 28.96 19.62 111 9616 456440 90162280
Seizure cluster 28.90 19.62 7 9720 382 90618338
Skin exfoliation 28.83 19.62 36 9691 67877 90550843
Therapeutic response shortened 28.71 19.62 22 9705 22857 90595863
Swelling 26.97 19.62 6 9721 419052 90199668
Pyelonephritis chronic 26.76 19.62 6 9721 233 90618487
Drug ineffective for unapproved indication 26.19 19.62 34 9693 66610 90552110
Hip fracture 25.44 19.62 24 9703 33053 90585667
Dyschezia 25.13 19.62 10 9717 2855 90615865
Dyspnoea 24.95 19.62 35 9692 880920 89737800
Nail disorder 24.57 19.62 31 9696 59036 90559684
Diarrhoea 24.33 19.62 178 9549 939012 89679708
Sudden unexplained death in epilepsy 23.57 19.62 6 9721 402 90618318
Blood pressure systolic increased 23.29 19.62 30 9697 58315 90560405
COVID-19 23.15 19.62 54 9673 168789 90449931
Neoplasm progression 22.86 19.62 26 9701 44460 90574260
Wound 22.41 19.62 3 9724 302977 90315743
Hand deformity 21.77 19.62 3 9724 296359 90322361
Intermittent explosive disorder 21.12 19.62 3 9724 6 90618714
Pharyngitis 20.97 19.62 18 9709 21929 90596791
Drug intolerance 20.90 19.62 11 9716 447580 90171140
Complement factor C4 decreased 20.21 19.62 5 9722 298 90618422
Neuropathy peripheral 20.09 19.62 45 9682 136925 90481795
Complement factor C3 decreased 20.00 19.62 5 9722 311 90618409
Acute kidney injury 19.79 19.62 5 9722 320382 90298338

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Seizure 806.54 28.02 377 5844 120184 42494930
Hospitalisation 361.64 28.02 188 6033 74142 42540972
Product administration interrupted 283.45 28.02 77 6144 4889 42610225
Off label use 186.45 28.02 331 5890 638004 41977110
Multiple-drug resistance 120.80 28.02 44 6177 7278 42607836
Status epilepticus 85.82 28.02 43 6178 15535 42599579
Atonic seizures 84.54 28.02 18 6203 398 42614716
Somnolence 82.32 28.02 102 6119 141003 42474111
Behaviour disorder 75.65 28.02 31 6190 7023 42608091
Emergency care 70.40 28.02 16 6205 482 42614632
Drug interaction 69.95 28.02 133 6088 266866 42348248
Seizure cluster 60.90 28.02 13 6208 291 42614823
Tonic convulsion 47.15 28.02 15 6206 1644 42613470
Product preparation issue 44.59 28.02 13 6208 1062 42614052
Intellectual disability 41.00 28.02 14 6207 1913 42613201
Death 37.88 28.02 152 6069 471033 42144081
Petit mal epilepsy 35.62 28.02 15 6206 3635 42611479
Generalised tonic-clonic seizure 35.50 28.02 30 6191 26349 42588765
Acute kidney injury 30.57 28.02 8 6213 367329 42247785
Vagal nerve stimulator implantation 30.31 28.02 6 6215 91 42615023
Social avoidant behaviour 30.10 28.02 13 6208 3351 42611763
Aggression 29.05 28.02 34 6187 44129 42570985

