Clinical trial NCT04709224: Pharmacokinetics, Safety, and Tolerability of Lumateperone Long-Acting Injectable in Patients With Schizophrenia
Official title: An Open-label Study to Determine the Pharmacokinetics, Safety and Tolerability of Single Ascending Doses of a Subcutaneous Injection of Lumateperone Long-Acting Injectable (LAI) Formulation in Patients With Schizophrenia
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Schizophrenia
Lead sponsor: Intra-Cellular Therapies, Inc.
Sponsor class: INDUSTRY
First posted: 2021-01-14
Enrollment: 37
Sex: ALL
Minimum age (years): 18
Maximum age (years): 50
Standard ages: ADULT
Accepts healthy volunteers: no
Allocation: NON_RANDOMIZED
Intervention model: SEQUENTIAL
Primary purpose: TREATMENT

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.


Eligibility criteria: Key Inclusion Criteria:

* 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

Key Exclusion Criteria:

* 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

Primary outcomes:
measure: Pharmacokinetics: Maximum observed plasma concentration (Cmax) of lumateperone and metabolites
timeFrame: predose and at multiple timepoints up to 7 weeks postdose
measure: Pharmacokinetics: Time of maximum observed plasma concentration (Tmax) of lumateperone and metabolites
timeFrame: predose and at multiple timepoints up to 7 weeks postdose
measure: Pharmacokinetics: Area under the plasma concentration-time curve from time zero to the last measurable concentration (AUC0-t) of lumateperone and metabolites
timeFrame: predose and at multiple timepoints up to 7 weeks postdose
measure: Pharmacokinetics: Area under the plasma concentration-time curve from time zero extrapolated to infinity (AUC0-inf) of lumateperone and metabolites
timeFrame: predose and at multiple timepoints up to 7 weeks postdose
measure: Pharmacokinetics: Terminal elimination half-life (T1/2) of lumateperone and metabolites
timeFrame: predose and at multiple timepoints up to 7 weeks postdose
measure: Pharmacokinetics: Maximum observed plasma concentration (Cmax,BR) of lumateperone and metabolites during burst-release phase
timeFrame: predose and at multiple timepoints up to 7 weeks postdose
measure: Pharmacokinetics: Time of maximum observed plasma concentration (Tmax,BR) of lumateperone and metabolites during burst-release phase
timeFrame: predose and at multiple timepoints up to 7 weeks postdose
measure: Pharmacokinetics: Area under the plasma concentration-time curve (AUC0-t,BR) of lumateperone and metabolites during burst-release phase
timeFrame: predose and at multiple timepoints up to 7 weeks postdose
measure: Pharmacokinetics: Maximum observed plasma concentration (Cmax,SR) of lumateperone and metabolites during sustained-release phase
timeFrame: predose and at multiple timepoints up to 7 weeks postdose
measure: Pharmacokinetics: Time of maximum observed plasma concentration (Tmax,SR) of lumateperone and metabolites during sustained-release phase
timeFrame: predose and at multiple timepoints up to 7 weeks postdose
measure: Pharmacokinetics: Area under the plasma concentration-time curve (AUC0-t,SR) of lumateperone and metabolites during sustained-release phase
timeFrame: predose and at multiple timepoints up to 7 weeks postdose
Secondary outcomes:
measure: Percentage of participants with treatment-emergent AEs
timeFrame: up to 7 weeks postdose
measure: Change from baseline in Systolic and Diastolic Blood Pressure
timeFrame: up to 7 weeks postdose
measure: Change from baseline in hemoglobin
timeFrame: up to 7 weeks postdose
measure: Change from baseline in platelet count
timeFrame: up to 7 weeks postdose
measure: Change from baseline in white blood cell count
timeFrame: up to 7 weeks postdose
measure: Change from baseline in aspartate aminotransferase
timeFrame: up to 7 weeks postdose
measure: Change from baseline in alanine aminotransferase
timeFrame: up to 7 weeks postdose
measure: Change from baseline in glucose
timeFrame: up to 7 weeks postdose
measure: Change from baseline in creatine kinase
timeFrame: up to 7 weeks postdose
measure: Change from baseline in ECG QT Interval
timeFrame: up to 7 weeks postdose
measure: Change from baseline in Abnormal Involuntary Movement Scale
timeFrame: up to 7 weeks postdose
Other outcomes:
Locations:
city: Long Beach
country: United States
facility: Clinical Site
state: California
city: Marlton
country: United States
facility: Clinical Site
state: New Jersey
Study officials:
References: