This is a Phase I, open-label, two-part in healthy adult males. There will be up to 12 subjects with 6 subjects in each part of the study. Subjects from Part A are eligible to participate in Part B. For Part A, each of the 6 subjects will complete two periods of the study with washout period of 7 days between. Each subject during participation in the study will receive a dose of PXS 5382A orally in a fed state and a fasted state. For Part B, repeated oral BID administration of PXS-5382A will be performed in the Fed state and dose will be dependent on analysis of Part A. In both part A and B PK, PD and safety assessments will be collected.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
18
Orally once daily or twice daily
CMAX
Adelaide, Australia
Cmax after oral administration of PXS-5382A
Maximum plasma concentration
Time frame: 6 days
Tmax after oral administration of PXS-5382A
Time of the observed maximum plasma concentration
Time frame: 6 days
AUC0-inf of PXS-5382A
Area under the plasma concentration-time curve (AUC) from time zero extrapolated to infinity
Time frame: 6 days
t1/2 of PXS-5382A
Terminal plasma elimination half-life
Time frame: 6 days
Maximum percentage inhibition plasma LOXL2 of PXS-5382A
Maximum measured plasma LOXL2 target engagement following PXS-5382A administration
Time frame: 6 days
Incidence and severity of Adverse Events
A treatment-emergent adverse events (TEAE) will be summarized by treatment and overall, and summarized for each treatment by severity and relationship to study drug. All TEAEs leading to withdrawal, or SAEs, will be summarized.
Time frame: 6 days
Number of subjects with clinical laboratory test abnormalities
The clinical laboratory will include hematology (hematocrit, hemoglobin, mean cell hemoglobin, mean cell hemoglobin concentration, mean cell volume, platelet count, red blood cell count, white blood cell count), clinical chemistry (alanine aminotransferase, albumin, alkaline phosphatase, aspartate aminotransferase, blood urea nitrogen, calcium, chloride, cholesterol, creatinine, creatine phosphokinase, direct bilirubin, estimated glomerular filtration rate, gamma glutamyl transferase, glucose. inorganic phosphate, iron, lactate dehydrogenase, phosphorus, potassium, sodium, total bilirubin, total CO2, total protein, triglyceride, urea, uric acid), and urinalysis (bilirubin, blood, color and appearance, glucose, ketones, leukocyte esterase, nitrite, pH, protein, specific gravity, urobilinogen, microscopic examination, electrolytes). Abnormality will be determined by the investigator.
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Time frame: 6 days
Number of subjects with vital signs abnormalities
The vital sign will include blood pressure (mmHg), pulse rate (bpm), respiratory rate (breaths/min), and body temperature (degree Celsius). Abnormality will be determined by the investigator.
Time frame: 6 days