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Completed

NCT Number: NCT05444556

A Study of Imlunestrant (LY3484356) in Female Healthy Participants

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.

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Key information

Conditions

Healthy

Age range

18 year–65 year

Sex eligibility

Female

Study type

Interventional

Phase

Phase 1

Primary location

Altasciences Clinical Los Angeles, Inc, Cypress, California, United States

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Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • 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.

Exclusion criteria

  • 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).

Treatment and study plan

Imlunestrant

Drug

Administered orally.

Other names: LY3484356

repaglinide

Drug

Administered orally.

Omeprazole

Drug

Administered orally.

dextromethorphan

Drug

Administered orally.

Quinidine

Drug

Administered orally.

Rosuvastatin

Drug

Administered orally.

Digoxin

Drug

Administered orally.

Primary outcomes

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

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

    PK: AUC[0-∞] of Repaglinide

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

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

    PK: Cmax of Repaglinide

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

    Time frame: 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

  4. PK: Cmax of Omeprazole (Cohort 2)

    Time frame: 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

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

    Time frame: 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

    5-hydroxyomeprazole is a major metabolite of omeprazole.

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

    Time frame: 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

    5-hydroxyomeprazole is a major metabolite of omeprazole.

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

    Time frame: 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

  8. PK: Cmax of Dextromethorphan (Cohort 2)

    Time frame: 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

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

    Time frame: 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

    Dextrorphan is a major metabolite of Dextromethorphan.

  10. PK: Cmax of Dextromethorphan Metabolite: Dextrorphan (Cohort 2)

    Time frame: 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

    Dextrorphan is a major metabolite of Dextromethorphan.

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

    Time frame: 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 Imlunestrant

  12. PK: Cmax of Imlunestrant (Cohort 3)

    Time frame: 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

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

    Time frame: 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 Rosuvastatin

  14. PK: Cmax of Rosuvastatin (Cohort 4)

    Time frame: 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

  15. PK: AUC[0-∞] of Digoxin (Cohort 4)

    Time frame: 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

  16. PK: Cmax of Digoxin (Cohort 4)

    Time frame: 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

Sponsors and collaborators

Lead sponsor

Eli Lilly and Company

Industry

Registry information

Official study title

The Effect of Imlunestrant on CYP2C8, CYP2C19, CYP2D6, P-gp, and BCRP Activity and the Effect of P-gp Inhibition on Imlunestrant Pharmacokinetics in Healthy Women of Non-childbearing Potential

Important dates

Study start
2022
Primary completion
2022
Study completion
2022
First posted
Jul 6, 2022
Registry last updated
Dec 12, 2025

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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