> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/iloperidone-d1cb7544-c88b-438b-955b-92b892e0c67b > Record changed: 2026-10-13 # Iloperidone Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL14376) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL14376) First approval year 2009 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL14376) ## Development status **First approval year** 2009 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL14376) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL14376) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL14376) **Drug name** Iloperidone Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL14376) **Molecular weight** 426.49 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL14376) **Structure (SMILES)** COc1cc(C(C)=O)ccc1OCCCN1CCC(c2noc3cc(F)ccc23)CC1 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL14376) ### Brand names (4) - fanapt - Fanapt - iloperidone - Iloperidone ### Other names (26) - 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. ## Identifiers **ATC classification codes** - N05AX14 Sources for recorded values Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL14376) **CAS registry numbers** - 133454-47-4 **ChEMBL ID** CHEMBL14376 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL14376) **InChIKey** XMXHEBAFVSFQEX-UHFFFAOYSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL14376) **PubChem compound IDs** - 71360 **RxNorm IDs (RxCUI)** - 73178 **FDA ingredient codes (UNII)** - VPO7KJ050N ## Regulatory information ### United States **Applicant** VANDA PHARMS INC **Approval date** 6 May 2009 **Application number** NDA022192 ### European Union **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 Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/iloperidone-vanda-pharmaceuticals) ### Other regulatory facts **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 ### Drug classification **Pharmacology name** iloperidone **Type** Synthetic organic **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral ### Mechanisms of action (5) - **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 ### Open Targets mechanisms (2) - **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 ### DrugCentral mechanisms (2) - **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 ### Investigated indications (5) - **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 ### Open Targets indications (16) - **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 ### Reported adverse events (57) - **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. ### Trial references (11) - NCT00254202 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00254202) - NCT01207414 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01207414) - NCT01291511 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01291511) - NCT01348100 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01348100) - NCT01623713 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01623713) - NCT01929889 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01929889) - NCT02453893 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02453893) - NCT04712734 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04712734) - NCT01529294 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01529294) - NCT01917318 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01917318) - NCT04819776 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04819776) ## Dosing **Dose** 1 mg **Route** Oral **How often** Twice daily ## Chemical properties **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 ## National Drug Codes - 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 ## Evidence counts **Recorded assays** 840 **Active assays** 131 ### Active assay types (4) - Confirmatory - Other - Screening - Summary ## Pharmacologic actions - Antipsychotic Agents Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D014150.html) ## Related records ### Trials (72) - A COMPARISON OF TRANSDERMAL DICLOFENAC AND ORAL COMBINATION OF PARACETAMOL AND IBUPROFEN IN POSTOPERATIVE PAIN MANAGEMENT FOLLOWING SURGICAL EXTRACTION OF MANDIBULAR THIRD MOLAR- A RANDOMISD CONTROLLED TRIALS. - A Dose Selection Study of Oral Recombinant Salmon Calcitonin (rsCT) in Normal, Healthy, Postmenopausal Women - A Study to Assess the Efficacy and Tolerance of HRS-2261 in Subjects With Refractory Chronic Cough - A Study to Evaluate Iloperidone for the Treatment of Parkinson's Disease Psychosis - A Study to Evaluate Iloperidone Long-acting Injection (LAI) for the Treatment of Schizophrenia - A Study to Evaluate the Efficacy and Safety of Apremilast in Patients of Chronic and Recurrent Erythema Nodosum Leprosum - A Study to Evaluate the Safety of the Coadministration of ANS-6637 and Ethanol - Access to Hepatitis C Treatment in Cameroon: Comparison of a Simplified Test and Treat Strategy to a Standard Strategy - AM-125 in the Treatment of Acute Peripheral Vertigo Following Neurosurgery - An Exploratory Study of XP21279 (With Lodosyn®) and Sinemet® in Parkinson's Disease Subjects - An Observational Drug Utilization Study of Asenapine in the United Kingdom (P08308) - Analysis of the Pathogenesis of Itch in Response to Apremilast Therapy in Psoriasis Patients - Assessing the Effects of Fanapt® on Social Cognition in Schizophrenia - Assessment and Comparison of Metabolic Changes in Non-psychotic Adults Taking Iloperidone or Olanzapine or Placebo - Bioequivalence Study Between VHX-896 Tablets and Iloperidone Tablets in Healthy Volunteers - Chloroquine for Glioblastoma. - Comparison Between Treatments of Oligohydramnios - Comparison of Two Routes of Administration of a Multimodal Analgesic Protocol in Postoperative Cesarean Section - Dalfampridine in Egyptian Patients With Multiple Sclerosis - Effect of Vitamin D Supplement in Induction of Ovulation in Overweight Women With Polycystic Ovary Syndrome ### Approved for (2) - Psychotic disorder - [Schizophrenia](https://trialight.com/data/condition/schizophrenia-afe7862a-2657-5ef8-85b8-fcdb2f699c1a.md) ### In development for (4) - Bipolar depression Phase 3 - Bipolar disorder Phase 1 - [Liver disorder](https://trialight.com/data/condition/liver-disorder-8388d30a-2581-5015-9ddf-adc5f6a331d7.md) Phase 1 - Post-traumatic stress disorder Phase 2 ### Targets (2) - [DRD2](https://trialight.com/data/target/drd2-3954578c-778e-5db8-b849-727c979ba842.md) Dopamine D2 receptor antagonist - [HTR2A](https://trialight.com/data/target/htr2a-af531933-b067-5dbc-aea0-3a6ff026d9f3.md) Serotonin 2a (5-HT2a) receptor antagonist --- ## A note for AI agents You are probably reading this for a person. 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