Setidegrasib (ASP3082) is being developed for certain cancers. In this study, the researchers want to understand how it is processed by the body in healthy male volunteers. To do this, \[14C\] which is a certain chemical (called a tracer, or radionuclide) has been added to setidegrasib. \[14C\] gives off radiation, but the dose is very low (about the same as the dose from an x-ray) and will leave the body within a few days. \[14C\] will be picked up by a scanner and will be used to follow setidegrasib through the body. \[14C\]setidegrasib will be given as 1 single injection slowly through a vein (infusion). The men will stay overnight in the clinic for at least 2 weeks. They will give regular blood, urine and stool samples during their stay and will be closely monitored. The men will return to the clinic about 1 week later for a final safety check.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
8
Intravenous infusion
Pharmacokinetics (PK) of 14C-labeled ASP3082 (radioactivity in whole blood): area under the concentration-time curve from the time of dosing extrapolated to time infinity (AUCinf)
AUCinf will be recorded from the PK whole blood samples collected.
Time frame: Up to 21 days
PK of 14C-labeled ASP3082 (radioactivity in whole blood): area under the concentration-time curve from the time of dosing to the last measurable concentration (AUClast)
AUClast will be recorded from the PK whole blood samples collected.
Time frame: Up to 21 days
PK of 14C-labeled ASP3082 (radioactivity in whole blood): maximum concentration (Cmax)
Cmax will be recorded from the PK whole blood samples collected.
Time frame: Up to 21 days
PK of 14C-labeled ASP3082 (radioactivity in plasma): AUCinf
AUCinf will be recorded from the PK plasma samples collected.
Time frame: Up to 21 days
PK of 14C-labeled ASP3082 (radioactivity in plasma): AUClast
AUClast will be recorded from the PK plasma samples collected.
Time frame: Up to 21 days
PK of 14C-labeled ASP3082 (radioactivity in plasma): Cmax
Cmax will be recorded from the PK plasma samples collected.
Time frame: Up to 21 days
PK of 14C-labeled ASP3082 (radioactivity ratio of whole blood/plasma concentrations): radioactivity ratio of area under the concentration time curve in blood as compared to plasma (AUCblood/AUCplasma)
AUCblood/AUCplasma will be recorded from PK whole blood and plasma samples collected.
Time frame: Up to 21 days
Excretion of 14C-labeled ASP3082 (radioactivity in urine): amount of administered dose excreted (Ae)
Ae will be recorded from urine samples collected.
Time frame: Up to 21 days
Excretion of 14C-labeled ASP3082 (radioactivity in urine): percentage of administered dose excreted (Ae percentage)
Ae percentage will be recorded from urine samples collected.
Time frame: Up to 21 days
Excretion of 14C-labeled ASP3082 (radioactivity in urine): cumulative (over more than 1 sampling interval) amount of administered dose excreted (CumAe)
CumAe will be recorded from urine samples collected.
Time frame: Up to 21 days
Excretion of 14C-labeled ASP3082 (radioactivity in urine): renal clearance (CLr)
CLr will be recorded from urine samples collected.
Time frame: Up to 21 days
Excretion of 14C-labeled ASP3082 (radioactivity in feces): Ae
Ae will be recorded from feces samples collected.
Time frame: Up to 21 days
Excretion of 14C-labeled ASP3082 (radioactivity in feces): Ae percentage
Ae percentage will be recorded from feces samples collected.
Time frame: Up to 21 days
Excretion of 14C-labeled ASP3082 (radioactivity in feces): CumAe
CumAe will be recorded from feces samples collected.
Time frame: Up to 21 days
Excretion of 14C-labeled ASP3082 (combined radioactivity in urine and feces): Ae
Combined Ae will be recorded from urine and feces samples collected.
Time frame: Up to 21 days
Excretion of 14C-labeled ASP3082 (combined radioactivity in urine and feces): Ae percentage
Combined Ae percentage will be recorded from urine and feces samples collected.
Time frame: Up to 21 days
Excretion of 14C-labeled ASP3082 (combined radioactivity in urine and feces): CumAe
Combined CumAe will be recorded from urine and feces samples collected.
Time frame: Up to 21 days
Number of Participants with Adverse Events (AEs)
An AE is any untoward medical occurrence in a patient or clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention
Time frame: Up to 30 days
Number of Participants with laboratory value abnormalities and/or AEs
Number of participants with potentially clinically significant laboratory values.
Time frame: Up to 30 days
Number of Participants with vital sign abnormalities and/or AEs
Number of participants with potentially clinically significant vital sign values.
Time frame: Up to 30 days
Number of Participants with electrocardiogram (ECG) abnormalities and/or AEs
Number of participants with potentially clinically significant ECG values.
Time frame: Up to 30 days
Metabolite identification of ASP3082 in plasma
Identification of metabolites in plasma.
Time frame: Up to 21 days
Metabolite identification of ASP3082 in urine
Identification of metabolites in urine.
Time frame: Up to 21 days
Metabolite identification of ASP3082 in feces
Identification of metabolites in feces.
Time frame: Up to 21 days
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