Trial Outcomes & Findings for A Study of Imlunestrant (LY3484356) in Healthy Women (NCT NCT05509816)

NCT ID: NCT05509816

Last Updated: 2025-11-12

Results Overview

PK: AUC\[0-∞\] of Midazolam

• Recruitment status: COMPLETED
• Study phase: PHASE1
• Target enrollment: 20 participants
• Primary outcome timeframe: Day 1: Predose, 0.25hours (h), 0.5h, 1h, 2h, 3h, 4h, 6h, 8h, 12h and 24h postdose; Day 9: Predose, 0.25h, 0.5h, 1h, 2h, 3h, 4h, 6h, 8h, 12h, 24, 36, 48h postdose
• Results posted on: 2025-11-12

Participant Flow

Participant milestones

Measure	Midazolam + Imlunestrant Participants received 400 milligram (mg) Imlunestrant (2 × 200 mg) tablets administered once daily (QD) orally for 7 days on Days 3 to 9 and a single dose of 0.5 mg midazolam solution orally on Day 1 and Day 9 as per below dosing sequence: Day 1: 0.5 mg midazolam alone Days 3 to 8: 400 mg imlunestrant QD alone Day 9: 0.5 mg midazolam + 400 mg imlunestrant There was a washout period of 8 days between doses of midazolam.
Overall Study STARTED	20
Overall Study Received at Least One Dose of Study Drug	20
Overall Study COMPLETED	19
Overall Study NOT COMPLETED	1

Reasons for withdrawal

Measure

Midazolam + Imlunestrant Participants received 400 milligram (mg) Imlunestrant (2 × 200 mg) tablets administered once daily (QD) orally for 7 days on Days 3 to 9 and a single dose of 0.5 mg midazolam solution orally on Day 1 and Day 9 as per below dosing sequence: Day 1: 0.5 mg midazolam alone Days 3 to 8: 400 mg imlunestrant QD alone Day 9: 0.5 mg midazolam + 400 mg imlunestrant There was a washout period of 8 days between doses of midazolam.

Overall Study Lost to Follow-up

1

Baseline Characteristics

A Study of Imlunestrant (LY3484356) in Healthy Women

Baseline characteristics by cohort

Measure	Midazolam + Imlunestrant n=20 Participants Participants received 400 mg Imlunestrant (2 × 200 mg) tablets administered QD orally for 7 days on Days 3 to 9 and a single 0.5 mg midazolam solution orally on Day 1 and Day 9 as per below dosing sequence: Day 1: 0.5 mg midazolam alone Days 3 to 8: 400 mg imlunestrant QD alone Day 9: 0.5 mg midazolam + 400 mg imlunestrant There was a washout period of 8 days between doses of midazolam.
Age, Continuous	50.8 years STANDARD_DEVIATION 7.5 • n=10 Participants
Sex: Female, Male Female	20 Participants n=10 Participants
Sex: Female, Male Male	0 Participants n=10 Participants
Ethnicity (NIH/OMB) Hispanic or Latino	14 Participants n=10 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	6 Participants n=10 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants n=10 Participants
Race (NIH/OMB) American Indian or Alaska Native	0 Participants n=10 Participants
Race (NIH/OMB) Asian	0 Participants n=10 Participants
Race (NIH/OMB) Native Hawaiian or Other Pacific Islander	0 Participants n=10 Participants
Race (NIH/OMB) Black or African American	5 Participants n=10 Participants
Race (NIH/OMB) White	15 Participants n=10 Participants
Race (NIH/OMB) More than one race	0 Participants n=10 Participants
Race (NIH/OMB) Unknown or Not Reported	0 Participants n=10 Participants
Region of Enrollment United States	20 Participants n=10 Participants

PRIMARY outcome

Timeframe: Day 1: Predose, 0.25hours (h), 0.5h, 1h, 2h, 3h, 4h, 6h, 8h, 12h and 24h postdose; Day 9: Predose, 0.25h, 0.5h, 1h, 2h, 3h, 4h, 6h, 8h, 12h, 24, 36, 48h postdose

Population: All participants who received at least one dose of study drug (midazolam) and had evaluable PK data.

