A Study of the Absorption, Distribution, Metabolism, and Elimination of Opevesostat (MK-5684) in Healthy Adult Male Participants (MK-5684-008)

NCT06566989 | Completed Phase 1

• 3 other identifiers: 5684-008MK-5684-0081010197
• Study Type: interventional
• Target: 8
• Locations: 1 country
• Sites: 1

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.

Conditions

Metastatic Prostate Cancer

Outcome Measures

Primary Outcomes (17)

• Cumulative amount of total radioactivity excreted in urine (CumAeu) after administration of single-dose [¹⁴C]Opevesostat

  Urine samples will be collected at pre-specified timepoints and used to determine CumAeu.

  Predose and at designated time points (up to 8 days)

• Cumulative amount of total radioactivity excreted in feces (CumAef) after administration of single-dose [¹⁴C]Opevesostat

  Fecal samples will be collected at pre-specified timepoints and used to determine CumAef.

  Predose and at designated time points (up to 8 days)

• Cumulative percentage of total radioactivity excreted in urine (Cumfeu) after administration of single-dose [¹⁴C]Opevesostat

  Urine samples will be collected at pre-specified timepoints and used to determine CumFeu.

  Predose and at designated time points (up to 8 days)

• Cumulative percentage of total radioactivity excreted in feces (Cumfef) after administration of single-dose [¹⁴C]Opevesostat

  Fecal samples will be collected at pre-specified timepoints and used to determine Cumfef.

  Predose and at designated time points (up to 8 days)

• Plasma Opevesostat Pharmacokinetics: Area under the curve from time 0 to the time of last measurable concentration (AUC0-t)

  Plasma samples will be collected at pre-specified timepoints and used to determine AUC0-t of opevesostat.

  Predose and at designated time points (up to 8 days)

• Plasma Opevesostat Pharmacokinetics: Area under the curve from time 0 to extrapolated infinity (AUC0-inf)

  Plasma samples will be collected at pre-specified timepoints and used to determine AUC0-inf of opevesostat.

  Predose and at designated time points (up to 8 days)

• Plasma Opevesostat Pharmacokinetics: Maximum observed concentration (Cmax)

  Plasma samples will be collected at pre-specified timepoints and used to determine Cmax of opevesostat.

  Predose and at designated time points (up to 8 days)

• Plasma Opevesostat Pharmacokinetics: Time of maximum observed concentration (Tmax)

  Plasma samples will be collected at pre-specified timepoints and used to determine Tmax of opevesostat.

  Predose and at designated time points (up to 8 days)

• Plasma Opevesostat Pharmacokinetics: Terminal elimination half-life (t1/2)

  Plasma samples will be collected at pre-specified timepoints and used to determine t1/2 of opevesostat.

  Predose and at designated time points (up to 8 days)

• Plasma Total Radioactivity Pharmacokinetics: Area under the curve from time 0 to the time of last measurable concentration (AUC0-t)

  Plasma samples will be collected at pre-specified timepoints and used to determine AUC0-t of total radioactivity.

  Predose and at designated time points (up to 8 days)

• Plasma Total Radioactivity Pharmacokinetics: Area under the curve from time 0 to extrapolated infinity (AUC0-inf)

  Plasma samples will be collected at pre-specified timepoints and used to determine AUC0-inf of total radioactivity.

  Predose and at designated time points (up to 8 days)

• Plasma Total Radioactivity Pharmacokinetics: Maximum observed concentration (Cmax)

  Plasma samples will be collected at pre-specified timepoints and used to determine Cmax of total radioactivity.

  Predose and at designated time points (up to 8 days)

• Plasma Total Radioactivity Pharmacokinetics: Time of maximum observed concentration (Tmax)

  Plasma samples will be collected at pre-specified timepoints and used to determine Tmax of total radioactivity.

  Predose and at designated time points (up to 8 days)

• Plasma Total Radioactivity Pharmacokinetics: Terminal elimination half-life (t1/2)

  Plasma samples will be collected at pre-specified timepoints and used to determine t1/2 of total radioactivity.

  Predose and at designated time points (up to 8 days)

• Total Number of Metabolites in Plasma that Represent at least 10% of the Dose of Radioactivity

  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.

  Predose and at designated time points (up to 8 days)

• Total Number of Metabolites in Urine that Represent at least 10% of the Dose of Radioactivity

  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.

  Predose and at designated time points (up to 8 days)

• Total Number of Metabolites in Feces that Represent at least 10% of the Dose of Radioactivity

  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.

  Predose and at designated time points (up to 8 days)

Secondary Outcomes (2)

• Number of Participants with One or More Adverse Events (AEs)

  Up to approximately 8 days

• Number of Participants who Discontinue from the Study Due to an AE

  Up to approximately 8 days

Study Arms (1)

[¹⁴C]Opevesostat

EXPERIMENTAL

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.

Drug: [¹⁴C]Opevesostat; Drug: Prednisone; Drug: Fludrocortisone

Interventions

[¹⁴C]Opevesostat DRUG

Oral solution

Also known as: MK-5684

[¹⁴C]Opevesostat

Prednisone DRUG

Tablet

Also known as: RAYOS®, STERAPRED®, DELTASONE®

[¹⁴C]Opevesostat

Fludrocortisone DRUG

Tablet

Also known as: FLORINEF®

[¹⁴C]Opevesostat

Eligibility Criteria

• Age: 30 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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)

You may not qualify if:

• 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

Sponsors & Collaborators

• Merck Sharp & Dohme LLC: lead
• Orion Corporation, Orion Pharma: collaborator

Study Sites (1)

Quotient Sciences ( Site 0001)

Nottingham, Nottinghamshire, NG11 6JS, United Kingdom

Location

Related Links

• Merck Clinical Trials Information

MeSH Terms

Conditions

Prostatic Neoplasms

Interventions

Prednisone; Fludrocortisone; fludrocortisone acetate

Condition Hierarchy (Ancestors)

Genital Neoplasms, Male; Urogenital Neoplasms; Neoplasms by Site; Neoplasms; Genital Diseases, Male; Genital Diseases; Urogenital Diseases; Prostatic Diseases; Male Urogenital Diseases

Intervention Hierarchy (Ancestors)

Pregnadienediols; Pregnadienes; Pregnanes; Steroids; Fused-Ring Compounds; Polycyclic Compounds; Hydrocortisone; Pregnenediones; Pregnenes

Study Officials

• Medical Director

  Merck Sharp & Dohme LLC

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 20, 2024
• First Posted: August 22, 2024
• Study Start: September 19, 2024
• Primary Completion: October 17, 2024
• Study Completion: October 17, 2024
• Last Updated: October 23, 2024

Record last verified: 2024-10

Data Sharing

• IPD Sharing: Will share

Locations

GB (1)