Iloperidone
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2009
- First approval year
- 2009
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Iloperidone
- Molecular weight
- 426.49
- Structure (SMILES)
- COc1cc(C(C)=O)ccc1OCCCN1CCC(c2noc3cc(F)ccc23)CC1
- fanapt
- Fanapt
- iloperidone
- Iloperidone
- hp 873
- HP 873
- HP-873
- iloperidona
- Iloperidona
- iloperidone
- Iloperidone
- iloperidone (oral tablet)
- iloperidone [INN]
- ILOPERIDONE [MART.]
- ILOPERIDONE [MI]
- ILOPERIDONE [ORANGE BOOK]
- ILOPERIDONE [USAN]
- ILOPERIDONE [USP-RS]
- ILOPERIDONE [VANDF]
- Iloperidone [WHO-DD]
- Iloperidone 1 MG
- iloperidone inn
- iloperidone mart
- iloperidone mi
- iloperidone orange book
- iloperidone usan
- iloperidone usp rs
- iloperidone vandf
- iloperidone who dd
And 1 more, listed on the interactive page.
- ATC classification codes
- N05AX14
Sources for recorded values
- CAS registry numbers
- 133454-47-4
- ChEMBL ID
- CHEMBL14376
- InChIKey
- XMXHEBAFVSFQEX-UHFFFAOYSA-N
- PubChem compound IDs
- 71360
- RxNorm IDs (RxCUI)
- 73178
- FDA ingredient codes (UNII)
- VPO7KJ050N
- Applicant
- VANDA PHARMS INC
- Approval date
- 6 May 2009
- Application number
- NDA022192
- Status
- refused
- Status date
- 12 Jun 2026
- Approved indications
- Iloperidone is indicated for: treatment of schizophrenia in adults acute treatment of manic or mixed episodes associated with bipolar I disorder in adults
- Product number
- EMEA/H/C/006561
- Authorisation holder
- Vanda Pharmaceuticals Netherlands B.V.
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Bipolar Disorder
- Schizophrenia
European medicines record
- Patents
- 8
- Designations
- 0
- Earliest recorded loss of exclusivity
- 28 Dec 2031
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- Pharmacology name
- iloperidone
- Type
- Synthetic organic
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Antagonist
- Action type
- Antagonist
- Target
- 5-HT1A receptor
- Gene symbol
- HTR1A
- Protein identifier
- P08908
- Median affinity
- 7
- Affinity units
- pKi
- Action
- Antagonist
- Action type
- Antagonist
- Target
- 5-HT7 receptor
- Gene symbol
- HTR7
- Protein identifier
- P34969
- Median affinity
- 7
- Affinity units
- pKi
- Action
- Antagonist
- Action type
- Antagonist
- Target
- 5-HT6 receptor
- Gene symbol
- HTR6
- Protein identifier
- P50406
- Median affinity
- 7.2
- Affinity units
- pKi
- Mechanism
- Dopamine D2 receptor antagonist
- Action type
- Antagonist
- Target
- D(2) dopamine receptor
- Protein identifier
- P14416
- Mechanism
- Serotonin 2a (5-HT2a) receptor antagonist
- Action type
- Antagonist
- Target
- 5-hydroxytryptamine receptor 2A
- Protein identifier
- P28223
- Mechanism
- Dopamine D2 receptor antagonist
- Action type
- Antagonist
- Target
- D(2) dopamine receptor
- Mechanism
- Serotonin 2a (5-HT2a) receptor antagonist
- Action type
- Antagonist
- Target
- 5-hydroxytryptamine receptor 2A
- Action type
- Antagonist
- Gene symbol
- DRD2
- Protein identifier
- P14416
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Antagonist
- Gene symbol
- HTR2A
- Protein identifier
- P28223
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Stress Disorders, Post-Traumatic
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001358
- Subject identifier
- D013313
- Condition
- Liver Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001421
- Subject identifier
- D008107
- Condition
- Psychotic Disorders
- Highest recorded phase
- 4
- Condition identifier
- EFO:0005407
- Subject identifier
- D011618
- Condition
- Bipolar Disorder
- Highest recorded phase
- 3
- Condition identifier
- EFO:0009963
- Subject identifier
- D001714
- Condition
- Schizophrenia
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0005090
- Subject identifier
- D012559
- Condition identifier
- EFO_0001358
- Highest recorded phase
- 2
- Condition identifier
- EFO_0001421
- Highest recorded phase
- 1
- Condition identifier
- EFO_0005407
- Condition identifier
- EFO_0009963
- Highest recorded phase
- 1
- Condition identifier
- EFO_0009963
- Highest recorded phase
- 3
- Condition identifier
- HP_0000737
- Highest recorded phase
- 2
- Condition identifier
- HP_0000822
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002025
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004985
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004985
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005090
- Condition identifier
- MONDO_0005090
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005146
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005485
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005487
- Condition identifier
- MONDO_0013600
- Highest recorded phase
- 2
Warnings
- Warning
- Black Box Warning
- Effect
- psychiatric toxicity
Open Targets warnings
- Warning
- Black Box Warning
- Effect
- psychiatric toxicity
- Country
- United States
- Event
- affect lability
- Reports
- 11
- Reporting signal score
- 23.7904
- Event
- aggression
- Reports
- 26
- Reporting signal score
- 44.9981
- Event
- akathisia
- Reports
- 14
- Reporting signal score
- 32.1868
- Event
- anxiety
- Reports
- 33
- Reporting signal score
- 27.1078
- Event
- bacterial infection
- Reports
- 9
- Reporting signal score
- 16.8623
- Event
- blood prolactin increased
- Reports
- 9
- Reporting signal score
- 22.9999
- Event
- bruxism
- Reports
- 21
- Reporting signal score
- 80.0217
- Event
- choreoathetosis
- Reports
- 12
- Reporting signal score
- 53.5127
- Event
- coordination abnormal
- Reports
- 24
- Reporting signal score
- 71.6309
- Event
- crying
- Reports
- 22
- Reporting signal score
- 50.3474
- Event
- decreased eye contact
- Reports
- 21
- Reporting signal score
- 134.208
- Event
- depressed mood
- Reports
- 13
- Reporting signal score
- 18.033
- Event
- dizziness
- Reports
- 46
- Reporting signal score
- 19.9002
- Event
- dry mouth
- Reports
- 12
- Reporting signal score
- 11.6213
- Event
- dyskinesia
- Reports
- 31
- Reporting signal score
- 69.0513
- Event
- dystonia
- Reports
- 17
- Reporting signal score
- 37.8678
- Event
- ejaculation failure
- Reports
- 8
- Reporting signal score
- 32.2762
- Event
- electrocardiogram qt prolonged
- Reports
- 22
- Reporting signal score
- 33.2284
- Event
- enuresis
- Reports
- 7
- Reporting signal score
- 21.2982
- Event
- extrapyramidal disorder
- Reports
- 12
- Reporting signal score
- 21.943
- Event
- galactorrhoea
- Reports
- 6
- Reporting signal score
- 13.9265
- Event
- hallucination, auditory
- Reports
- 11
- Reporting signal score
- 21.1188
- Event
- homicidal ideation
- Reports
- 21
- Reporting signal score
- 82.6445
- Event
- hyperkinesia
- Reports
- 11
- Reporting signal score
- 42.7825
- Event
- hyperprolactinaemia
- Reports
- 5
- Reporting signal score
- 11.8206
And 32 more, listed on the interactive page.
- NCT00254202
- NCT01207414
- NCT01291511
- NCT01348100
- NCT01623713
- NCT01929889
- NCT02453893
- NCT04712734
- NCT01529294
- NCT01917318
- NCT04819776
- Dose
- 1 mg
- Route
- Oral
- How often
- Twice daily
- Hydrogen bond acceptors
- 6
- Hydrogen bond donors
- 0
- Polar surface area
- 64.8
- Calculated partition coefficient (ALogP)
- 4.83
- Calculated partition coefficient (XLogP)
- 4.1
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 8
- Heavy atoms
- 31
- Molecular formula
- C24H27FN2O4
- Monoisotopic mass
- 426.19548551
- Natural product
- No
- 0378-0630
- 0378-0631
- 0378-0632
- 0378-0633
- 0378-0634
- 0378-0635
- 0378-0636
- 43068-101
- 43068-102
- 43068-104
- 43068-106
- 43068-108
- 43068-110
- 43068-112
- 43068-113
- 43068-114
- 43068-115
- 43068-901
- 43068-902
- 43068-903
- 43068-904
- 43068-905
- 43068-906
- 43068-907
- Recorded assays
- 840
- Active assays
- 131
- Confirmatory
- Other
- Screening
- Summary
- Antipsychotic Agents
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Approved for (2)
- Psychotic disorder
- Schizophrenia
In development for (4)
- Bipolar depression Phase 3
- Bipolar disorder Phase 1
- Liver disorder Phase 1
- Post-traumatic stress disorder Phase 2