This is a Phase 1, open-label, single-ascending-dose study evaluating the safety, tolerability, and pharmacokinetics (PK) of Viaca - a fixed-dose oral combination of sildenafil (a PDE5 inhibitor) and cabergoline (a dopamine D2 agonist) - versus sildenafil monotherapy and cabergoline monotherapy in healthy adult male volunteers. Approximately 30 participants are enrolled across 5 sequential cohorts (6 each). Each participant receives a single oral dose. The combination targets erectile dysfunction through both vascular and neuroendocrine pathways, aiming for efficacy at lower component doses.
Five cohorts of 6 healthy male participants each (n≈30). Viaca dose cohorts: Cohort 1 (25/0.25 mg), Cohort 2 (50/0.5 mg), Cohort 3 (75/0.75 mg). Active-comparator cohorts: Cohort 4 (sildenafil 50 mg) and Cohort 5 (cabergoline 0.5 mg). Cohort 1 runs first; after Safety Review Committee (SRC) review of safety/tolerability/PK through Day 3, Cohorts 2, 4 and 5 may proceed in parallel; Cohort 3 proceeds after SRC review of Cohort 2. Participants fast ≥8 h overnight before dosing and 2 h after. They are confined to a Phase 1 unit and discharged on Day 5 (Cohorts 1-3 and 5) or Day 2 (Cohort 4), with a follow-up visit on Day 8 (±1). Total participation \~33 days including screening. (V2.0 amendment removed the former optional high-dose Viaca cohort.)
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
30
fixed-dose oral tablet of sildenafil + cabergoline (low-dose 25/0.25 mg; high-dose 50/0.5 mg). Single oral dose.
single oral dose
single oral dose
Nucleus Network Brisbane
Herston, Queensland, Australia
Participants with AEs/SAEs
Number of participants with treatment-emergent adverse events (TEAEs) and serious adverse events (SAEs). Unit: participants (summarised by severity and relatedness).
Time frame: Day 1 (dosing) through Day 8
Blood pressure
Change from Baseline in systolic and diastolic blood pressure. Unit: mmHg.
Time frame: Baseline through Day 8.
Pulse rate
Change from Baseline in pulse rate. Unit: beats/min.
Time frame: Baseline through Day 8.
Respiratory rate
Change from Baseline in respiratory rate. Unit: breaths/min.
Time frame: Baseline through Day 8.
Body temperature
Change from Baseline in body temperature. Unit: °C.
Time frame: Baseline through Day 8.
ECG heart rate
Change from Baseline in 12-lead ECG heart rate. Unit: beats/min.
Time frame: Baseline through Day 8.
ECG intervals
Change from Baseline in 12-lead ECG intervals (QTcF, PR, QRS). Unit: milliseconds.
Time frame: Baseline through Day 8.
Laboratory tests
Number of participants with clinically significant safety laboratory abnormalities. Unit: participants.
Time frame: Baseline through Day 8.
Physical examination
Number of participants with clinically significant physical examination findings. Unit: participants.
Time frame: Baseline through Day 8.
Cmax
Maximum observed plasma concentration (Cmax). Unit: e.g. ng/mL.
Time frame: Predose (Day 1) through 168 hours post-dose (Day 8).
Tmax
Time to maximum plasma concentration (Tmax). Unit: hours.
Time frame: Predose (Day 1) through 168 hours post-dose (Day 8).
AUC0-t
Area under the plasma concentration-time curve from time 0 to the last measurable concentration (AUC0-t). Unit: e.g. ng·h/mL.
Time frame: Predose (Day 1) through 168 hours post-dose (Day 8)
AUC0-24
AUC from time 0 to 24 hours (AUC0-24). Unit: e.g. ng·h/mL.
Time frame: Predose (Day 1) through 168 hours post-dose (Day 8).
AUC0-inf
AUC from time 0 extrapolated to infinity (AUC0-inf). Unit: e.g. ng·h/mL.
Time frame: Predose (Day 1) through 168 hours post-dose (Day 8).
%AUCextrap
Percentage of AUC0-inf obtained by extrapolation (%AUCextrap). Unit: percentage.
Time frame: Predose (Day 1) through 168 hours post-dose (Day 8).
t½
Apparent terminal elimination half-life (t½). Unit: hours.
Time frame: Predose (Day 1) through 168 hours post-dose (Day 8).
kel
Terminal elimination rate constant (kel). Unit: 1/hour.
Time frame: Predose (Day 1) through 168 hours post-dose (Day 8).
CL/F
Apparent total clearance after oral dosing (CL/F). Unit: e.g. L/h.
Clinical Research Coordinator at Nucleus Network Brisbane
CONTACT
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Time frame: Predose (Day 1) through 168 hours post-dose (Day 8).
Vz/F
Apparent volume of distribution during the terminal phase after oral dosing (Vz/F). Unit: e.g. L.
Time frame: Predose (Day 1) through 168 hours post-dose (Day 8).
Cmax/D
Dose-normalised maximum plasma concentration (Cmax/D). Unit: e.g. ng/mL per mg.
Time frame: Predose (Day 1) through 168 hours post-dose (Day 8).
AUC0-inf/D
Dose-normalised AUC0-inf (AUC0-inf/D). Unit: e.g. ng·h/mL per mg.
Time frame: Predose (Day 1) through 168 hours post-dose (Day 8).
AUC0-t/D
Dose-normalised AUC0-t (AUC0-t/D). Unit: e.g. ng·h/mL per mg.
Time frame: Predose (Day 1) through 168 hours post-dose (Day 8).
Dose proportionality
Dose proportionality of Cmax and AUC across Viaca dose levels. Unit: e.g. slope (power-model estimate).
Time frame: Predose (Day 1) through 168 hours post-dose (Day 8).