asenapine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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: 4.58
  • 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 O

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 ┬ÁM/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

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
Inappropriate schedule of product administration 951.08 47.00 229 1752 11975 2344129
Hypoaesthesia oral 623.27 47.00 120 1861 2066 2354038
Underdose 622.81 47.00 143 1838 5935 2350169
Incorrect route of product administration 386.23 47.00 95 1886 5241 2350863
Sedation 380.45 47.00 86 1895 3276 2352828
Akathisia 361.50 47.00 73 1908 1601 2354503
Weight increased 346.57 47.00 120 1861 22217 2333887
Dystonia 291.13 47.00 64 1917 2130 2353974
Dysgeusia 261.50 47.00 77 1904 8382 2347722
Dyskinesia 236.69 47.00 63 1918 4726 2351378
Anosognosia 222.01 47.00 31 1950 46 2356058
Glossodynia 210.16 47.00 48 1933 1897 2354207
Swollen tongue 202.23 47.00 57 1924 5286 2350818
Blood prolactin abnormal 187.67 47.00 28 1953 82 2356022
Somnolence 164.51 47.00 71 1910 23414 2332690
Disturbance in social behaviour 164.40 47.00 27 1954 169 2355935
Sexual dysfunction 156.77 47.00 28 1953 304 2355800
Tardive dyskinesia 141.55 47.00 34 1947 1670 2354434
Mania 134.25 47.00 35 1946 2405 2353699
Blood glucose increased 133.56 47.00 51 1930 12239 2343865
Metabolic disorder 133.44 47.00 27 1954 591 2355513
Personality change 122.12 47.00 27 1954 914 2355190
Dizziness 120.45 47.00 78 1903 58587 2297517
Restless legs syndrome 107.85 47.00 29 1952 2242 2353862
Suicidal ideation 102.69 47.00 41 1940 11046 2345058
Suicide attempt 101.99 47.00 41 1940 11241 2344863
Tooth discolouration 100.90 47.00 19 1962 281 2355823
Oedema peripheral 98.30 47.00 50 1931 23713 2332391
Extrapyramidal disorder 93.01 47.00 26 1955 2321 2353783
Insomnia 91.61 47.00 49 1932 25738 2330366
Oral discomfort 87.88 47.00 22 1959 1281 2354823
Tremor 86.94 47.00 44 1937 20617 2335487
Agitation 82.36 47.00 35 1946 11016 2345088
Dysphagia 80.60 47.00 36 1945 12769 2343335
Anxiety 80.31 47.00 47 1934 29312 2326792
Insurance issue 76.84 47.00 16 1965 404 2355700
Hypoaesthesia 73.38 47.00 39 1942 20176 2335928
Condition aggravated 71.51 47.00 45 1936 31934 2324170
Increased appetite 71.23 47.00 19 1962 1421 2354683
Tongue blistering 70.11 47.00 14 1967 285 2355819
Oropharyngeal blistering 65.75 47.00 13 1968 251 2355853
Completed suicide 63.67 47.00 36 1945 20998 2335106
Feeling abnormal 59.85 47.00 36 1945 23545 2332559
Schizophrenia 58.16 47.00 16 1965 1343 2354761
Drooling 57.65 47.00 14 1967 717 2355387
Nausea 56.63 47.00 67 1914 112122 2243982
Drug ineffective 53.43 47.00 62 1919 101562 2254542
Restlessness 53.29 47.00 20 1961 4543 2351561
Mouth ulceration 52.52 47.00 19 1962 3893 2352211
Seizure 51.07 47.00 33 1948 24433 2331671
Off label use 49.22 47.00 51 1930 73547 2282557
Rash 48.56 47.00 46 1935 59512 2296592
Pharyngeal oedema 47.02 47.00 17 1964 3476 2352628