PK: AUC[0-∞] of Midazolam

Outcome measures

Measure	0.5 mg Midazolam n=20 Participants Participants received single dose of 0.5 mg midazolam solution orally on Day 1.	0.5 mg Midazolam + 400 mg Imlunestrant n=20 Participants Participants received 0.5 mg midazolam solution orally in combination with 400 mg Imlunestrant (2 × 200 mg) tablets administered orally on Day 9.
Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Midazolam	12.3 nanogram*hour per milliliter (ng*hr/mL) Geometric Coefficient of Variation 32	11.4 nanogram*hour per milliliter (ng*hr/mL) Geometric Coefficient of Variation 41

PRIMARY outcome

Timeframe: Day 1: Predose, 0.25h, 0.5h, 1h, 2h, 3h, 4h, 6h, 8h, 12h and 24h postdose; Day 9: Predose, 0.25h, 0.5h, 1h, 2h, 3h, 4h, 6h, 8h, 12h, 24, 36, 48h postdose

Population: All participants who received at least one dose of study drug (midazolam) and had evaluable PK data.

PK: Cmax of Midazolam

Outcome measures

Measure	0.5 mg Midazolam n=20 Participants Participants received single dose of 0.5 mg midazolam solution orally on Day 1.	0.5 mg Midazolam + 400 mg Imlunestrant n=20 Participants Participants received 0.5 mg midazolam solution orally in combination with 400 mg Imlunestrant (2 × 200 mg) tablets administered orally on Day 9.
PK: Maximum Observed Concentration (Cmax) of Midazolam	3.84 nanograms per milliliter (ng/mL) Geometric Coefficient of Variation 35	4.12 nanograms per milliliter (ng/mL) Geometric Coefficient of Variation 31

SECONDARY outcome

Timeframe: Day 1: Predose, 0.25h, 0.5h, 1h, 2h, 3h, 4h, 6h, 8h, 12h and 24h postdose; Day 9: Predose, 0.25h, 0.5h, 1h, 2h, 3h, 4h, 6h, 8h, 12h, 24, 36, 48h postdose

Population: All participants who received at least one dose of study drug (midazolam) and had evaluable PK data.

PK: AUC[0-∞] of 1'-hydroxymidazolam

Outcome measures

Measure	0.5 mg Midazolam n=20 Participants Participants received single dose of 0.5 mg midazolam solution orally on Day 1.	0.5 mg Midazolam + 400 mg Imlunestrant n=20 Participants Participants received 0.5 mg midazolam solution orally in combination with 400 mg Imlunestrant (2 × 200 mg) tablets administered orally on Day 9.
PK: AUC[0-∞] of 1'-Hydroxymidazolam	2.75 ng*hr/mL Geometric Coefficient of Variation 40	2.26 ng*hr/mL Geometric Coefficient of Variation 40

SECONDARY outcome

Timeframe: Day 1: Predose, 0.25h, 0.5h, 1h, 2h, 3h, 4h, 6h, 8h, 12h and 24h postdose; Day 9: Predose, 0.25h, 0.5h, 1h, 2h, 3h, 4h, 6h, 8h, 12h, 24, 36, 48h postdose

Population: All participants who received at least one dose of study drug (midazolam) and had evaluable PK data.

PK: Cmax of 1'-hydroxymidazolam

Outcome measures

Measure	0.5 mg Midazolam n=20 Participants Participants received single dose of 0.5 mg midazolam solution orally on Day 1.	0.5 mg Midazolam + 400 mg Imlunestrant n=20 Participants Participants received 0.5 mg midazolam solution orally in combination with 400 mg Imlunestrant (2 × 200 mg) tablets administered orally on Day 9.
PK: Cmax of 1'-Hydroxymidazolam	0.748 ng/mL Geometric Coefficient of Variation 40	0.722 ng/mL Geometric Coefficient of Variation 35

SECONDARY outcome

Timeframe: Day 9: Predose, 0.25 h, 0.5h, 1h, 2h, 3h, 4h, 6h, 8h, 12h and 24h postdose

Population: All participants who received at least one dose of study drug (imlunestrant or midazolam) and had evaluable PK data.

