A Study to Learn How ASP3082 is Processed in Healthy Men

NCT07773129 | Not Yet Recruiting Phase 1 FDA Drug

• 1 other identifier: 3082-CL-0103
• Study Type: interventional
• Target: 8
• Locations: 0 countries
• Sites: N/A

Brief Summary

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.

Conditions

Healthy Volunteer

Keywords

ASP3082; Setidegrasib; Pharmacokinetics; Healthy Volunteers

Outcome Measures

Primary Outcomes (17)

• 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.

  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.

  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.

  Up to 21 days

• PK of 14C-labeled ASP3082 (radioactivity in plasma): AUCinf

  AUCinf will be recorded from the PK plasma samples collected.

  Up to 21 days

• PK of 14C-labeled ASP3082 (radioactivity in plasma): AUClast

  AUClast will be recorded from the PK plasma samples collected.

  Up to 21 days

• PK of 14C-labeled ASP3082 (radioactivity in plasma): Cmax

  Cmax will be recorded from the PK plasma samples collected.

  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.

  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.

  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.

  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.

  Up to 21 days

• Excretion of 14C-labeled ASP3082 (radioactivity in urine): renal clearance (CLr)

  CLr will be recorded from urine samples collected.

  Up to 21 days

• Excretion of 14C-labeled ASP3082 (radioactivity in feces): Ae

  Ae will be recorded from feces samples collected.

  Up to 21 days

• Excretion of 14C-labeled ASP3082 (radioactivity in feces): Ae percentage

  Ae percentage will be recorded from feces samples collected.

  Up to 21 days

• Excretion of 14C-labeled ASP3082 (radioactivity in feces): CumAe

  CumAe will be recorded from feces samples collected.

  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.

  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.

  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.

  Up to 21 days

Secondary Outcomes (7)

• Number of Participants with Adverse Events (AEs)

  Up to 30 days

• Number of Participants with laboratory value abnormalities and/or AEs

  Up to 30 days

• Number of Participants with vital sign abnormalities and/or AEs

  Up to 30 days

• Number of Participants with electrocardiogram (ECG) abnormalities and/or AEs

  Up to 30 days

• Metabolite identification of ASP3082 in plasma

  Up to 21 days

Study Arms (1)

14C-labeled ASP3082

EXPERIMENTAL

Participants will receive single dose of 14C-labeled ASP3082 on Day 1.

Drug: 14C-labeled ASP3082

Interventions

14C-labeled ASP3082 DRUG

Intravenous infusion

Also known as: Setidegrasib

14C-labeled ASP3082

Eligibility Criteria

• Age: 18 Years - 65 Years
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Participant is healthy and has no clinically significant medical conditions based on the physical examination, electrocardiogram (ECG) and protocol-defined clinical laboratory tests at screening or on day -1.
• Participant has regular bowel habits (i.e., at least 1 bowel movement per day).
• Male participant:
• Must agree to use contraception with female partner(s) of childbearing potential (including breastfeeding partner) throughout the investigational period and for 3 months after study intervention administration.
• Must agree to remain abstinent or use a condom with pregnant partner(s) for the duration of the pregnancy throughout the investigational period and for 3 months after study intervention administration.
• Must not donate sperm during the investigational period and for 3 months after investigational study intervention administration.
• Participant agrees not to participate in another interventional study while participating in the present study.
• Participant has a body mass index (BMI) range of 18.0 to 32.0 kg/m\^2, inclusive and weighs at least 50 kg at screening.

You may not qualify if:

• Participant has any history or evidence of any clinically significant cardiovascular, gastrointestinal, endocrinologic, hematologic, hepatic, immunologic, metabolic, urologic, pulmonary, neurologic, dermatologic, psychiatric, renal and/or other major disease.
• Participant has a history of malignancy within 2 years before screening (exceptions are squamous and basal cell carcinomas of the skin and carcinoma in situ of the cervix, or malignancy that with concurrence with the sponsor's medical monitor, is considered cured with minimal risk of recurrence).
• Participant has had major surgery (e.g., requiring general anesthesia) within 90 days before screening, or will not have fully recovered from surgery, or has surgery planned during the time the participant is expected to participate in the study or within 5 half-lives (approximately 8 to 9 days) after the dose of study drug administration or end-of-study visit (ESV), whichever is longer.
• Participant has previously undergone a cholecystectomy.
• Participant has/had febrile illness or symptomatic, viral, bacterial (including upper respiratory infection) or fungal (noncutaneous) infection within 28 days prior to day -1.
• Participant has a history of drug or alcohol abuse according to Diagnostic and Statistical Manual of Mental Disorders (5th edition) (DSM-5) criteria within 2 years before screening.
• Participant has a history of unexplained syncope, cardiac arrest, unexplained cardiac arrhythmias or torsades de pointes, structural heart disease or a family history of long QT syndrome.
• Participant has used any prescribed or nonprescribed drugs (including vitamins and natural and herbal remedies, e.g., St. John's Wort) in the 28 days prior to day -1, except for occasional use of acetaminophen (up to 2 g/day) and topical dermatological products (including corticosteroid products).
• Participant has used any inducer of metabolism (e.g., barbiturates and rifampin) in the 28 days prior to day -1.
• Participant has received a coronavirus disease 2019 (COVID-19) vaccine within the 14 days prior to day -1 or will have a COVID-19 vaccine dose before the ESV.
• Participant has received any investigational therapy within 28 days or 5 half-lives, whichever is longer, prior to screening.
• Participant has participated in more than 2 radiolabeled studies within 12 months prior to day -1 (participation in a previous radiolabeled study has to have been at least 4 months prior to day -1 where exposures are known to the investigator, or 6 months prior to day -1 where exposures are not known to the investigator).
• Participant has any liver test result (alkaline phosphatase \[ALP\], alanine aminotransferase \[ALT\], aspartate aminotransferase \[AST\] and total bilirubin \[TBL\]) ≥ 1.5 × upper limit of normal (ULN) on day -1.
• Participant has clinically significant creatinine elevation.
• Participant has any of the following conditions on day -1: mean pulse \< 45 or \> 90 bpm; mean systolic blood pressure (SBP) \> 140 mmHg; mean diastolic blood pressure (DBP) \> 90 mmHg (measurements taken in triplicate after participant has been resting in the supine position for at least 5 minutes; pulse measured automatically). If the mean blood pressure exceeds the limits above, 1 additional triplicate may be taken.

Sponsors & Collaborators

• Astellas Pharma Global Development, Inc.: lead

Study Officials

• Medical Director

  Astellas Pharma Global Development, Inc.

  STUDY DIRECTOR

Central Study Contacts

Astellas Pharma Global Development, Inc.

CONTACT

800-888-7704; astellas.registration@astellas.com

Study Design

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

Study Record Dates

• First Submitted: August 16, 2026
• First Posted: August 19, 2026
• Study Start: August 31, 2026
• Primary Completion (Estimated): October 31, 2026
• Study Completion (Estimated): October 31, 2026
• Last Updated: August 19, 2026

Record last verified: 2026-08

Data Sharing

• IPD Sharing: Will not share