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 4321.81 46.24 1232 12987 52606 53282241
Death 1406.82 46.24 971 13248 356261 52978586
Underdose 836.62 46.24 285 13934 21237 53313610
Delusion 792.67 46.24 238 13981 11771 53323076
Prescribed underdose 718.18 46.24 235 13984 15432 53319415
Hallucination, visual 535.98 46.24 198 14021 18634 53316213
Product dose omission issue 527.28 46.24 423 13796 191197 53143650
Nonspecific reaction 505.11 46.24 115 14104 1866 53332981
Drug ineffective 457.49 46.24 790 13429 816455 52518392
Confusional state 421.06 46.24 374 13845 193847 53141000
Abnormal behaviour 370.04 46.24 158 14061 21708 53313139
Adverse drug reaction 239.09 46.24 159 14060 53466 53281381
Fall 226.46 46.24 368 13851 358072 52976775
Aggression 195.21 46.24 104 14115 23299 53311548
Dementia 194.13 46.24 93 14126 16657 53318190
Dementia with Lewy bodies 168.68 46.24 34 14185 296 53334551
Somnolence 157.44 46.24 208 14011 167526 53167321
Peripheral swelling 156.82 46.24 231 13988 205877 53128970
Paranoia 131.04 46.24 63 14156 11361 53323486
Therapeutic response unexpected 130.76 46.24 72 14147 17198 53317649
Gait disturbance 123.53 46.24 180 14039 158662 53176185
Nightmare 115.45 46.24 67 14152 17684 53317163
Inappropriate schedule of product administration 113.78 46.24 119 14100 74759 53260088
Urinary tract infection 105.62 46.24 211 14008 239692 53095155
Metabolic function test abnormal 96.59 46.24 19 14200 144 53334703
Abnormal dreams 90.86 46.24 48 14171 10553 53324294
Hypersomnia 88.88 46.24 55 14164 16300 53318547
Hip fracture 74.23 46.24 61 14158 28196 53306651
Pyrexia 74.05 46.24 10 14209 403183 52931664
Psychotic disorder 73.36 46.24 57 14162 24328 53310519
Hospitalisation 71.01 46.24 91 14128 70921 53263926
Arthralgia 63.98 46.24 19 14200 439764 52895083
Screaming 63.13 46.24 26 14193 3251 53331596
Agitation 61.57 46.24 77 14142 58549 53276298
Balance disorder 58.28 46.24 84 14135 73123 53261724
Tremor 58.09 46.24 113 14106 125623 53209224
Insomnia 56.78 46.24 142 14077 186930 53147917
Cognitive disorder 53.84 46.24 63 14156 44715 53290132
Pain 52.42 46.24 48 14171 588350 52746497
Anaemia 50.43 46.24 7 14212 276711 53058136
Drug hypersensitivity 50.04 46.24 6 14213 265236 53069611
Dysphagia 49.30 46.24 84 14135 84313 53250534
Freezing phenomenon 49.08 46.24 18 14201 1649 53333198
Diarrhoea 48.98 46.24 57 14162 625489 52709358
Sleep terror 48.30 46.24 15 14204 825 53334022