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Seizure 789.94 18.52 434 13550 220751 110354564
Multiple-drug resistance 250.78 18.52 85 13899 13150 110562165
Product administration interrupted 243.72 18.52 80 13904 11212 110564103
Off label use 189.85 18.52 512 13472 1499673 109075642
Drug interaction 141.75 18.52 238 13746 499945 110075370
Atonic seizures 135.30 18.52 31 13953 1123 110574192
Behaviour disorder 133.26 18.52 49 13935 9598 110565717
Tonic convulsion 122.94 18.52 35 13949 3039 110572276
Somnolence 106.91 18.52 158 13826 297291 110278024
Hospitalisation 105.51 18.52 109 13875 142384 110432931
Petit mal epilepsy 103.01 18.52 38 13946 7509 110567806
Device related thrombosis 101.53 18.52 31 13953 3431 110571884
Status epilepticus 101.31 18.52 58 13926 31513 110543802
Drug ineffective 96.80 18.52 413 13571 1520127 109055188
Seizure cluster 90.32 18.52 21 13963 812 110574503
Blood pressure diastolic decreased 89.36 18.52 56 13928 35829 110539486
Generalised tonic-clonic seizure 83.23 18.52 63 13921 54617 110520698
Tricuspid valve incompetence 82.38 18.52 46 13938 23827 110551488
Drug resistance 75.04 18.52 60 13924 56314 110519001
Vagal nerve stimulator implantation 65.29 18.52 13 13971 237 110575078
Product preparation issue 65.26 18.52 21 13963 2758 110572557
Change in seizure presentation 54.55 18.52 14 13970 820 110574495
Mitral valve incompetence 54.28 18.52 40 13944 33289 110542026
Bone loss 51.54 18.52 18 13966 3037 110572278
Sudden unexplained death in epilepsy 49.87 18.52 13 13971 810 110574505
Agitation 49.35 18.52 66 13918 112985 110462330
Acute kidney injury 47.65 18.52 11 13973 635419 109939896
Breast cancer metastatic 45.39 18.52 24 13960 11157 110564158
Emergency care 42.56 18.52 13 13971 1440 110573875
Mitral valve thickening 41.12 18.52 11 13973 758 110574557
Heart rate irregular 40.40 18.52 34 13950 34240 110541075
Therapeutic product effective for unapproved indication 39.71 18.52 8 13976 155 110575160
Sinus headache 39.68 18.52 18 13966 6014 110569301
Myoclonic epilepsy 38.39 18.52 14 13970 2677 110572638
Aortic valve incompetence 37.44 18.52 21 13963 10960 110564355
Psychomotor hyperactivity 36.81 18.52 26 13958 20251 110555064
Blood pressure systolic increased 35.52 18.52 48 13936 82943 110492372
Aggression 34.55 18.52 40 13944 59170 110516145
Therapeutic product ineffective for unapproved indication 34.49 18.52 8 13976 306 110575009
Feeling jittery 34.21 18.52 22 13962 14700 110560615
Therapeutic response shortened 34.16 18.52 29 13955 29554 110545761
