cannabidiol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
cannabinoid receptors agonists	5288	13956-29-1

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.70	g	O

ADMET properties:

Property	Value	Reference
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

Approvals:

Date	Agency	Company	Orphan
Sept. 19, 2019	EMA	GW Pharma (International) B.V.
June 25, 2018	FDA	GW RESEARCH LTD

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
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
Tonic convulsion	47.44	21.28	13	6141	1284	63481584
Breast cancer metastatic	46.81	21.28	23	6131	11995	63470873
Skin exfoliation	43.65	21.28	35	6119	43067	63439801
Drug interaction	42.45	21.28	78	6076	229053	63253815
Cystic fibrosis	39.26	21.28	14	6140	3282	63479586
Body temperature decreased	38.02	21.28	24	6130	20295	63462573
Metastases to bone	37.27	21.28	24	6130	20995	63461873
Drug ineffective	36.12	21.28	197	5957	1044568	62438300
Blood pressure systolic increased	32.84	21.28	31	6123	47366	63435502
Pyelonephritis chronic	32.80	21.28	7	6147	239	63482629
Bone loss	32.56	21.28	12	6142	3087	63479781
Therapeutic product effective for unapproved indication	32.46	21.28	6	6148	96	63482772
Metastases to liver	32.37	21.28	23	6131	23616	63459252
Drug level increased	30.86	21.28	22	6132	22714	63460154
Sinus headache	28.81	21.28	13	6141	5603	63477265
Finger deformity	27.73	21.28	14	6140	7731	63475137
Therapeutic product ineffective for unapproved indication	27.70	21.28	6	6148	220	63482648
Therapeutic response shortened	27.26	21.28	16	6138	11872	63470996
Hip fracture	25.80	21.28	22	6132	29452	63453416
Neoplasm progression	25.56	21.28	24	6130	36404	63446464
Cough	23.57	21.28	72	6082	292671	63190197
Psychomotor hyperactivity	23.53	21.28	14	6140	10649	63472219
Feeling jittery	23.01	21.28	15	6139	13388	63469480
Skin reaction	21.61	21.28	15	6139	14834	63468034

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
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
Status epilepticus	34.40	30.17	19	3368	12595	34940949
Blood pressure systolic abnormal	33.24	30.17	13	3374	3935	34949609
Blood pressure diastolic abnormal	30.74	30.17	13	3374	4805	34948739
Blood pressure diastolic increased	30.21	30.17	13	3374	5012	34948532

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
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
Nail disorder	67.14	20.46	30	8236	11822	79724300
Tonic convulsion	60.72	20.46	18	8248	2202	79733920
Blood pressure systolic increased	53.80	20.46	49	8217	66937	79669185
Breast cancer metastatic	52.68	20.46	23	8243	8579	79727543
Somnolence	46.04	20.46	86	8180	238895	79497227
Heart rate irregular	45.56	20.46	33	8233	32646	79703476
Status epilepticus	43.63	20.46	29	8237	25012	79711110
Large intestine polyp	41.28	20.46	22	8244	12686	79723436
Acute kidney injury	39.59	20.46	4	8262	519400	79216722
Blood pressure diastolic abnormal	35.30	20.46	23	8243	19179	79716943
Bone loss	33.98	20.46	12	8254	2555	79733567
Social avoidant behaviour	33.19	20.46	14	8252	4800	79731322
Metastases to bone	32.54	20.46	24	8242	24403	79711719
Skin exfoliation	32.41	20.46	34	8232	55066	79681056
Cough	32.08	20.46	97	8169	366692	79369430
Therapeutic response shortened	31.63	20.46	20	8246	15843	79720279
Therapeutic product effective for unapproved indication	31.29	20.46	6	8260	110	79736012
Pyelonephritis chronic	31.16	20.46	7	8259	284	79735838
Intentional product use issue	30.84	20.46	56	8210	152056	79584066
Sudden unexplained death in epilepsy	30.07	20.46	8	8258	660	79735462
Metastases to liver	29.40	20.46	24	8242	28290	79707832
Sinus headache	29.22	20.46	13	8253	5067	79731055
Therapeutic product ineffective for unapproved indication	28	20.46	6	8260	195	79735927
Petit mal epilepsy	27.73	20.46	13	8253	5714	79730408
Alcohol intolerance	27.61	20.46	7	8259	478	79735644
Finger deformity	27.31	20.46	14	8252	7460	79728662
Microsporidia infection	27.15	20.46	8	8258	958	79735164
Body temperature decreased	26.75	20.46	24	8242	32121	79704001
Drug level increased	26.10	20.46	26	8240	39625	79696497
Intentional product misuse to child	26.06	20.46	5	8261	92	79736030
Epilepsy	25.44	20.46	26	8240	40834	79695288
Throat irritation	25.40	20.46	26	8240	40920	79695202
Hip fracture	23.70	20.46	22	8244	30739	79705383
Feeling jittery	22.67	20.46	15	8251	12826	79723296
Diarrhoea	22.53	20.46	162	8104	880327	78855795
Psychomotor hyperactivity	21.20	20.46	16	8250	16833	79719289
Blood pressure systolic abnormal	20.87	20.46	16	8250	17231	79718891
Hypersomnia	20.73	20.46	18	8248	23068	79713054
Infantile spasms	20.64	20.46	5	8261	283	79735839