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
Inappropriate schedule of product administration 368.53 45.23 94 911 7365 1738411
Akathisia 202.00 45.23 42 963 1286 1744490
Underdose 200.95 45.23 51 954 3829 1741947
Hypoaesthesia oral 178.21 45.23 35 970 796 1744980
Sedation 177.26 45.23 45 960 3372 1742404
Dysgeusia 146.25 45.23 42 963 5007 1740769
Incorrect route of product administration 123.82 45.23 34 971 3431 1742345
Dystonia 116.57 45.23 29 976 1985 1743791
Swollen tongue 107.01 45.23 29 976 2779 1742997
Weight increased 101.87 45.23 39 966 11318 1734458
Insomnia 91.55 45.23 40 965 16236 1729540
Dyskinesia 89.48 45.23 27 978 3792 1741984
Feeling abnormal 81.29 45.23 33 972 11133 1734643
Somnolence 77.72 45.23 36 969 16703 1729073
Agitation 74.84 45.23 31 974 10995 1734781
Suicide attempt 72.03 45.23 27 978 7354 1738422
Anosognosia 70.66 45.23 11 994 57 1745719
Extrapyramidal disorder 69.65 45.23 20 985 2357 1743419
Mania 67.23 45.23 19 986 2114 1743662
Suicidal ideation 64.78 45.23 26 979 8492 1737284
Dizziness 63.35 45.23 40 965 34321 1711455
Increased appetite 61.24 45.23 15 990 956 1744820
Anxiety 58.62 45.23 29 976 15498 1730278
Blood prolactin abnormal 57.74 45.23 9 996 47 1745729
Therapeutic product effect variable 56.65 45.23 10 995 122 1745654
Antipsychotic drug level below therapeutic 53.07 45.23 10 995 179 1745597
Glossodynia 49.96 45.23 12 993 703 1745073
Blood glucose increased 49.74 45.23 23 982 10561 1735215
Euphoric mood 47.97 45.23 12 993 833 1744943
Drug ineffective 47.17 45.23 43 962 63758 1682018
Disinhibition 47.09 45.23 10 995 334 1745442

Pharmacologic Action:

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

Drug Use (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

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 ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 5763476 June 9, 2020 METHOD OF TREATING SCHIZOPHRENIA AND BIPOLAR DISORDER
EQ 10MG BASE SAPHRIS ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 5763476 June 9, 2020 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 ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 5763476 June 9, 2020 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 ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 5763476 June 9, 2020 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 ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 5763476 June 9, 2020 USE OF THE ATYPICAL ANTIPSYCHOTIC ASENAPINE FOR TREATMENT OF SCHIZOPHRENIA IN ADULTS
EQ 2.5MG BASE SAPHRIS ALLERGAN N022117 March 12, 2015 RX TABLET SUBLINGUAL 5763476 June 9, 2020 METHOD OF TREATING MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR DISORDER IN PEDIATRIC PATIENTS
EQ 2.5MG BASE SAPHRIS ALLERGAN N022117 March 12, 2015 RX TABLET SUBLINGUAL 5763476 June 9, 2020 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 ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 5763476 June 9, 2020 METHOD OF TREATING SCHIZOPHRENIA AND BIPOLAR DISORDER
EQ 5MG BASE SAPHRIS ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 5763476 June 9, 2020 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 ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 5763476 June 9, 2020 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 ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 5763476 June 9, 2020 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 ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 5763476 June 9, 2020 USE OF THE ATYPICAL ANTIPSYCHOTIC ASENAPINE FOR TREATMENT OF SCHIZOPHRENIA IN ADULTS
EQ 10MG BASE SAPHRIS ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 7741358 April 6, 2026 TREATMENT OF BIPOLAR DISORDER AND SCHIZOPHRENIA
EQ 10MG BASE SAPHRIS ALLERGAN 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 ALLERGAN 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 ALLERGAN 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 ALLERGAN 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 ALLERGAN 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 ALLERGAN 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 ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL 7741358 April 6, 2026 TREATMENT OF BIPOLAR DISORDER AND SCHIZOPHRENIA
EQ 5MG BASE SAPHRIS ALLERGAN 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 ALLERGAN 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 ALLERGAN 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 ALLERGAN 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
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
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

