A Study of the Absorption, Distribution, Metabolism, and Elimination of Opevesostat (MK-5684) in Healthy Adult Male Participants (MK-5684-008)
- Conditions
- Metastatic Prostate Cancer
- Interventions
- Registration Number
- NCT06566989
- Lead Sponsor
- Merck Sharp & Dohme LLC
- Brief Summary
This is a study of opevesostat in healthy adult male participants. The purpose of this study is to understand the absorption, distribution, metabolism, and elimination of opevesostat in humans, as well as its pharmacokinetics (PK), metabolic profile, and safety and tolerability.
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- Male
- Target Recruitment
- 8
- Is a healthy male according to the assessment of the investigator
- Has a body mass index of 18.0 to 32.0 kg/m2
- Has regular bowel movements (i.e., average stool production of ≥1 and ≤3 stools per day)
- Has the presence or history of clinically significant allergy requiring treatment
- Has a history of adrenal insufficiency
- Has veins not suitable for multiple venipunctures/cannulation
- Has previously taken part in more than 3 radiolabeled drug studies in the last 12 months
- Has donated blood or plasma within the previous 3 months or lost greater than 400 mL of blood
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- SINGLE_GROUP
- Arm && Interventions
Group Intervention Description [¹⁴C]Opevesostat Fludrocortisone On Day 1, participants receive a single dose of \[¹⁴C\]opevesostat as an oral solution. Participants then receive single doses of 5.0 mg prednisone and 0.05 mg fludrocortisone tablets 4 hours later as hormone replacement therapy. [¹⁴C]Opevesostat [¹⁴C]Opevesostat On Day 1, participants receive a single dose of \[¹⁴C\]opevesostat as an oral solution. Participants then receive single doses of 5.0 mg prednisone and 0.05 mg fludrocortisone tablets 4 hours later as hormone replacement therapy. [¹⁴C]Opevesostat Prednisone On Day 1, participants receive a single dose of \[¹⁴C\]opevesostat as an oral solution. Participants then receive single doses of 5.0 mg prednisone and 0.05 mg fludrocortisone tablets 4 hours later as hormone replacement therapy.
- Primary Outcome Measures
Name Time Method Cumulative percentage of total radioactivity excreted in feces (Cumfef) after administration of single-dose [¹⁴C]Opevesostat Predose and at designated time points (up to 8 days) Fecal samples will be collected at pre-specified timepoints and used to determine Cumfef.
Plasma Opevesostat Pharmacokinetics: Area under the curve from time 0 to the time of last measurable concentration (AUC0-t) Predose and at designated time points (up to 8 days) Plasma samples will be collected at pre-specified timepoints and used to determine AUC0-t of opevesostat.
Total Number of Metabolites in Feces that Represent at least 10% of the Dose of Radioactivity Predose and at designated time points (up to 8 days) Fecal samples will be collected at pre-specified timepoints and used to determine the total number of metabolites that represent at least 10% of the dose of radioactivity. Metabolites will be determined using liquid scintillation and high-resolution mass spectrometry.
Cumulative percentage of total radioactivity excreted in urine (Cumfeu) after administration of single-dose [¹⁴C]Opevesostat Predose and at designated time points (up to 8 days) Urine samples will be collected at pre-specified timepoints and used to determine CumFeu.
Plasma Opevesostat Pharmacokinetics: Area under the curve from time 0 to extrapolated infinity (AUC0-inf) Predose and at designated time points (up to 8 days) Plasma samples will be collected at pre-specified timepoints and used to determine AUC0-inf of opevesostat.
Plasma Total Radioactivity Pharmacokinetics: Time of maximum observed concentration (Tmax) Predose and at designated time points (up to 8 days) Plasma samples will be collected at pre-specified timepoints and used to determine Tmax of total radioactivity.
Cumulative amount of total radioactivity excreted in urine (CumAeu) after administration of single-dose [¹⁴C]Opevesostat Predose and at designated time points (up to 8 days) Urine samples will be collected at pre-specified timepoints and used to determine CumAeu.
Plasma Opevesostat Pharmacokinetics: Maximum observed concentration (Cmax) Predose and at designated time points (up to 8 days) Plasma samples will be collected at pre-specified timepoints and used to determine Cmax of opevesostat.
Plasma Opevesostat Pharmacokinetics: Terminal elimination half-life (t1/2) Predose and at designated time points (up to 8 days) Plasma samples will be collected at pre-specified timepoints and used to determine t1/2 of opevesostat.
Plasma Total Radioactivity Pharmacokinetics: Maximum observed concentration (Cmax) Predose and at designated time points (up to 8 days) Plasma samples will be collected at pre-specified timepoints and used to determine Cmax of total radioactivity.
Plasma Total Radioactivity Pharmacokinetics: Terminal elimination half-life (t1/2) Predose and at designated time points (up to 8 days) Plasma samples will be collected at pre-specified timepoints and used to determine t1/2 of total radioactivity.
Total Number of Metabolites in Plasma that Represent at least 10% of the Dose of Radioactivity Predose and at designated time points (up to 8 days) Plasma samples will be collected at pre-specified timepoints and used to determine the total number of metabolites that represent at least 10% of the dose of radioactivity. Metabolites will be determined using liquid scintillation and high-resolution mass spectrometry.
Cumulative amount of total radioactivity excreted in feces (CumAef) after administration of single-dose [¹⁴C]Opevesostat Predose and at designated time points (up to 8 days) Fecal samples will be collected at pre-specified timepoints and used to determine CumAef.
Plasma Opevesostat Pharmacokinetics: Time of maximum observed concentration (Tmax) Predose and at designated time points (up to 8 days) Plasma samples will be collected at pre-specified timepoints and used to determine Tmax of opevesostat.
Plasma Total Radioactivity Pharmacokinetics: Area under the curve from time 0 to the time of last measurable concentration (AUC0-t) Predose and at designated time points (up to 8 days) Plasma samples will be collected at pre-specified timepoints and used to determine AUC0-t of total radioactivity.
Plasma Total Radioactivity Pharmacokinetics: Area under the curve from time 0 to extrapolated infinity (AUC0-inf) Predose and at designated time points (up to 8 days) Plasma samples will be collected at pre-specified timepoints and used to determine AUC0-inf of total radioactivity.
Total Number of Metabolites in Urine that Represent at least 10% of the Dose of Radioactivity Predose and at designated time points (up to 8 days) Urine samples will be collected at pre-specified timepoints and used to determine the total number of metabolites that represent at least 10% of the dose of radioactivity. Metabolites will be determined using liquid scintillation and high-resolution mass spectrometry.
- Secondary Outcome Measures
Name Time Method Number of Participants with One or More Adverse Events (AEs) Up to approximately 8 days An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of study intervention. The number of participants who experienced an AE will be reported.
Number of Participants who Discontinue from the Study Due to an AE Up to approximately 8 days An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of study intervention. The number of participants who discontinue from the study due to an AE will be reported.
Trial Locations
- Locations (1)
Quotient Sciences ( Site 0001)
🇬🇧Nottingham, Nottinghamshire, United Kingdom
Quotient Sciences ( Site 0001)🇬🇧Nottingham, Nottinghamshire, United Kingdom