A Drug-Drug Interaction Study of Itraconazole and Opevesostat (MK-5684) in Healthy Adult Male Participants (MK-5684-017)

NCT07548606 — Phase 1, Completed, 14 participants, Merck Sharp & Dohme LLC

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A Phase 1, Open-Label, Fixed-Sequence Study to Evaluate the Effects of Multiple Doses of Itraconazole on the Single-Dose Pharmacokinetics of MK-5684 in Healthy Adult Male Participants

Registry	NCT07548606
Status	Completed
Phase	Phase 1
Study type	Interventional; non randomized, sequential, masking: none, basic science
Enrollment	14 (Actual)
Sponsor	Merck Sharp & Dohme LLC (Industry)
Conditions	Healthy
Interventions	Opevesostat, Prednisone, Fludrocortisone acetate, Itraconazole (Drug)
Dates	start 2026-05-11, primary completion 2026-06-01, completion 2026-06-18, first posted 2026-04-23, last updated 2026-06-25
Locations	1 site in United States

-Summary

Researchers have designed a study medicine called opevesostat as a new way to treat prostate cancer.

The purpose of this study is to learn what happens to opevesostat in a person's body over time (a pharmacokinetic or PK study). Researchers will compare what happens to opevesostat in the body when it is given with and without another medicine called itraconazole.

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+Arms and interventions

Arm	Type	Interventions	Description
Opevesostat Period 1	Experimental	Drug: Opevesostat; Drug: Prednisone; Drug: Fludrocortisone acetate	On Day 1, a single dose of opevesostat will be administered under fed conditions. A single dose of steroid replacement (prednisone and fludrocortisone) will be administered under fed conditions approximately 4.5 hours after opevesostat dosing.
Opevesostat Period 2	Experimental	Drug: Opevesostat; Drug: Prednisone; Drug: Fludrocortisone acetate; Drug: Itraconazole	There will be a washout of at least 5 days between opevesostat dosing in Period 1 and the first itraconazole dosing in Period 2. In Period 2, itraconazole will be administered once daily (QD) for 9 consecutive days with a single dose of opevesostat coadministered on Day 4 under fed conditions. Steroid replacement (prednisone and fludrocortisone) will be administered under fed conditions QD on Days 4 through 6, approximately 4.5 hours after opevesostat and/or itraconazole dosing.

Opevesostat (Drug), also known as MK-5684, ODM-208: Administered via oral film-coated tablet
Prednisone (Drug): Administered via oral tablet
Fludrocortisone acetate (Drug): Administered via oral tablet
Itraconazole (Drug): Administered via oral capsule

+Outcome measures

Primary outcomes

Area under the concentration versus time curve from 0 to infinity after single dosing (AUC0-inf) of opevesostat [Predose, and at designated timepoints up to 144 hours post-dose]: Blood samples will be collected to determine the AUC0-inf of opevesostat.
Area under the concentration versus time curve from 0 to last quantifiable sample (AUC0-last) of opevesostat [Predose, and at designated timepoints up to 144 hours post-dose]: Blood samples will be collected to determine the AUC0-last of opevesostat.
Maximum concentration (Cmax) of opevesostat [Predose, and at designated timepoints up to 144 hours post-dose]: Blood samples will be collected to determine the Cmax of opevesostat.
Time to Maximum concentration (Tmax) of opevesostat [Predose, and at designated timepoints up to 144 hours post-dose]: Blood samples will be collected to determine the Tmax of opevesostat.
Apparent terminal half-life (t1/2) of opevesostat [Predose, and at designated timepoints up to 144 hours post-dose]: Blood samples will be collected to determine the t1/2 of opevesostat.
Apparent Clearance (CL/F) of opevesostat [Predose, and at designated timepoints up to 144 hours post-dose]: Blood samples will be collected to determine the CL/F of opevesostat.
Apparent volume of distribution during terminal phase (Vz/F) of opevesostat [Predose, and at designated timepoints up to 144 hours post-dose]: Blood samples will be collected to determine the Vz/F of opevesostat.

Secondary outcomes

Number of participants who experience one or more adverse events (AEs) [Up to approximately 28 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. The number of participants who experience an AE will be reported.
Number of participants who discontinue study intervention due to an AE [Up to approximately 28 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. The number of participants who discontinue study intervention due to an AE will be reported.

+Eligibility

Sex: Male, ages: 19 Years to 55 Years, accepts healthy volunteers

Inclusion Criteria:

The main inclusion criteria include but are not limited to the following:

* Has a body mass index ≥18.0 and ≤32.0 kg/m\^2
* Is medically healthy with no clinically significant medical history

Exclusion Criteria:

The main exclusion criteria include but are not limited to the following:

* Has a history or presence of any of the following: adrenal insufficiency; hepatic or renal impairment; clinically significant hypotension, cardiac arrhythmia, cardiac conduction abnormalities, or recurrent unexplained syncopal events; second- or third-degree atrioventricular heart block; clinically significant sick sinus syndrome; any systemic fungal infection; chronic infection; glaucoma; hypothyroidism; stomach ulcer; ocular herpes simplex; ventricular dysfunction or risk factors for Torsades de Pointes (e.g., heart failure, cardiomyopathy, family history of Long QT Syndrome)
* Has a history of cancer (malignancy)

+Locations (1)

Facility	City	Country	Status
Celerion, Inc. ( Site 0001)	Lincoln, Nebraska	United States

+Investigators

Medical Director, Study director, Merck Sharp & Dohme LLC