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 6522.88 51.17 2117 21405 50502 32439502
Death 2135.33 51.17 1920 21602 380597 32109407
Delusion 1319.94 51.17 455 23067 12653 32477351
Prescribed underdose 1193.38 51.17 381 23141 8278 32481726
Underdose 1178.81 51.17 418 23104 12651 32477353
Confusional state 1035.88 51.17 841 22681 142274 32347730
Nonspecific reaction 852.87 51.17 197 23325 1135 32488869
Product dose omission issue 727.85 51.17 597 22925 101978 32388026
Abnormal behaviour 688.51 51.17 350 23172 26116 32463888
Hallucination, visual 612.68 51.17 282 23240 16877 32473127
Drug ineffective 548.79 51.17 983 22539 382494 32107510
Adverse drug reaction 431.02 51.17 255 23267 25606 32464398
Fall 409.90 51.17 599 22923 195602 32294402
Peripheral swelling 382.42 51.17 348 23174 67997 32422007
Gait disturbance 369.22 51.17 367 23155 80041 32409963
Dementia 365.16 51.17 183 23339 13203 32476801
Aggression 355.63 51.17 265 23257 39124 32450880
Therapeutic response unexpected 302.79 51.17 145 23377 9467 32480537
Somnolence 265.44 51.17 350 23172 103447 32386557
Gait inability 215.34 51.17 150 23372 19897 32470107
Hypersomnia 207.10 51.17 121 23401 11840 32478164
Nightmare 198.91 51.17 122 23400 13044 32476960
Agitation 197.97 51.17 225 23297 57011 32432993
Dysstasia 190.47 51.17 113 23409 11373 32478631
Acute kidney injury 172.63 51.17 10 23512 293458 32196546
Inappropriate schedule of product administration 163.26 51.17 183 23339 45642 32444362
Dementia with Lewy bodies 162.89 51.17 46 23476 640 32489364
Paranoia 160.39 51.17 99 23423 10700 32479304
Pyrexia 149.54 51.17 26 23496 319942 32170062
Posture abnormal 138.13 51.17 54 23468 2139 32487865
Metabolic function test abnormal 134.80 51.17 25 23497 33 32489971
Anaemia 130.23 51.17 8 23514 223616 32266388
Hospitalisation 127.73 51.17 167 23355 48804 32441200
Balance disorder 122.76 51.17 147 23375 39312 32450692
Insomnia 120.17 51.17 240 23282 100108 32389896
Cognitive disorder 116.27 51.17 117 23405 25777 32464227
Drooling 113.79 51.17 53 23469 3244 32486760
Abnormal dreams 110.89 51.17 72 23450 8492 32481512
Psychotic disorder 110.74 51.17 108 23414 22912 32467092
Feeling abnormal 90.31 51.17 159 23363 60264 32429740
Dysphagia 89.60 51.17 160 23362 61316 32428688
Dyspnoea 86.56 51.17 81 23441 361964 32128040
Anger 85.37 51.17 70 23452 11834 32478170
Hip fracture 77.23 51.17 66 23456 11809 32478195
Tremor 76.05 51.17 176 23346 81101 32408903
Urinary tract infection 72.30 51.17 171 23351 79900 32410104
Intentional underdose 71.45 51.17 26 23496 842 32489162
Disorientation 69.13 51.17 102 23420 33323 32456681
Abdominal pain 67.83 51.17 13 23509 149516 32340488
Diarrhoea 67.45 51.17 100 23422 364702 32125302
Constipation 66.74 51.17 222 23300 126151 32363853
Arthralgia 65.06 51.17 14 23508 148434 32341570
Drug interaction 64.62 51.17 39 23483 218146 32271858
Speech disorder 62.97 51.17 86 23436 26167 32463837
Restlessness 58.91 51.17 81 23441 24800 32465204
Freezing phenomenon 57.68 51.17 30 23492 2333 32487671
Screaming 55.94 51.17 25 23497 1389 32488615
Memory impairment 55.94 51.17 103 23419 40376 32449628
Renal impairment 54.33 51.17 3 23519 91969 32398035
White blood cell count decreased 53.79 51.17 3 23519 91195 32398809
Motor dysfunction 52.54 51.17 41 23481 6455 32483549
Completed suicide 51.75 51.17 4 23518 92513 32397491

