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

Stem definitionDrug idCAS RN
psychoactive 4115 65576-45-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • Org-5222
  • Org 5222
  • asenapine
  • saphris
  • asenapine maleate
  • sycrest
  • Molecular weight: 285.77
  • Formula: C17H16ClNO
  • CLOGP: 4.28
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 12.47
  • ALOGS: -3.96
  • ROTB: 0
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
20 mg SL

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.71 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 23 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 12.40 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.05 % Lombardo F, Berellini G, Obach RS
S (Water solubility) 3.70 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,STK33,TEK,TGFBR1,TTK 36
kinase-selectivity-class AXL,EIF2AK3,PDK4 3
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Aug. 13, 2009 FDA FOREST LABS INC

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
Blood prolactin abnormal 1390.17 35.04 251 9965 3015 90615216
Anosognosia 1384.21 35.04 253 9963 3269 90614962
Disturbance in social behaviour 1334.16 35.04 252 9964 3936 90614295
Sexual dysfunction 1293.48 35.04 251 9965 4553 90613678
Metabolic disorder 1177.25 35.04 250 9966 7220 90611011
Personality change 1125.10 35.04 240 9976 7081 90611150
Dystonia 1104.28 35.04 276 9940 16543 90601688
Sedation 986.56 35.04 318 9898 47853 90570378
Dyskinesia 964.81 35.04 293 9923 36241 90581990
Suicide attempt 693.13 35.04 275 9941 75124 90543107
Blood glucose increased 634.32 35.04 276 9940 94970 90523261
Inappropriate schedule of product administration 481.54 35.04 264 9952 149669 90468562
Hypoaesthesia oral 462.36 35.04 137 10079 15463 90602768
Underdose 357.16 35.04 156 10060 53861 90564370
Akathisia 278.95 35.04 86 10130 11073 90607158
Incorrect route of product administration 227.67 35.04 112 10104 50514 90567717
Insurance issue 162.80 35.04 57 10159 10901 90607330
Dysgeusia 142.31 35.04 83 10133 52477 90565754
Personality change due to a general medical condition 121.31 35.04 22 10194 268 90617963
Swollen tongue 115.04 35.04 69 10147 45887 90572344
Mania 110.41 35.04 46 10170 14078 90604153
Completed suicide 107 35.04 105 10111 144953 90473278
Adverse drug reaction 102.36 35.04 93 10123 116608 90501623
Condition aggravated 85.23 35.04 199 10017 595346 90022885
Tooth discolouration 85.14 35.04 21 10195 1177 90617054
Tardive dyskinesia 80.09 35.04 34 10182 10896 90607335
Extrapyramidal disorder 75.99 35.04 37 10179 16266 90601965
Drug ineffective 72.43 35.04 327 9889 1383971 89234260
Suicidal ideation 68.95 35.04 61 10155 73794 90544437
Weight increased 62.23 35.04 142 10074 417785 90200446
Restless legs syndrome 62.14 35.04 36 10180 22434 90595797
Oral discomfort 58.70 35.04 27 10189 10456 90607775
Oropharyngeal blistering 53.04 35.04 14 10202 1029 90617202
Somnolence 53.04 35.04 89 10127 208995 90409236
Diarrhoea 51.25 35.04 21 10195 939169 89679062
Fatigue 49.58 35.04 35 10181 1153988 89464243
Tongue blistering 48.73 35.04 15 10201 1915 90616316
Polydipsia 47.85 35.04 18 10198 4213 90614018
Arthralgia 46.52 35.04 15 10201 778507 89839724
Agitation 46.50 35.04 47 10169 67051 90551180
Hallucination, auditory 45.25 35.04 26 10190 15949 90602282
Pain 43.04 35.04 30 10186 996311 89621920
Myocarditis 40.52 35.04 23 10193 13783 90604448
Tremor 38.54 35.04 65 10151 153108 90465123
Psychotic disorder 37.83 35.04 30 10186 31200 90587031
Embolic stroke 37.77 35.04 15 10201 4057 90614174
Restlessness 36.34 35.04 31 10185 35689 90582542
Neuroleptic malignant syndrome 36.03 35.04 22 10194 15074 90603157
Peripheral swelling 35.43 35.04 3 10213 413103 90205128
Delusion 35.17 35.04 21 10195 13819 90604412

