Iloperidone

Atypical Antipsychotic — NERVOUS SYSTEM

Key facts

Iloperidone is an ofp drug in the Atypical Antipsychotic class catalogued in DrugCentral. It was first approved by the FDA in 2009. DrugCentral lists 33 molecular targets, including HTR2A, Adra2a and DRD2. Recorded indications include Schizophrenia.

• Approval status: ofp (first approved 2009 by the FDA).
• Drug class: Atypical Antipsychotic.
• Molecular targets: HTR2A, Adra2a, DRD2 and DRD3 (33 listed in DrugCentral).
• Indications: Schizophrenia.
• ATC code: N05AX14 (Other antipsychotics).
• Molecular formula: C24H27FN2O4; molecular weight 426.49 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Schizophrenia

Off-label uses (1)

• Depression Treatment Adjunct

Contraindications (30)

• Bradycardia
• Breastfeeding (mother)
• Carcinoma of female breast
• Conduction disorder of the heart
• Congenital long QT syndrome
• Decompensated chronic heart failure
• Diabetes mellitus
• Disease of liver
• Dysphagia
• Hyperglycemia
• Hyperprolactinemia
• Hypokalemia
• Hypomagnesemia
• Impaired cognition
• Leukopenia
• Lowered convulsive threshold
• Myocardial infarction
• Neuroleptic malignant syndrome
• Neutropenic disorder
• Obesity
• Orthostatic hypotension
• Poor metabolizer due to cytochrome p450 CYP2D6 variant
• Priapism
• Prolonged QT interval
• Seizure disorder
• Senile dementia
• Suicidal
• Tardive dyskinesia
• Torsades de pointes
• Weight gain finding

Mechanism & targets

• Established pharmacologic class: Atypical Antipsychotic

Molecular targets (33)

Target	Gene	Action	Activity
5-hydroxytryptamine receptor 2A	HTR2A	antagonist	Ki 9.86
Alpha-2A adrenergic receptor	Adra2a	unknown	IC50 9.40
D(2) dopamine receptor	DRD2	antagonist	Ki 8.97
D(3) dopamine receptor	DRD3	unknown	Ki 8.15
5-hydroxytryptamine receptor 2A	HTR2A	unknown	IC50 8.05
Serotonin 2 (5-HT2) receptor	Htr2c|Htr2a|Htr2b	unknown	IC50 8.05
Histamine H1 receptor	HRH1	unknown	Ki 7.91
5-hydroxytryptamine receptor 1D	HTR1D	unknown	Ki 7.82
Alpha-2C adrenergic receptor	ADRA2C	unknown	Ki 7.79
5-hydroxytryptamine receptor 7	Htr7	antagonist	Ki 7.70
5-hydroxytryptamine receptor 7	HTR7	unknown	Ki 7.66
D(4) dopamine receptor	DRD4	unknown	Ki 7.60
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 7.44
5-hydroxytryptamine receptor 6	Htr6	antagonist	Ki 7.40
5-hydroxytryptamine receptor 6	HTR6	unknown	Ki 7.37
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 7.23
Sigma non-opioid intracellular receptor 1	SIGMAR1	unknown	IC50 7.19
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 7.18
5-hydroxytryptamine receptor 1B	HTR1B	unknown	Ki 7.05
D(2) dopamine receptor	Drd2	unknown	IC50 6.96

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2009-05-06	FDA	—	VANDA PHARMS INC

ATC classification

ATC code	Therapeutic hierarchy
N05AX14	NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Other antipsychotics

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label
• FDA label: CYP2D6 · Actionable PGx

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Oppositional defiant disorder	198.8
Decreased eye contact	189.5
Retrograde ejaculation	166.7
Homicidal ideation	148.7
Bruxism	132.9
Dyskinesia	103.2
Coordination abnormal	102.0
Priapism	100.5
Choreoathetosis	97.4
Crying	91.3
Trismus	90.0
Aggression	81.5

Chemical structure

• Molecular formula: C₂₄H₂₇FN₂O₄
• Molecular weight: 426.49 g/mol
• CAS number: —
• InChIKey: XMXHEBAFVSFQEX-UHFFFAOYSA-N
• PubChem CID: 71360

COC1=C(OCCCN2CCC(CC2)C2=NOC3=CC(F)=CC=C23)C=CC(=C1)C(C)=O

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Iloperidone used for?

DrugCentral lists the following indications for Iloperidone: Schizophrenia.

How does Iloperidone work?

Its molecular targets in DrugCentral include HTR2A (antagonist), Adra2a, DRD2 (antagonist) and DRD3.

When was Iloperidone first approved?

Iloperidone was first approved by the FDA in 2009.

What drug class does Iloperidone belong to?

Iloperidone is in the Atypical Antipsychotic class.

What is the chemical formula of Iloperidone?

Iloperidone has the molecular formula C24H27FN2O4 and a molecular weight of 426.49 g/mol.

Sources

• DrugCentral drug card 3294 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL14376 — compound record and bioactivity
• PubChem CID 71360 — chemical identifiers
• DrugBank DB04946 — drug record
• FDA UNII VPO7KJ050N — substance identity
• DailyMed: FDA labels for Iloperidone — current prescribing information (label search)
• UniProt P28223 (HTR2A) — target protein
• UniProt P14416 (DRD2) — target protein
• UniProt P35462 (DRD3) — target protein
• UniProt P35367 (HRH1) — target protein
• UniProt P28221 (HTR1D) — target protein
• UniProt P18825 (ADRA2C) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.