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

Stem definition	Drug id	CAS RN
	228	58-00-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: apomorphine (-)-Apomorphine apomorphin L-Apomorphine apomorphine hydrochloride apomorphine hydrochloride hydrate apomorphine hydrochloride hemihydrate apomorphine HCl apomorphine chloride	A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use. Molecular weight: 267.33 Formula: C17H17NO2 CLOGP: 2.49 LIPINSKI: 0 HAC: 3 HDO: 2 TPSA: 43.70 ALOGS: -2.72 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

apomorphine
(-)-Apomorphine
apomorphin
L-Apomorphine
apomorphine hydrochloride
apomorphine hydrochloride hydrate
apomorphine hydrochloride hemihydrate
apomorphine HCl
apomorphine chloride

A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.

Molecular weight: 267.33
Formula: C17H17NO2
CLOGP: 2.49
LIPINSKI: 0
HAC: 3
HDO: 2
TPSA: 43.70
ALOGS: -2.72
ROTB: 0

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
2	mg	SL
20	mg	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	20 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.30 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.32 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	10 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1.60 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	40 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.05 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	0.68 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
April 20, 2004	FDA	US WORLDMEDS

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
Somnolence	358.12	39.76	179	3241	178506	63307096
Nausea	329.98	39.76	306	3114	854165	62631437
Blood pressure decreased	260.51	39.76	106	3314	64916	63420686
Dizziness	197.30	39.76	171	3249	429754	63055848
Yawning	170.13	39.76	32	3388	1048	63484554
Orthostatic hypotension	95.38	39.76	44	3376	36116	63449486
Feeling abnormal	92.65	39.76	71	3349	148321	63337281
Dyskinesia	90.88	39.76	41	3379	31961	63453641
Product taste abnormal	89.21	39.76	21	3399	2046	63483556
Dysgeusia	81.81	39.76	43	3377	46667	63438935
Blood pressure increased	80.84	39.76	68	3352	161994	63323608
Hyperhidrosis	79.36	39.76	57	3363	107779	63377823
Vomiting	75.72	39.76	119	3301	559498	62926104
Freezing phenomenon	71.36	39.76	16	3404	1256	63484346
On and off phenomenon	70.65	39.76	17	3403	1818	63483784
Injection site nodule	67.17	39.76	19	3401	3816	63481786
Hyperkinesia	61.57	39.76	15	3405	1689	63483913
Heart rate decreased	55.35	39.76	33	3387	45527	63440075
Injection site necrosis	54.57	39.76	13	3407	1331	63484271
Feeling hot	52.30	39.76	33	3387	50321	63435281
Product packaging difficult to open	50.20	39.76	8	3412	95	63485507
Hallucination	47.33	39.76	32	3388	54785	63430817
Cold sweat	45.86	39.76	19	3401	12028	63473574
Dysstasia	44.32	39.76	22	3398	21144	63464458
Tremor	41.62	39.76	43	3377	132196	63353406
Drug monitoring procedure not performed	41.44	39.76	9	3411	609	63484993

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
Somnolence	433.83	35.47	244	4970	110872	34840845
Dizziness	398.72	35.47	297	4917	218224	34733493
Blood pressure decreased	372.95	35.47	172	5042	51343	34900374
Nausea	369.92	35.47	342	4872	339566	34612151
Yawning	310.66	35.47	56	5158	486	34951231
Orthostatic hypotension	191.56	35.47	88	5126	25831	34925886
Hyperhidrosis	150.37	35.47	109	5105	75583	34876134
Dyskinesia	119.81	35.47	61	5153	22352	34929365
Feeling abnormal	107.46	35.47	83	5131	63152	34888565
On and off phenomenon	106.53	35.47	31	5183	2466	34949251
Heart rate decreased	84.86	35.47	55	5159	31690	34920027
Drug monitoring procedure not performed	82.59	35.47	17	5197	310	34951407
Hallucination	77.55	35.47	63	5151	51435	34900282
Cold sweat	70.82	35.47	33	5181	9954	34941763
Freezing phenomenon	69.65	35.47	20	5194	1516	34950201
Pallor	65.27	35.47	43	5171	25437	34926280
Hallucination, visual	63.26	35.47	37	5177	17754	34933963
Dysstasia	61.67	35.47	32	5182	12163	34939554
Injection site necrosis	55.81	35.47	13	5201	428	34951289
Oral discomfort	54.96	35.47	19	5195	2638	34949079
Dysgeusia	49.81	35.47	37	5177	26460	34925257
Blood pressure increased	49.13	35.47	63	5151	88039	34863678
Injection site nodule	46.63	35.47	15	5199	1668	34950049
Vomiting	45.31	35.47	108	5106	247513	34704204
Fall	44.35	35.47	95	5119	202790	34748927
Oesophageal achalasia	41.34	35.47	10	5204	388	34951329
Feeling hot	40.84	35.47	29	5185	19343	34932374
Akinesia	38.99	35.47	14	5200	2170	34949547
Illusion	38.53	35.47	11	5203	816	34950901
Rhinorrhoea	35.66	35.47	30	5184	25638	34926079