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
Suicide attempt 587.44 36.86 240 7173 45860 42568062
Akathisia 568.94 36.86 162 7251 10289 42603633
Antipsychotic drug level below therapeutic 515.43 36.86 118 7295 3086 42610836
Disinhibition 497.68 36.86 119 7294 3776 42610146
Therapeutic product effect variable 497.43 36.86 114 7299 2995 42610927
Obsessive-compulsive disorder 456.15 36.86 124 7289 6619 42607303
Euphoric mood 438.05 36.86 119 7294 6334 42607588
Increased appetite 430.83 36.86 126 7287 8780 42605142
Anosognosia 359.29 36.86 72 7341 972 42612950
Sedation 348.09 36.86 147 7266 30328 42583594
Blood prolactin abnormal 328.80 36.86 67 7346 988 42612934
Disturbance in social behaviour 293.03 36.86 67 7346 1736 42612186
Dystonia 272.02 36.86 97 7316 12693 42601229
Sexual dysfunction 238.05 36.86 75 7338 6700 42607222
Leukaemia 232.71 36.86 71 7342 5701 42608221
Metabolic disorder 232.51 36.86 68 7345 4720 42609202
Emotional poverty 214.67 36.86 44 7369 668 42613254
Weight increased 209.42 36.86 163 7250 107820 42506102
Dyskinesia 195.35 36.86 93 7320 25297 42588625
Therapeutic product effect incomplete 187.04 36.86 129 7284 70810 42543112
Personality change 174.96 36.86 57 7356 5662 42608260
Dyslipidaemia 172.49 36.86 64 7349 9354 42604568
Leukopenia 149.40 36.86 115 7298 74631 42539291
Prescribed overdose 146.14 36.86 62 7351 12865 42601057
Obesity 141.10 36.86 65 7348 16394 42597528
Inappropriate schedule of product administration 116.67 36.86 111 7302 95791 42518131
Toxicity to various agents 114.69 36.86 168 7245 228968 42384954
Schizoaffective disorder 109.06 36.86 31 7382 1939 42611983
Hypoaesthesia oral 104.41 36.86 37 7376 4736 42609186
Underdose 101.19 36.86 52 7361 16614 42597308
Extrapyramidal disorder 99.04 36.86 51 7362 16361 42597561
Irritability 92.99 36.86 59 7354 28069 42585853
Hallucination, auditory 89.14 36.86 46 7367 14818 42599104
Blood glucose increased 88.97 36.86 85 7328 73614 42540308
Drug ineffective 87.58 36.86 273 7140 629924 41983998
Suicidal ideation 85.12 36.86 69 7344 48092 42565830
Head titubation 79.24 36.86 18 7395 451 42613471
Cogwheel rigidity 71.89 36.86 22 7391 1779 42612143
Mania 67.17 36.86 34 7379 10513 42603409
Incorrect route of product administration 63.41 36.86 44 7369 24261 42589661
Sedation complication 54.01 36.86 20 7393 2899 42611023
Dysgeusia 48.11 36.86 43 7370 34146 42579776
Hallucination, visual 43.32 36.86 33 7380 20987 42592935
Swollen tongue 43.03 36.86 33 7380 21198 42592724
Anticholinergic syndrome 41.24 36.86 14 7399 1575 42612347
Psychotic disorder 39.64 36.86 36 7377 29172 42584750
Pneumonia 38.16 36.86 13 7400 422136 42191786
Anaemia 37.53 36.86 3 7410 280275 42333647

