apomorphine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
228 58-00-4

Description:

MoleculeDescription

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:

DoseUnitRoute
2 mg SL
20 mg P

ADMET properties:

PropertyValueReference
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 ยตM/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:

DateAgencyCompanyOrphan
April 20, 2004 FDA US WORLDMEDS

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
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 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
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 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
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:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.88 acidic
pKa2 12.98 acidic
pKa3 8.36 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
D(2) dopamine receptor GPCR AGONIST Ki 9.21 CHEMBL CHEMBL
D(4) dopamine receptor GPCR AGONIST Ki 8.05 CHEMBL
D(1A) dopamine receptor GPCR Ki 8.34 CHEMBL
Alpha-2A adrenergic receptor GPCR AGONIST Ki 6.90 IUPHAR
5-hydroxytryptamine receptor 1A GPCR Ki 6.53 CHEMBL
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 6.90 IUPHAR
5-hydroxytryptamine receptor 2B GPCR ANTAGONIST Ki 6.90 IUPHAR
5-hydroxytryptamine receptor 2C GPCR ANTAGONIST Ki 7 IUPHAR
Alpha-1A adrenergic receptor GPCR Ki 5.70 PDSP
Alpha-2B adrenergic receptor GPCR ANTAGONIST Ki 7.20 IUPHAR
D(3) dopamine receptor GPCR AGONIST Ki 8.59 CHEMBL
D(1B) dopamine receptor GPCR AGONIST Ki 7.80 IUPHAR
5-hydroxytryptamine receptor 1B GPCR Ki 5.53 PDSP
5-hydroxytryptamine receptor 1D GPCR Ki 5.91 PDSP
Alpha-1D adrenergic receptor GPCR Ki 7.19 WOMBAT-PK
Alpha-1B adrenergic receptor GPCR Ki 6.17 PDSP
Solute carrier family 22 member 1 Transporter IC50 4.68 CHEMBL
Transient receptor potential cation channel subfamily A member 1 Ion channel ACTIVATOR EC50 5.10 IUPHAR
Mannose-6-phosphate isomerase Enzyme IC50 4.84 CHEMBL
Alpha-2C adrenergic receptor GPCR ANTAGONIST Ki 7.40 IUPHAR
E3 ubiquitin-protein ligase Mdm2 Nuclear other IC50 6.71 CHEMBL
D(2) dopamine receptor GPCR Ki 8.74 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 6.53 CHEMBL
5-hydroxytryptamine receptor 7 GPCR Ki 6.73 CHEMBL
D(1A) dopamine receptor GPCR Ki 7.28 CHEMBL
D(2) dopamine receptor GPCR Ki 6.70 CHEMBL
D(3) dopamine receptor GPCR Ki 7.44 CHEMBL
D(4) dopamine receptor GPCR EC50 8.82 CHEMBL
D(1A) dopamine receptor GPCR Ki 7 CHEMBL
Zinc finger protein mex-5 Cytosolic other EC50 5.35 CHEMBL
Opioid receptor GPCR IC50 6.52 CHEMBL
Serotonin (5-HT) receptor GPCR IC50 5.35 CHEMBL
Adrenergic receptor alpha-2 GPCR IC50 7.20 CHEMBL
Dopamine receptor GPCR IC50 9 CHEMBL
Dopamine receptor GPCR IC50 9 CHEMBL
Adrenergic receptor alpha-1 GPCR IC50 5.11 CHEMBL
Cytoplasmic zinc-finger protein Unclassified EC50 4.77 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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