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

PropertyValueReference
S (Water solubility) 100 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAP3K7,MAPK7,MET,NTRK2,PDK2,PDK4,PIK3CB,PRKCD,PRKDC,SIK2,SIK3,TEK 27
kinase-selectivity-class AXL,EIF2AK3,PDK4 3
pfas-class PFAS structural alert (1 = True, 0 = False) 0

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 4270.21 49.90 1149 13677 64810 90548811
Death 2455.89 49.90 1271 13555 455280 90158341
Underdose 647.28 49.90 265 14561 53752 90559869
Product dose omission issue 548.13 49.90 421 14405 291266 90322355
Nonspecific reaction 526.52 49.90 116 14710 2693 90610928
Drug ineffective 515.61 49.90 851 13975 1383447 89230174
Hallucination, visual 501.02 49.90 175 14651 22917 90590704
Abnormal behaviour 450.93 49.90 161 14665 22467 90591154
Prescribed underdose 422.92 49.90 218 14608 74801 90538820
Fall 368.89 49.90 422 14404 481388 90132233
Confusional state 357.55 49.90 374 14452 385831 90227790
Delusion 319.82 49.90 110 14716 13730 90599891
Dementia 254.86 49.90 108 14718 23753 90589868
Aggression 249.75 49.90 110 14716 26558 90587063
Adverse drug reaction 234.87 49.90 176 14650 116525 90497096
Somnolence 199.08 49.90 206 14620 208878 90404743
Dementia with Lewy bodies 194.85 49.90 37 14789 394 90613227
Urinary tract infection 184.55 49.90 238 14588 305394 90308227
Paranoia 146.40 49.90 61 14765 12847 90600774
Hip fracture 133.05 49.90 77 14749 33000 90580621
Psychotic disorder 121.11 49.90 71 14755 31159 90582462
Agitation 119.08 49.90 94 14732 67004 90546617
Therapeutic response unexpected 118.52 49.90 62 14764 21818 90591803
Gait disturbance 113.99 49.90 174 14652 260322 90353299
Nightmare 110.42 49.90 59 14767 21666 90591955
Hypersomnia 97.02 49.90 54 14772 21477 90592144
Peripheral swelling 91.83 49.90 206 14620 412900 90200721
Inappropriate schedule of product administration 89.05 49.90 116 14710 149817 90463804
Metabolic function test abnormal 88.18 49.90 19 14807 395 90613226
Abnormal dreams 88.12 49.90 41 14785 11216 90602405
Tremor 85.56 49.90 115 14711 153058 90460563
Screaming 83.46 49.90 29 14797 3721 90609900
Refusal of treatment by patient 74.90 49.90 30 14796 5708 90607913
Hospitalisation 72.78 49.90 97 14729 128003 90485618
Pyrexia 72.24 49.90 11 14815 660474 89953147
Balance disorder 70.29 49.90 83 14743 96997 90516624
Arthralgia 67.11 49.90 22 14804 778500 89835121
Dysphagia 66.84 49.90 87 14739 112191 90501430
Feeling abnormal 65.14 49.90 106 14720 167129 90446492
Pain 61.86 49.90 44 14782 996297 89617324
Cognitive disorder 59.86 49.90 65 14761 69342 90544279
Dysstasia 57.57 49.90 41 14785 25011 90588610
Terminal state 55.88 49.90 20 14806 2798 90610823
Anger 55.31 49.90 32 14794 13688 90599933
Freezing phenomenon 52.14 49.90 17 14809 1795 90611826

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 6006.86 52.20 1915 22078 55592 42541750
Death 3241.27 52.20 2396 21597 468789 42128553
Prescribed underdose 1089.90 52.20 349 23644 9933 42587409
Confusional state 1067.37 52.20 824 23169 166773 42430569
Underdose 1057.41 52.20 385 23608 16281 42581061
Nonspecific reaction 855.20 52.20 195 23798 1406 42595936
Abnormal behaviour 743.85 52.20 341 23652 26110 42571232
Product dose omission issue 601.55 52.20 574 23419 153791 42443551
Fall 556.43 52.20 670 23323 233850 42363492
Hallucination, visual 498.29 52.20 241 23752 20779 42576563
Adverse drug reaction 440.99 52.20 270 23723 37164 42560178
Aggression 414.54 52.20 276 23717 43887 42553455
Drug ineffective 401.03 52.20 1001 22992 629196 41968146
Dementia 396.69 52.20 191 23802 16289 42581053
Gait disturbance 395.24 52.20 372 23621 97628 42499714
Delusion 319.35 52.20 159 23834 14575 42582767
Peripheral swelling 299.18 52.20 308 23685 89962 42507380
Therapeutic response unexpected 253.07 52.20 125 23868 11256 42586086
Somnolence 247.04 52.20 348 23645 140757 42456585
Agitation 245.34 52.20 237 23756 64077 42533265
Gait inability 229.34 52.20 149 23844 22684 42574658
Hypersomnia 199.40 52.20 116 23877 14502 42582840
Dementia with Lewy bodies 185.16 52.20 51 23942 842 42596500
Paranoia 180.00 52.20 107 23886 13919 42583423
Dysstasia 176.97 52.20 106 23887 13980 42583362
Acute kidney injury 158.61 52.20 13 23980 367324 42230018
Urinary tract infection 153.33 52.20 231 23762 99053 42498289
Posture abnormal 151.30 52.20 56 23937 2465 42594877
Psychotic disorder 139.18 52.20 122 23871 29086 42568256
Nightmare 138.71 52.20 114 23879 24898 42572444
Anaemia 132.64 52.20 6 23987 280272 42317070
Pyrexia 132.57 52.20 30 23963 394012 42203330
Hospitalisation 132.26 52.20 185 23808 74145 42523197
Drooling 125.56 52.20 57 23936 4242 42593100
Balance disorder 121.76 52.20 142 23851 47503 42549839
Abnormal dreams 119.07 52.20 68 23925 8203 42589139
Insomnia 114.89 52.20 224 23769 118029 42479313
Cognitive disorder 110.06 52.20 115 23878 34057 42563285
Feeling abnormal 105.70 52.20 161 23832 69625 42527717
Metabolic function test abnormal 104.25 52.20 25 23968 229 42597113
Anger 102.23 52.20 73 23920 12945 42584397
Dysphagia 99.34 52.20 160 23833 72559 42524783
Inappropriate schedule of product administration 97.20 52.20 185 23808 95717 42501625
Neutropenia 88.93 52.20 6 23987 199425 42397917
Hip fracture 86.63 52.20 67 23926 13405 42583937
Disorientation 85.60 52.20 104 23889 36285 42561057
Tremor 83.81 52.20 175 23818 96754 42500588
Refusal of treatment by patient 80.20 52.20 45 23948 5246 42592096
Arthralgia 76.58 52.20 12 23981 205226 42392116
Speech disorder 76.38 52.20 88 23905 29033 42568309
Dyspnoea 74.41 52.20 84 23909 442537 42154805
Intentional underdose 73.40 52.20 24 23969 726 42596616
Abdominal pain 71.37 52.20 11 23982 190460 42406882
Diarrhoea 70.58 52.20 94 23899 460755 42136587
Screaming 67.11 52.20 29 23964 1918 42595424
Constipation 65.05 52.20 220 23773 162071 42435271
Motor dysfunction 64.68 52.20 46 23947 8100 42589242
Pruritus 64.07 52.20 14 23979 188757 42408585
Product use in unapproved indication 61.95 52.20 14 23979 184442 42412900
Freezing phenomenon 61.41 52.20 27 23966 1862 42595480
Restlessness 59.87 52.20 78 23915 29171 42568171
Memory impairment 55.98 52.20 101 23892 50121 42547221
Pain 53.72 52.20 36 23957 244812 42352530