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
Anosognosia 1577.54 30.03 290 12445 3784 110572780
Blood prolactin abnormal 1543.07 30.03 282 12453 3553 110573011
Disturbance in social behaviour 1471.36 30.03 283 12452 4775 110571789
Sexual dysfunction 1363.74 30.03 290 12445 8240 110568324
Metabolic disorder 1265 30.03 283 12452 10227 110566337
Personality change 1197.98 30.03 273 12462 10729 110565835
Dystonia 1170.20 30.03 317 12418 25488 110551076
Sedation 1118.91 30.03 385 12350 69298 110507266
Dyskinesia 1039.16 30.03 338 12397 51108 110525456
Suicide attempt 1016.56 30.03 398 12337 102996 110473568
Blood glucose increased 627.13 30.03 305 12430 132191 110444373
Akathisia 388.01 30.03 123 12612 16990 110559574
Inappropriate schedule of product administration 381.51 30.03 256 12479 203381 110373183
Hypoaesthesia oral 295.67 30.03 100 12635 16902 110559662
Underdose 266.47 30.03 135 12600 63419 110513145
Emotional poverty 192.63 30.03 40 12695 1000 110575564
Antipsychotic drug level below therapeutic 188.25 30.03 43 12692 1692 110574872
Insurance issue 186.76 30.03 63 12672 10549 110566015
Therapeutic product effect variable 169.06 30.03 43 12692 2675 110573889
Disinhibition 167.78 30.03 44 12691 3090 110573474
Increased appetite 161.96 30.03 62 12673 14915 110561649
Drug ineffective 149.04 30.03 446 12289 1520094 109056470
Obsessive-compulsive disorder 139.39 30.03 46 12689 7195 110569369
Adverse drug reaction 136.06 30.03 106 12629 105453 110471111
Incorrect route of product administration 127.93 30.03 84 12651 63977 110512587
Euphoric mood 126.66 30.03 45 12690 8782 110567782
Suicidal ideation 113.87 30.03 91 12644 93846 110482718
Mania 113.64 30.03 53 12682 20743 110555821
Schizoaffective disorder 107.43 30.03 31 12704 3105 110573459
Personality change due to a general medical condition 106.30 30.03 20 12715 295 110576269
Dyslipidaemia 100.81 30.03 45 12690 15920 110560644
Hallucination, auditory 98.79 30.03 52 12683 26345 110550219
Irritability 98.64 30.03 64 12671 47745 110528819
Extrapyramidal disorder 88.95 30.03 50 12685 28817 110547747
Swollen tongue 87.39 30.03 65 12670 60297 110516267
Condition aggravated 83.42 30.03 228 12507 734608 109841956
Completed suicide 83.26 30.03 120 12615 242261 110334303
Dysgeusia 76.80 30.03 64 12671 69921 110506643
Neuroleptic malignant syndrome 71.24 30.03 46 12689 34013 110542551
Tardive dyskinesia 66.20 30.03 32 12703 13547 110563017
Leukaemia 63.35 30.03 26 12709 7492 110569072
Weight increased 63.02 30.03 145 12590 419499 110157065
Parkinsonism 56.60 30.03 34 12701 22153 110554411
Diarrhoea 53.05 30.03 33 12702 1139472 109437092
Pneumonia 50.49 30.03 19 12716 876695 109699869
Myocarditis 49.48 30.03 35 12700 30020 110546544
Agitation 49.45 30.03 63 12672 112988 110463576
Fatigue 49.06 30.03 41 12694 1215917 109360647
Arthralgia 48.16 30.03 15 12720 779617 109796947
Psychotic disorder 42.70 30.03 40 12695 50897 110525667
Anaemia 40.74 30.03 7 12728 547079 110029485
Somnolence 40.49 30.03 99 12636 297350 110279214
Tooth discolouration 40.20 30.03 12 12723 1351 110575213
Prescribed overdose 40.20 30.03 50 12685 87531 110489033
Peripheral swelling 35.38 30.03 3 12732 404031 110172533
Cogwheel rigidity 35.33 30.03 14 12721 3684 110572880
Delusion 35.30 30.03 26 12709 23729 110552835
Product solubility abnormal 33.28 30.03 10 12725 1152 110575412
Abdominal pain 33.24 30.03 9 12726 512980 110063584
Oral discomfort 33.24 30.03 19 12716 11292 110565272
Cataplexy 33.22 30.03 10 12725 1159 110575405
Pain 32.88 30.03 37 12698 954918 109621646
Drooling 32.33 30.03 16 12719 7123 110569441
Paranoia 32.15 30.03 24 12711 22350 110554214
Pharyngeal hypoaesthesia 31.76 30.03 8 12727 478 110576086
Head titubation 31.75 30.03 10 12725 1347 110575217
Infection 30.87 30.03 3 12732 362197 110214367
Toxicity to various agents 30.76 30.03 123 12612 480432 110096132
Bipolar I disorder 30.34 30.03 11 12724 2272 110574292

