apomorphine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.466 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.755 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 29.376 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 55.847 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 9.520 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 22.670 % High 1
herg hERG pIC50 5.322 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 36.308 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 14.223 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 7.050 % High 1
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AURKC,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK2,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FGFR1,FLT3,GRK2,GRK3,GSK3B,IGF1R,ITK,JAK1,JAK2,JAK3,KDR,KIT,MAP2K6,MAP3K1,MAP3K14,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK10,MAPK12,MAPK14,MAPK7,MAPK8,MAPK9,MAPKAPK2,MAPKAPK5,MARK4,MELK,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM1,PIM2,PIM3,PLK1,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2,ZAP70 82
kinase-selectivity-class ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK4,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,INSR,IRAK1,JAK2,KIT,MAP2K6,MAP3K14,MAPK1,MAPK12,MAPK7,MAPK8,MARK4,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,TTK,ULK1 32
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 4.519 High 1
mh-clint Mouse hepatocyte intrinsic clearance 177.419 High 1
mppb Mouse plasma protein binding (% unbound) 9.300 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 7.261 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 19.930 % High 1
rh-clint Rat hepatocyte intrinsic clearance 191.867 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 46.210 % High 1
rppb Rat plasma protein binding (% unbound) 9.660 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 169.434 uM High 1

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 484.42 34.09 227 4366 208857 90414997
Nausea 421.87 34.09 384 4209 1109932 89513922
Blood pressure decreased 261.98 34.09 109 4484 74786 90549068
Dizziness 235.05 34.09 211 4382 589073 90034781
Yawning 229.42 34.09 41 4552 1071 90622783
Dyskinesia 140.53 34.09 57 4536 36477 90587377
Freezing phenomenon 120.96 34.09 26 4567 1786 90622068
On and off phenomenon 106.89 34.09 25 4568 2518 90621336
Feeling abnormal 104.13 34.09 78 4515 167157 90456697
Orthostatic hypotension 91.76 34.09 44 4549 41783 90582071
Product taste abnormal 86.83 34.09 21 4572 2439 90621415
Hyperhidrosis 85.74 34.09 64 4529 136241 90487613
Vomiting 80.48 34.09 143 4450 788150 89835704
Injection site nodule 78.93 34.09 22 4571 4451 90619403
Dysgeusia 76.67 34.09 42 4551 52518 90571336
Hallucination 75.53 34.09 45 4548 65914 90557940
Blood pressure increased 68.92 34.09 66 4527 197151 90426703
Tremor 64.67 34.09 57 4536 153116 90470738
Infusion site nodule 62.31 34.09 15 4578 1708 90622146
Hyperkinesia 60.70 34.09 15 4578 1904 90621950
Heart rate decreased 54.80 34.09 34 4559 53471 90570383
Injection site necrosis 53.93 34.09 13 4580 1488 90622366
Fall 52.30 34.09 90 4503 481720 90142134
Product packaging difficult to open 48.35 34.09 8 4585 130 90623724
Feeling hot 45.39 34.09 35 4558 77973 90545881
Dysstasia 44.95 34.09 23 4570 25029 90598825
Infusion site erythema 44.65 34.09 19 4574 13651 90610203
Cold sweat 44.11 34.09 19 4574 14062 90609792
Injection site irritation 39.90 34.09 14 4579 6001 90617853
Drug monitoring procedure not performed 39.82 34.09 9 4584 778 90623076
Hallucination, visual 35.16 34.09 19 4574 23073 90600781