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
Death 5757.56 44.73 2871 22206 695998 109868224
Hallucination 5395.14 44.73 1631 23446 99801 110464421
Underdose 1158.44 44.73 462 24615 63092 110501130
Confusional state 882.11 44.73 776 24301 467904 110096318
Prescribed underdose 864.79 44.73 378 24699 64796 110499426
Abnormal behaviour 835.24 44.73 319 24758 38720 110525502
Product dose omission issue 744.85 44.73 601 24476 321181 110243041
Fall 740.49 44.73 790 24287 602692 109961530
Nonspecific reaction 678.44 44.73 154 24923 2920 110561302
Hallucination, visual 571.80 44.73 244 24833 39361 110524861
Aggression 561.10 44.73 272 24805 58938 110505284
Dementia 430.36 44.73 187 24890 31486 110532736
Delusion 415.84 44.73 168 24909 23587 110540635
Somnolence 341.14 44.73 377 24700 297072 110267150
Gait disturbance 314.44 44.73 350 24727 277858 110286364
Agitation 290.16 44.73 225 24852 112826 110451396
Hypersomnia 247.92 44.73 123 24954 27938 110536284
Therapeutic response unexpected 245.30 44.73 116 24961 23727 110540495
Urinary tract infection 237.22 44.73 329 24748 325953 110238269
Paranoia 218.42 44.73 105 24972 22269 110541953
Psychotic disorder 206.30 44.73 134 24943 50803 110513419
Metabolic function test abnormal 204.83 44.73 44 25033 638 110563584
Dementia with Lewy bodies 200.98 44.73 47 25030 1019 110563203
Drug ineffective 184.96 44.73 755 24322 1519785 109044437
Dysstasia 182.70 44.73 106 24971 32880 110531342
Hip fracture 176.45 44.73 106 24971 35045 110529177
Adverse drug reaction 175.94 44.73 164 24913 105395 110458827
Abnormal dreams 168.76 44.73 74 25003 12706 110551516
Balance disorder 140.65 44.73 152 24925 116408 110447814
Peripheral swelling 140.06 44.73 293 24784 403741 110160481
Cognitive disorder 138.22 44.73 132 24945 87379 110476843
Anger 137.96 44.73 73 25004 18934 110545288
Drooling 137.07 44.73 54 25023 7085 110557137
Posture abnormal 134.71 44.73 47 25030 4391 110559831
Inappropriate schedule of product administration 131.08 44.73 194 24883 203443 110360779
Nightmare 125.75 44.73 89 24988 38774 110525448
Pyrexia 113.05 44.73 32 25045 898233 109665989
Disorientation 112.35 44.73 107 24970 70564 110493658
Dysphagia 110.03 44.73 154 24923 153446 110410776
Tremor 106.91 44.73 176 24901 202056 110362166
Acute kidney injury 105.15 44.73 11 25066 635419 109928803
Feeling abnormal 101.95 44.73 162 24915 180549 110383673
Arthralgia 99.50 44.73 27 25050 779605 109784617
Hospitalisation 99.29 44.73 141 24936 142352 110421870
Anaemia 94.40 44.73 8 25069 547078 110017144
Speech disorder 93.67 44.73 91 24986 61478 110502744
Gait inability 93.62 44.73 134 24943 136242 110427980
Screaming 90.49 44.73 36 25041 4845 110559377
Insomnia 90.08 44.73 230 24847 360360 110203862
Sedation 87.76 44.73 93 24984 69590 110494632
Orthostatic hypotension 86.26 44.73 90 24987 66159 110498063
Motor dysfunction 83.86 44.73 58 25019 24348 110539874
Pain 81.33 44.73 59 25018 954896 109609326
Refusal of treatment by patient 79.07 44.73 40 25037 9454 110554768
Unresponsive to stimuli 78.33 44.73 84 24993 63706 110500516
Freezing phenomenon 76.77 44.73 27 25050 2582 110561640
Lethargy 70.24 44.73 96 24981 93480 110470742
Intentional underdose 69.74 44.73 25 25052 2527 110561695
Abdominal pain 68.79 44.73 16 25061 512973 110051249
Incoherent 63.20 44.73 33 25044 8325 110555897
Diarrhoea 62.07 44.73 102 24975 1139403 109424819
Drug hypersensitivity 61.19 44.73 14 25063 454076 110110146
Constipation 60.96 44.73 199 24878 357587 110206635
Pruritus 59.16 44.73 29 25048 581531 109982691
Neutropenia 58.17 44.73 8 25069 374612 110189610
Restlessness 56.94 44.73 67 25010 56192 110508030
Dyspnoea 55.80 44.73 104 24973 1106768 109457454
Product use in unapproved indication 50.76 44.73 19 25058 447358 110116864
Arthropathy 50.11 44.73 4 25073 287518 110276704
Alopecia 49.62 44.73 11 25066 364742 110199480
Hypokinesia 48.56 44.73 40 25037 21786 110542436
Patient elopement 48.24 44.73 12 25065 340 110563882
Treatment failure 47.92 44.73 4 25073 277230 110286992
Sinusitis 46.85 44.73 6 25071 296682 110267540
Immobile 45.97 44.73 26 25051 7676 110556546
Belligerence 45.97 44.73 11 25066 264 110563958

