A Study of Imlunestrant (LY3484356) in Female Healthy Participants

NCT05444556 | Completed Phase 1 Results FDA Drug

• 2 other identifiers: 18413J2J-MC-JZLI
• Study Type: interventional
• Target: 113
• Locations: 1 country
• Sites: 3

Brief Summary

The main purpose of this study is to evaluate the effect of imlunestrant on repaglinide, omeprazole and dextromethorphan, and rosuvastatin and digoxin. The study will also investigate the effect of quinidine on imlunestrant in female healthy participants of non-childbearing potential. The safety and tolerability of imlunestrant will be investigated in female healthy participants of non-childbearing potential. The study will last approximately up to 32 days for each participant excluding the screening period.

Conditions

Healthy

Outcome Measures

Primary Outcomes (16)

• Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Repaglinide (Cohort 1)

  PK: AUC\[0-∞\] of Repaglinide

  Day 1 and Day 3: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12 and 24 hours post-dose

• PK: Maximum Observed Concentration (Cmax) of Repaglinide (Cohort 1)

  PK: Cmax of Repaglinide

  Day 1 and Day 3: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12 and 24 hours post-dose

• PK: AUC[0-∞] of Omeprazole (Cohort 2)

  PK: AUC\[0-∞\] of Omeprazole

  Day 1: Predose, 0.5, 1, 2, 3, 4, 6, 8,12, and 24 h postdose; Day 3: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, and 48 h postdose

• PK: Cmax of Omeprazole (Cohort 2)

  PK: Cmax of Omeprazole

  Day 1: Predose, 0.5, 1, 2, 3, 4, 6, 8,12, and 24 h postdose; Day 3: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, and 48 h postdose

• PK: AUC[0-∞] of Omeprazole Metabolite: 5-hydroxyomeprazole (Cohort 2)

  5-hydroxyomeprazole is a major metabolite of omeprazole.

  Day 1: Predose, 0.5, 1, 2, 3, 4, 6, 8,12, and 24 h postdose; Day 3: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, and 48 h postdose

• PK: Cmax of Omeprazole Metabolite: 5-hydroxyomeprazole (Cohort 2)

  5-hydroxyomeprazole is a major metabolite of omeprazole.

  Day 1: Predose, 0.5, 1, 2, 3, 4, 6, 8,12, and 24 h postdose; Day 3: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, and 48 h postdose

• PK: AUC[0-∞] of Dextromethorphan (Cohort 2)

  PK: AUC\[0-∞\] of Dextromethorphan

  Day 1: Predose, 0.5, 1, 2, 3, 4, 6, 8,12, and 24 h postdose; Day 3: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, and 48 h postdose

• PK: Cmax of Dextromethorphan (Cohort 2)

  PK: Cmax of Dextromethorphan

  Day 1: Predose, 0.5, 1, 2, 3, 4, 6, 8,12, and 24 h postdose; Day 3: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, and 48 h postdose

• PK: Area Under the Concentration Versus Time Curve (AUC) From Time Zero to Tlast (AUC[0-tlast]) of Dextromethorphan Metabolite: Dextrorphan (Cohort 2)

  Dextrorphan is a major metabolite of Dextromethorphan.

  Day 1: Predose, 0.5, 1, 2, 3, 4, 6, 8,12, and 24 h postdose; Day 3: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, and 48 h postdose

• PK: Cmax of Dextromethorphan Metabolite: Dextrorphan (Cohort 2)

  Dextrorphan is a major metabolite of Dextromethorphan.

  Day 1: Predose, 0.5, 1, 2, 3, 4, 6, 8,12, and 24 h postdose; Day 3: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, and 48 h postdose

• PK: AUC[0-∞] of Imlunestrant (Cohort 3)

  PK: AUC\[0-∞\] of Imlunestrant

  Day 1 and Day 18: Predose, 1, 2, 3, 4, 5, 6 ,8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 h post dose

• PK: Cmax of Imlunestrant (Cohort 3)

  PK: Cmax of Imlunestrant

  Day 1 and Day 18: Predose, 1, 2, 3, 4, 5, 6 ,8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 h post dose

• PK: AUC[0-∞] of Rosuvastatin (Cohort 4)

  PK: AUC\[0-∞\] of Rosuvastatin

  Day 1: Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, 72, and 96 h post dose; Day 10: Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, 72, 96, and 120 h post dose

• PK: Cmax of Rosuvastatin (Cohort 4)

  PK: Cmax of Rosuvastatin

  Day 1: Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, 72, and 96 h post dose; Day 10: Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, 72, 96, and 120 h post dose

• PK: AUC[0-∞] of Digoxin (Cohort 4)

  PK: AUC\[0-∞\] of Digoxin

  Day 1: Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, 72, and 96 h post dose; Day 10: Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, 72, 96, and 120 h post dose

• PK: Cmax of Digoxin (Cohort 4)

  PK: Cmax of Digoxin

  Day 1: Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, 72, and 96 h post dose; Day 10: Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, 72, 96, and 120 h post dose

Study Arms (4)

Imlunestrant + Repaglinide (Cohort 1)

EXPERIMENTAL

Participants received: Day 1: A single oral dose of 0.5 mg repaglinide administered alone. Day 3: A single oral dose of 800 mg imlunestrant, followed approximately 2 hours later by 0.5 mg repaglinide, both administered orally.

Drug: Imlunestrant; Drug: Repaglinide

mlunestrant + Omeprazole & Dextromethorphan (Cohort 2)

EXPERIMENTAL

Participants received: Day 1: A single oral dose of 20 mg omeprazole and 30 mg dextromethorphan, administered in the morning. Day 3: A single oral dose of 800 mg imlunestrant, followed immediately by 20 mg omeprazole and 30 mg dextromethorphan, all administered orally.