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AH05 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Diazepines, oxazepines, thiazepines and oxepines
FDA EPC N0000175430 Atypical Antipsychotic
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents
MeSH PA D014150 Antipsychotic Agents
CHEBI has role CHEBI:35471 psychotropic drug
CHEBI has role CHEBI:35530 β-adrenergic antagonist
CHEBI has role CHEBI:37890 α-adrenergic antagonist
CHEBI has role CHEBI:48279 serotonergic antagonist
CHEBI has role CHEBI:48561 dopaminergic antagonist
CHEBI has role CHEBI:65191 second generation antipsychotic

Related Drugs by ATC class:

N05AH Diazepines, oxazepines, thiazepines and oxepines 6 drugs
clotiapineclozapineloxapineolanzapinequetiapinesamidorphan

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

DiseaseRelationSNOMED_IDDOID
Mixed bipolar I disorder indication 16506000 DOID:3312
Schizophrenia indication 58214004 DOID:5419
Bipolar affective disorder, current episode manic indication 191618007
Depression Treatment Adjunct off-label use
Suicidal thoughts contraindication 6471006
Weight gain finding contraindication 8943002
Neuroleptic malignant syndrome contraindication 15244003 DOID:14464
Agranulocytosis contraindication 17182001 DOID:12987
Lowered convulsive threshold contraindication 19260006
Myocardial infarction contraindication 22298006 DOID:5844
Alzheimer's disease contraindication 26929004 DOID:10652
Hypovolemia contraindication 28560003
Orthostatic hypotension contraindication 28651003
Torsades de pointes contraindication 31722008
Dehydration contraindication 34095006
Dysphagia contraindication 40739000
Hypokalemia contraindication 43339004
Bradycardia contraindication 48867003
Hepatic failure contraindication 59927004
Cerebrovascular disease contraindication 62914000 DOID:6713
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Leukopenia contraindication 84828003 DOID:615
Tardive dyskinesia contraindication 102449007
Prolonged QT interval contraindication 111975006
Seizure disorder contraindication 128613002
Hypomagnesemia contraindication 190855004
Cerebrovascular accident contraindication 230690007
Hyperprolactinemia contraindication 237662005 DOID:12700
Transient ischemic attack contraindication 266257000 DOID:224
Esophageal dysmotility contraindication 266434009 DOID:9192
Syncope contraindication 271594007
Neutropenic disorder contraindication 303011007 DOID:1227
Senile dementia with psychosis contraindication 371026009
At risk for aspiration contraindication 371736008
Impaired cognition contraindication 386806002
Myocardial ischemia contraindication 414795007 DOID:3393
Obesity contraindication 414916001 DOID:9970
Congenital long QT syndrome contraindication 442917000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.13 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 10MG BASE SAPHRIS ABBVIE N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 7741358 April 6, 2026 TREATMENT OF BIPOLAR DISORDER AND SCHIZOPHRENIA
EQ 10MG BASE SAPHRIS ABBVIE N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 7741358 April 6, 2026 USE OF THE ATYPICAL ANTIPSYCHOTIC ASENAPINE FOR TREATMENT OF MANIC OR MIXED EPISODES OF BIPOLAR I DISORDER: ACUTE MONOTHERAPY OF MANIC OR MIXED EPISODES (AGES 10 TO ADULT)