PK: AUC[0-24], ss of Imlunestrant

Outcome measures

Measure	0.5 mg Midazolam n=20 Participants Participants received single dose of 0.5 mg midazolam solution orally on Day 1.	0.5 mg Midazolam + 400 mg Imlunestrant Participants received 0.5 mg midazolam solution orally in combination with 400 mg Imlunestrant (2 × 200 mg) tablets administered orally on Day 9.
PK: Area Under the Concentration Versus Time Curve From Zero to 24 Hours at Steady State (AUC[0-24], ss) of Imlunestrant When Dosed in the Presence of Midazolam	2020 ng*hr/mL Geometric Coefficient of Variation 53	—

SECONDARY outcome

Timeframe: Day 9: Predose, 0.25 h, 0.5h, 1h, 2h, 3h, 4h, 6h, 8h, 12h and 24h postdose

Population: All participants who received at least one dose of study drug (imlunestrant or midazolam) and had evaluable PK data.

PK: Cmax, ss of Imlunestrant when dosed in the presence of Midazolam is evaluated.

Outcome measures

Measure	0.5 mg Midazolam n=20 Participants Participants received single dose of 0.5 mg midazolam solution orally on Day 1.	0.5 mg Midazolam + 400 mg Imlunestrant Participants received 0.5 mg midazolam solution orally in combination with 400 mg Imlunestrant (2 × 200 mg) tablets administered orally on Day 9.
PK: Maximum Observed Concentration at Steady State (Cmax, ss) of Imlunestrant When Dosed in the Presence of Midazolam	120 ng/mL Geometric Coefficient of Variation 51	—

Adverse Events

0.5 mg Midazolam

Serious events: 0 serious events

Other events: 0 other events

Deaths: 0 deaths

400 mg Imlunestrant

Serious events: 0 serious events

Other events: 5 other events

Deaths: 0 deaths

0.5 mg Midazolam + 400 mg Imlunestrant

Serious events: 0 serious events

Other events: 1 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Measure	0.5 mg Midazolam n=20 participants at risk Participants received single dose of 0.5 mg midazolam solution orally on Day 1.	400 mg Imlunestrant n=20 participants at risk Participants received 400 mg imlunestrant (2 × 200 mg) tablets administered QD orally for 7 days on Days 3 to 8.	0.5 mg Midazolam + 400 mg Imlunestrant n=20 participants at risk Participants received 0.5 mg midazolam solution orally in combination with 400 mg Imlunestrant (2 × 200 mg) tablets administered orally on Day 9.
Gastrointestinal disorders Diarrhoea	0.00% 0/20 • Baseline Up to Day 18 All participants who received at least one dose of study drug (imlunestrant or midazolam). Participants were analyzed according to the treatment they actually received.	15.0% 3/20 • Number of events 4 • Baseline Up to Day 18 All participants who received at least one dose of study drug (imlunestrant or midazolam). Participants were analyzed according to the treatment they actually received.	5.0% 1/20 • Number of events 1 • Baseline Up to Day 18 All participants who received at least one dose of study drug (imlunestrant or midazolam). Participants were analyzed according to the treatment they actually received.
Nervous system disorders Headache	0.00% 0/20 • Baseline Up to Day 18 All participants who received at least one dose of study drug (imlunestrant or midazolam). Participants were analyzed according to the treatment they actually received.	10.0% 2/20 • Number of events 2 • Baseline Up to Day 18 All participants who received at least one dose of study drug (imlunestrant or midazolam). Participants were analyzed according to the treatment they actually received.	0.00% 0/20 • Baseline Up to Day 18 All participants who received at least one dose of study drug (imlunestrant or midazolam). Participants were analyzed according to the treatment they actually received.

Additional Information

Chief Medical Officer

Eli Lilly and Company

Phone: 08005455979

Email: ClinicalTrials.gov@lilly.com

Results disclosure agreements

• Principal investigator is a sponsor employee
• Publication restrictions are in place

Restriction type: GT60