Healthy Volunteers
Conditions
Brief summary
The primary objective is to characterize the pharmacokinetics (PK) of praliciguat and total radioactivity and to assess the elimination of total radioactivity from a single oral dose of \[14C\]-praliciguat.
Interventions
DRUG[14C]-praliciguat
10 mg praliciguat containing approximately 500 μCi of \[14C\]-praliciguat
Sponsors
Cyclerion Therapeutics
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
OTHER
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Males of any race, between 18 and 55 years of age, inclusive * Body mass index between 18 and 32 kg/m2, inclusive * Subject is in good health and has no clinically significant findings on physical examination * Men must agree to use protocol-specified contraception and also to not donate sperm throughout the study and for at least 90 days after the final dose of study drug
Exclusion criteria
* Any active or unstable clinically significant medical condition * Use of any prescribed or non-prescribed medication Additional inclusion/
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| AUC0-inf of whole blood total radioactivity to AUC0-inf of plasma total radioactivity (AUC0-inf Ratio of Blood Total Radioactivity/Plasma Total Radioactivity) | up to Day 15 |
| AUC from time zero to the last quantifiable concentration (AUC0-last) of praliciguat in plasma | up to Day 15 |
| AUC0-last of total radioactivity in plasma and whole blood | up to Day 15 |
| Maximum observed concentration (Cmax) of praliciguat in plasma | up to Day 15 |
| Cmax of total radioactivity in plasma and whole blood | up to Day 15 |
| Time of Cmax (Tmax) of praliciguat in plasma | up to Day 15 |
| Tmax of total radioactivity in plasma and whole blood | up to Day 15 |
| Apparent terminal elimination half-life (t1/2) of praliciguat in plasma | up to Day 15 |
| t1/2 total radioactivity in plasma and whole blood | up to Day 15 |
| Apparent total clearance of praliciguat (CL/F) | up to Day 15 |
| Apparent volume of distribution of praliciguat (Vz/F) | up to Day 15 |
| AUC0-inf of plasma praliciguat concentration relative to AUC0-inf of plasma total radioactivity (AUC0-inf Ratio of Plasma Praliciguat/Plasma Total Radioactivity) | up to Day 15 |
| Amount of total radioactivity excreted in urine (Aeu) and feces (Aef) | up to Day 15 |
| Cumulative Aeu and cumulative Aef | up to Day 15 |
| Percentage of total radioactivity excreted in urine (feu) and feces (fef) | up to Day 15 |
| Cumulative feu and cumulative fef | up to Day 15 |
| Percentage of total radioactivity in total excreta (feces + urine) | up to Day 15 |
| Area under the concentration-time curve (AUC) from time zero to infinity (AUC0-inf) of praliciguat in plasma | up to Day 15 |
| AUC0-inf of total radioactivity in plasma and whole blood | up to Day 15 |
Secondary
| Measure | Time frame |
|---|---|
| AUC0-inf of metabolite radioactivity levels in plasma | up to Day 15 |
| AUC0-inf of plasma metabolite radioactivity levels relative to AUC0-inf of plasma total radioactivity (Plasma AUC0-inf Ratio of Metabolite Radioactivity/Total Radioactivity) | up to Day 15 |
| Chromatographic retention time of metabolites | up to Day 15 |
| Levels of metabolite radioactivity excreted in urine and feces | up to Day 15 |
| Characteristic mass spectrometry fragmentation ions of metabolites | up to Day 15 |
| Chemical structures (graphical representations showing atom connectivity) proposed for plasma, urine, and feces metabolites | up to Day 15 |
| Number(s) of participants with ≥1 treatment-emergent serious adverse event (SAE) | up to Day 15 |
| Number(s) of participants with ≥1 adverse event (AE) leading to study drug discontinuation | up to Day 15 |
| Number(s) of participants with ≥1 Grade ≥3 AE (per CTCAE v. 5.0) | up to Day 15 |
| Number(s) of participants with ≥1 clinically significant abnormal physical examination finding | up to Day 15 |
| Molecular ion mass of metabolites | up to Day 15 |
Countries
United States
Outcome results
None listed