A Study to Learn How Fluconazole, Carbamazepine and Itraconazole Affect How the Body Processes ASP3082 in Healthy Adults

NCT07395024 | Recruiting Phase 1 FDA Drug

• 1 other identifier: 3082-CL-0102
• Study Type: interventional
• Target: 54
• Locations: 1 country
• Sites: 1

Brief Summary

Genes give your body instructions on how to make proteins. Proteins are needed to keep the body working properly. Many types of cancer are caused by changes in certain genes, making them faulty. Some people with solid tumors have a faulty KRAS gene. One such change in the KRAS gene is called a G12D mutation. Researchers are looking for ways to stop the actions of abnormal proteins made from the KRAS G12D mutation. ASP3082 is thought to replace some of the abnormal proteins made from the faulty KRAS gene. If other medicines are given at the same time as ASP3082, they may affect how the body processes ASP3082. In this study, fluconazole, itraconazole and carbamazepine are given with ASP3082 in healthy adults. The main aims are to check if fluconazole, itraconazole and carbamazepine affect how the body processes ASP3082. These medicines may affect how the body processes ASP3082 when they are taken at the same time. This study will have 3 groups of adults. One group will be given fluconazole and ASP3082, the second group will be given carbamazepine and ASP3082, and the third group will be given itraconazole and ASP3082. ASP3082 will be given to people slowly through a tube into the vein (infusion). Fluconazole and carbamazepine will be given as a tablet and itraconazole will be given as a liquid by mouth. People will be given study treatments for about 1 month. They will then return to the clinic about 1 week after they finish study treatment for a final safety check.

Conditions

Healthy Volunteer

Keywords

ASP3082; Pharmacokinetics; Setidegrasib; Healthy Volunteers; Fluconazole; Itraconazole; Carbamazepine

Outcome Measures

Primary Outcomes (21)

• Pharmacokinetics (PK) of ASP3082 in plasma: Maximum Concentration (Cmax) in ASP3082

  Cmax will be recorded from the PK plasma samples collected.

  Up to 29 days

• PK of ASP3082 in plasma: area under the concentration-time curve from time zero to the time of the last measurable concentration (AUClast) in ASP3082

  AUClast will be recorded from the PK plasma samples collected.

  Up to 29 days

• PK of ASP3082 in plasma: area under the concentration-time curve extrapolated to infinity (AUCinf) in ASP3082

  AUCinf will be calculated from the PK plasma samples collected.

  Up to 29 days

• PK of ASP3082 in plasma: Cmax in ASP3082+ Fluconazole (FLZ)

  Cmax will be recorded from the PK plasma samples collected.

  Up to 29 days

• PK of ASP3082 in plasma: AUClast in ASP3082+FLZ

  AUClast will be recorded from the PK plasma samples collected.

  Up to 29 days

• PK of ASP3082 in plasma: AUCinf in ASP3082+FLZ

  AUCinf will be calculated from the PK plasma samples collected.

  Up to 29 days

• Ratio of Cmax of ASP3082 and ASP3082+FLZ

  Ratios of Cmax will be calculated from the PK plasma samples collected.

  Up to 29 days

• Ratio of AUClast of ASP3082 and ASP3082+FLZ

  Ratios of AUClast will be calculated from the PK plasma samples collected.

  Up to 29 days

• Ratio of AUCinf of ASP3082 and ASP3082+FLZ

  Ratios of AUCinf will be calculated from the PK plasma samples collected.

  Up to 29 days

• PK of ASP3082 in plasma: Cmax in ASP3082+ Itraconazole (ITZ)

  Cmax will be recorded from the PK plasma samples collected.

  Up to 29 days

• PK of ASP3082 in plasma: AUClast in ASP3082+ITZ

  AUClast will be recorded from the PK plasma samples collected.

  Up to 29 days

• PK of ASP3082 in plasma: AUCinf in ASP3082+ITZ

  AUCinf will be calculated from the PK plasma samples collected.

  Up to 29 days

• Ratio of Cmax of ASP3082 and ASP3082+ITZ

  Ratios of Cmax will be recorded from the PK plasma samples collected.

  Up to 29 days

• Ratio of AUClast for ASP3082 and ASP3082+ITZ

  Ratios of AUClast will be recorded from the PK plasma samples collected.

  Up to 29 days

• Ratio of AUCinf for ASP3082 and ASP3082+ITZ

  Ratios of AUCinf will be calculated from the PK plasma samples collected.

  Up to 29 days

• PK of ASP3082 in plasma: Cmax in ASP3082+ Carbamazepine (CAR)

  Cmax will be recorded from the PK plasma samples collected.

  Up to 29 days

• PK of ASP3082 in plasma: AUClast in ASP3082+CAR

  AUClast will be recorded from the PK plasma samples collected.

