Phase 1
N=113
A Study of Imlunestrant (LY3484356) in Female Healthy Participants
Healthy
Bottom Line
View on ClinicalTrials.gov: NCT05444556 ↗Enrolled (actual)
113
Serious AEs
0.0%
Results posted
Dec 2025
Primary outcome: Primary: Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Repaglinide (Cohort 1) — 13.0; 13.6 nanogram*hour per milliliter (ng*hr/mL)
Study Design & Population
- Study type
- Interventional
- Phase
- Phase 1
- Interventions
- Imlunestrant (Drug); Repaglinide (Drug); Omeprazole (Drug); Dextromethorphan (Drug); Quinidine (Drug); Rosuvastatin (Drug); Digoxin (Drug)
- Age
- Adult, Older Adult · 18+ yrs
- Sex
- Female
- Sponsor
- Eli Lilly and Company
- Primary completion
- Nov 2022
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Repaglinide (Cohort 1) |
13.0; 13.6 | — |
| PRIMARY PK: Maximum Observed Concentration (Cmax) of Repaglinide (Cohort 1) |
10.5; 9.84 | — |
| PRIMARY PK: AUC[0-∞] of Omeprazole (Cohort 2) |
703; 825 | — |
| PRIMARY PK: Cmax of Omeprazole (Cohort 2) |
316; 405 | — |
| PRIMARY PK: AUC[0-∞] of Omeprazole Metabolite: 5-hydroxyomeprazole (Cohort 2) |
571; 592 | — |
| PRIMARY PK: Cmax of Omeprazole Metabolite: 5-hydroxyomeprazole (Cohort 2) |
200; 230 | — |
| PRIMARY PK: AUC[0-∞] of Dextromethorphan (Cohort 2) |
14.7; 16.1 | — |
| PRIMARY PK: Cmax of Dextromethorphan (Cohort 2) |
0.864; 1.13 | — |
| PRIMARY PK: Area Under the Concentration Versus Time Curve (AUC) From Time Zero to Tlast (AUC[0-tlast]) of Dextromethorphan Metabolite: Dextrorphan (Cohort 2) |
11.8; 11.9 | — |
| PRIMARY PK: Cmax of Dextromethorphan Metabolite: Dextrorphan (Cohort 2) |
1.79; 1.97 | — |
| PRIMARY PK: AUC[0-∞] of Imlunestrant (Cohort 3) |
1970; 1870 | — |
| PRIMARY PK: Cmax of Imlunestrant (Cohort 3) |
61.0; 54.3 | — |
| PRIMARY PK: AUC[0-∞] of Rosuvastatin (Cohort 4) |
29.0; 44.9 | — |
| PRIMARY PK: Cmax of Rosuvastatin (Cohort 4) |
2.99; 5.08 | — |
| PRIMARY PK: AUC[0-∞] of Digoxin (Cohort 4) |
20.2; 28.0 | — |
| PRIMARY PK: Cmax of Digoxin (Cohort 4) |
1.17; 1.88 | — |
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.
Eligibility Criteria
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).
Data sourced from ClinicalTrials.gov (NCT05444556). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.