Large intestine polyp 33.68 18.52 22 13962 15095 110560220
Death 32.52 18.52 174 13810 698695 109876620
Aortic valve thickening 31.33 18.52 7 13977 226 110575089
Drug level increased 30.85 18.52 34 13950 47685 110527630
Oedema peripheral 30.73 18.52 3 13981 328657 110246658
Hypersomnia 29.35 18.52 26 13958 28035 110547280
Febrile neutropenia 29.33 18.52 3 13981 316764 110258551
Social avoidant behaviour 29.05 18.52 14 13970 5355 110569960
Metastases to liver 27.84 18.52 28 13956 35358 110539957
Metastases to bone 26.87 18.52 26 13958 31346 110543969
Alcohol intolerance 26.79 18.52 7 13977 440 110574875
Partial seizures with secondary generalisation 26.51 18.52 8 13976 851 110574464
Blood pressure diastolic abnormal 25.19 18.52 23 13961 25792 110549523
Drug ineffective for unapproved indication 25.16 18.52 46 13938 102792 110472523
Fatigue 25.12 18.52 249 13735 1215709 109359606
COVID-19 25.07 18.52 78 13906 244982 110330333
Inappropriate affect 24.83 18.52 9 13975 1690 110573625
Throat irritation 24.49 18.52 32 13952 53520 110521795
Pyelonephritis chronic 24.48 18.52 6 13978 291 110575024
Illness 24.34 18.52 40 13944 82131 110493184
Pulmonary valve incompetence 24.17 18.52 10 13974 2676 110572639
Infantile spasms 22.84 18.52 6 13978 385 110574930
Microsporidia infection 22.45 18.52 8 13976 1431 110573884
Diarrhoea 22.39 18.52 231 13753 1139274 109436041
Product dose omission issue 22.22 18.52 90 13894 321692 110253623
Partial seizures 21.64 18.52 15 13969 11334 110563981
Drug abuse 21.51 18.52 60 13924 177351 110397964
Cough 21.47 18.52 115 13869 461526 110113789
Hypotonia 21.46 18.52 17 13967 15728 110559587
Intentional product misuse to child 21.17 18.52 5 13979 207 110575108
Nail disorder 21.07 18.52 31 13953 57904 110517411
Behavioural addiction 20.30 18.52 4 13980 69 110575246
Heart rate decreased 20.22 18.52 37 13947 82719 110492596
Intellectual disability 19.97 18.52 8 13976 1971 110573344
Body temperature decreased 19.97 18.52 24 13960 36911 110538404
Anaemia 19.85 18.52 24 13960 547062 110028253
Electroencephalogram 19.77 18.52 3 13981 9 110575306
Dyspnoea 19.61 18.52 73 13911 1106799 109468516
Stomatitis 19.59 18.52 5 13979 270237 110305078
Hip fracture 19.26 18.52 23 13961 35128 110540187
Hypotension 18.98 18.52 23 13961 523826 110051489
Hand dermatitis 18.97 18.52 6 13978 745 110574570
Mood altered 18.84 18.52 18 13966 21357 110553958
Lower respiratory tract infection 18.61 18.52 4 13980 243102 110332213
Therapy change 18.57 18.52 13 13971 9984 110565331

