The goal of this clinical trial is to learn if BLKR201 is safe in healthy adults. Researchers will also learn how the body absorbs and processes BLKR201 and how food may affect it. The main questions this study aims to answer are: * Is BLKR201 safe and well tolerated when taken as a single dose or for several days in a row? * How does BLKR201 move through and leave the body? * Does taking BLKR201 with food change how the body absorbs it? Researchers will compare BLKR201 to a placebo (a look-alike tablet that contains no drug) in most parts of the study to see how the drug affects participants. Participants will: * Take BLKR201 or a placebo by mouth * Stay at a clinical research unit for several days during dosing * Give blood and urine samples * Have heart tests, vital signs, and lab tests * Report any side effects In one part of the study, a small group of participants will receive BLKR201 only (no placebo). These participants will also have a sample of spinal fluid collected to measure how much BLKR201 reaches the fluid around the brain and spinal cord.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
OTHER
Masking
QUADRUPLE
Enrollment
128
BLKR201 is administered orally as a single ascending dose in the SAD stage, under fasted or fed conditions.
BLKR201 is administered orally once daily (QD) or twice daily (BID), under fasted or fed conditions, for 7 consecutive days in the MAD stage.
BLKR201 is administered orally once daily (QD) or twice daily (BID), under fasted or fed conditions, for 10 consecutive days in the CSF cohort. Dosing frequency may be adjusted based on emerging pharmacokinetic and safety data.
A matching placebo tablet administered orally, corresponding to the dose level and dosing condition of BLKR201 in each assigned cohort.
Celerion
Lincoln, Nebraska, United States
RECRUITINGNumber of Participants with Treatment-Emergent Adverse Events (TEAEs)
Treatment-emergent adverse events are defined as adverse events that begin or worsen after administration of BLKR201 or placebo. Events will be summarized by frequency and severity.
Time frame: Baseline through approximately 7 days after final dose
Change From Baseline in Clinical Laboratory Parameters
Clinical laboratory parameters include hematology, clinical chemistry, coagulation, lipid panel, and urinalysis. Change from baseline values will be summarized at scheduled post-dose assessments.
Time frame: Baseline through approximately 7 days after final dose
Change From Baseline in Systolic Blood Pressure
Systolic blood pressure will be measured in millimeters of mercury (mmHg). Change from baseline will be summarized at scheduled post-dose assessments.
Time frame: Baseline through approximately 7 days after final dose
Change From Baseline in Diastolic Blood Pressure
Diastolic blood pressure will be measured in millimeters of mercury (mmHg). Change from baseline will be summarized at scheduled post-dose assessments.
Time frame: Baseline through approximately 7 days after final dose
Change From Baseline in Pulse Rate
Pulse rate will be measured in beats per minute (bpm). Change from baseline will be summarized at scheduled post-dose assessments.
Time frame: Baseline through approximately 7 days after final dose
Change From Baseline in Respiratory Rate
Respiratory rate will be measured in breaths per minute. Change from baseline will be summarized at scheduled post-dose assessments.
Time frame: Baseline through approximately 7 days after final dose
Change From Baseline in Body Temperature
Body temperature will be measured in degrees Fahrenheit (°F). Change from baseline will be summarized at scheduled post-dose assessments.
Time frame: Baseline through approximately 7 days after final dose
Change From Baseline in 12-Lead Electrocardiogram (ECG) Parameters
ECG parameters include QT interval corrected using Fridericia's formula (QTcF), PR interval, QRS duration, and heart rate. Change from baseline values will be summarized at scheduled post-dose assessments.
Time frame: Baseline through approximately 7 days after final dose
Maximum Observed Plasma Concentration (Cmax) of BLKR201 After Single Oral Dose
Cmax is the highest measured plasma concentration of BLKR201 following a single oral dose.
Time frame: From predose through approximately 7 days after final dose
Area Under the Plasma Concentration-Time Curve (AUC) of BLKR201 After Single Oral Dose
Area under the plasma concentration-time curve (AUClast and AUCinf) will be calculated using non-compartmental analysis to describe overall drug exposure.
Time frame: From predose through approximately 7 days after final dose
Maximum Observed Plasma Concentration (Cmax) After Multiple Doses
Cmax at steady state will be calculated after repeated dosing.
Time frame: From predose through approximately 7 days after final dose
Area Under the Plasma Concentration-Time Curve Over the Dosing Interval (AUCtau) After Multiple Doses
AUCtau will be calculated to describe total drug exposure during a dosing interval after repeated dosing.
Time frame: From predose through approximately 7 days after final dose
BLKR201 Concentration in Cerebrospinal Fluid (CSF)
BLKR201 concentrations will be measured in cerebrospinal fluid to assess central nervous system exposure.
Time frame: Day 10 post-dose in the CSF cohort (single CSF sampling time point per participant)
Amount of BLKR201 Excreted in Urine
The amount of BLKR201 excreted in urine will be calculated over defined collection intervals.
Time frame: From predose through 48 hours post-dose (in certain SAD cohorts only)
Ratio of Maximum Observed Plasma Concentration (Cmax) of BLKR201 Under Fed Versus Fasted Conditions
The ratio of Cmax under fed and fasted conditions will be calculated to evaluate the effect of a high-fat meal on BLKR201 exposure.
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Time frame: From predose through 48 hours post-dose (in certain SAD cohorts only)
Ratio of Area Under the Plasma Concentration Versus Time Curve (AUC) of BLKR201 Under Fed Versus Fasted Conditions
The ratio of AUC under fed and fasted conditions will be calculated to evaluate the effect of a high-fat meal on BLKR201 exposure.
Time frame: From predose through 48 hours post-dose (in certain SAD cohorts only)