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N03AX24	NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Other antiepileptics
FDA CS	M0003267	Cannabinoids
MeSH PA	D000927	Anticonvulsants
MeSH PA	D002491	Central Nervous System Agents
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	antibiotics
CHEBI has role	CHEBI:76924	plant metabolites

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

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	9.34	acidic
pKa2	11.34	acidic

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
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
100MG/ML	EPIDIOLEX	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	N210365	Sept. 28, 2018	RX	SOLUTION	ORAL	11154516	June 17, 2035	USE FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME
100MG/ML	EPIDIOLEX	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	N210365	Sept. 28, 2018	RX	SOLUTION	ORAL	11207292	April 26, 2039	USE FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME
100MG/ML	EPIDIOLEX	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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	GW RES LTD	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

Orange Book exclusivity data (new drug applications)

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

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Transient receptor potential cation channel subfamily V member 1	Ion channel	Q8NER1	TRPV1_HUMAN	INHIBITOR	IC50	5.43	CHEMBL	SCIENTIFIC LITERATURE
G-protein coupled receptor 55	GPCR	Q9Y2T6	GPR55_HUMAN	ANTAGONIST	EC50	6.35	CHEMBL	SCIENTIFIC LITERATURE
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	5.57	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		EC50	5.10	CHEMBL
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	5.96	CHEMBL
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	5.50	CHEMBL
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	5.43	CHEMBL
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN		Ki	5.64	CHEMBL
Delta-type opioid receptor	GPCR	P41143	OPRD_HUMAN		Ki	5.19	CHEMBL
Caspase-1	Enzyme	P29466	CASP1_HUMAN		Kd	7.73	CHEMBL
Cannabinoid receptor 2	GPCR	P34972	CNR2_HUMAN		Ki	5.54	CHEMBL
Histamine H3 receptor	GPCR	Q9Y5N1	HRH3_HUMAN		Ki	5.51	CHEMBL
N-arachidonyl glycine receptor	GPCR	Q14330	GPR18_HUMAN	AGONIST	EC50	4.29	IUPHAR
Cannabinoid receptor 1	GPCR	P21554	CNR1_HUMAN		Ki	5.62	CHEMBL
L-lactate dehydrogenase A chain	Enzyme	P00338	LDHA_HUMAN		Ki	4.62	CHEMBL
Transmembrane protein 97	Enzyme	Q5BJF2	TMM97_HUMAN		Ki	5.47	CHEMBL
Transient receptor potential cation channel subfamily V member 2	Ion channel	Q9Y5S1	TRPV2_HUMAN	ACTIVATOR	EC50	4.50	IUPHAR
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN		Ki	5.89	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR		5HT2A_RAT		EC50	4.50	CHEMBL
Cannabinoid receptor 1	GPCR		CNR1_RAT		Ki	5.90	CHEMBL
Cannabinoid receptor 2	GPCR		CNR2_MOUSE		Ki	6.64	CHEMBL
Fatty-acid amide hydrolase 1	Enzyme		FAAH1_RAT		IC50	4.27	CHEMBL
Cholinesterase	Enzyme		CHLE_HORSE		IC50	6.17	CHEMBL
Transient receptor potential cation channel subfamily M member 8	Ion channel		TRPM8_RAT		IC50	5.55	CHEMBL
Transient receptor potential cation channel subfamily V member 2	Ion channel		TRPV2_RAT	ACTIVATOR	EC50	5.43	IUPHAR
Transient receptor potential cation channel subfamily A member 1	Ion channel		TRPA1_RAT		IC50	6.35	CHEMBL
Heat sensitive channel TRPV3	Unclassified		Q4QYD9_RAT		EC50	6.29	CHEMBL
Transient receptor potential cation channel subfamily V member 4, TrpV4	Unclassified		TRPV4_RAT		EC50	6.05	CHEMBL
Acetylcholinesterase	Enzyme		ACES_ELEEL		IC50	4.77	CHEMBL

External reference:

ID	Source
19GBJ60SN5	UNII
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
20468	MMSL
291103	MMSL
d08919	MMSL
010751	NDDF
771981005	SNOMEDCT_US
96223000	SNOMEDCT_US
4036658	VANDF
2045371	RXNORM

Pharmaceutical products:

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
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