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:

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

Approvals:

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

FDA Adverse Event Reporting System (Female)

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
Delusion	258.02	46.70	98	14017	11919	63462988
Fall	254.75	46.70	370	13745	391964	63082943
Adverse drug reaction	228.38	46.70	168	13947	79546	63395361
Aggression	212.65	46.70	104	14011	23394	63451513
Dementia	200.01	46.70	93	14022	18701	63456206
Dementia with Lewy bodies	174.02	46.70	34	14081	304	63474603
Somnolence	167.17	46.70	202	13913	178483	63296424
Paranoia	137.45	46.70	62	14053	11617	63463290
Therapeutic response unexpected	137.44	46.70	72	14043	18687	63456220
Peripheral swelling	134.46	46.70	224	13891	265718	63209189
Gait disturbance	120.05	46.70	174	13941	183004	63291903
Nightmare	116.42	46.70	65	14050	19129	63455778
Urinary tract infection	111.73	46.70	206	13909	264478	63210429
Abnormal dreams	96.45	46.70	47	14068	10469	63464438
Inappropriate schedule of product administration	96.17	46.70	117	13998	103848	63371059
Metabolic function test abnormal	95.96	46.70	19	14096	183	63474724
Hypersomnia	90.46	46.70	54	14061	18001	63456906
Hip fracture	88.53	46.70	64	14051	29410	63445497
Psychotic disorder	84.54	46.70	59	14056	25653	63449254
Agitation	77.07	46.70	80	14035	59677	63415230
Arthralgia	72.03	46.70	19	14096	569691	62905216
Pyrexia	71.44	46.70	10	14105	470468	63004439
Hospitalisation	71.05	46.70	91	14024	84990	63389917
Tremor	70.15	46.70	114	14001	132125	63342782
Screaming	67.81	46.70	26	14089	3236	63471671
Dysphagia	65.10	46.70	89	14026	88496	63386411
Pain	64.45	46.70	43	14072	740585	62734322
Balance disorder	59.31	46.70	83	14032	84339	63390568
Insomnia	57.37	46.70	139	13976	215113	63259794
Freezing phenomenon	57.06	46.70	18	14097	1254	63473653
Cognitive disorder	53.49	46.70	64	14051	55751	63419156
Hallucination, auditory	50.69	46.70	33	14082	12791	63462116
Drug hypersensitivity	48.55	46.70	6	14109	310681	63164226

FDA Adverse Event Reporting System (Male)

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
Fall	449.36	51.69	609	22604	202276	34731442
Adverse drug reaction	437.02	51.69	261	22952	29081	34904637
Gait disturbance	383.75	51.69	370	22843	84770	34848948
Aggression	373.97	51.69	263	22950	38701	34895017
Peripheral swelling	364.57	51.69	343	22870	76198	34857520
Dementia	363.44	51.69	179	23034	13569	34920149
Delusion	302.97	51.69	154	23059	12481	34921237
Therapeutic response unexpected	297.09	51.69	140	23073	9617	34924101
Somnolence	276.61	51.69	354	22859	110762	34822956
Gait inability	222.25	51.69	150	23063	20608	34913110
Agitation	218.72	51.69	228	22985	57171	34876547
Hypersomnia	209.95	51.69	120	23093	12287	34921431
Nightmare	193.46	51.69	120	23093	14271	34919447
Dysstasia	187.91	51.69	111	23102	12084	34921634
Dementia with Lewy bodies	164.90	51.69	46	23167	669	34933049
Paranoia	163.13	51.69	101	23112	11967	34921751
Acute kidney injury	160.28	51.69	11	23202	304977	34628741
Posture abnormal	145.14	51.69	55	23158	2184	34931534
Pyrexia	140.30	51.69	26	23187	332987	34600731
Drooling	136.16	51.69	59	23154	3323	34930395
Inappropriate schedule of product administration	133.92	51.69	185	23028	62111	34871607
Metabolic function test abnormal	132.25	51.69	25	23188	45	34933673
Hospitalisation	131.44	51.69	175	23038	56727	34876991
Abnormal dreams	127.38	51.69	73	23140	7505	34926213
Anaemia	126.74	51.69	7	23206	233328	34700390
Insomnia	125.06	51.69	237	22976	103670	34830048
Balance disorder	124.37	51.69	144	23069	40510	34893208
Psychotic disorder	116.88	51.69	110	23103	24342	34909376
Cognitive disorder	109.19	51.69	114	23099	28579	34905139
Dysphagia	96.59	51.69	159	23054	62222	34871496
Feeling abnormal	93.65	51.69	158	23055	63077	34870641
Anger	92.96	51.69	71	23142	11813	34921905
Urinary tract infection	89.24	51.69	182	23031	83899	34849819
Neutropenia	87.29	51.69	4	23209	156774	34776944
Tremor	83.21	51.69	175	23038	82412	34851306
Hip fracture	81.94	51.69	66	23147	11859	34921859
Dyspnoea	79.61	51.69	80	23133	376702	34557016
Intentional underdose	76.25	51.69	25	23188	643	34933075
Arthralgia	74.23	51.69	12	23201	170029	34763689
Disorientation	73.41	51.69	100	23113	33088	34900630
Speech disorder	71.92	51.69	87	23126	25599	34908119
Constipation	68.31	51.69	223	22990	136759	34796959
Abdominal pain	68.25	51.69	13	23200	163605	34770113
Diarrhoea	64.33	51.69	100	23113	389812	34543906
Restlessness	62.85	51.69	81	23132	25401	34908317
Freezing phenomenon	62.49	51.69	27	23186	1509	34932209
Screaming	60.09	51.69	26	23187	1458	34932260
Motor dysfunction	59.73	51.69	44	23169	6930	34926788
Memory impairment	58.55	51.69	104	23109	43214	34890504
Drug interaction	57.42	51.69	40	23173	225906	34707812
Refusal of treatment by patient	55.33	51.69	37	23176	4995	34928723