EQ 10MG BASE SAPHRIS ABBVIE N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 7741358 April 6, 2026 USE OF THE ATYPICAL ANTIPSYCHOTIC ASENAPINE FOR TREATMENT OF MANIC OR MIXED EPISODES OF BIPOLAR I DISORDER: AS ADJUNCTIVE TREATMENT TO LITHIUM OR VALPROATE IN ADULTS
EQ 10MG BASE SAPHRIS ABBVIE N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 7741358 April 6, 2026 USE OF THE ATYPICAL ANTIPSYCHOTIC ASENAPINE FOR TREATMENT OF MANIC OR MIXED EPISODES OF BIPOLAR I DISORDER: MAINTENANCE MONOTHERAPY IN ADULTS
EQ 10MG BASE SAPHRIS ABBVIE N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 7741358 April 6, 2026 USE OF THE ATYPICAL ANTIPSYCHOTIC ASENAPINE FOR TREATMENT OF SCHIZOPHRENIA IN ADULTS
EQ 2.5MG BASE SAPHRIS ABBVIE N022117 March 12, 2015 RX TABLET SUBLINGUAL 7741358 April 6, 2026 METHOD OF TREATING MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR DISORDER IN PEDIATRIC PATIENTS
EQ 2.5MG BASE SAPHRIS ABBVIE N022117 March 12, 2015 RX TABLET SUBLINGUAL 7741358 April 6, 2026 USE OF THE ATYPICAL ANTIPSYCHOTIC ASENAPINE FOR TREATMENT OF MANIC OR MIXED EPISODES OF BIPOLAR I DISORDER: ACUTE MONOTHERAPY OF MANIC OR MIXED EPISODES IN PEDIATRIC PATIENTS AGE 10-17
EQ 5MG BASE SAPHRIS ABBVIE N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 7741358 April 6, 2026 TREATMENT OF BIPOLAR DISORDER AND SCHIZOPHRENIA
EQ 5MG BASE SAPHRIS ABBVIE N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 7741358 April 6, 2026 USE OF THE ATYPICAL ANTIPSYCHOTIC ASENAPINE FOR TREATMENT OF MANIC OR MIXED EPISODES OF BIPOLAR I DISORDER: ACUTE MONOTHERAPY OF MANIC OR MIXED EPISODES (AGES 10 TO ADULT)
EQ 5MG BASE SAPHRIS ABBVIE N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 7741358 April 6, 2026 USE OF THE ATYPICAL ANTIPSYCHOTIC ASENAPINE FOR TREATMENT OF MANIC OR MIXED EPISODES OF BIPOLAR I DISORDER: AS ADJUNCTIVE TREATMENT TO LITHIUM OR VALPROATE IN ADULTS
EQ 5MG BASE SAPHRIS ABBVIE N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 7741358 April 6, 2026 USE OF THE ATYPICAL ANTIPSYCHOTIC ASENAPINE FOR TREATMENT OF MANIC OR MIXED EPISODES OF BIPOLAR I DISORDER: MAINTENANCE MONOTHERAPY IN ADULTS
EQ 5MG BASE SAPHRIS ABBVIE N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 7741358 April 6, 2026 USE OF THE ATYPICAL ANTIPSYCHOTIC ASENAPINE FOR TREATMENT OF SCHIZOPHRENIA IN ADULTS
3.8MG/24HR SECUADO HISAMITSU N212268 Oct. 11, 2019 RX SYSTEM TRANSDERMAL 10583121 July 25, 2033 METHOD OF TREATING ADULTS WITH SCHIZOPHRENIA COMPRISING ADMINISTERING ASENAPINE VIA A TRANSDERMAL PATCH
3.8MG/24HR SECUADO HISAMITSU N212268 Oct. 11, 2019 RX SYSTEM TRANSDERMAL 10814002 July 25, 2033 METHOD OF TREATING ADULTS WITH SCHIZOPHRENIA COMPRISING ADMINISTERING ASENAPINE VIA A TRANSDERMAL PATCH
5.7MG/24HR SECUADO HISAMITSU N212268 Oct. 11, 2019 RX SYSTEM TRANSDERMAL 10583121 July 25, 2033 METHOD OF TREATING ADULTS WITH SCHIZOPHRENIA COMPRISING ADMINISTERING ASENAPINE VIA A TRANSDERMAL PATCH
5.7MG/24HR SECUADO HISAMITSU N212268 Oct. 11, 2019 RX SYSTEM TRANSDERMAL 10814002 July 25, 2033 METHOD OF TREATING ADULTS WITH SCHIZOPHRENIA COMPRISING ADMINISTERING ASENAPINE VIA A TRANSDERMAL PATCH
7.6MG/24HR SECUADO HISAMITSU N212268 Oct. 11, 2019 RX SYSTEM TRANSDERMAL 10583121 July 25, 2033 METHOD OF TREATING ADULTS WITH SCHIZOPHRENIA COMPRISING ADMINISTERING ASENAPINE VIA A TRANSDERMAL PATCH
7.6MG/24HR SECUADO HISAMITSU N212268 Oct. 11, 2019 RX SYSTEM TRANSDERMAL 10814002 July 25, 2033 METHOD OF TREATING ADULTS WITH SCHIZOPHRENIA COMPRISING ADMINISTERING ASENAPINE VIA A TRANSDERMAL PATCH

