Safety, Tolerability, and Pharmacokinetics of Lumateperone Long-Acting Injectable Formulations in Patients With Schizophrenia or Schizoaffective Disorder

Intra-Cellular Therapies

Status and phase: Enrolling; Phase 1

Conditions: Schizophrenia or Schizoaffective

Treatments: Drug: Lumateperone Capsule; Drug: Lumateperone LAI

Study type: Interventional

Funder types: Industry

Identifiers

NCT06627413

ITI-007-037

Details and patient eligibility

About

Study ITI-007-037 is a Phase 1b, open-label study to evaluate the safety, tolerability, and PK of lumateperone long-acting injectable (LAI) formulations after a single intramuscular injection in patients with stale schizophrenia or schizoaffective disorder.

Enrollment: 72 estimated patients

Sex: All

Ages: 18 to 55 years old

Volunteers: No Healthy Volunteers

Inclusion and exclusion criteria

Main Inclusion Criteria:

• Male or female patients between 18 and 55 years of age, inclusive;
• Clinical diagnosis of schizophrenia or schizoaffective disorder according to Diagnostic and Statistical Manual of Mental Disorders (DSM-5);
• Clinically stable and free from acute exacerbation of psychosis for at least 3 months prior to Screening;
• Clinical Global Impression - Severity (CGI-S) score ≤ 3 at Screening and prior to dosing on Day 1;
• Body mass index (BMI) between 18.0 and 38.0 kg/m2, inclusive at Screening, and a minimum body weight of 50 kg at Screening.

Main Exclusion Criteria:

• History of psychiatric condition other than schizophrenia that, in the Investigator's opinion, may be detrimental to participation in the study;
• Any suicidal ideation or wish to be dead within the past 6 months of Screening, any suicide attempt within the past 2 years prior to Screening, or any current concern for the patient's safety based on the Columbia-Suicide Severity Rating Scale (C-SSRS) (excluding self-injurious, non-suicidal behavior), and/or Investigator assessment that the patient is a safety risk to him/herself or others;
• Clinically significant abnormality within 2 years of Screening that in the Investigator's opinion may place the patient at risk or interfere with study outcome variables;
• Has a QT interval corrected for heart rate using Fridericia formula > 450 msec in males or > 470 msec in females, or evidence of clinically significant bundle branch blocks on ECG at Screening.

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Parallel Assignment

Masking: None (Open label)

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72 participants in 9 patient groups

Cohort 1

Experimental group

Description:

Lumateperone 42 mg once daily for 5 days following by a single IM dose of lumateperone 100 mg LAI formulation X500-E2 after a 5-day washout

Treatment:

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone Capsule

Cohort 2

Experimental group

Description:

Lumateperone 42 mg once daily for 5 days following by a single IM dose of lumateperone 100 mg LAI formulation X500-E3 after a 5-day washout

Treatment:

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone Capsule

Cohort 3

Experimental group

Description:

Lumateperone 42 mg once daily for 5 days following by a single IM dose of lumateperone 100 mg LAI formulation X500-X2 after a 5-day washout

Treatment:

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone Capsule

Cohort 4

Experimental group

Description:

Lumateperone 42 mg once daily for 5 days following by a single IM dose of lumateperone 100 mg LAI formulation X500-X5 after a 5-day washout

Treatment:

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone Capsule

Cohort 5

Experimental group

Description:

Lumateperone 42 mg once daily for 5 days following by a single IM dose (\> 100 mg) of lumateperone LAI formulation (chosen from Part A) after a 5-day washout

Treatment:

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone Capsule

Cohort 6

Experimental group

Description:

Lumateperone 42 mg once daily for 5 days following by a single IM dose (\> 100 mg) of lumateperone LAI formulation (chosen from Part A) after a 5-day washout

Treatment:

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone Capsule

Cohort 7

Experimental group

Description:

Lumateperone 42 mg once daily for 5 days following by a single IM dose (\> 100 mg) of lumateperone LAI formulation (chosen from Part A) after a 5-day washout

Treatment:

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone Capsule

Cohort 8

Experimental group

Description:

Lumateperone 42 mg once daily for 5 days following by a single IM dose (\> dose in Part B) of lumateperone LAI formulation (chosen from Part B) after a 5-day washout

Treatment:

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone Capsule

Cohort 9

Experimental group

Description:

Lumateperone 42 mg once daily for 5 days following by a single IM dose (\> dose in Part B) of lumateperone LAI formulation (chosen from Part B) after a 5-day washout

Treatment:

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone LAI

Drug: Lumateperone Capsule