FDA Adverse Event Reporting System (Geriatric)

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
Aggression	500.98	43.94	264	24018	50694	79669412
Dementia	374.68	43.94	172	24110	24487	79695619
Delusion	369.58	43.94	161	24121	20262	79699844
Somnolence	336.23	43.94	388	23894	238593	79481513
Gait disturbance	320.96	43.94	354	23928	207152	79512954
Therapeutic response unexpected	271.59	43.94	129	24153	19817	79700289
Hypersomnia	256.60	43.94	130	24152	22956	79697150
Metabolic function test abnormal	237.55	43.94	44	24238	197	79719909
Agitation	234.95	43.94	214	24068	99501	79620605
Adverse drug reaction	210.53	43.94	169	24113	66223	79653883
Paranoia	197.37	43.94	103	24179	19329	79700777
Peripheral swelling	197.23	43.94	319	23963	269298	79450808
Drug ineffective	185.64	43.94	732	23550	1080181	78639925
Abnormal dreams	177.66	43.94	81	24201	11331	79708775
Dysstasia	175.85	43.94	108	24174	27638	79692468
Psychotic disorder	172.33	43.94	124	24158	41278	79678828
Dementia with Lewy bodies	167.16	43.94	41	24241	805	79719301
Inappropriate schedule of product administration	158.09	43.94	199	24083	133429	79586677
Gait inability	155.69	43.94	135	24147	58782	79661324
Nightmare	147.12	43.94	94	24188	25767	79694339
Drooling	134.73	43.94	55	24227	5879	79714227
Hip fracture	134.61	43.94	95	24187	30666	79689440
Cognitive disorder	134.05	43.94	134	24148	69792	79650314
Posture abnormal	131.21	43.94	48	24234	3818	79716288
Balance disorder	126.17	43.94	153	24129	98704	79621402
Anger	122.18	43.94	72	24210	17090	79703016
Pyrexia	121.37	43.94	29	24253	678680	79041426
Acute kidney injury	121.00	43.94	10	24272	519394	79200712
Urinary tract infection	113.61	43.94	255	24027	274257	79445849
Insomnia	110.82	43.94	236	24046	244934	79475172
Dysphagia	105.16	43.94	156	24126	121980	79598126
Anaemia	102.43	43.94	9	24273	445006	79275100
Tremor	100.15	43.94	183	24099	169900	79550206
Arthralgia	99.13	43.94	26	24256	571777	79148329
Sedation	87.76	43.94	93	24189	51802	79668304
Motor dysfunction	87.39	43.94	55	24227	14678	79705428
Disorientation	86.38	43.94	101	24181	62675	79657431
Speech disorder	82.36	43.94	92	24190	54353	79665753
Freezing phenomenon	81.02	43.94	28	24254	1886	79718220
Pain	81.01	43.94	58	24224	703744	79016362
Hospitalisation	79.13	43.94	119	24163	94117	79625989
Feeling abnormal	78.60	43.94	159	24123	159040	79561066
Orthostatic hypotension	78.34	43.94	91	24191	56073	79664033
Screaming	74.35	43.94	32	24250	3901	79716205
Intentional underdose	71.71	43.94	27	24255	2327	79717779
Neutropenia	71.41	43.94	4	24278	287706	79432400
Abdominal pain	65.03	43.94	19	24263	389550	79330556
Completed suicide	62.29	43.94	3	24279	245764	79474342
Incoherent	62.01	43.94	35	24247	7657	79712449
Dyspnoea	59.06	43.94	107	24175	856918	78863188
Diarrhoea	58.85	43.94	112	24170	880377	78839729
Restlessness	57.71	43.94	71	24211	46421	79673685
Patient elopement	56.98	43.94	11	24271	64	79720042
Drug hypersensitivity	56.91	43.94	11	24271	298905	79421201
Constipation	55.66	43.94	201	24081	282849	79437257
Lethargy	54.95	43.94	93	24189	81199	79638907
Refusal of treatment by patient	54.41	43.94	34	24248	8957	79711149
Product use in unapproved indication	52.62	43.94	7	24275	250352	79469754
Unresponsive to stimuli	51.95	43.94	74	24208	55714	79664392
Pruritus	50.12	43.94	29	24253	394619	79325487
Haemoglobin decreased	49.69	43.94	5	24277	222114	79497992
Hypokinesia	46.96	43.94	42	24240	19018	79701088
Memory impairment	46.33	43.94	104	24178	111630	79608476
Belligerence	46.09	43.94	12	24270	302	79719804
Rapid eye movement sleep behaviour disorder	45.87	43.94	13	24269	453	79719653
White blood cell count decreased	45.54	43.94	3	24279	188285	79531821
Drug interaction	44.13	43.94	37	24245	415146	79304960

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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	neuroleptics
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:133016	5-hydroxytryptamine (2A) receptor inverse agonist

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)

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 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:

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

External reference:

ID	Source
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
8423	IUPHAR_LIGAND_ID
1791685	RXNORM
240624	MMSL
31639	MMSL
d08433	MMSL
016844	NDDF
016845	NDDF
721997002	SNOMEDCT_US
763543000	SNOMEDCT_US
C510793	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

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