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
Somnolence	695.14	34.11	366	6936	238615	79498471
Nausea	585.89	34.11	562	6740	956634	78780452
Blood pressure decreased	577.86	34.11	246	7056	99220	79637866
Dizziness	498.95	34.11	398	6904	526043	79211043
Yawning	424.51	34.11	78	7224	1288	79735798
Orthostatic hypotension	260.88	34.11	119	7183	56045	79681041
Hyperhidrosis	187.07	34.11	135	7167	151357	79585729
On and off phenomenon	171.40	34.11	43	7259	3197	79733889
Feeling abnormal	148.31	34.11	120	7182	159079	79578007
Dyskinesia	147.44	34.11	75	7227	44698	79692388
Heart rate decreased	125.86	34.11	79	7223	70237	79666849
Dysgeusia	114.44	34.11	69	7233	57108	79679978
Freezing phenomenon	114.29	34.11	28	7274	1886	79735200
Drug monitoring procedure not performed	109.52	34.11	24	7278	987	79736099
Product taste abnormal	104.65	34.11	27	7275	2244	79734842
Cold sweat	103.94	34.11	45	7257	18654	79718432
Hallucination	102.42	34.11	75	7227	85670	79651416
Blood pressure increased	92.42	34.11	105	7197	211255	79525831
Vomiting	90.41	34.11	192	7110	665636	79071450
Dysstasia	89.90	34.11	46	7256	27700	79709386
Hallucination, visual	82.75	34.11	46	7256	32683	79704403
Feeling hot	77.58	34.11	55	7247	59679	79677407
Injection site necrosis	70.18	34.11	18	7284	1460	79735626
Injection site nodule	69.72	34.11	22	7280	3758	79733328
Pallor	64.78	34.11	46	7256	50016	79687070
Hyperkinesia	63.57	34.11	19	7283	2710	79734376
Product packaging difficult to open	59.26	34.11	9	7293	41	79737045
Oral discomfort	49.40	34.11	22	7280	9738	79727348
Dopamine dysregulation syndrome	48.99	34.11	11	7291	506	79736580
Fatigue	45.21	34.11	186	7116	929541	78807545
Akinesia	43.84	34.11	15	7287	3297	79733789
Heart rate increased	42.83	34.11	54	7248	120670	79616416
Retching	39.95	34.11	23	7279	17444	79719642
Oesophageal achalasia	39.32	34.11	10	7292	784	79736302
Illusion	35.74	34.11	11	7291	1730	79735356
Infusion site necrosis	34.73	34.11	6	7296	68	79737018

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	G04BE07	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS UROLOGICALS Drugs used in erectile dysfunction
ATC	N04BC07	NERVOUS SYSTEM ANTI-PARKINSON DRUGS DOPAMINERGIC AGENTS Dopamine agonists
FDA MoA	N0000000117	Dopamine Agonists
FDA EPC	N0000175580	Dopaminergic Agonist
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D015259	Dopamine Agents
MeSH PA	D018491	Dopamine Agonists
MeSH PA	D004639	Emetics
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018373	Peripheral Nervous System Agents
CHEBI has role	CHEBI:48278	serotonergic drugs
CHEBI has role	CHEBI:48407	antiparkinson agent
CHEBI has role	CHEBI:48539	alpha-adrenergic drugs
CHEBI has role	CHEBI:51065	Dopamine receptor agonist
CHEBI has role	CHEBI:66956	antidyskinetic agent
CHEBI has role	CHEBI:149552	emetics

