This study will assess the PK and rates of elimination and mass balance of total radioactivity from \[14C\]-PC14586
PC14586 is a first-in-class, oral, small molecule p53 reactivator that is selective for the TP53 Y220C mutation. The study will assess the PK, absorption, metabolism, and excretion of \[14C\]-PC14586 following a single dose in healthy male participants. The aim is to recruit approximately 8 participants with a minimum number of 6 evaluable participants. Each participant will be admitted to the study site pre-dose on Day -1 and will remain at the study site until at least Day 14. Participants will receive a single administration of \[14C\]-PC14586 as oral capsules on Day 1. During this study, whole blood, plasma, urine, feces, and vomit samples (if presented) will be collected at various timepoints to characterize the absorption, metabolism, excretion, and PK of \[14C\]-PC14586. The duration of the residential period will be evaluated following the administration of \[14C\]-PC14586 and may be extended to ensure recovery of at least 90% of the total radioactivity, or until less than 1% of dose is recovered in urine and/or feces.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
OTHER
Masking
NONE
Enrollment
8
Single, oral dose of \[14C\]-PC14586
Labcorp Clinical Research Unit Inc.
Madison, Wisconsin, United States
Characterize Maximum Plasma Concentration (Cmax) of PC14586 and PC14586 metabolite M1 (PC16163).
Determine Cmax for PC14586 and PC16163 in plasma.
Time frame: 1 month
Characterize Time to Maximum Plasma Concentration (tmax) of PC14586 and PC14586 metabolite M1 (PC16163).
Determine tmax for PC14586 and PC16163 in plasma.
Time frame: 1 month
Characterize Total Drug Exposure (AUC0-inf) of PC14586 and PC14586 metabolite M1 (PC16163).
Determine AUC0-inf for PC14586 and PC16163 in plasma.
Time frame: 1 month
Characterize Total Drug Exposure to the last measurable concentration (AUC0-t) of PC14586 and PC14586 metabolite M1 (PC16163).
Determine AUC0-t for PC14586 and PC16163 in plasma.
Time frame: 1 month
Characterize the Half-Life (t 1/2) of PC14586 and PC14586 metabolite M1 (PC16163).
Determine t 1/2 for PC14586 and PC16163 in plasma.
Time frame: 1 month
Characterize the Clearance (CL/F) of PC14586 and PC14586 metabolite M1 (PC16163) after oral administration.
Determine CL/F for PC14586 and PC16163 in plasma.
Time frame: 1 month
Characterize the Volume of Distribution (Vd/F) of PC14586 and PC14586 metabolite M1 (PC16163) after oral administration.
Determine Vd/F for PC14586 and PC16163 in plasma.
Time frame: 1 month
Determine the total radioactivity in whole blood and plasma of PC14586 and PC14586 metabolite M1 (PC16163).
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Determine total radioactivity for PC14586 and PC16163 in whole blood and plasma.
Time frame: 1 month
Characterize total radioactivity (Xlast, feces) of PC14586 excreted in feces.
Determine total radioactivity of PC14586 excreted in feces
Time frame: 1 month
Characterize the half life of total radioactivity (Xt1-t2, feces) of PC14586 excreted in feces.
Determine half life of total radioactivity of PC14586 excreted in feces.
Time frame: 1 month
Characterize the fraction excreted of total radioactivity (fe last, feces) of PC14586 in feces.
Determine the fraction excreted of total radioactivity of PC14586 in feces.
Time frame: 1 month
Characterize the half-life of fraction excreted of total radioactivity (fe t1-t2, feces) of PC14586 in feces.
Determine half-life of fraction excreted of total radioactivity of PC14586 in feces.
Time frame: 1 month
Characterize total radioactivity (Xlast, urine) of PC14586 excreted in urine.
Determine total radioactivity of PC14586 excreted in urine.
Time frame: 1 month
Characterize the half life of total radioactivity (Xt1-t2, urine) of PC14586 excreted in urine.
Determine half life of total radioactivity of PC14586 excreted in urine.
Time frame: 1 month
Characterize the fraction excreted of total radioactivity (fe last, urine) of PC14586 in urine.
Determine the fraction excreted of total radioactivity of PC14586 in urine.
Time frame: 1 month
Characterize the half-life of fraction excreted of total radioactivity (fe t1-t2, urine) of PC14586 in urine.
Determine half-life of fraction excreted of total radioactivity of PC14586 in urine.
Time frame: 1 month
Characterize the renal clearance (CLr) of PC14586 in urine.
Determine the renal clearance of PC14586 in urine.
Time frame: 1 month
Identification of PC14586 metabolite profiles in plasma, urine and feces.
Identification of PC14586 metabolites in plasma (\>10% relative total drug related exposure) and excreta (\>10% of excreted dose).
Time frame: 1 month
Identification of the incidence and severity of adverse events after administration of PC14586.
Number of participants with adverse events.
Time frame: 1 month
Identification of the incidence of laboratory abnormalities based on hematology, clinical chemistry and urine test results of PC14586.
Number of participants with an incidence of laboratory abnormalities in test results.
Time frame: 1 month
Identification of 12-lead electrocardiogram (ECG) abnormalities after a single dose of PC14586.
Number of participants with abnormal 12-lead ECG results.
Time frame: 1 month
Identification of abnormal blood pressure after a single dose of PC14586.
Number of participants with abnormal blood pressure.
Time frame: 1 month
Identification of abnormal pulse rate after a single dose of PC14586.
Number of participants with abnormal pulse rate.
Time frame: 1 month
Identification of abnormal oral body temperature after a single dose of PC14586.
Number of participants with abnormal oral body temperature.
Time frame: 1 month