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AX17 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Other antipsychotics
FDA EPC N0000175430 Atypical Antipsychotic
MeSH PA D000978 Antiparkinson Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D011619 Psychotropic Drugs
MeSH PA D012702 Serotonin Antagonists
MeSH PA D014149 Tranquilizing Agents
MeSH PA D014150 Antipsychotic Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018490 Serotonin Agents
MeSH PA D018726 Anti-Dyskinesia Agents
MeSH PA D058830 Serotonin 5-HT2 Receptor Antagonists
CHEBI has role CHEBI:35476 antipsychotic agent
CHEBI has role CHEBI:48279 serotonergic antagonist
CHEBI has role CHEBI:133016 5-hydroxytryptamine 2A receptor inverse agonist
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:48407 antiparkinson drug

Related Drugs by ATC class:

N05AX Other antipsychotics 11 drugs
aripiprazolebrexpiprazolecariprazineiloperidonemosapraminepaliperidoneprothipendylrisperidonetrospiumxanomelinezotepine

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

DiseaseRelationSNOMED_IDDOID
Parkinson's disease indication 49049000 DOID:14330




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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 7659285 Aug. 24, 2026 TREATMENT OF PARKINSONS DISEASE PSYCHOSIS
EQ 17MG BASE **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** 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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG BASE NUPLAZID ACADIA PHARMS INC N207318 June 28, 2018 RX TABLET ORAL April 27, 2029 ADDITIONAL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION
EQ 17MG BASE **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** NUPLAZID ACADIA PHARMS INC N207318 April 29, 2016 DISCN TABLET ORAL April 27, 2029 ADDITIONAL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION
EQ 34MG BASE NUPLAZID ACADIA PHARMS INC N210793 June 28, 2018 RX CAPSULE ORAL April 27, 2029 ADDITIONAL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION
EQ 10MG BASE NUPLAZID ACADIA PHARMS INC N207318 June 28, 2018 RX TABLET ORAL Oct. 27, 2029 PEDIATRIC EXCLUSIVITY
EQ 17MG BASE **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** NUPLAZID ACADIA PHARMS INC N207318 April 29, 2016 DISCN TABLET ORAL Oct. 27, 2029 PEDIATRIC EXCLUSIVITY
EQ 34MG BASE NUPLAZID ACADIA PHARMS INC N210793 June 28, 2018 RX CAPSULE ORAL Oct. 27, 2029 PEDIATRIC EXCLUSIVITY

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
8877 INN_ID
C510793 MESH_SUPPLEMENTAL_RECORD_UI
8423 IUPHAR_LIGAND_ID
1791685 RXNORM
240624 MMSL
31639 MMSL
d08433 MMSL
016844 NDDF
016845 NDDF
451861000221107 SNOMEDCT_US
721997002 SNOMEDCT_US
763543000 SNOMEDCT_US
A1L11 PDB_CHEM_ID
JZ963P0DIK INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
NUPLAZID HUMAN PRESCRIPTION DRUG LABEL 1 63090-100 TABLET, COATED 10 mg ORAL NDA 31 sections
NUPLAZID HUMAN PRESCRIPTION DRUG LABEL 1 63090-340 CAPSULE 34 mg ORAL NDA 31 sections
pimavanserin Human Prescription Drug Label 1 72205-055 CAPSULE 34 mg ORAL ANDA 31 sections