  Up to 29 days

• PK of ASP3082 in plasma: AUCinf in ASP3082+CAR

  AUCinf will be calculated from the PK plasma samples collected.

  Up to 29 days

• Ratio of Cmax of ASP3082 and ASP3082+CAR

  Ratios of Cmax will be calculated from the PK plasma samples collected.

  Up to 29 days

• Ratio of AUClast for ASP3082 and ASP3082+CAR

  Ratios of AUClast will be calculated from the PK plasma samples collected.

  Up to 29 days

• Ratio of AUCinf for ASP3082 and ASP3082+CAR

  Ratios of AUCinf will be calculated from the PK plasma samples collected.

  Up to 29 days

Secondary Outcomes (7)

• Number of Participants with Adverse Events (AEs)

  Up to 36 days

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

  Up to 36 days

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

  Up to 36 days

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

  Up to 36 days

• PK of FLZ in plasma: trough concentration (Ctrough)

  Up to 25 days

Study Arms (3)

Group 1: ASP3082 + Fluconazole

EXPERIMENTAL

Participants receive ASP3082 on Days 1 and 15 and fluconazole on Days 8 to 28.

Drug: Setidegrasib; Drug: Fluconazole

Group 2: ASP3082 + Carbamazepine

EXPERIMENTAL

Participants receive ASP3082 on Days 1 and 22 and carbamazepine on Days 8 to 28.

Drug: Setidegrasib; Drug: Carbamazepine

Group 3: ASP3082 + Itraconazole

EXPERIMENTAL

Participants receive ASP3082 on Days 1 and 15 and itraconazole on Days 8 to 28.

Drug: Setidegrasib; Drug: Itraconazole

Interventions

Setidegrasib DRUG

Intravenous (IV) infusion

Also known as: ASP3082

Group 1: ASP3082 + Fluconazole; Group 2: ASP3082 + Carbamazepine; Group 3: ASP3082 + Itraconazole

Fluconazole DRUG

Oral

Group 1: ASP3082 + Fluconazole

Carbamazepine DRUG

Oral

Group 2: ASP3082 + Carbamazepine

Itraconazole DRUG

Oral

Group 3: ASP3082 + Itraconazole

Eligibility Criteria

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

You may qualify if:

• Participant is healthy and has no clinically significant medical condition based on the physical examination, electrocardiograms (ECGs) and protocol-defined clinical laboratory tests at screening or on day -1.
• Female participant is not pregnant and is not a woman of childbearing potential (WOCBP)
• Female participant must not be breastfeeding or lactating starting at screening and throughout the investigational period and for 5 half-lives (approximately 28 days after final study intervention administration).
• Female participant must not donate ova starting at first administration of study intervention and throughout the investigational period and for 3 months after final study intervention administration.
• Male participant must agree to use contraception with female partner(s) of childbearing potential (including breastfeeding partner) throughout the treatment period and for 3 months after final study intervention administration.
• Male participant 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 final study intervention administration.
• Male participant must not donate sperm during the treatment period and for 3 months after final 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 is positive for Human Leukocyte Antigen (HLA) -B15:02 or HLA-A31:01, for Group 2 only.
• Participant has been pregnant within 6 months prior to screening.
• 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 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 28 days) after the last dose of study drug administration or end-of-study visit (ESV), whichever is longer.
• 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), topical dermatological products (including corticosteroid products) and hormone replacement therapy (HRT).
• 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 any liver test result alkaline phosphatase (ALP), alanine aminotransferase (ALT), aspartate aminotransferase (AST) or total bilirubin (TBL )) ≥ 1.5 ×upper limit of normal (ULN ) on day -1.
• Participant has a creatinine level outside normal limits on day -1.
• Participant has any of the following conditions on day -1: a mean pulse \< 45 or \> 90 bpm, mean systolic blood pressure (SBP ) \> 140 mmHg, or 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 measurement may be taken.

Sponsors & Collaborators

• Astellas Pharma Global Development, Inc.: lead

Study Sites (1)

Parexel

Baltimore, Maryland, 21225, United States

RECRUITING

MeSH Terms

Interventions

Fluconazole; Carbamazepine; Itraconazole

Intervention Hierarchy (Ancestors)

Triazoles; Azoles; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Dibenzazepines; Heterocyclic Compounds, 3-Ring; Heterocyclic Compounds, Fused-Ring; Piperazines

Study Officials

• Medical Director

  Astellas Pharma 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: NON RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: January 28, 2026
• First Posted: February 9, 2026
• Study Start: February 3, 2026
• Primary Completion (Estimated): July 31, 2026
• Study Completion (Estimated): July 31, 2026
• Last Updated: March 5, 2026

Record last verified: 2026-03

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)