A single ascending oral dose(s) study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of YCT-529 in healthy male subjects.
This is a Phase 1a, double-blind, placebo controlled, first in human study to evaluate the safety, tolerability, PK, and PD of YCT-529 in 2 cohorts of 8 subjects. Cohorts 1 and 2 will be dosed in the fasted state in Periods 1 and 2. Each cohort will receive two doses of study drug separated by a washout period. One cohort will then return for a third dose of study drug under fed conditions in Period 3 to study the effect of food on YCT-529.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
OTHER
Masking
QUADRUPLE
Enrollment
16
Single oral dose (planned doses of 10, 30, 90 and 200 mg; dose levels will not exceed 250 mg
YCT-529 Placebo
Quotient Sciences
Nottingham, East Midlands, United Kingdom
The incidence and nature of any adverse events, dose-limiting adverse events and serious adverse adverse events.
Assessment of the number and type of adverse events, dose-limiting adverse events and serious adverse events following dosing.
Time frame: Baseline to 43 days for subjects participating in Cohorts 1 and 2 participating in the 2 periods; Baseline to 10 weeks for Cohorts 1 and 2 that also complete the fed portion of the study; and Baseline to 16 weeks if waiting for other cohorts to finish
Vital signs assessment (heart rate)
Changes from pre-dose values (beats per minute)
Time frame: Baseline to Day 15
Vital signs assessment (blood pressure)
Changes from pre-dose values (mm hg)
Time frame: Baseline to Day 15
Vital signs assessment (oral temperature)
Changes from pre-dose values (temperature in celsius degrees)
Time frame: Baseline to Day 15
12-lead ECG assessment (heart rate)
Changes from pre-dose values (beats per minute)
Time frame: Baseline to Day 15
12-lead ECG assessment (QT interval)
Changes from pre-dose values for QT internal length (msec)
Time frame: Baseline to Day 15
12-lead ECG assessment (QTcF Interval)
Changes from pre-dose values for QTcF interval length (msec)
Time frame: Baseline to Day 15
12-lead ECG assessment (PR Interval)
Changes from pre-dose values for PR interval length (msec)
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Time frame: Baseline to Day 15
12-lead ECG assessment (QRS Duration)
Changes from pre-dose values for QRS duration (msec)
Time frame: Baseline to Day 15
Clinical laboratory assessments (hematology blood sample tests)
Changes from pre-dose values (Tests: Hemoglobin, Hematocrit, packed cell volume, Red blood cell, erythrocyte count, mean corpuscular volume, mean corpuscular hemoglobin, Mean corpuscular hemoglobin concentration, Platelet count, White blood cell, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils
Time frame: Baseline to Day 15
Clinical laboratory assessments (coagulation blood sample tests)
Changes from pre-dose values (Tests: Prothrombin time, Activated partial thromboplastin time (APTT), Fibrinogen)
Time frame: Baseline to Day 15
Clinical laboratory assessments (clinical chemistry blood sample tests)
Changes from pre-dose values (Tests: Sodium, Potassium, Chloride, Bicarbonate, Urea, Creatinine, Bilirubin (total), Bilirubin (direct; only if total is elevated), Alkaline phosphatase, Aspartate aminotransferase (AST), Alanine aminotransferase (ALT), Lactate dehydrogenase (LDH), Creatine kinase (CK), Gamma glutamyl transferase (GGT), Protein (Total), Albumin, Calcium, Glucose (fasting), Glucose,Triglycerides (fasting) Cholesterol (total; fasting)
Time frame: Baseline to Day 15
Clinical laboratory assessments (urine sample tests)
Changes from pre-dose values (Bilirubin, Urobilinogen, Ketones, Glucose, Protein, Blood, Nitrites, pH, Specific gravity, Leukocytes)
Time frame: Baseline to Day 15
Plasma PK Parameter of YCT-529 (Area under the curve to Infinity [AUCinf])
Plasma PK Parameter as measured by area under the curve from time 0 extrapolated to infinity \[AUCinf\],
Time frame: Pre-dose to 336 hours after dosing
Plasma PK Parameter of YCT-529 (Area under the curve to the last measured concentration [AUC0-t])
Plasma PK Parameter as measured by area under the curve from time 0 to the last measured concentration \[AUC0-t\]
Time frame: Pre-dose to 336 hours after dosing
Plasma PK Parameter of YCT-529 (Area under the curve to 24 hours [AUC0--24])
Plasma PK Parameter as measured by area under the curve from time 0 to 24 hours \[AUC0--24\]
Time frame: Pre-dose to 336 hours after dosing
Plasma PK Parameter of YCT-529 (Time to maximum concentration [Tmax])
Plasma PK Parameter as measured by time to maximum concentration \[Tmax\]
Time frame: Pre-dose to 336 hours after dosing
Plasma PK Parameter of YCT-529 (Terminal elimination half life [T1/2])
Plasma PK Parameter as measured by terminal elimination half life \[T1/2\]
Time frame: Pre-dose to 336 hours after dosing
Plasma PK Parameter of YCT-529 (Lag time [Tlag])
Plasma PK Parameter as measured by lag time \[Tlag\]
Time frame: Pre-dose to 336 hours after dosing
Plasma PK Parameter of YCT-529 (Volume of distribution [Vz/F])
Plasma PK Parameter as measured by apparent volume of distribution \[Vz/F\]
Time frame: Pre-dose to 336 hours after dosing
Plasma PK Parameter of YCT-529 (oral clearance [CL/F])
Plasma PK Parameter as measured by oral clearance \[CL/F\] of YCT-529, including the effect of food on the PK
Time frame: Pre-dose to 336 hours after dosing
Plasma PK Parameter of YCT-529 (maximum concentration [Cmax])
Plasma PK Parameter as measured by maximum concentration \[Cmax\]) of YCT-529, including the effect of food on the PK
Time frame: Pre-dose to 336 hours after dosing
Pharmacodynamic parameter of YCT-529, including follicle-stimulating hormone
Changes from pre-dose values of follicle-stimulating hormone
Time frame: Pre-dose to 336 hours after dosing
Pharmacodynamic parameter of YCT-529, including luteinizing hormone
Changes from pre-dose values of luteinizing hormone
Time frame: Pre-dose to 336 hours after dosing
Pharmacodynamic parameter of YCT-529, including testosterone
Changes from pre-dose values of testosterone
Time frame: Pre-dose to 336 hours after dosing
Pharmacodynamic parameter of YCT-529, including sex hormone binding globulin
Changes from pre-dose values of including sex hormone binding globulin
Time frame: Pre-dose to 336 hours after dosing