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
D(2) dopamine receptor GPCR ANTAGONIST Ki 8.75 WOMBAT-PK CHEMBL
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 9.61 WOMBAT-PK CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 6.11 PDSP
Beta-1 adrenergic receptor GPCR Ki 5.30 PDSP
Beta-2 adrenergic receptor GPCR Ki 5.30 PDSP
D(1A) dopamine receptor GPCR Ki 8.70 WOMBAT-PK
Alpha-2A adrenergic receptor GPCR Ki 8.19 PDSP
5-hydroxytryptamine receptor 1A GPCR Ki 7.97 WOMBAT-PK
5-hydroxytryptamine receptor 2B GPCR Ki 9.80 WOMBAT-PK
5-hydroxytryptamine receptor 2C GPCR Ki 9.93 WOMBAT-PK
5-hydroxytryptamine receptor 6 GPCR Ki 9.22 WOMBAT-PK
5-hydroxytryptamine receptor 7 GPCR Ki 9.47 WOMBAT-PK
Alpha-1A adrenergic receptor GPCR Ki 8.92 WOMBAT-PK
Alpha-2B adrenergic receptor GPCR Ki 8.73 WOMBAT-PK
D(3) dopamine receptor GPCR Ki 9.06 WOMBAT-PK
D(1B) dopamine receptor GPCR Ki 7.64 PDSP
Histamine H1 receptor GPCR Ki 9 WOMBAT-PK
Histamine H2 receptor GPCR IC50 8.21 WOMBAT-PK
Muscarinic acetylcholine receptor M5 GPCR Ki 6.57 PDSP
5-hydroxytryptamine receptor 1B GPCR Ki 8.40 WOMBAT-PK
5-hydroxytryptamine receptor 1D GPCR AGONIST Ki 8.40 IUPHAR
Alpha-2C adrenergic receptor GPCR Ki 7.89 PDSP
Sodium-dependent dopamine transporter Transporter Ki 5.50 PDSP
D(4) dopamine receptor GPCR Ki 8.71 WOMBAT-PK
5-hydroxytryptamine receptor 3A Ion channel Ki 6.35 PDSP
Alpha-1B adrenergic receptor GPCR Ki 8.41 PDSP
5-hydroxytryptamine receptor 5A GPCR Ki 8.60 WOMBAT-PK
Muscarinic acetylcholine receptor M2 GPCR Ki 6.04 PDSP
5-hydroxytryptamine receptor 1E GPCR AGONIST Ki 8 IUPHAR
Muscarinic acetylcholine receptor M3 GPCR Ki 5.49 PDSP

External reference:

IDSource
4029058 VUID
N0000179817 NUI
D02995 KEGG_DRUG
85650-56-2 SECONDARY_CAS_RN
4029058 VANDF
C2000088 UMLSCUI
CHEBI:71253 CHEBI
CHEMBL3187365 ChEMBL_ID
CHEMBL3544974 ChEMBL_ID
DB06216 DRUGBANK_ID
C522667 MESH_SUPPLEMENTAL_RECORD_UI
163091 PUBCHEM_CID
22 IUPHAR_LIGAND_ID
8278 INN_ID
JKZ19V908O UNII
784649 RXNORM
167374 MMSL
26689 MMSL
341671 MMSL
d07473 MMSL
013233 NDDF
013234 NDDF
19504511000001109 SNOMEDCT_US
443374004 SNOMEDCT_US
443375003 SNOMEDCT_US
JKZ19V908O INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SAPHRIS HUMAN PRESCRIPTION DRUG LABEL 1 0456-2402 TABLET 2.50 mg SUBLINGUAL NDA 35 sections
SAPHRIS HUMAN PRESCRIPTION DRUG LABEL 1 0456-2405 TABLET 5 mg SUBLINGUAL NDA 35 sections
SAPHRIS HUMAN PRESCRIPTION DRUG LABEL 1 0456-2410 TABLET 10 mg SUBLINGUAL NDA 35 sections
SAPHRIS HUMAN PRESCRIPTION DRUG LABEL 1 16590-936 TABLET 10 mg SUBLINGUAL NDA 34 sections
ASENAPINE HUMAN PRESCRIPTION DRUG LABEL 1 42794-016 TABLET 5 mg SUBLINGUAL ANDA 21 sections
ASENAPINE HUMAN PRESCRIPTION DRUG LABEL 1 42794-017 TABLET 10 mg SUBLINGUAL ANDA 21 sections
Asenapine Human Prescription Drug Label 1 46708-198 TABLET 5 mg SUBLINGUAL ANDA 29 sections
Asenapine Human Prescription Drug Label 1 46708-199 TABLET 10 mg SUBLINGUAL ANDA 29 sections
Asenapine Human Prescription Drug Label 1 46708-544 TABLET 2.50 mg SUBLINGUAL ANDA 29 sections
Asenapine HUMAN PRESCRIPTION DRUG LABEL 1 51991-358 TABLET 5 mg SUBLINGUAL ANDA 36 sections
Asenapine HUMAN PRESCRIPTION DRUG LABEL 1 51991-359 TABLET 5 mg SUBLINGUAL ANDA 36 sections
Asenapine HUMAN PRESCRIPTION DRUG LABEL 1 51991-360 TABLET 10 mg SUBLINGUAL ANDA 36 sections
Asenapine HUMAN PRESCRIPTION DRUG LABEL 1 51991-361 TABLET 10 mg SUBLINGUAL ANDA 36 sections
Asenapine HUMAN PRESCRIPTION DRUG LABEL 1 51991-928 TABLET 2.50 mg SUBLINGUAL ANDA 36 sections
Asenapine Human Prescription Drug Label 1 62332-198 TABLET 5 mg SUBLINGUAL ANDA 30 sections
Asenapine Human Prescription Drug Label 1 62332-199 TABLET 10 mg SUBLINGUAL ANDA 30 sections
Asenapine Human Prescription Drug Label 1 62332-544 TABLET 2.50 mg SUBLINGUAL ANDA 30 sections
SECUADO HUMAN PRESCRIPTION DRUG LABEL 1 68968-0172 FILM, EXTENDED RELEASE 3.80 mg TRANSDERMAL NDA 33 sections
SECUADO HUMAN PRESCRIPTION DRUG LABEL 1 68968-0173 FILM, EXTENDED RELEASE 5.70 mg TRANSDERMAL NDA 33 sections
SECUADO HUMAN PRESCRIPTION DRUG LABEL 1 68968-0174 FILM, EXTENDED RELEASE 7.60 mg TRANSDERMAL NDA 33 sections
Asenapine Human Prescription Drug Label 1 69539-057 TABLET 5 mg SUBLINGUAL ANDA 20 sections
Asenapine Human Prescription Drug Label 1 69539-058 TABLET 5 mg SUBLINGUAL ANDA 20 sections
Asenapine Human Prescription Drug Label 1 69539-059 TABLET 10 mg SUBLINGUAL ANDA 20 sections
Asenapine Human Prescription Drug Label 1 69539-060 TABLET 10 mg SUBLINGUAL ANDA 20 sections
Asenapine Human Prescription Drug Label 1 69539-245 TABLET 2.50 mg SUBLINGUAL ANDA 20 sections