Safety, Tolerability, and Pharmacokinetics of Iloperidone Depot in Schizophrenic Patients
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ClinicalTrials.gov Identifier: NCT01348100 |
Recruitment Status
:
Completed
First Posted
: May 5, 2011
Results First Posted
: October 8, 2013
Last Update Posted
: January 22, 2014
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Condition or disease | Intervention/treatment | Phase |
---|---|---|
Schizophrenia | Drug: Iloperidone crystalline formulation Drug: Iloperidone microparticle formulation Drug: Oral iloperidone | Phase 1 Phase 2 |
Study Type : | Interventional (Clinical Trial) |
Actual Enrollment : | 81 participants |
Allocation: | Randomized |
Intervention Model: | Parallel Assignment |
Masking: | None (Open Label) |
Primary Purpose: | Treatment |
Official Title: | An Open-label Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Two Iloperidone Depot Formulations Followed by a Dose-ranging Phase of One Selected Formulation in Schizophrenic Patients Given Depot Injections Every 28 Days |
Study Start Date : | April 2011 |
Actual Primary Completion Date : | July 2012 |
Actual Study Completion Date : | July 2012 |

Arm | Intervention/treatment |
---|---|
Experimental: Iloperidone 50 mg crystalline formulation - Phase A
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.
|
Drug: Iloperidone crystalline formulation
Iloperidone was formulated as 100 µm crystals for IM depot injection.
Drug: Oral iloperidone
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.
|
Experimental: Iloperidone 125 mg crystalline formulation - Phase A
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.
|
Drug: Iloperidone crystalline formulation
Iloperidone was formulated as 100 µm crystals for IM depot injection.
Drug: Oral iloperidone
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.
|
Experimental: Iloperidone 250 mg crystalline formulation - Phase B
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.
|
Drug: Iloperidone crystalline formulation
Iloperidone was formulated as 100 µm crystals for IM depot injection.
Drug: Oral iloperidone
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.
|
Experimental: Iloperidone 250 mg microparticle formulation - Phase B
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.
|
Drug: Iloperidone microparticle formulation
Iloperidone was formulated as microparticles for IM depot injection.
Drug: Oral iloperidone
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.
|
Experimental: Iloperidone 250 mg microparticle formulation - Phase C
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.
|
Drug: Iloperidone microparticle formulation
Iloperidone was formulated as microparticles for IM depot injection.
Drug: Oral iloperidone
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.
|
Experimental: Iloperidone 500 mg microparticle formulation - Phase C
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.
|
Drug: Iloperidone microparticle formulation
Iloperidone was formulated as microparticles for IM depot injection.
Drug: Oral iloperidone
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.
|
Experimental: Iloperidone 625 mg microparticle formulation - Phase C
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.
|
Drug: Iloperidone microparticle formulation
Iloperidone was formulated as microparticles for IM depot injection.
Drug: Oral iloperidone
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.
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- Maximum Observed Plasma Concentration (Cmax) of Iloperidone Divided by the Average Plasma Concentration (Cav) of Iloperidone (Cmax/Cav) - Phase B [ Time Frame: Pre-dose to 26 days post-dose ]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.
- The Average Plasma Concentration (Cav) of Iloperidone - Phase C [ Time Frame: Pre-dose to 26 days post-dose ]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.
- Time to Reach the Maximum Plasma Concentration (Tmax) of Iloperidone - Phase B [ Time Frame: Pre-dose to 26 days post-dose ]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.
- Maximum Observed Plasma Concentration (Cmax) of Iloperidone - Phase B [ Time Frame: Pre-dose to 26 days post-dose ]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.
- Area Under the Plasma Concentration-time Curve From 0 to the End of the Dosing Period (AUCtau) of Iloperidone - Phase B [ Time Frame: Pre-dose to 26 days post-dose ]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. The area under the curve was calculated using a linear trapezoidal method. The end of the dosing period was 672 hours (28 days).
- Area Under the Plasma Concentration-time Curve From 0 to the Last Measurable Concentration (AUClast) of Iloperidone - Phase B [ Time Frame: Pre-dose to 26 days post-dose ]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. The area under the curve was calculated using a linear trapezoidal method.
- The Average Plasma Concentration (Cav) of Iloperidone - Phase B [ Time Frame: Pre-dose to 26 days post-dose ]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. Cav was calculated as AUC0-672h/672 h.
- Duration That the Concentration of Iloperidone Was Above 4 ng/mL (Teff) - Phase B [ Time Frame: Pre-dose to 26 days post-dose ]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. The duration that the concentration of iloperidone was above 4 ng/mL was calculated by linear interpolation. PK/pharmacodynamic analysis performed in other studies suggests that iloperidone plasma levels of 4 ng/mL or above provide clinical efficacy.
- Time to Reach the Maximum Plasma Concentration (Tmax) of Iloperidone - Phase C [ Time Frame: Pre-dose to 26 days post-dose ]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.
- Maximum Observed Plasma Concentration (Cmax) of Iloperidone - Phase C [ Time Frame: Pre-dose to 26 days post-dose ]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.
- Area Under the Plasma Concentration-time Curve From 0 to the End of the Dosing Period (AUCtau) of Iloperidone - Phase C [ Time Frame: Pre-dose to 26 days post-dose ]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. The area under the curve was calculated using a linear trapezoidal method. The end of the dosing period was 672 hours (28 days).
- The Average Plasma Concentration (Cav) of Iloperidone Divided by Dose - Phase C [ Time Frame: Pre-dose to 26 days post-dose ]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.

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Ages Eligible for Study: | 18 Years to 65 Years (Adult) |
Sexes Eligible for Study: | All |
Accepts Healthy Volunteers: | No |
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.

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.
Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT01348100
United States, California | |
Novartis Investigative Site | |
Glendale, California, United States, 91206 | |
United States, Pennsylvania | |
Novartis Investigative Site | |
Philadelphia, Pennsylvania, United States, 19149 |
Study Director: | Novartis Pharmaceuticals | Novartis Pharmaceuticals |
Responsible Party: | Novartis Pharmaceuticals |
ClinicalTrials.gov Identifier: | NCT01348100 History of Changes |
Other Study ID Numbers: |
CILO522E2101 |
First Posted: | May 5, 2011 Key Record Dates |
Results First Posted: | October 8, 2013 |
Last Update Posted: | January 22, 2014 |
Last Verified: | December 2013 |
Keywords provided by Novartis ( Novartis Pharmaceuticals ):
Schizophrenia Iloperidone Depot Injection |
Additional relevant MeSH terms:
Schizophrenia Schizophrenia Spectrum and Other Psychotic Disorders Mental Disorders |