Pharmacokinetics, Safety, and Tolerability of Lumateperone Long-Acting Injectable in Patients With Schizophrenia

NCT04709224 | Completed Phase 1 FDA Drug

• 1 other identifier: ITI-007-025
• Study Type: interventional
• Target: 37
• Locations: 1 country
• Sites: 2

Brief Summary

This is an open-label study to determine the pharmacokinetics, safety and tolerability of single ascending doses of lumateperone long-acting injectable formulation in patients with schizophrenia. Patients will be enrolled in one of up to four cohorts. All patients will receive oral lumateperone for 5 days, followed by a 5-day washout of oral lumateperone, then followed by a single dose of lumateperone LAI.

Conditions

Schizophrenia

Outcome Measures

Primary Outcomes (11)

• Pharmacokinetics: Maximum observed plasma concentration (Cmax) of lumateperone and metabolites

  predose and at multiple timepoints up to 7 weeks postdose

• Pharmacokinetics: Time of maximum observed plasma concentration (Tmax) of lumateperone and metabolites

  predose and at multiple timepoints up to 7 weeks postdose

• Pharmacokinetics: Area under the plasma concentration-time curve from time zero to the last measurable concentration (AUC0-t) of lumateperone and metabolites

  predose and at multiple timepoints up to 7 weeks postdose

• Pharmacokinetics: Area under the plasma concentration-time curve from time zero extrapolated to infinity (AUC0-inf) of lumateperone and metabolites

  predose and at multiple timepoints up to 7 weeks postdose

• Pharmacokinetics: Terminal elimination half-life (T1/2) of lumateperone and metabolites

  predose and at multiple timepoints up to 7 weeks postdose

• Pharmacokinetics: Maximum observed plasma concentration (Cmax,BR) of lumateperone and metabolites during burst-release phase

  predose and at multiple timepoints up to 7 weeks postdose

• Pharmacokinetics: Time of maximum observed plasma concentration (Tmax,BR) of lumateperone and metabolites during burst-release phase

  predose and at multiple timepoints up to 7 weeks postdose

• Pharmacokinetics: Area under the plasma concentration-time curve (AUC0-t,BR) of lumateperone and metabolites during burst-release phase

  predose and at multiple timepoints up to 7 weeks postdose

• Pharmacokinetics: Maximum observed plasma concentration (Cmax,SR) of lumateperone and metabolites during sustained-release phase

  predose and at multiple timepoints up to 7 weeks postdose

• Pharmacokinetics: Time of maximum observed plasma concentration (Tmax,SR) of lumateperone and metabolites during sustained-release phase

  predose and at multiple timepoints up to 7 weeks postdose

• Pharmacokinetics: Area under the plasma concentration-time curve (AUC0-t,SR) of lumateperone and metabolites during sustained-release phase

  predose and at multiple timepoints up to 7 weeks postdose

Secondary Outcomes (11)

• Percentage of participants with treatment-emergent AEs

  up to 7 weeks postdose

• Change from baseline in Systolic and Diastolic Blood Pressure

  up to 7 weeks postdose

• Change from baseline in hemoglobin

  up to 7 weeks postdose

• Change from baseline in platelet count

  up to 7 weeks postdose

• Change from baseline in white blood cell count

  up to 7 weeks postdose

Study Arms (4)

Cohort 1: LAI Lumateperone 50 mg SC in the abdomen

EXPERIMENTAL

Drug: Lumateperone Long-Acting Injectable

Cohort 2: LAI Lumateperone 100 mg SC in the abdomen

EXPERIMENTAL

Drug: Lumateperone Long-Acting Injectable

Cohort 3: LAI Lumateperone 200 mg SC in the abdomen

EXPERIMENTAL

Drug: Lumateperone Long-Acting Injectable

Cohort 4: LAI Lumateperone 100 or 200 mg SC in the outer area of the upper arm

EXPERIMENTAL

Drug: Lumateperone Long-Acting Injectable

Interventions

Lumateperone Long-Acting Injectable DRUG

Lumateperone Long-Acting Injectable

Cohort 1: LAI Lumateperone 50 mg SC in the abdomen; Cohort 2: LAI Lumateperone 100 mg SC in the abdomen; Cohort 3: LAI Lumateperone 200 mg SC in the abdomen; Cohort 4: LAI Lumateperone 100 or 200 mg SC in the outer area of the upper arm

Eligibility Criteria

• Age: 18 Years - 50 Years
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64)

You may qualify if:

• Male or female patients aged 18 to 50 years, inclusive
• Clinical diagnosis of schizophrenia according to Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition (DSM-5)
• Clinically stable and free from acute exacerbation of psychosis for at least 3 months prior to Screening per Investigator assessment
• On a stable dose of antipsychotic medication, including lumateperone, for at least 3 months prior to the Screening Visit
• Clinical Global Impression - Severity (CGI-S) score ≤ 3

You may not qualify if:

• 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
• History of psychiatric condition other than schizophrenia that, in the Investigator's opinion, may be detrimental to participation in the study
• Any suicidal ideation within the 6 months prior to Screening, any suicidal behavior within 2 years prior to Screening 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
• Surgical or medical condition (active or chronic) that in the Investigator's opinion may interfere with drug absorption, distribution, metabolism, or excretion of the study drug or any other condition that may place the patient at risk; history of gastric bypass or sleeve gastrectomy; history of severe dystonic reaction on antipsychotics such as laryngeal spasm

Sponsors & Collaborators

• Intra-Cellular Therapies, Inc.: lead

Study Sites (2)

Clinical Site

Long Beach, California, 90806, United States

Location

Clinical Site

Marlton, New Jersey, 08053, United States

Location

MeSH Terms

Conditions

Schizophrenia

Condition Hierarchy (Ancestors)

Schizophrenia Spectrum and Other Psychotic Disorders; Mental Disorders

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: December 29, 2020
• First Posted: January 14, 2021
• Study Start: December 30, 2020
• Primary Completion: May 23, 2022
• Study Completion: May 23, 2022
• Last Updated: December 5, 2022

Record last verified: 2022-12

Data Sharing

• IPD Sharing: Will not share

Locations

US (2)