pimavanserin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
serotonin receptor antagonists (mostly 5-HT2) 5142 706779-91-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pimavanserin
  • pimavanserin tartrate
  • ACP-103
  • nuplazid
an atypical antipsychotic, mechanism of action of pimavanserin in the treatment of hallucinations and delusions associated with Parkinson's disease psychosis is unknown. however, the effect of pimavanserin could be mediated through a combination of inverse agonist and antagonist activity at serotonin 5-HT2A receptors and to a lesser extent at serotonin 5-HT2C receptors
  • Molecular weight: 427.56
  • Formula: C25H34FN3O2
  • CLOGP: 4.11
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 44.81
  • ALOGS: -4.76
  • ROTB: 8

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
April 29, 2016 FDA ACADIA PHARMACEUTICALS 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
Hallucination 3847.14 44.95 1115 11751 48836 46624360
Death 1003.34 44.95 784 12082 334764 46338432
Underdose 751.83 44.95 259 12607 19299 46653897
Prescribed underdose 728.76 44.95 225 12641 11828 46661368
Delusion 702.44 44.95 215 12651 10973 46662223
Nonspecific reaction 509.16 44.95 115 12751 1735 46671461
Hallucination, visual 466.64 44.95 178 12688 17695 46655501
Product dose omission issue 440.04 44.95 366 12500 168154 46505042
Drug ineffective 397.78 44.95 682 12184 677156 45996040
Confusional state 396.04 44.95 337 12529 159555 46513641
Abnormal behaviour 324.99 44.95 144 12722 20914 46652282
Fall 206.47 44.95 343 12523 328754 46344442
Adverse drug reaction 192.47 44.95 131 12735 44231 46628965
Peripheral swelling 169.74 44.95 213 12653 157858 46515338
Aggression 161.70 44.95 92 12774 22652 46650544
Dementia 155.82 44.95 78 12788 14852 46658344
Somnolence 138.69 44.95 192 12674 156329 46516867
Dementia with Lewy bodies 132.95 44.95 27 12839 236 46672960
Inappropriate schedule of product administration 130.37 44.95 122 12744 64891 46608305
Gait disturbance 125.38 44.95 176 12690 145087 46528109
Therapeutic response unexpected 121.39 44.95 67 12799 15549 46657647
Paranoia 115.40 44.95 57 12809 10540 46662656
Nightmare 109.57 44.95 64 12802 16534 46656662
Urinary tract infection 96.34 44.95 197 12669 220069 46453127
Metabolic function test abnormal 96.19 44.95 19 12847 142 46673054
Hypersomnia 87.56 44.95 54 12812 15385 46657811
Abnormal dreams 85.13 44.95 46 12820 10233 46662963
Hospitalisation 78.54 44.95 92 12774 63293 46609903
Pyrexia 66.11 44.95 9 12857 348793 46324403
Hip fracture 61.33 44.95 54 12812 26502 46646694
Insomnia 61.05 44.95 138 12728 164786 46508410
Screaming 56.26 44.95 24 12842 3167 46670029
Psychotic disorder 54.25 44.95 47 12819 22574 46650622
Balance disorder 53.77 44.95 77 12789 64444 46608752
Cognitive disorder 51.53 44.95 57 12809 36826 46636370
Arthralgia 50.09 44.95 19 12847 364584 46308612
Tremor 47.56 44.95 101 12765 115538 46557658
Anaemia 47.48 44.95 7 12859 255772 46417424
Agitation 47.45 44.95 67 12799 55348 46617848
Drug hypersensitivity 46.85 44.95 6 12860 243819 46429377
Diarrhoea 46.10 44.95 52 12814 559550 46113646

