Approval Probability
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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.
Iloperidone crystalline formulation is an investigational small molecule being developed for the treatment of schizophrenia. It is a crystalline formulation of iloperidone, an atypical antipsychotic, designed for use as a long-acting depot injection. The drug is currently in Phase 1 clinical development.
Iloperidone crystalline formulation is being developed by Novartis AG, a multinational pharmaceutical company traded on the New York Stock Exchange under the ticker symbol NVS. The company is conducting clinical trials to evaluate the safety, tolerability, and pharmacokinetics of this investigational drug in patients with schizophrenia.
Iloperidone crystalline formulation is in Phase 1 clinical development. A Phase 1 study has been completed, which evaluated the safety, tolerability, and pharmacokinetics of the drug in schizophrenic patients. The drug is investigational and has not been approved by regulatory authorities.
Iloperidone crystalline formulation has one completed clinical trial, identified as NCT01348100, titled "Safety, Tolerability, and Pharmacokinetics of Iloperidone Depot in Schizophrenic Patients." This Phase 1 study enrolled 81 participants in the United States and was a controlled, randomized trial.
Iloperidone crystalline formulation is a specific formulation of iloperidone, an atypical antipsychotic. While the active ingredient is the same, the crystalline formulation is designed as a depot injection for extended release, differing from immediate-release oral formulations. This investigational product is being studied for schizophrenia.