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

Stem definition	Drug id	CAS RN
serotonin receptor antagonists (mostly 5-HT2)	5142	706779-91-1

Description:

Molecule	Description
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

Molecule

Description

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:

Show entries

Search:

Property	Value	Reference
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

Showing 1 to 2 of 2 entries

Previous1Next

Approvals:

Date	Agency	Company	Orphan
April 29, 2016	FDA	ACADIA PHARMACEUTICALS INC

FDA Adverse Event Reporting System (Female)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hallucination	4147.86	46.70	1152	12963	53665	63421242
Death	1721.16	46.70	1047	13068	373334	63101573
Underdose	800.01	46.70	280	13835	27176	63447731
Prescribed underdose	609.40	46.70	234	13881	29455	63445452
Hallucination, visual	543.36	46.70	192	13923	19106	63455801
Product dose omission issue	530.57	46.70	428	13687	233885	63241022
Nonspecific reaction	525.50	46.70	118	13997	2174	63472733
Drug ineffective	428.30	46.70	796	13319	1043969	62430938
Confusional state	414.23	46.70	373	13742	236007	63238900
Abnormal behaviour	400.85	46.70	158	13957	21268	63453639

Showing 1 to 10 of 43 entries

Previous1 2 3 4 5Next

FDA Adverse Event Reporting System (Male)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hallucination	6137.21	51.69	1971	21242	49527	34884191
Death	2423.41	51.69	2021	21192	396028	34537690
Prescribed underdose	1205.52	51.69	379	22834	8554	34925164
Underdose	1161.59	51.69	410	22803	13370	34920348
Confusional state	1087.82	51.69	838	22375	143322	34790396
Nonspecific reaction	853.03	51.69	196	23017	1215	34932503
Abnormal behaviour	739.45	51.69	351	22862	24618	34909100
Product dose omission issue	659.62	51.69	581	22632	119130	34814588
Hallucination, visual	591.26	51.69	271	22942	17520	34916198
Drug ineffective	497.27	51.69	992	22221	455759	34477959

Showing 1 to 10 of 61 entries

Previous1 2 3 4 5 6 7Next

FDA Adverse Event Reporting System (Geriatric)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hallucination	5425.20	43.94	1686	22596	84059	79636047
Death	4320.78	43.94	2445	21837	564069	79156037
Underdose	1470.31	43.94	501	23781	32650	79687456
Prescribed underdose	1153.35	43.94	406	23876	29108	79690998
Confusional state	981.52	43.94	793	23489	317204	79402902
Abnormal behaviour	792.69	43.94	327	23955	36094	79684012
Product dose omission issue	789.43	43.94	630	23652	246907	79473199
Nonspecific reaction	694.94	43.94	160	24122	2372	79717734
Hallucination, visual	635.47	43.94	271	24011	32458	79687648
Fall	548.15	43.94	705	23577	486924	79233182

Showing 1 to 10 of 77 entries

Previous1 2 3 4 5…8Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
ATC	N05AX17	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Other antipsychotics
CHEBI has role	CHEBI:35476	neuroleptics
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:133016	5-hydroxytryptamine (2A) receptor inverse agonist
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

Showing 1 to 10 of 16 entries

Previous1 2Next

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

Disease	Relation	SNOMED_ID	DOID
Parkinson's disease	indication	49049000	DOID:14330

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.42	Basic

Orange Book patent data (new drug applications)

Show entries

Search:

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
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 10MG BASE	NUPLAZID	ACADIA PHARMS INC	N207318	June 28, 2018	RX	TABLET	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 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

Showing 1 to 10 of 18 entries

Previous1 2Next

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	INVERSE AGONIST	Ki	9.30		SCIENTIFIC LITERATURE	DRUG LABEL
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	INVERSE AGONIST	Ki	8.80		SCIENTIFIC LITERATURE

Showing 1 to 2 of 2 entries

Previous1Next

External reference:

Show entries

Search:

ID	Source
016844	NDDF
016845	NDDF
10071196	PUBCHEM_CID
1791685	RXNORM
240624	MMSL
31639	MMSL
4035717	VANDF
706782-28-7	SECONDARY_CAS_RN
721997002	SNOMEDCT_US
763543000	SNOMEDCT_US

Showing 1 to 10 of 21 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
NUPLAZID	HUMAN PRESCRIPTION DRUG LABEL	1	63090-100	TABLET, COATED	10 mg	ORAL	NDA	32 sections
NUPLAZID	HUMAN PRESCRIPTION DRUG LABEL	1	63090-100	TABLET, COATED	10 mg	ORAL	NDA	32 sections
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
NUPLAZID	HUMAN PRESCRIPTION DRUG LABEL	1	63090-340	CAPSULE	34 mg	ORAL	NDA	32 sections
NUPLAZID	HUMAN PRESCRIPTION DRUG LABEL	1	63090-340	CAPSULE	34 mg	ORAL	NDA	32 sections

Showing 1 to 7 of 7 entries

Previous1Next