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
Hallucination 5940.90 51.91 1930 19332 47129 29884087
Death 1616.24 51.91 1585 19677 355698 29575518
Delusion 1214.43 51.91 416 20846 11573 29919643
Prescribed underdose 1170.07 51.91 364 20898 7395 29923821
Underdose 1040.32 51.91 372 20890 11769 29919447
Confusional state 959.03 51.91 778 20484 134056 29797160
Nonspecific reaction 817.76 51.91 189 21073 1117 29930099
Product dose omission issue 707.78 51.91 556 20706 91075 29840141
Abnormal behaviour 641.11 51.91 328 20934 25295 29905921
Hallucination, visual 543.22 51.91 253 21009 15860 29915356
Drug ineffective 472.26 51.91 852 20410 339535 29591681
Gait disturbance 369.12 51.91 352 20910 74425 29856791
Fall 357.17 51.91 534 20728 181338 29749878
Peripheral swelling 336.97 51.91 306 20956 60768 29870448
Aggression 334.54 51.91 247 21015 36660 29894556
Adverse drug reaction 322.10 51.91 202 21060 22943 29908273
Dementia 318.44 51.91 162 21100 12299 29918917
Therapeutic response unexpected 297.35 51.91 139 21123 8764 29922452
Somnolence 259.83 51.91 331 20931 96432 29834784
Hypersomnia 202.04 51.91 116 21146 11200 29920016
Gait inability 200.16 51.91 139 21123 18702 29912514
Nightmare 179.53 51.91 110 21152 11966 29919250
Inappropriate schedule of product administration 171.33 51.91 174 21088 39554 29891662
Dysstasia 169.87 51.91 101 21161 10404 29920812
Agitation 167.48 51.91 199 21063 53874 29877342
Acute kidney injury 158.55 51.91 9 21253 273833 29657383
Hospitalisation 152.12 51.91 172 21090 44147 29887069
Paranoia 149.38 51.91 92 21170 10096 29921120
Posture abnormal 140.29 51.91 52 21210 1812 29929404
Metabolic function test abnormal 136.60 51.91 25 21237 30 29931186
Dementia with Lewy bodies 134.40 51.91 38 21224 542 29930674
Pyrexia 133.91 51.91 24 21238 294465 29636751
Anaemia 122.90 51.91 6 21256 207986 29723230
Balance disorder 112.40 51.91 134 21128 36359 29894857
Drooling 109.91 51.91 50 21212 2955 29928261
Cognitive disorder 109.87 51.91 108 21154 23582 29907634
Insomnia 108.43 51.91 218 21044 93118 29838098
Psychotic disorder 99.61 51.91 98 21164 21417 29909799
Abnormal dreams 93.54 51.91 63 21199 8052 29923164
Feeling abnormal 89.08 51.91 151 21111 56605 29874611
Dysphagia 75.01 51.91 140 21122 56558 29874658
Anger 73.75 51.91 62 21200 11058 29920158
Dyspnoea 72.64 51.91 78 21184 333217 29597999
Constipation 70.90 51.91 208 21054 112698 29818518
Intentional underdose 70.08 51.91 25 21237 779 29930437
Disorientation 69.51 51.91 98 21164 31320 29899896
Urinary tract infection 69.27 51.91 158 21104 73501 29857715
Tremor 69.05 51.91 160 21102 75203 29856013
Abdominal pain 61.60 51.91 11 21251 135643 29795573
Restlessness 61.49 51.91 78 21184 22521 29908695
Freezing phenomenon 60.82 51.91 29 21233 1907 29929309
Memory impairment 58.41 51.91 99 21163 37075 29894141
Completed suicide 58.26 51.91 3 21259 99489 29831727
Drug interaction 58 51.91 35 21227 199533 29731683
Diarrhoea 57.60 51.91 93 21169 334010 29597206
Hip fracture 53.95 51.91 52 21210 11072 29920144
Motor dysfunction 52.23 51.91 39 21223 5863 29925353
Speech disorder 52.05 51.91 75 21187 24437 29906779

Pharmacologic Action:

SourceCodeDescription
ATC N05AX17 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Other antipsychotics
FDA EPC N0000175430 Atypical Antipsychotic
MeSH PA D018726 Anti-Dyskinesia Agents
MeSH PA D000978 Antiparkinson Agents
MeSH PA D014150 Antipsychotic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D058830 Serotonin 5-HT2 Receptor Antagonists
MeSH PA D018490 Serotonin Agents
MeSH PA D012702 Serotonin Antagonists
MeSH PA D014149 Tranquilizing Agents
CHEBI has role CHEBI:35476 grosser tranquilizer
CHEBI has role CHEBI:48279 serotonin antagonists
CHEBI has role CHEBI:133016 5ht(2a) inverse agonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Parkinson's disease indication 49049000 DOID:14330

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.42 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG BASE NUPLAZID ACADIA PHARMS INC N207318 June 28, 2018 RX TABLET ORAL April 29, 2021 NEW CHEMICAL ENTITY
EQ 17MG BASE NUPLAZID ACADIA PHARMS INC N207318 April 29, 2016 DISCN TABLET ORAL April 29, 2021 NEW CHEMICAL ENTITY
EQ 34MG BASE NUPLAZID ACADIA PHARMS INC N210793 June 28, 2018 RX CAPSULE ORAL April 29, 2021 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
5-hydroxytryptamine receptor 2A GPCR INVERSE AGONIST Ki 9.30 SCIENTIFIC LITERATURE DRUG LABEL
5-hydroxytryptamine receptor 2C GPCR INVERSE AGONIST Ki 8.80 SCIENTIFIC LITERATURE

External reference:

IDSource
706782-28-7 SECONDARY_CAS_RN
4035717 VANDF
C1722268 UMLSCUI
CHEBI:133014 CHEBI
CHEMBL2448613 ChEMBL_ID
D08969 KEGG_DRUG
10071196 PUBCHEM_CID
CHEMBL2111101 ChEMBL_ID
DB05316 DRUGBANK_ID
C510793 MESH_SUPPLEMENTAL_RECORD_UI
8423 IUPHAR_LIGAND_ID
8877 INN_ID
JZ963P0DIK UNII
1791685 RXNORM
240624 MMSL
31639 MMSL
d08433 MMSL
016844 NDDF
016845 NDDF
721997002 SNOMEDCT_US
763543000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
NUPLAZID HUMAN PRESCRIPTION DRUG LABEL 1 63090-100 TABLET, COATED 10 mg ORAL NDA 32 sections
NUPLAZID HUMAN PRESCRIPTION DRUG LABEL 1 63090-170 TABLET, COATED 17 mg ORAL NDA 32 sections
NUPLAZID HUMAN PRESCRIPTION DRUG LABEL 1 63090-340 CAPSULE 34 mg ORAL NDA 32 sections