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

Stem definition	Drug id	CAS RN
antipsychotics, risperidone derivatives	3294	133454-47-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: HP-873 HP 873 iloperidone zomaril fanapt	an atypical, negative symptom antipsychotic agent Molecular weight: 426.49 Formula: C24H27FN2O4 CLOGP: 3.92 LIPINSKI: 0 HAC: 6 HDO: 0 TPSA: 64.80 ALOGS: -4.15 ROTB: 8 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

HP-873
HP 873
iloperidone
zomaril
fanapt

an atypical, negative symptom antipsychotic agent

Molecular weight: 426.49
Formula: C24H27FN2O4
CLOGP: 3.92
LIPINSKI: 0
HAC: 6
HDO: 0
TPSA: 64.80
ALOGS: -4.15
ROTB: 8

Status: OFP

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

Drug dosage:

Dose	Unit	Route
18	mg	O

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.80 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.03 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
May 6, 2009	FDA	VANDA PHARMS INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

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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
Decreased eye contact	150.80	60.69	24	1153	471	34955283
Oppositional defiant disorder	148.32	60.69	24	1153	525	34955229
Retrograde ejaculation	131.93	60.69	21	1156	412	34955342
Bruxism	120.74	60.69	24	1153	1711	34954043
Homicidal ideation	110.32	60.69	24	1153	2658	34953096
Crying	91.66	60.69	24	1153	5838	34949916
Priapism	85.60	60.69	22	1155	4972	34950782
Coordination abnormal	85.35	60.69	24	1153	7620	34948134
Dyskinesia	77.91	60.69	29	1148	22384	34933370
Choreoathetosis	75.69	60.69	15	1162	1049	34954705

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FDA Adverse Event Reporting System (Geriatric)

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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
Oppositional defiant disorder	170.22	58.59	24	1166	473	79742725
Decreased eye contact	156.93	58.59	24	1166	841	79742357
Homicidal ideation	123.72	58.59	24	1166	3433	79739765
Bruxism	120.07	58.59	24	1166	4002	79739196
Coordination abnormal	99.09	58.59	27	1163	17285	79725913
Dyskinesia	92.89	58.59	32	1158	44741	79698457
Choreoathetosis	88.55	58.59	16	1174	1554	79741644
Crying	78.47	58.59	24	1166	23019	79720179
Trismus	73.97	58.59	17	1173	5450	79737748
Hyperkinesia	73.77	58.59	15	1175	2714	79740484

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05AX14	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Other antipsychotics
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:48561	dopaminergic antagonists
CHEBI has role	CHEBI:65191	atypical antipsychotic agent
FDA EPC	N0000175430	Atypical Antipsychotic
MeSH PA	D014150	Antipsychotic Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D014149	Tranquilizing Agents

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

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Disease	Relation	SNOMED_ID	DOID
Schizophrenia	indication	58214004	DOID:5419
Depression Treatment Adjunct	off-label use
Priapism	contraindication	6273006	DOID:9286
Weight gain finding	contraindication	8943002
Neuroleptic malignant syndrome	contraindication	15244003	DOID:14464
Senile dementia	contraindication	15662003
Lowered convulsive threshold	contraindication	19260006
Myocardial infarction	contraindication	22298006	DOID:5844
Orthostatic hypotension	contraindication	28651003
Torsades de pointes	contraindication	31722008

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.55	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10MG	FANAPT	VANDA PHARMS INC	N022192	May 6, 2009	RX	TABLET	ORAL	9138432	Sept. 30, 2025	METHOD OF TREATING SCHIZOPHRENIA BY ADMINISTERING ILOPERIDONE TO A PATIENT BY REDUCING THE DOSE IN PATIENTS WHO ARE BEING TREATED WITH FLUOXETINE
10MG	FANAPT	VANDA PHARMS INC	N022192	May 6, 2009	RX	TABLET	ORAL	8586610	Nov. 2, 2027	METHOD OF TREATING SCHIZOPHRENIA BY ADMINISTERING ILOPERIDONE TO A PATIENT BY REDUCING THE DOSE IN PATIENTS WHO ARE POOR METABOLIZERS OF CYP2D6
10MG	FANAPT	VANDA PHARMS INC	N022192	May 6, 2009	RX	TABLET	ORAL	9157121	April 5, 2030	DOSAGE MODIFICATION TO REDUCE RISKS ASSOCIATED WITH QT PROLONGATION NOT INDUCED BY OTHER DRUGS DURING TREATMENT WITH ILOPERIDONE
10MG	FANAPT	VANDA PHARMS INC	N022192	May 6, 2009	RX	TABLET	ORAL	8652776	Aug. 31, 2030	DOSAGE MODIFICATION TO REDUCE THE RISK ASSOCIATED WITH QT PROLONGATION NOT INDUCED BY OTHER DRUGS DURING TREATMENT WITH ILOPERIDONE
10MG	FANAPT	VANDA PHARMS INC	N022192	May 6, 2009	RX	TABLET	ORAL	8999638	Oct. 28, 2030	DOSAGE MODIFICATION TO REDUCE RISKS ASSOCIATED WITH QT PROLONGATION NOT INDUCED BY OTHER DRUGS DURING TREATMENT WITH ILOPERIDONE
10MG	FANAPT	VANDA PHARMS INC	N022192	May 6, 2009	RX	TABLET	ORAL	9074255	Dec. 17, 2030	DOSAGE MODIFICATION TO REDUCE RISKS ASSOCIATED WITH QT PROLONGATION NOT INDUCED BY OTHER DRUGS DURING TREATMENT WITH ILOPERIDONE
10MG	FANAPT	VANDA PHARMS INC	N022192	May 6, 2009	RX	TABLET	ORAL	9072742	Jan. 16, 2031	DOSAGE MODIFICATION TO REDUCE RISKS ASSOCIATED WITH QT PROLONGATION NOT INDUCED BY OTHER DRUGS DURING TREATMENT WITH ILOPERIDONE
10MG	FANAPT	VANDA PHARMS INC	N022192	May 6, 2009	RX	TABLET	ORAL	9074256	Feb. 10, 2031	DOSAGE MODIFICATION TO REDUCE RISKS ASSOCIATED WITH QT PROLONGATION NOT INDUCED BY OTHER DRUGS DURING TREATMENT WITH ILOPERIDONE
10MG	FANAPT	VANDA PHARMS INC	N022192	May 6, 2009	RX	TABLET	ORAL	9074254	Dec. 28, 2031	DOSAGE MODIFICATION TO REDUCE RISKS ASSOCIATED WITH QT PROLONGATION NOT INDUCED BY OTHER DRUGS DURING TREATMENT WITH ILOPERIDONE
12MG	FANAPT	VANDA PHARMS INC	N022192	May 6, 2009	RX	TABLET	ORAL	9138432	Sept. 30, 2025	METHOD OF TREATING SCHIZOPHRENIA BY ADMINISTERING ILOPERIDONE TO A PATIENT BY REDUCING THE DOSE IN PATIENTS WHO ARE BEING TREATED WITH FLUOXETINE

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	8.97	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	9.86	WOMBAT-PK	CHEMBL
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	5.31	PDSP
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	5.48	PDSP
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	6.67	WOMBAT-PK
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.79	WOMBAT-PK
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		IC50	7.19	CHEMBL
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.83	WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	7.18	WOMBAT-PK
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	7.23	WOMBAT-PK

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External reference:

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ID	Source
013338	NDDF
164543	MMSL
26436	MMSL
4028716	VUID
4028716	VANDF
442849001	SNOMEDCT_US
442910003	SNOMEDCT_US
7045	INN_ID
71360	PUBCHEM_CID
73178	RXNORM

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Fanapt	HUMAN PRESCRIPTION DRUG LABEL	1	43068-101	TABLET	1 mg	ORAL	NDA	32 sections
Fanapt	HUMAN PRESCRIPTION DRUG LABEL	1	43068-102	TABLET	2 mg	ORAL	NDA	32 sections
Fanapt	HUMAN PRESCRIPTION DRUG LABEL	1	43068-104	TABLET	4 mg	ORAL	NDA	32 sections
Fanapt	HUMAN PRESCRIPTION DRUG LABEL	1	43068-106	TABLET	6 mg	ORAL	NDA	32 sections
Fanapt	HUMAN PRESCRIPTION DRUG LABEL	1	43068-108	TABLET	8 mg	ORAL	NDA	32 sections
Fanapt	HUMAN PRESCRIPTION DRUG LABEL	1	43068-110	TABLET	10 mg	ORAL	NDA	32 sections
Fanapt	HUMAN PRESCRIPTION DRUG LABEL	1	43068-112	TABLET	12 mg	ORAL	NDA	32 sections
Fanapt	HUMAN PRESCRIPTION DRUG LABEL	1	43068-901	TABLET	6 mg	ORAL	NDA	32 sections
Fanapt	HUMAN PRESCRIPTION DRUG LABEL	1	43068-902	TABLET	8 mg	ORAL	NDA	32 sections
FANAPT	HUMAN PRESCRIPTION DRUG LABEL	1	69189-0597	TABLET	4 mg	ORAL	NDA	31 sections

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