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N03AX24 NERVOUS SYSTEM
ANTIEPILEPTICS
ANTIEPILEPTICS
Other antiepileptics
FDA CS M0003267 Cannabinoids
MeSH PA D000927 Anticonvulsants
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
FDA MoA N0000191273 UGT2B7 Inhibitors
FDA MoA N0000191278 UGT1A9 Inhibitors
CHEBI has role CHEBI:33281 antimicrobial agent
CHEBI has role CHEBI:76924 plant metabolite

Related Drugs by ATC class:

N03AX Other antiepileptics 18 drugs
beclamidebrivaracetamcarisbamatecenobamatefelbamatefenfluramineganaxolonelacosamidelamotriginelevetiracetamperampanelphenacemide show all 18 →

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Lennox-Gastaut syndrome indication 230418006
Severe myoclonic epilepsy in infancy indication 230437002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.34 acidic
pKa2 11.34 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MG/ML EPIDIOLEX JAZZ PHARMS RES 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 JAZZ PHARMS RES 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 JAZZ PHARMS RES 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 JAZZ PHARMS RES 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 JAZZ PHARMS RES 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 JAZZ PHARMS RES 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 JAZZ PHARMS RES 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 JAZZ PHARMS RES 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 JAZZ PHARMS RES 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 JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 10709671 June 17, 2035 USE FOR THE TREATMENT OF FOCAL SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 10709674 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 10709674 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH LENNOX-GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 10849860 June 17, 2035 USE FOR THE TREATMENT OF DROP SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 10849860 June 17, 2035 USE FOR THE TREATMENT OF DROP SEIZURES IN PATIENTS WITH LENNOX-GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 10966939 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 10966939 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH LENNOX-GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11154516 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11154516 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH LENNOX-GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11311498 June 17, 2035 USE FOR THE TREATMENT OF ABSENCE SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11311498 June 17, 2035 USE FOR THE TREATMENT OF ABSENCE SEIZURES IN PATIENTS WITH LENNOX-GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11357741 June 17, 2035 USE FOR THE TREATMENT OF FOCAL SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11446258 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11446258 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH LENNOX-GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11446258 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH TUBEROUS SCLEROSIS COMPLEX
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11633369 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11633369 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH LENNOX-GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11633369 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH TUBEROUS SCLEROSIS COMPLEX
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11701330 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11701330 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH LENNOX-GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11766411 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11963937 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11963937 June 17, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH LENNOX-GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 12064399 June 17, 2035 USE FOR THE TREATMENT OF FOCAL SEIZURES ASSOCIATED WITH LENNOX-GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 12064399 June 17, 2035 USE FOR THE TREATMENT OF FOCAL SEIZURES ASSOCIATED WITH TUBEROUS SCLEROSIS COMPLEX
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 9949937 June 17, 2035 USE IN COMBINATION WITH CLOBAZAM FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 9956183 June 17, 2035 USE IN COMBINATION WITH CLOBAZAM FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH DRAVET SYNDROME WHO HAVE BEEN PREVIOUSLY TREATED WITH CLOBAZAM
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 9956183 June 17, 2035 USE IN COMBINATION WITH CLOBAZAM FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH LENNOX GASTAUT SYNDROME WHO HAVE BEEN PREVIOUSLY TREATED WITH CLOBAZAM
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 9956184 June 17, 2035 USE IN COMBINATION WITH CLOBAZAM FOR TREATMENT OF SEIZURES IN PATIENTS WITH LENNOX GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 9956185 June 17, 2035 USE FOR THE TREATMENT OF CONVULSIVE SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 9956186 June 17, 2035 USE FOR THE TREATMENT OF CONVULSIVE SEIZURES IN PATIENTS WITH LENNOX GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 10918608 Oct. 13, 2035 USE FOR REDUCING SEIZURE FREQUENCY IN PATIENTS WITH TUBEROUS SCLEROSIS COMPLEX
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 10918608 Oct. 13, 2035 USE FOR THE TREATMENT OF GENERALIZED SEIZURES OR FOCAL SEIZURES WITH IMPAIRMENT IN PATIENTS WITH TUBEROUS SCLEROSIS COMPLEX
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 10918608 Oct. 13, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH TUBEROUS SCLEROSIS COMPLEX
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11065209 Oct. 13, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH TUBEROUS SCLEROSIS COMPLEX
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11096905 Oct. 13, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11096905 Oct. 13, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH LENNOX-GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11400055 Oct. 13, 2035 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH TUBEROUS SCLEROSIS COMPLEX
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11207292 April 26, 2039 USE FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11207292 April 26, 2039 USE FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH LENNOX-GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11207292 April 26, 2039 USE FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH TUBEROUS SCLEROSIS COMPLEX
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11865102 April 26, 2039 USE FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH LENNOX-GASTAUT SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11865102 April 26, 2039 USE FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH TUBEROUS SCLEROSIS COMPLEX
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11865102 April 26, 2039 USE FOR THE TREATMENT OF SEIZURES IN PATIENTS WITH DRAVET SYNDROME
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11160795 March 1, 2041 USE FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH TUBEROUS SCLEROSIS COMPLEX IN PATIENTS TAKING EVEROLIMUS
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 11406623 March 1, 2041 USE FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH TUBEROUS SCLEROSIS COMPLEX IN PATIENTS TAKING EVEROLIMUS
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL 12102619 March 1, 2041 USE FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH TUBEROUS SCLEROSIS COMPLEX IN PATIENTS TAKING EVEROLIMUS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG/ML EPIDIOLEX JAZZ PHARMS RES N210365 Sept. 28, 2018 RX SOLUTION ORAL Oct. 20, 2026 INFORMATION ADDED TO CLINICAL PHARMACOLOGY SECTION
100MG/ML EPIDIOLEX JAZZ PHARMS RES 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 JAZZ PHARMS RES 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