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 570.51 38.35 330 6805 140775 42473425
Nausea 474.23 38.35 443 6692 396356 42217844
Dizziness 466.97 38.35 361 6774 248893 42365307
Yawning 453.14 38.35 83 7052 699 42613501
Blood pressure decreased 359.30 38.35 181 6954 58151 42556049
On and off phenomenon 205.27 38.35 57 7078 3410 42610790
Orthostatic hypotension 185.27 38.35 94 7041 30476 42583724
Dyskinesia 180.38 38.35 87 7048 25303 42588897
Cerebral hypoperfusion 172.22 38.35 39 7096 1004 42613196
Hyperhidrosis 167.67 38.35 131 7004 90381 42523819
Hallucination 132.63 38.35 95 7040 57412 42556788
Freezing phenomenon 116.13 38.35 32 7103 1857 42612343
Feeling abnormal 103.82 38.35 89 7046 69697 42544503
Feeling cold 90.68 38.35 44 7091 12929 42601271
Injection site nodule 85.55 38.35 26 7109 2135 42612065
Fall 76.70 38.35 139 6996 234381 42379819
Drug monitoring procedure not performed 74.20 38.35 17 7118 461 42613739
Hallucination, visual 70.78 38.35 44 7091 20976 42593224
Heart rate decreased 69.90 38.35 54 7081 36478 42577722
Cold sweat 66.10 38.35 34 7101 11296 42602904
Injection site necrosis 65.15 38.35 16 7119 588 42613612
Binocular eye movement disorder 64.70 38.35 14 7121 290 42613910
Pallor 62.58 38.35 46 7089 28840 42585360
Speech disorder 62.24 38.35 46 7089 29075 42585125
Rhinorrhoea 60.82 38.35 47 7088 31747 42582453
Cerebellar stroke 59.32 38.35 15 7120 622 42613578
Dysstasia 53.87 38.35 32 7103 14054 42600146
Balance disorder 53.60 38.35 52 7083 47593 42566607
Infusion site nodule 52.21 38.35 10 7125 109 42614091
Oral discomfort 50.70 38.35 19 7116 2958 42611242
Gait disturbance 48.17 38.35 70 7065 97930 42516270
Hypotension 43.28 38.35 117 7018 257514 42356686
Akinesia 42.91 38.35 16 7119 2456 42611744
Vomiting 42.26 38.35 125 7010 289598 42324602
Off label use 41.80 38.35 28 7107 638307 41975893
Dopamine dysregulation syndrome 41.27 38.35 11 7124 562 42613638
Dysgeusia 39.73 38.35 38 7097 34151 42580049
Feeling hot 39.09 38.35 32 7103 23450 42590750
Oesophageal achalasia 38.88 38.35 10 7125 444 42613756

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 1004.87 33.17 503 9572 296946 110282278
Nausea 792.06 33.17 743 9332 1234947 109344277
Yawning 636.69 33.17 112 9963 1435 110577789
Blood pressure decreased 588.39 33.17 260 9815 114831 110464393
Dizziness 587.42 33.17 492 9583 697701 109881523
Dyskinesia 267.99 33.17 118 9957 51328 110527896
On and off phenomenon 260.93 33.17 64 10011 4360 110574864
Orthostatic hypotension 260.57 33.17 125 9950 66124 110513100
Hyperhidrosis 236.73 33.17 169 9906 187129 110392095
Freezing phenomenon 217.80 33.17 50 10025 2559 110576665
Hallucination 197.52 33.17 120 9955 101312 110477912
Feeling abnormal 164.11 33.17 134 9941 180577 110398647
Infusion site nodule 142.60 33.17 26 10049 411 110578813
Injection site nodule 124.44 33.17 36 10039 4610 110574614
Heart rate decreased 114.39 33.17 79 9996 82677 110496547
Fall 114.31 33.17 200 9875 603282 109975942
Cold sweat 109.68 33.17 49 10026 21982 110557242
Dysgeusia 104.30 33.17 70 10005 69915 110509309
Drug monitoring procedure not performed 103.08 33.17 24 10051 1306 110577918
Product taste abnormal 101.65 33.17 27 10048 2525 110576699
Hallucination, visual 101.31 33.17 56 10019 39549 110539675
Vomiting 92.75 33.17 234 9841 910441 109668783
Dysstasia 82.60 33.17 46 10029 32940 110546284
Injection site necrosis 81.49 33.17 21 10054 1745 110577479
Blood pressure increased 78.90 33.17 107 9968 258266 110320958
Injection site irritation 75.99 33.17 25 10050 4899 110574325
Infusion site erythema 73.93 33.17 31 10044 11928 110567296
Pallor 73.55 33.17 52 10023 56415 110522809
Feeling hot 69.11 33.17 61 10014 91045 110488179
Rhinorrhoea 66.66 33.17 63 10012 102603 110476621
Infusion site irritation 64.23 33.17 16 10059 1159 110578065
Hyperkinesia 60.77 33.17 19 10056 3165 110576059
Tremor 57.56 33.17 81 9994 202151 110377073
Product packaging difficult to open 53.73 33.17 9 10066 84 110579140
Off label use 53.15 33.17 36 10039 1500149 109079075
Dopamine dysregulation syndrome 52.23 33.17 12 10063 615 110578609
Fatigue 51.77 33.17 233 9842 1215725 109363499
Injection site erythema 50.37 33.17 52 10023 94124 110485100
Akinesia 50.15 33.17 17 10058 3650 110575574
Drug effect less than expected 48.70 33.17 20 10055 7300 110571924
Device issue 47.75 33.17 33 10042 34502 110544722
Retching 41.93 33.17 26 10049 22656 110556568
Oral discomfort 40.36 33.17 20 10055 11291 110567933
Dystonia 38.86 33.17 26 10049 25779 110553445
Oesophageal achalasia 36.87 33.17 10 10065 1011 110578213
Drooling 35.91 33.17 16 10059 7123 110572101
Heart rate increased 35.66 33.17 54 10021 143780 110435444
Infusion site haemorrhage 35.56 33.17 14 10061 4584 110574640
Stoma site pain 34.50 33.17 11 10064 1952 110577272
Arthralgia 34.45 33.17 14 10061 779618 109799606
Illusion 34.26 33.17 11 10064 1996 110577228
Infusion site swelling 33.87 33.17 17 10058 9860 110569364
Stoma site erythema 33.68 33.17 11 10064 2106 110577118

