Safety, Tolerability, and Pharmacokinetics of Iloperidone Depot in Schizophrenic Patients

Novartis

Status and phase: Completed; Phase 2; Phase 1

Conditions: Schizophrenia

Treatments: Drug: Iloperidone crystalline formulation; Drug: Iloperidone microparticle formulation; Drug: Oral iloperidone

Study type: Interventional

Funder types: Industry

Identifiers

NCT01348100

CILO522E2101

Details and patient eligibility

About

This study is designed as a 3-part trial to evaluate the safety of a novel depot formulation of iloperidone, compare 2 depot dosage forms, and perform dose ranging of 1 chosen form in support of a monthly depot dosing regimen. In Phase A, the study is designed to evaluate the safety of a crystalline iloperidone depot formulation. In Phase B, the pharmacokinetic and safety profile of 2 depot clinical dosage forms will be compared, and 1 form will be selected for assessment in Phase C. Phase C of this study is designed to define the dose-exposure relationship of the selected form and to provide information that will permit a comparison of the risk-benefit ratio of several doses of the study drug to enable optimal dose selection for later studies.

Enrollment: 81 patients

Sex: All

Ages: 18 to 65 years old

Volunteers: No Healthy Volunteers

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.

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Parallel Assignment

Masking: None (Open label)

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81 participants in 7 patient groups

Iloperidone 50 mg crystalline formulation - Phase A

Experimental group

Description:

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.

Treatment:

Drug: Oral iloperidone

Drug: Iloperidone crystalline formulation

Iloperidone 125 mg crystalline formulation - Phase A

Experimental group

Description:

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.

Treatment:

Drug: Oral iloperidone

Drug: Iloperidone crystalline formulation

Iloperidone 250 mg crystalline formulation - Phase B

Experimental group

Description:

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.

Treatment:

Drug: Oral iloperidone

Drug: Iloperidone crystalline formulation

Iloperidone 250 mg microparticle formulation - Phase B

Experimental group

Description:

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.

Treatment:

Drug: Oral iloperidone

Drug: Iloperidone microparticle formulation

Iloperidone 250 mg microparticle formulation - Phase C

Experimental group

Description:

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.

Treatment:

Drug: Oral iloperidone

Drug: Iloperidone microparticle formulation

Iloperidone 500 mg microparticle formulation - Phase C

Experimental group

Description:

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.

Treatment:

Drug: Oral iloperidone

Drug: Iloperidone microparticle formulation

Iloperidone 625 mg microparticle formulation - Phase C

Experimental group

Description:

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.

Treatment:

Drug: Oral iloperidone

Drug: Iloperidone microparticle formulation