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

Disease	Relation	SNOMED_ID	DOID
Parkinson's disease	indication	49049000	DOID:14330
Priapism	contraindication	6273006	DOID:9286
Alcoholism	contraindication	7200002
Dyskinesia	contraindication	9748009
Acute vomiting	contraindication	23971007
Alcohol intoxication	contraindication	25702006
Orthostatic hypotension	contraindication	28651003
Torsades de pointes	contraindication	31722008
Hypokalemia	contraindication	43339004
Acute nephropathy	contraindication	58574008
Cerebrovascular disease	contraindication	62914000	DOID:6713
Psychotic disorder	contraindication	69322001
Prolonged QT interval	contraindication	111975006
Hypomagnesemia	contraindication	190855004
Impaired renal function disorder	contraindication	197663003
Disease of liver	contraindication	235856003	DOID:409
Drowsy	contraindication	271782001
Disorder of coronary artery	contraindication	414024009
Congenital long QT syndrome	contraindication	442917000
Progressive Angina Pectoris	contraindication
Severe Nausea	contraindication
Predisposition to Nausea and Vomiting	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.88	acidic
pKa2	12.98	acidic
pKa3	8.36	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
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10420763	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9283219	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9326981	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9669019	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9669021	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
15MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10420763	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
15MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9283219	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
15MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9326981	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
15MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9669019	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
15MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9669021	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
20MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10420763	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
20MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9283219	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
20MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9326981	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
20MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9669019	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
20MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9669021	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
25MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10420763	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
25MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9283219	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
25MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9326981	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
25MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9669019	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
25MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9669021	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
30MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10420763	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
30MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9283219	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
30MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9326981	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
30MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9669019	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
30MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9669021	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	11419769	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	8414922	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	8846074	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
15MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	11419769	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
15MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	8414922	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
15MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	8846074	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
20MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	11419769	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
20MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	8414922	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
20MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	8846074	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
25MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	11419769	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
25MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	8414922	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
25MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	8846074	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
30MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	11419769	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
30MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	8414922	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
30MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	8846074	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10449146	April 19, 2036	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10959943	April 19, 2036	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
15MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10449146	April 19, 2036	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
15MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10959943	April 19, 2036	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
20MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10449146	April 19, 2036	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
20MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10959943	April 19, 2036	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
25MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10449146	April 19, 2036	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
25MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10959943	April 19, 2036	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
30MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10449146	April 19, 2036	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
30MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10959943	April 19, 2036	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	May 21, 2023	NEW PRODUCT
15MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	May 21, 2023	NEW PRODUCT
20MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	May 21, 2023	NEW PRODUCT
25MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	May 21, 2023	NEW PRODUCT
30MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	May 21, 2023	NEW PRODUCT

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	AGONIST	Ki	9.21	CHEMBL	CHEMBL
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN	AGONIST	Ki	8.05	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	8.34	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN	AGONIST	Ki	6.90	IUPHAR
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	6.53	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	6.90	IUPHAR
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN	ANTAGONIST	Ki	6.90	IUPHAR
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	ANTAGONIST	Ki	7	IUPHAR
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	5.70	PDSP
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN	ANTAGONIST	Ki	7.20	IUPHAR
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN	AGONIST	Ki	8.59	CHEMBL
D(1B) dopamine receptor	GPCR	P21918	DRD5_HUMAN	AGONIST	Ki	7.80	IUPHAR
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN		Ki	5.53	PDSP
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN		Ki	5.91	PDSP
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	7.19	WOMBAT-PK
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	6.17	PDSP
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	4.68	CHEMBL
Transient receptor potential cation channel subfamily A member 1	Ion channel	O75762	TRPA1_HUMAN	ACTIVATOR	EC50	5.10	IUPHAR
Mannose-6-phosphate isomerase	Enzyme	P34949	MPI_HUMAN		IC50	4.84	CHEMBL
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN	ANTAGONIST	Ki	7.40	IUPHAR
E3 ubiquitin-protein ligase Mdm2	Nuclear other	Q00987	MDM2_HUMAN		IC50	6.71	CHEMBL
D(2) dopamine receptor	GPCR		DRD2_RAT		Ki	8.74	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		Ki	6.53	CHEMBL
5-hydroxytryptamine receptor 7	GPCR		5HT7R_RAT		Ki	6.73	CHEMBL
D(1A) dopamine receptor	GPCR		DRD1_RAT		Ki	7.28	CHEMBL
D(2) dopamine receptor	GPCR		DRD2_BOVIN		Ki	6.70	CHEMBL
D(3) dopamine receptor	GPCR		DRD3_RAT		Ki	7.44	CHEMBL
D(4) dopamine receptor	GPCR		DRD4_RAT		EC50	8.82	CHEMBL
D(1A) dopamine receptor	GPCR		DRD1_MOUSE		Ki	7	CHEMBL
Zinc finger protein mex-5	Cytosolic other		MEX5_CAEEL		EC50	5.35	CHEMBL
Opioid receptor	GPCR		OPRD_RAT OPRM_RAT OPRK_RAT SGMR1_RAT		IC50	6.52	CHEMBL
Serotonin (5-HT) receptor	GPCR		5HT2C_RAT 5HT2A_RAT 5HT1A_RAT 5HT1B_RAT 5HT1D_RAT 5HT1F_RAT 5HT2B_RAT 5HT6R_RAT 5HT7R_RAT 5HT5A_RAT 5HT5B_RAT 5HT3A_RAT 5HT4R_RAT 5HT3B_RAT		IC50	5.35	CHEMBL
Adrenergic receptor alpha-2	GPCR		ADA2B_RAT ADA2C_RAT ADA2A_RAT		IC50	7.20	CHEMBL
Dopamine receptor	GPCR		DRD2_BOVIN DRD1_BOVIN		IC50	9	CHEMBL
Dopamine receptor	GPCR		DRD1_RAT DRD3_RAT DRD5_RAT DRD4_RAT DRD2_RAT		IC50	9	CHEMBL
Adrenergic receptor alpha-1	GPCR		ADA1B_RAT ADA1D_RAT ADA1A_RAT		IC50	5.11	CHEMBL
Cytoplasmic zinc-finger protein	Unclassified		G5EF15_CAEEL		EC50	4.77	CHEMBL

External reference:

ID	Source
4019618	VUID
N0000147712	NUI
D02004	KEGG_DRUG
41372-20-7	SECONDARY_CAS_RN
1043	RXNORM
C0003596	UMLSCUI
CHEBI:48538	CHEBI
5RL	PDB_CHEM_ID
CHEMBL53	ChEMBL_ID
DB00714	DRUGBANK_ID
CHEMBL1616	ChEMBL_ID
D001058	MESH_DESCRIPTOR_UI
6005	PUBCHEM_CID
33	IUPHAR_LIGAND_ID
N21FAR7B4S	UNII
17790	MMSL
71829	MMSL
d04991	MMSL
387375001	SNOMEDCT_US
67939000	SNOMEDCT_US
725667002	SNOMEDCT_US
74950007	SNOMEDCT_US
CHEMBL1256708	ChEMBL_ID
4017524	VANDF
4019618	VANDF
001665	NDDF
004677	NDDF

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
APOKYN	HUMAN PRESCRIPTION DRUG LABEL	1	27505-004	INJECTION	30 mg	SUBCUTANEOUS	NDA	35 sections
APOKYN	HUMAN PRESCRIPTION DRUG LABEL	1	27505-004	INJECTION	30 mg	SUBCUTANEOUS	NDA	35 sections
APOKYN	HUMAN PRESCRIPTION DRUG LABEL	1	27505-004	INJECTION	30 mg	SUBCUTANEOUS	NDA	35 sections
APOKYN	HUMAN PRESCRIPTION DRUG LABEL	1	27505-004	INJECTION	30 mg	SUBCUTANEOUS	NDA	35 sections
apomorphine hydrocloride	HUMAN PRESCRIPTION DRUG LABEL	1	52817-720	INJECTION	30 mg	SUBCUTANEOUS	ANDA	33 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-010	FILM, SOLUBLE	10 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-010	FILM, SOLUBLE	10 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-010	FILM, SOLUBLE	10 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-015	FILM, SOLUBLE	15 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-015	FILM, SOLUBLE	15 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-015	FILM, SOLUBLE	15 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-020	FILM, SOLUBLE	20 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-020	FILM, SOLUBLE	20 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-020	FILM, SOLUBLE	20 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-025	FILM, SOLUBLE	25 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-025	FILM, SOLUBLE	25 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-025	FILM, SOLUBLE	25 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-030	FILM, SOLUBLE	30 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-030	FILM, SOLUBLE	30 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-030	FILM, SOLUBLE	30 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-110	FILM, SOLUBLE	10 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-110	FILM, SOLUBLE	10 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-110	FILM, SOLUBLE	10 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-115	FILM, SOLUBLE	15 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-115	FILM, SOLUBLE	15 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-115	FILM, SOLUBLE	15 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-120	FILM, SOLUBLE	20 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-120	FILM, SOLUBLE	20 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-120	FILM, SOLUBLE	20 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-125	FILM, SOLUBLE	25 mg	SUBLINGUAL	NDA	34 sections