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.

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