iloperidone ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antipsychotics, risperidone derivatives 3294 133454-47-4

Description:

MoleculeDescription

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:

DoseUnitRoute
18 mg O

ADMET properties:

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

Approvals:

DateAgencyCompanyOrphan
May 6, 2009 FDA VANDA PHARMS INC

FDA Adverse Event Reporting System (Female)

None

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
Decreased eye contact 148.01 60.81 24 1118 461 29572924
Oppositional defiant disorder 145.84 60.81 24 1118 507 29572878
Bruxism 119.60 60.81 24 1118 1563 29571822
Homicidal ideation 108.50 60.81 24 1118 2500 29570885
Retrograde ejaculation 105.68 60.81 17 1125 309 29573076
Crying 90.57 60.81 24 1118 5327 29568058
Priapism 84.95 60.81 22 1120 4466 29568919
Coordination abnormal 83.81 60.81 24 1118 7090 29566295
Dyskinesia 77.18 60.81 29 1113 20032 29553353
Choreoathetosis 74.27 60.81 15 1127 1005 29572380
Trismus 72.01 60.81 17 1125 2356 29571029
Hyperkinesia 67.55 60.81 15 1127 1584 29571801
Speech disorder 65.80 60.81 27 1115 23489 29549896
Streptococcal infection 61.26 60.81 17 1125 4471 29568914
Affect lability 61.08 60.81 16 1126 3386 29569999

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
Oppositional defiant disorder 165.95 57.19 24 1152 462 64497094
Decreased eye contact 155.07 57.19 24 1152 741 64496815
Homicidal ideation 120.35 57.19 24 1152 3233 64494323
Bruxism 117.79 57.19 24 1152 3600 64493956
Coordination abnormal 97.64 57.19 27 1149 14937 64482619
Dyskinesia 90.64 57.19 32 1144 39356 64458200
Choreoathetosis 86.66 57.19 16 1160 1431 64496125
Crying 76.98 57.19 24 1152 20066 64477490
Trismus 72.43 57.19 17 1159 4884 64492672
Hyperkinesia 71.81 57.19 15 1161 2531 64495025
Aggression 67.74 57.19 27 1149 46205 64451351
Streptococcal infection 65.29 57.19 17 1159 7462 64490094
Speech disorder 63.09 57.19 26 1150 48415 64449141
Suicidal ideation 61.41 57.19 28 1148 66514 64431042
Psychomotor hyperactivity 58.43 57.19 18 1158 14433 64483123
Affect lability 57.57 57.19 16 1160 8974 64488582

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AX14 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Other antipsychotics
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
CHEBI has role CHEBI:48279 serotonin antagonists
CHEBI has role CHEBI:48561 dopaminergic antagonists
CHEBI has role CHEBI:65191 atypical antipsychotic agent

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

DiseaseRelationSNOMED_IDDOID
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
Dysphagia contraindication 40739000
Hypokalemia contraindication 43339004
Conduction disorder of the heart contraindication 44808001
Bradycardia contraindication 48867003
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Leukopenia contraindication 84828003 DOID:615
Tardive dyskinesia contraindication 102449007
Prolonged QT interval contraindication 111975006
Seizure disorder contraindication 128613002
Hypomagnesemia contraindication 190855004
Disease of liver contraindication 235856003 DOID:409
Hyperprolactinemia contraindication 237662005 DOID:12700
Suicidal contraindication 267073005
Neutropenic disorder contraindication 303011007 DOID:1227
Impaired cognition contraindication 386806002
Breastfeeding (mother) contraindication 413712001
Obesity contraindication 414916001 DOID:9970
Poor metabolizer due to cytochrome p450 CYP2D6 variant contraindication 423629005
Decompensated chronic heart failure contraindication 424404003
Congenital long QT syndrome contraindication 442917000
Carcinoma of female breast contraindication 447782002




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.55 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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
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
1MG 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
2MG 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
4MG 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
6MG 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
8MG 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
12MG 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
1MG 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
2MG 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
4MG 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
6MG 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
8MG 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
12MG 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
1MG 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
2MG 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
4MG 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
6MG 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
8MG 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
12MG 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
1MG 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
2MG 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
4MG 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
6MG 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
8MG 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
12MG 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
1MG 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
2MG 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
4MG 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
6MG 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
8MG 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
12MG 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
1MG 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
2MG 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
4MG 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
6MG 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
8MG 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
12MG 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
1MG 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
2MG 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
4MG 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
6MG 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
8MG 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
12MG 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
1MG 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
2MG 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
4MG 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
6MG 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
8MG 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 9074254 Dec. 28, 2031 DOSAGE MODIFICATION TO REDUCE RISKS ASSOCIATED WITH QT PROLONGATION NOT INDUCED BY OTHER DRUGS DURING TREATMENT WITH ILOPERIDONE
1MG 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
2MG 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
4MG 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
6MG 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
8MG 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