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA 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
Sodium channel protein type 5 subunit alpha Ion channel BLOCKER IC50 5.42 IUPHAR
Mu-type opioid receptor GPCR Ki 5.89 CHEMBL
D(2) dopamine receptor GPCR Ki 10.18 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
Sodium channel protein type 1 subunit alpha Ion channel BLOCKER IC50 5.54 IUPHAR
Sodium channel protein type 2 subunit alpha Ion channel BLOCKER IC50 5.54 IUPHAR
Sodium channel protein type 3 subunit alpha Ion channel BLOCKER IC50 5.48 IUPHAR
Sodium channel protein type 4 subunit alpha Ion channel BLOCKER IC50 5.72 IUPHAR
Sodium channel protein type 8 subunit alpha Ion channel BLOCKER IC50 5.52 IUPHAR
Sodium channel protein type 9 subunit alpha Ion channel BLOCKER IC50 6.70 IUPHAR
Kappa-type opioid receptor GPCR Ki 5.64 CHEMBL
Glycine receptor subunit alpha-2 Ion channel IC50 5.57 CHEMBL
Calcium-activated potassium channel subunit alpha-1 Ion channel IC50 6.55 CHEMBL
Delta-type opioid receptor GPCR Ki 5.19 CHEMBL
Caspase-1 Enzyme Kd 7.73 CHEMBL
Equilibrative nucleoside transporter 1 Transporter Ki 6.60 CHEMBL
Cannabinoid receptor 2 GPCR Ki 5.54 CHEMBL
Histamine H3 receptor GPCR Ki 5.51 CHEMBL
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A Enzyme IC50 6.96 CHEMBL
N-arachidonyl glycine receptor GPCR AGONIST EC50 4.29 IUPHAR
Transient receptor potential cation channel subfamily M member 8 Ion channel IC50 7.22 CHEMBL
L-lactate dehydrogenase A chain Enzyme Ki 4.62 CHEMBL
Transmembrane protein 97 Enzyme Ki 5.47 CHEMBL
Transient receptor potential cation channel subfamily V member 2 Ion channel ACTIVATOR EC50 4.50 IUPHAR
D(1A) dopamine receptor GPCR Ki 5.57 CHEMBL
Sodium channel protein type 5 subunit alpha Ion channel BLOCKER IC50 5.42 IUPHAR
Cannabinoid receptor 1 GPCR Ki 5.62 CHEMBL
5-hydroxytryptamine receptor 2A GPCR EC50 4.50 CHEMBL
Acetylcholinesterase Enzyme IC50 4.77 CHEMBL
Cannabinoid receptor 1 GPCR Ki 5.90 CHEMBL
Cannabinoid receptor 2 GPCR Ki 6.64 CHEMBL
Cannabinoid receptor 1 GPCR Ki 5.36 CHEMBL
Fatty-acid amide hydrolase 1 Enzyme IC50 4.27 CHEMBL
Cholinesterase Enzyme IC50 6.17 CHEMBL
Fatty-acid amide hydrolase 1 Enzyme IC50 4.56 CHEMBL
Transient receptor potential cation channel subfamily M member 8 Ion channel IC50 5.55 CHEMBL
Transient receptor potential cation channel subfamily V member 2 Ion channel ACTIVATOR EC50 5.43 IUPHAR
Transient receptor potential cation channel subfamily A member 1 Ion channel IC50 6.35 CHEMBL
Heat sensitive channel TRPV3 Ion channel EC50 6.29 CHEMBL
Transient receptor potential cation channel subfamily V member 4, TrpV4 Ion channel EC50 6.05 CHEMBL
Sodium channel protein type 10 subunit alpha Ion channel BLOCKER IC50 5.70 IUPHAR

External reference:

IDSource
19GBJ60SN5 UNII
4036658 VANDF
C0006863 UMLSCUI
CHEBI:69478 CHEBI
P0T PDB_CHEM_ID
CHEMBL190461 ChEMBL_ID
644019 PUBCHEM_CID
DB09061 DRUGBANK_ID
D002185 MESH_DESCRIPTOR_UI
D10915 KEGG_DRUG
10423 INN_ID
4150 IUPHAR_LIGAND_ID
771981005 SNOMEDCT_US
96223000 SNOMEDCT_US
20468 MMSL
291103 MMSL
d08919 MMSL
010751 NDDF
2045371 RXNORM
19GBJ60SN5 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Epidiolex HUMAN PRESCRIPTION DRUG LABEL 1 70127-100 SOLUTION 100 mg ORAL NDA 30 sections
Epidiolex HUMAN PRESCRIPTION DRUG LABEL 1 70127-100 SOLUTION 100 mg ORAL NDA 30 sections
NanoCDB HUMAN OTC DRUG LABEL 1 70658-122 SOLUTION/ DROPS 1.94 g BUCCAL Export only 8 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 FS QP 20% HUMAN OTC DRUG LABEL 1 73674-005 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
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 Softgels FS QP 20 HUMAN OTC DRUG LABEL 1 73674-052 CAPSULE, LIQUID FILLED 20 mg ORAL unapproved drug other 15 sections
leafPro CBDmed Softgels T-FS QD 20 HUMAN OTC DRUG LABEL 1 73674-061 CAPSULE, LIQUID FILLED 20 mg ORAL unapproved drug other 15 sections
Kaydia Patch HUMAN OTC DRUG LABEL 3 75140-002 PATCH 0.15 g TOPICAL unapproved drug other 8 sections