iloperidone 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 ┬ÁM/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)

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
Dizziness 55.09 50.68 24 257 58641 2299163
Orthostatic hypotension 54.74 50.68 12 269 2867 2354937
Weight increased 53.00 50.68 18 263 22319 2335485

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 113.85 54.16 14 263 44 1746460
Oppositional defiant disorder 111.22 54.16 14 263 56 1746448
Retrograde ejaculation 109.72 54.16 15 262 126 1746378
Priapism 105.47 54.16 20 257 1444 1745060
Bruxism 90.08 54.16 14 263 303 1746201
Dyskinesia 81.03 54.16 19 258 3800 1742704
Homicidal ideation 80.45 54.16 14 263 617 1745887
Sydenham's chorea 72.46 54.16 8 269 5 1746499
Insomnia 69.60 54.16 23 254 16253 1730251
Crying 68.58 54.16 14 263 1461 1745043
Coordination abnormal 68.38 54.16 14 263 1483 1745021
Suicidal ideation 61.44 54.16 18 259 8500 1738004
Aggression 57.85 54.16 17 260 8098 1738406
Speech disorder 57.73 54.16 15 262 4533 1741971
Sleep disorder 54.46 54.16 14 263 4049 1742455

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
CHEBI has role CHEBI:48279 serotonergic antagonist
CHEBI has role CHEBI:48561 dopaminergic antagonist
CHEBI has role CHEBI:65191 second generation antipsychotic
MeSH PA D014149 Tranquilizing Agents

Drug Use (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

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

External reference:

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-0636 TABLET 12 mg ORAL ANDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 1 43068-101 TABLET 1 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 1 43068-102 TABLET 2 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 1 43068-104 TABLET 4 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 1 43068-106 TABLET 6 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 1 43068-108 TABLET 8 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 1 43068-110 TABLET 10 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 1 43068-112 TABLET 12 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 4 43068-113 KIT 1 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 4 43068-113 KIT 2 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 4 43068-113 KIT 4 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 4 43068-113 KIT 6 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 1 43068-901 TABLET 6 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 1 43068-902 TABLET 8 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 4 43068-903 KIT 6 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 4 43068-903 KIT 1 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 4 43068-903 KIT 4 mg ORAL NDA 19 sections
Fanapt HUMAN PRESCRIPTION DRUG LABEL 4 43068-903 KIT 2 mg ORAL NDA 19 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4178 TABLET 1 mg ORAL ANDA 20 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4179 TABLET 2 mg ORAL ANDA 20 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4180 TABLET 4 mg ORAL ANDA 20 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4181 TABLET 6 mg ORAL ANDA 20 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4182 TABLET 8 mg ORAL ANDA 20 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4183 TABLET 10 mg ORAL ANDA 20 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4184 TABLET 12 mg ORAL ANDA 20 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 4 51672-4213 KIT 4 mg None ANDA 20 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 4 51672-4213 KIT 1 mg None ANDA 20 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 4 51672-4213 KIT 6 mg None ANDA 20 sections
Iloperidone HUMAN PRESCRIPTION DRUG LABEL 4 51672-4213 KIT 2 mg None ANDA 20 sections
FANAPT HUMAN PRESCRIPTION DRUG LABEL 1 69189-0597 TABLET 4 mg ORAL NDA 19 sections