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 D004639 Emetics
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D015259 Dopamine Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018491 Dopamine Agonists
CHEBI has role CHEBI:35476 antipsychotic agent
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:48278 serotonergic drug
CHEBI has role CHEBI:48407 antiparkinson drug
CHEBI has role CHEBI:48539 ฮฑ-adrenergic drug
CHEBI has role CHEBI:51065 dopamine agonist
CHEBI has role CHEBI:63726 neuroprotective agent
CHEBI has role CHEBI:66956 antidyskinesia agent
CHEBI has role CHEBI:149552 emetic

Related Drugs by ATC class:

G04BE Drugs used in erectile dysfunction 9 drugs
alprostadilavanafilmoxisylytepapaverinesildenafiltadalafiludenafilvardenafilyohimbine
N04BC Dopamine agonists 8 drugs
bromocriptinecabergolinedihydroergocryptinepergolidepiribedilpramipexoleropinirolerotigotine

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
98MG/20ML (4.9MG/ML) ONAPGO MDD US N214056 Feb. 3, 2025 RX SOLUTION SUBCUTANEOUS Feb. 3, 2028 NEW PRODUCT

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
D(2) dopamine receptor GPCR AGONIST Ki 9.21 CHEMBL CHEMBL
Alpha-2A adrenergic receptor GPCR AGONIST Ki 6.90 IUPHAR
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.62 CHEMBL
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-2C adrenergic receptor GPCR ANTAGONIST Ki 7.40 IUPHAR
D(4) dopamine receptor GPCR AGONIST Ki 8.05 CHEMBL
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
D(1A) dopamine receptor GPCR Ki 8.34 CHEMBL
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
M18 aspartyl aminopeptidase Enzyme IC50 5.43 CHEMBL
Cytoplasmic zinc-finger protein Cytosolic other 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
CHEMBL3187985 ChEMBL_ID
D001058 MESH_DESCRIPTOR_UI
6005 PUBCHEM_CID
33 IUPHAR_LIGAND_ID
N21FAR7B4S UNII
17790 MMSL
71829 MMSL
d04991 MMSL
4017524 VANDF
4019618 VANDF
001665 NDDF
004677 NDDF
387375001 SNOMEDCT_US
67939000 SNOMEDCT_US
725667002 SNOMEDCT_US
74950007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
APOKYN HUMAN PRESCRIPTION DRUG LABEL 1 27505-004 INJECTION 30 mg SUBCUTANEOUS NDA 35 sections
ONAPGO HUMAN PRESCRIPTION DRUG LABEL 1 27505-006 INJECTION, SOLUTION 4.90 mg SUBCUTANEOUS NDA 35 sections
ONAPGO HUMAN PRESCRIPTION DRUG LABEL 1 27505-006 INJECTION, SOLUTION 4.90 mg SUBCUTANEOUS NDA 35 sections
apomorphine hydrocloride HUMAN PRESCRIPTION DRUG LABEL 1 52817-720 INJECTION 30 mg SUBCUTANEOUS ANDA 33 sections