Drug: Imlunestrant; Drug: Omeprazole; Drug: Dextromethorphan

Imlunestrant + Quinidine (Cohort 3)

EXPERIMENTAL

Participants received: Day 1: A single oral dose of 400 mg imlunestrant, administered in the morning. Days 15 to 17 and 19 to 24: Twice-daily oral doses of 200 mg quinidine, administered alone. Day 18: A single oral dose of 400 mg imlunestrant administered in combination with 200 mg quinidine (quinidine was dosed twice on this day as part of the regular regimen).

Drug: Imlunestrant; Drug: Quinidine

Imlunestrant + Rosuvastatin & Digoxin (Cohort 4)

EXPERIMENTAL

Participants received: Day 1: A single oral dose of 10 mg rosuvastatin and 0.25 mg digoxin, administered in the morning. Day 10: A single oral dose of 400 mg imlunestrant, administered in combination with 10 mg rosuvastatin and 0.25 mg digoxin, all administered orally.

Drug: Imlunestrant; Drug: Rosuvastatin; Drug: Digoxin

Interventions

Repaglinide DRUG

Administered orally.

Imlunestrant + Repaglinide (Cohort 1)

Omeprazole DRUG

Administered orally.

mlunestrant + Omeprazole & Dextromethorphan (Cohort 2)

Dextromethorphan DRUG

Administered orally.

mlunestrant + Omeprazole & Dextromethorphan (Cohort 2)

Quinidine DRUG

Administered orally.

Imlunestrant + Quinidine (Cohort 3)

Rosuvastatin DRUG

Administered orally.

Imlunestrant + Rosuvastatin & Digoxin (Cohort 4)

Digoxin DRUG

Administered orally.

Imlunestrant + Rosuvastatin & Digoxin (Cohort 4)

Imlunestrant DRUG

Administered orally.

Also known as: LY3484356

Imlunestrant + Quinidine (Cohort 3); Imlunestrant + Repaglinide (Cohort 1); Imlunestrant + Rosuvastatin & Digoxin (Cohort 4); mlunestrant + Omeprazole & Dextromethorphan (Cohort 2)

Eligibility Criteria

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

You may qualify if:

• Participants who are overtly healthy as determined by medical assessment
• Body mass index (BMI) within the range 18.0 to 35.0 kilograms per meter squared (kg/m²)
• Female participants of non childbearing potential.

You may not qualify if:

• Have known allergies to imlunestrant, related compounds or any components of the formulation, repaglinide, omeprazole, dextromethorphan, quinidine, rosuvastatin, or digoxin, as appropriate, or history of significant atopy.
• Significant history or clinical manifestation of any metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, respiratory, endocrine, or psychiatric disorder, as determined by the investigator
• Use or intend to use any medications/products known to alter drug absorption, metabolism, or elimination processes, including St. John's wort, within 30 days prior to dosing
• Use or intend to use any prescription medications/products within 14 days prior to first dose until completion of the follow-up visit, unless deemed acceptable by the investigator (or designee), including but not limited to medications that inhibit or induce cytochrome P450 (CYP) 2C8, CYP2C19, CYP2D6, P-glycoprotein (P-gp) or breast cancer resistance protein (BCRP).

Sponsors & Collaborators

• Eli Lilly and Company: lead

Study Sites (3)

Altasciences Clinical Los Angeles, Inc

Cypress, California, 90630, United States

Location

Qps-Mra, Llc

South Miami, Florida, 33143-4875, United States

Location

ICON Early Phase Services

San Antonio, Texas, 78209, United States

Location

MeSH Terms

Interventions

Imlunestrant; repaglinide; Omeprazole; Dextromethorphan; Quinidine; Rosuvastatin Calcium; Digoxin

Intervention Hierarchy (Ancestors)

2-Pyridinylmethylsulfinylbenzimidazoles; Sulfoxides; Sulfur Compounds; Organic Chemicals; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Benzimidazoles; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Morphinans; Opiate Alkaloids; Alkaloids; Heterocyclic Compounds, Bridged-Ring; Heterocyclic Compounds, 4 or More Rings; Phenanthrenes; Polycyclic Aromatic Hydrocarbons; Polycyclic Compounds; Cinchona Alkaloids; Quinuclidines; Quinolines; Sulfonamides; Amides; Fluorobenzenes; Hydrocarbons, Fluorinated; Hydrocarbons, Halogenated; Hydrocarbons; Sulfones; Pyrimidines; Digitalis Glycosides; Cardenolides; Cardiac Glycosides; Cardanolides; Steroids; Fused-Ring Compounds; Glycosides; Carbohydrates

Results Point of Contact

• Title: Chief Medical Officer
• Organization: Eli Lilly and Company

ClinicalTrials.gov@lilly.com

800-545-5979

Study Officials

• Call 1-877-CTLILLY (1-877-285-4559) or 1-317-615-4559 Mon - Fri 9 AM - 5 PM Eastern time (UTC/GMT - 5 hours, EST)

  Eli Lilly and Company

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: GT60
• Restrictive Agreement: Yes

Study Design

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

Study Record Dates

• First Submitted: June 30, 2022
• First Posted: July 6, 2022
• Study Start: July 7, 2022
• Primary Completion: November 2, 2022
• Study Completion: November 2, 2022
• Last Updated: December 12, 2025
• Results First Posted: December 12, 2025

Record last verified: 2025-11-15

Data Sharing

• IPD Sharing: Will not share

Locations

US (3)