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 5-hydroxytryptamine 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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 10MG BASE NUPLAZID ACADIA PHARMS INC N207318 June 28, 2018 RX TABLET ORAL 9765053 July 27, 2022 TREATMENT OF HALLUCINATIONS AND DELUSIONS ASSOCIATED WITH PARKINSONS DISEASE PSYCHOSIS
EQ 17MG BASE NUPLAZID ACADIA PHARMS INC N207318 April 29, 2016 DISCN TABLET ORAL 9765053 July 27, 2022 TREATMENT OF HALLUCINATIONS AND DELUSIONS ASSOCIATED WITH PARKINSONS DISEASE PSYCHOSIS
EQ 34MG BASE NUPLAZID ACADIA PHARMS INC N210793 June 28, 2018 RX CAPSULE ORAL 9765053 July 27, 2022 TREATMENT OF HALLUCINATIONS AND DELUSIONS ASSOCIATED WITH PARKINSONS DISEASE PSYCHOSIS
EQ 10MG BASE NUPLAZID ACADIA PHARMS INC N207318 June 28, 2018 RX TABLET ORAL 10028944 Jan. 15, 2024 TREATMENT OF HALLUCINATIONS AND DELUSIONS ASSOCIATED WITH PARKINSONS DISEASE PSYCHOSIS
EQ 10MG BASE NUPLAZID ACADIA PHARMS INC N207318 June 28, 2018 RX TABLET ORAL 8618130 Jan. 15, 2024 TREATMENT OF PSYCHOSIS OR A SYMPTOM THEREOF
EQ 10MG BASE NUPLAZID ACADIA PHARMS INC N207318 June 28, 2018 RX TABLET ORAL 8921393 Jan. 15, 2024 TREATMENT OF A NEURODEGENERATIVE DISEASE OR A SYMPTOM THEREOF
EQ 10MG BASE NUPLAZID ACADIA PHARMS INC N207318 June 28, 2018 RX TABLET ORAL 9566271 Jan. 15, 2024 TREATMENT OF HALLUCINATIONS AND DELUSIONS ASSOCIATED WITH PARKINSONS DISEASE PSYCHOSIS
EQ 17MG BASE NUPLAZID ACADIA PHARMS INC N207318 April 29, 2016 DISCN TABLET ORAL 10028944 Jan. 15, 2024 TREATMENT OF HALLUCINATIONS AND DELUSIONS ASSOCIATED WITH PARKINSONS DISEASE PSYCHOSIS
EQ 17MG BASE NUPLAZID ACADIA PHARMS INC N207318 April 29, 2016 DISCN TABLET ORAL 8618130 Jan. 15, 2024 TREATMENT OF PSYCHOSIS OR A SYMPTOM THEREOF
EQ 17MG BASE NUPLAZID ACADIA PHARMS INC N207318 April 29, 2016 DISCN TABLET ORAL 8921393 Jan. 15, 2024 TREATMENT OF A NEURODEGENERATIVE DISEASE OR A SYMPTOM THEREOF
EQ 17MG BASE NUPLAZID ACADIA PHARMS INC N207318 April 29, 2016 DISCN TABLET ORAL 9566271 Jan. 15, 2024 TREATMENT OF HALLUCINATIONS AND DELUSIONS ASSOCIATED WITH PARKINSONS DISEASE PSYCHOSIS
EQ 34MG BASE NUPLAZID ACADIA PHARMS INC N210793 June 28, 2018 RX CAPSULE ORAL 10028944 Jan. 15, 2024 TREATMENT OF HALLUCINATIONS AND DELUSIONS ASSOCIATED WITH PARKINSONS DISEASE PSYCHOSIS
EQ 34MG BASE NUPLAZID ACADIA PHARMS INC N210793 June 28, 2018 RX CAPSULE ORAL 8618130 Jan. 15, 2024 TREATMENT OF PSYCHOSIS OR A SYMPTOM THEREOF
EQ 34MG BASE NUPLAZID ACADIA PHARMS INC N210793 June 28, 2018 RX CAPSULE ORAL 8921393 Jan. 15, 2024 TREATMENT OF A NEURODEGENERATIVE DISEASE OR A SYMPTOM THEREOF
EQ 34MG BASE NUPLAZID ACADIA PHARMS INC N210793 June 28, 2018 RX CAPSULE ORAL 9566271 Jan. 15, 2024 TREATMENT OF HALLUCINATIONS AND DELUSIONS ASSOCIATED WITH PARKINSONS DISEASE PSYCHOSIS
EQ 10MG BASE NUPLAZID ACADIA PHARMS INC N207318 June 28, 2018 RX TABLET ORAL 7659285 Aug. 24, 2026 TREATMENT OF PARKINSONS DISEASE PSYCHOSIS
EQ 17MG BASE NUPLAZID ACADIA PHARMS INC N207318 April 29, 2016 DISCN TABLET ORAL 7659285 Aug. 24, 2026 TREATMENT OF PARKINSONS DISEASE PSYCHOSIS
EQ 34MG BASE NUPLAZID ACADIA PHARMS INC N210793 June 28, 2018 RX CAPSULE ORAL 7659285 Aug. 24, 2026 TREATMENT OF PARKINSONS DISEASE PSYCHOSIS
EQ 10MG BASE NUPLAZID ACADIA PHARMS INC N207318 June 28, 2018 RX TABLET ORAL 10517860 March 23, 2037 TREATMENT OF HALLUCINATIONS AND DELUSIONS ASSOCIATED WITH PARKINSONS DISEASE PSYCHOSIS
EQ 10MG BASE NUPLAZID ACADIA PHARMS INC N207318 June 28, 2018 RX TABLET ORAL 10953000 March 23, 2037 TREATMENT OF HALLUCINATIONS AND DELUSIONS ASSOCIATED WITH PARKINSONS DISEASE PSYCHOSIS
EQ 34MG BASE NUPLAZID ACADIA PHARMS INC N210793 June 28, 2018 RX CAPSULE ORAL 10849891 Aug. 27, 2038 TREATMENT OF HALLUCINATIONS AND DELUSIONS ASSOCIATED WITH PARKINSONS DISEASE PSYCHOSIS

Orange Book exclusivity data (new drug applications)

None

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
JZ963P0DIK UNII
706782-28-7 SECONDARY_CAS_RN
4035717 VANDF
C1722267 UMLSCUI
CHEBI:133017 CHEBI
CHEMBL2111101 ChEMBL_ID
D08969 KEGG_DRUG
10071196 PUBCHEM_CID
DB05316 DRUGBANK_ID
CHEMBL2448613 ChEMBL_ID
C510793 MESH_SUPPLEMENTAL_RECORD_UI
8423 IUPHAR_LIGAND_ID
8877 INN_ID
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