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG BASE SAPHRIS ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL Jan. 13, 2020 BROADEN INITIAL STARTING DOSE FOR BIPOLAR I DISORDER TO 5-10MG TWICE DAILY
EQ 10MG BASE SAPHRIS ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL Jan. 13, 2020 MONOTHERAPY FOR THE MAINTENANCE TREATMENT OF BIPOLAR I DISORDER
EQ 2.5MG BASE SAPHRIS ALLERGAN N022117 March 12, 2015 RX TABLET SUBLINGUAL Jan. 13, 2020 BROADEN INITIAL STARTING DOSE FOR BIPOLAR I DISORDER TO 5-10MG TWICE DAILY
EQ 2.5MG BASE SAPHRIS ALLERGAN N022117 March 12, 2015 RX TABLET SUBLINGUAL Jan. 13, 2020 MONOTHERAPY FOR THE MAINTENANCE TREATMENT OF BIPOLAR I DISORDER
EQ 5MG BASE SAPHRIS ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL Jan. 13, 2020 BROADEN INITIAL STARTING DOSE FOR BIPOLAR I DISORDER TO 5-10MG TWICE DAILY
EQ 5MG BASE SAPHRIS ALLERGAN N022117 Aug. 13, 2009 RX TABLET SUBLINGUAL Jan. 13, 2020 MONOTHERAPY FOR THE MAINTENANCE TREATMENT OF BIPOLAR I DISORDER
3.8MG/24HR SECUADO HISAMITSU N212268 Oct. 11, 2019 RX SYSTEM TRANSDERMAL Oct. 11, 2022 NEW PRODUCT
5.7MG/24HR SECUADO HISAMITSU N212268 Oct. 11, 2019 RX SYSTEM TRANSDERMAL Oct. 11, 2022 NEW PRODUCT
7.6MG/24HR SECUADO HISAMITSU N212268 Oct. 11, 2019 RX SYSTEM TRANSDERMAL Oct. 11, 2022 NEW PRODUCT

Bioactivity Summary:

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

External reference:

IDSource
4029058 VUID
N0000179817 NUI
C2000088 UMLSCUI
D02995 KEGG_DRUG
443374004 SNOMEDCT_US
784649 RXNORM
26689 MMSL
d07473 MMSL
4029058 VANDF
443375003 SNOMEDCT_US
013233 NDDF
CU9463U2E2 UNII
85650-56-2 SECONDARY_CAS_RN
CHEBI:71253 CHEBI
8278 INN_ID
DB06216 DRUGBANK_ID
22 IUPHAR_LIGAND_ID
3036780 PUBCHEM_CID
CHEMBL1201756 ChEMBL_ID
CHEMBL3187365 ChEMBL_ID
CHEMBL3544974 ChEMBL_ID
C522667 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SAPHRIS HUMAN PRESCRIPTION DRUG LABEL 1 0052-0118 TABLET 5 mg SUBLINGUAL NDA 19 sections
SAPHRIS HUMAN PRESCRIPTION DRUG LABEL 1 0052-0119 TABLET 10 mg SUBLINGUAL NDA 19 sections
SAPHRIS HUMAN PRESCRIPTION DRUG LABEL 1 0052-2139 TABLET 5 mg SUBLINGUAL NDA 19 sections
SAPHRIS HUMAN PRESCRIPTION DRUG LABEL 1 0052-2142 TABLET 10 mg SUBLINGUAL NDA 19 sections
SAPHRIS HUMAN PRESCRIPTION DRUG LABEL 1 0456-2402 TABLET 2.50 mg SUBLINGUAL NDA 20 sections
SAPHRIS HUMAN PRESCRIPTION DRUG LABEL 1 0456-2405 TABLET 5 mg SUBLINGUAL NDA 20 sections
SAPHRIS HUMAN PRESCRIPTION DRUG LABEL 1 0456-2410 TABLET 10 mg SUBLINGUAL NDA 20 sections
SAPHRIS HUMAN PRESCRIPTION DRUG LABEL 1 16590-936 TABLET 10 mg SUBLINGUAL NDA 20 sections
Asenapine HUMAN PRESCRIPTION DRUG LABEL 1 59762-1091 TABLET 2.50 mg SUBLINGUAL NDA AUTHORIZED GENERIC 20 sections
Asenapine HUMAN PRESCRIPTION DRUG LABEL 1 59762-2012 TABLET 5 mg SUBLINGUAL NDA AUTHORIZED GENERIC 20 sections
Asenapine HUMAN PRESCRIPTION DRUG LABEL 1 59762-2888 TABLET 10 mg SUBLINGUAL NDA AUTHORIZED GENERIC 20 sections
SECUADO HUMAN PRESCRIPTION DRUG LABEL 1 68968-0172 FILM, EXTENDED RELEASE 3.80 mg TRANSDERMAL NDA 19 sections
SECUADO HUMAN PRESCRIPTION DRUG LABEL 1 68968-0173 FILM, EXTENDED RELEASE 5.70 mg TRANSDERMAL NDA 19 sections
SECUADO HUMAN PRESCRIPTION DRUG LABEL 1 68968-0174 FILM, EXTENDED RELEASE 7.60 mg TRANSDERMAL NDA 19 sections