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 9.86 WOMBAT-PK CHEMBL
D(2) dopamine receptor GPCR ANTAGONIST Ki 8.97 WOMBAT-PK CHEMBL
Sodium-dependent dopamine transporter Transporter Ki 5.53 WOMBAT-PK
D(4) dopamine receptor GPCR Ki 7.60 WOMBAT-PK
Gastrin/cholecystokinin type B receptor GPCR Ki 5.03 PDSP
D(1A) dopamine receptor GPCR Ki 6.67 WOMBAT-PK
Alpha-2A adrenergic receptor GPCR Ki 6.79 WOMBAT-PK
Sigma non-opioid intracellular receptor 1 Membrane receptor IC50 7.19 CHEMBL
Sodium-dependent noradrenaline transporter Transporter Ki 5.83 WOMBAT-PK
5-hydroxytryptamine receptor 1A GPCR Ki 7.18 WOMBAT-PK
5-hydroxytryptamine receptor 2C GPCR Ki 7.23 WOMBAT-PK
5-hydroxytryptamine receptor 6 GPCR Ki 7.37 WOMBAT-PK
5-hydroxytryptamine receptor 7 GPCR Ki 7.66 WOMBAT-PK
Alpha-1A adrenergic receptor GPCR Ki 7.44 WOMBAT-PK
Alpha-2B adrenergic receptor GPCR Ki 6.79 WOMBAT-PK
D(3) dopamine receptor GPCR Ki 8.15 WOMBAT-PK
D(1B) dopamine receptor GPCR Ki 6.50 WOMBAT-PK
Histamine H1 receptor GPCR Ki 7.91 WOMBAT-PK
Muscarinic acetylcholine receptor M1 GPCR Ki 5.31 PDSP
Muscarinic acetylcholine receptor M2 GPCR Ki 5.48 PDSP
Muscarinic acetylcholine receptor M4 GPCR Ki 5.08 PDSP
5-hydroxytryptamine receptor 1B GPCR Ki 7.05 WOMBAT-PK
5-hydroxytryptamine receptor 1D GPCR Ki 7.82 WOMBAT-PK
Alpha-2C adrenergic receptor GPCR Ki 7.79 WOMBAT-PK
D(2) dopamine receptor GPCR IC50 6.96 CHEMBL
5-hydroxytryptamine receptor 1A GPCR ANTAGONIST Ki 6.80 IUPHAR
5-hydroxytryptamine receptor 7 GPCR ANTAGONIST Ki 7.70 IUPHAR
Alpha-2A adrenergic receptor GPCR IC50 9.40 CHEMBL
5-hydroxytryptamine receptor 1A GPCR IC50 6.68 CHEMBL
D(1A) dopamine receptor GPCR IC50 6.12 CHEMBL
5-hydroxytryptamine receptor 2A GPCR IC50 8.05 CHEMBL
5-hydroxytryptamine receptor 6 GPCR ANTAGONIST Ki 7.40 IUPHAR
Serotonin 2 (5-HT2) receptor GPCR IC50 8.05 CHEMBL

External reference:

IDSource
4028716 VUID
N0000178412 NUI
D02666 KEGG_DRUG
4028716 VANDF
C0247194 UMLSCUI
CHEBI:65173 CHEBI
CHEMBL14376 ChEMBL_ID
DB04946 DRUGBANK_ID
C081732 MESH_SUPPLEMENTAL_RECORD_UI
71360 PUBCHEM_CID
87 IUPHAR_LIGAND_ID
7045 INN_ID
VPO7KJ050N UNII
73178 RXNORM
164543 MMSL
26436 MMSL
d07441 MMSL
013338 NDDF
442849001 SNOMEDCT_US
442910003 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4178 TABLET 1 mg ORAL ANDA 31 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4179 TABLET 2 mg ORAL ANDA 31 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4180 TABLET 4 mg ORAL ANDA 31 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4181 TABLET 6 mg ORAL ANDA 31 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4182 TABLET 8 mg ORAL ANDA 31 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4183 TABLET 10 mg ORAL ANDA 31 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4184 TABLET 12 mg ORAL ANDA 31 sections
FANAPT HUMAN PRESCRIPTION DRUG LABEL 1 69189-0597 TABLET 4 mg ORAL NDA 31 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 1 69189-0665 TABLET 4 mg ORAL NDA 31 sections