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Iloperidone crystalline formulation · 1 trial · 1 indication
Blood samples for pharmacokinetic (PK) evaluation were drawn pre-dose and at 3, 6, and 12 hours on Day 1; at 0 and 12 hours on Day 2; and on Days 3, 4, 6, 8, 10, 14, 18, 22, and 26 following administration of iloperidone. PK parameters were calculated from plasma concentration-time data using non-compartmental methods.
Blood samples for pharmacokinetic (PK) evaluation were drawn pre-dose and at 3, 6, and 12 hours on Day 1; at 0 and 12 hours on Day 2; and on Days 3, 4, 6, 8, 10, 14, 18, 22, and 26 following administration of iloperidone. Blood samples were collected after each depot injection. PK parameters were calculated from plasma concentration-time data using non-compartmental methods. Cav was calculated as AUC0-672h/672 h.
| Arm | Type | Description |
|---|---|---|
| Iloperidone 50 mg crystalline formulation - Phase A | EXPERIMENTAL | Participants received a crystalline formulation of iloperidone 50 mg in a depot intramuscular (IM) injection 1 time. Prior to receiving IM iloperidone, participants were gradually titrated up with oral iloperidone for at least 7 days to stable doses of 12 to 24 mg daily. |
| Iloperidone 125 mg crystalline formulation - Phase A | EXPERIMENTAL | Participants received a crystalline formulation of iloperidone 125 mg in a depot IM injection 1 time. Prior to receiving IM iloperidone, participants were gradually titrated up with oral iloperidone for at least 7 days to stable doses of 12 to 24 mg daily. |
| Iloperidone 250 mg crystalline formulation - Phase B | EXPERIMENTAL | Participants received a crystalline formulation of iloperidone 250 mg in a depot IM injection 1 time. Prior to receiving IM iloperidone, participants were gradually titrated up with oral iloperidone for at least 10 to 14 days to stable doses of 12 to 24 mg daily. |
| Iloperidone 250 mg microparticle formulation - Phase B | EXPERIMENTAL | Participants received a microparticle formulation of iloperidone 250 mg in a depot IM injection 1 time. Prior to receiving IM iloperidone, participants were gradually titrated up with oral iloperidone for at least 10 to 14 days to stable doses of 12 to 24 mg daily. |
| Iloperidone 250 mg microparticle formulation - Phase C | EXPERIMENTAL | Participants received a microparticle formulation of iloperidone 250 mg in a depot IM injection 2 times 28 days apart. Prior to receiving IM iloperidone, participants were gradually titrated up with oral iloperidone for at least 10 to 14 days to stable doses of 12 to 24 mg daily. |
| Iloperidone 500 mg microparticle formulation - Phase C | EXPERIMENTAL | Participants received a microparticle formulation of iloperidone 500 mg in a depot IM injection 2 times 28 days apart. Prior to receiving IM iloperidone, participants were gradually titrated up with oral iloperidone for at least 10 to 14 days to stable doses of 12 to 24 mg daily. |
| Iloperidone 625 mg microparticle formulation - Phase C | EXPERIMENTAL | Participants received a microparticle formulation of iloperidone 625 mg in a depot IM injection 2 times 28 days apart. Prior to receiving IM iloperidone, participants were gradually titrated up with oral iloperidone for at least 10 to 14 days to stable doses of 12 to 24 mg daily. |
| Name | Type | Description |
|---|---|---|
| Iloperidone crystalline formulation | DRUG | Iloperidone was formulated as 100 µm crystals for IM depot injection. |
| Iloperidone microparticle formulation | DRUG | Iloperidone was formulated as microparticles for IM depot injection. |
| Oral iloperidone | DRUG | Prior to receiving an intramuscular (IM) injection of iloperidone, patients were gradually titrated up with oral iloperidone to stable doses of 12 to 24 mg daily. In Phase A, oral iloperidone dosing lasted for at least 7 days and, in Phases B and C, for at least 10 to 14 days. |
Inclusion Criteria: * Patients with schizophrenia that have been stable for 3 months. Exclusion Criteria: * Women who can become or are currently pregnant or lactating. * Hypersensitivity to iloperidone or related drugs. Other protocol-defined inclusion/exclusion criteria may apply.
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Iloperidone crystalline formulation is being developed for the treatment of schizophrenia. It is an investigational long-acting injectable depot formulation of iloperidone, studied in adult patients with schizophrenia. The formulation is designed to provide extended drug release, but it has not been approved by the FDA and remains in clinical development.
Iloperidone crystalline formulation targets dopamine D2 receptors (DRD2) and serotonin 5-HT2A receptors (HTR2A). It acts as an antagonist at both receptor types. This dual antagonism is the mechanism thought to underlie its antipsychotic activity in schizophrenia, though the crystalline depot formulation is still under investigation.
Iloperidone crystalline formulation is being developed by Novartis AG, which trades under the ticker NVS. Novartis is responsible for the clinical development of this long-acting injectable depot formulation for schizophrenia.
Iloperidone crystalline formulation is in Phase 1 clinical development. It is an investigational product and has not been approved by the FDA for any indication. The Phase 1 program has been completed, with no active trials currently listed.
Iloperidone crystalline formulation has been studied in one completed Phase 1 trial, NCT01348100, titled "Safety, Tolerability, and Pharmacokinetics of Iloperidone Depot in Schizophrenic Patients." The trial enrolled 81 adults with schizophrenia in the United States. It was randomized and controlled, but not double-blind.