Repositioning Candidate Details
| Candidate ID: | R0434 |
| Source ID: | DB04946 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Iloperidone |
| Synonyms: | |
| Molecular Formula: | C24H27FN2O4 |
| SMILES: | COC1=C(OCCCN2CCC(CC2)C2=NOC3=C2C=CC(F)=C3)C=CC(=C1)C(C)=O |
| Structure: |
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| DrugBank Description: | Iloperidone is an atypical antipsychotic for the treatment of schizophrenia symptoms. Hoechst Marion Roussel Inc. researched the drug until May 1996. In June 1997 they gave the research rights to Titan Pharmaceuticals, who gave the worldwide development, manufacturing, and marketing rights to Novartis in August 1998. On June 9, 2004, Titan Pharmaceuticals gave the Phase III development rights to Vanda Pharmaceuticals. FDA approved on May 9, 2009. |
| CAS Number: | 133454-47-4 |
| Molecular Weight: | 426.4806 |
| DrugBank Indication: | Treatment of acute schizophrenia. |
| DrugBank Pharmacology: | Iloperidone shows high affinity and maximal receptor occupancy for dopamine D2 receptors in the caudate nucleus and putamen of the brains of schizophrenic patients. The improvement in cognition is attributed to iloperidone's high affinity for α adrenergic receptors. Iloperidone also binds with high affinity to serotonin 5-HT2a and dopamine 3 receptors. Iloperidone binds with moderate affinity to dopamine D4, serotonin 5-HT6 and 5-HT7, and norepinephrine NEα1 receptors. Furthermore, iloperidone binds with weak affinity to serotonin 5-HT1A, dopamine D1, and histamine H1 receptors. |
| DrugBank MoA: | Iloperidone is a dopamine D2 and 5-HT2A receptor antagonist and acts as a neuroleptic agent. |
| Targets: | 5-hydroxytryptamine receptor 2A; Dopamine D2 receptor; Dopamine D1 receptor; Dopamine D3 receptor; Dopamine D4 receptor; 5-hydroxytryptamine receptor 1A; 5-hydroxytryptamine receptor 6; 5-hydroxytryptamine receptor 7; Alpha-1A adrenergic receptor; Histamine H1 receptor; Alpha-2C adrenergic receptor |
| Inclusion Criteria: |
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