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.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
37
Lumateperone Long-Acting Injectable
Clinical Site
Long Beach, California, United States
Clinical Site
Marlton, New Jersey, United States
Pharmacokinetics: Maximum observed plasma concentration (Cmax) of lumateperone and metabolites
Time frame: predose and at multiple timepoints up to 7 weeks postdose
Pharmacokinetics: Time of maximum observed plasma concentration (Tmax) of lumateperone and metabolites
Time frame: 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
Time frame: 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
Time frame: predose and at multiple timepoints up to 7 weeks postdose
Pharmacokinetics: Terminal elimination half-life (T1/2) of lumateperone and metabolites
Time frame: 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
Time frame: 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
Time frame: 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
Time frame: predose and at multiple timepoints up to 7 weeks postdose
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Pharmacokinetics: Maximum observed plasma concentration (Cmax,SR) of lumateperone and metabolites during sustained-release phase
Time frame: 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
Time frame: 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
Time frame: predose and at multiple timepoints up to 7 weeks postdose
Percentage of participants with treatment-emergent AEs
Time frame: up to 7 weeks postdose
Change from baseline in Systolic and Diastolic Blood Pressure
Time frame: up to 7 weeks postdose
Change from baseline in hemoglobin
Time frame: up to 7 weeks postdose
Change from baseline in platelet count
Time frame: up to 7 weeks postdose
Change from baseline in white blood cell count
Time frame: up to 7 weeks postdose
Change from baseline in aspartate aminotransferase
Time frame: up to 7 weeks postdose
Change from baseline in alanine aminotransferase
Time frame: up to 7 weeks postdose
Change from baseline in glucose
Time frame: up to 7 weeks postdose
Change from baseline in creatine kinase
Time frame: up to 7 weeks postdose
Change from baseline in ECG QT Interval
Time frame: up to 7 weeks postdose
Change from baseline in Abnormal Involuntary Movement Scale
AIMS is a measure of facial and oral movements, extremity movements and trunk movements. Items are rated on a scale from none (0) to severe (4).
Time frame: up to 7 weeks postdose