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A Safety Study of LY3526318 in Healthy Participants

A Safety, Tolerability and Pharmacokinetic Study of Single and Multiple Doses of LY3526318 in Healthy Participants

Status
Completed
Phases
Phase 1
Study type
Interventional
Source
ClinicalTrials.gov
Registry ID
NCT04682119
Enrollment
16
Registered
2020-12-23
Start date
2020-12-29
Completion date
2021-04-21
Last updated
2025-09-10

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

Brief summary

The main purpose of this study is to learn more about how the drug is absorbed in to the blood stream and how it is eliminated from the body. The safety and tolerability of LY3526318 will also be evaluated when given by mouth either by single or multiple doses to healthy participants. The study will have two parts. Each participant will enroll in only one part. For each participant, Part A will last up to 44 days and Part B will last up to 50 days, including screening and follow-up.

Interventions

Administered orally.

DRUGPlacebo

Administered orally.

Sponsors

Eli Lilly and Company
Lead SponsorINDUSTRY

Study design

Allocation
RANDOMIZED
Intervention model
SEQUENTIAL
Primary purpose
BASIC_SCIENCE
Masking
DOUBLE (Subject, Investigator)

Eligibility

Sex/Gender
ALL
Age
18 Years to 65 Years
Healthy volunteers
Yes

Inclusion criteria

* Are overtly healthy males or females, as determined through medical history and physical examination * Have a body mass index (BMI) between 18 and 32 kilograms per square meter (kg/m²) * Have clinical laboratory test results within normal reference range

Exclusion criteria

* Have a history or presence of medical illness including, but not limited to, cardiovascular, hepatic, respiratory, hematological, endocrine, psychiatric or neurological disease, convulsions, or any clinically significant laboratory abnormality * Have an abnormality in the 12-lead electrocardiogram (ECG) * Have a history of clinically significant multiple or severe drug allergies * Show evidence of human immunodeficiency virus (HIV) and/or positive human HIV antibodies, hepatitis C and/or positive hepatitis C antibody, or hepatitis B and/or positive hepatitis B surface antigen. * Have an abnormal blood pressure * Have received treatment with biologic agents (such as monoclonal antibodies, including marketed drugs) within 3 months or 5 half-lives (whichever is longer) * Are unwilling to stop herbal supplements, over the counter or prescription medicines * Are currently enrolled in a clinical drug study or any other type of medical research judged not to be scientifically or medically compatible with this study. * Participants with a history of drug abuse

Design outcomes

Primary

MeasureTime frameDescription
Part A - SAD, Pharmacokinetics (PK): Area Under the Concentration Time Curve From Time 0 to Infinity (AUC 0-∞) of LY3526318Predose,1, 2, 4, 6, 8,12, 24, 48, 72, 96 hours post-doseArea Under the Concentration Time Curve From Time 0 to Infinity (AUC 0-∞) of LY3526318
Part A - SAD, PK: Maximum Observed Drug Concentration (Cmax) of LY3526318Predose,1, 2, 4, 6, 8,12, 24, 48, 72, 96 hours post-dosePart A - SAD, PK: Maximum Observed Drug Concentration (Cmax) of LY3526318
Part B - MAD, PK: Area Under the Concentration Time Curve From Time Zero to the End of the Dosing Interval, Tau (AUC[0-tau ]) of LY3526318Day 5: Predose,1, 2, 4, 6, 8,12, 24 hours post dosePart B - MAD, PK: Area Under the Concentration Time Curve From Time Zero to the End of the Dosing Interval, Tau (AUC\[0-tau \]) of LY3526318
Part B - MAD, PK: Maximum Observed Drug Concentration (Cmax) of LY3526318Day 5: Predose,1, 2, 4, 6, 8,12, 24 hours post dosePart B - MAD, PK: Maximum Observed Drug Concentration (Cmax) of LY3526318

Secondary

MeasureTime frameDescription
Part A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)Single oral dose to up to 11 days of follow-upA TEAE started on or after the date and time of the first dose of study drug administered in this study, or started prior to the study drug administration but worsened after the study drug started. Clinically significant events were defined as SAEs and other non-serious adverse events (AEs). A summary of SAEs and other non-serious AEs is located in the Reported Adverse Events module.
Part A, Effect of a Meal on Pharmacokinetics of LY3526318: Time at Maximal Concentration (Tmax)Predose,1, 2, 4, 6, 8,12, 24, 48, 72, 96 hours post-dosePart A, Effect of a Meal on Pharmacokinetics of LY3526318: Time at Maximal Concentration (Tmax)
Part B, MAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)Up to 14 days following first doseA TEAE started on or after the date and time of the first dose of study drug administered in this study, or started prior to the study drug administration but worsened after the study drug started. Clinically significant events were defined as SAEs and other non-serious adverse events (AEs). A summary of SAEs and other non-serious AEs is located in the Reported Adverse Events module.
Part A, Effect of a Meal on Pharmacokinetics of LY3526318: Maximum Concentration (Cmax)Predose,1, 2, 4, 6, 8,12, 24, 48, 72, 96 hours post-dosePart A, Effect of a meal on pharmacokinetics of LY3526318: Maximum Concentration (Cmax)
Part A, Effect of a Meal on Pharmacokinetics of LY3526318: Area Under the Concentration Time Curve From Time 0 to Infinity (AUC 0-∞)Predose,1, 2, 4, 6, 8,12, 24, 48, 72, 96 hours post-dosePart A, Effect of a meal on pharmacokinetics of LY3526318: Area under the concentration time curve from time 0 to infinity (AUC 0-∞)

Countries

Netherlands

Participant flow

Pre-assignment details

This study consists of 2 parts: * Part A: Single-ascending dose (SAD, \[including a food effect (FE)\]). * Part B: Multiple-ascending dose (MAD), \[including a food effect (FE)\]). Both parts were randomized, double-blind, and placebo-controlled.

Participants by arm

ArmCount
Part A SAD: Sequence P1-L2-L3-L4
P1: Participants received placebo administered orally under fasted condition during period 1. L2: Participants received 250 mg LY3526318 administered orally under fasted condition during period 2. L3: Participants received 250 mg LY3526318 administered orally in fed state after a light breakfast during period 3. L4: Participants received 250 mg LY3526318 administered orally in fed state after a high-fat breakfast during period 4.
2
Part A SAD: L1-P1-L3-L4
L1: Participants received 100 mg LY3526318 administered orally under fasted condition during period 1. P1: Participants received placebo administered orally under fasted condition during period 2. L3: Participants received 250 mg LY3526318 administered orally in fed state after a light breakfast during period 3. L4: Participants received 250 mg LY3526318 administered orally in fed state after a high-fat breakfast during period 4.
2
Part A SAD: L1-L2-P3-L4
L1: Participants received 100 mg LY3526318 administered orally under fasted condition during period 1. L2: Participants received 250 mg LY3526318 administered orally under fasted conditions during period 2. P3: Participants received placebo administered orally in fed state after a light breakfast during period 3. L4: Participants received 250 mg LY3526318 administered orally in fed state after a high-fat breakfast during period 4.
2
Part A: L1-L2-L3-P4
L1: Participants received 100 mg LY3526318 administered orally under fasted condition during period 1 L2: Participants received 250 mg LY3526318 administered orally under fasted condition during period 2. L3: Participants received 250 mg LY3526318 administered orally in fed state after a light breakfast during period 3. P4: Participants received placebo administered orally in fed state after a high-fat breakfast during period 4.
2
Part B MAD: Placebo
Participants received placebo administered orally under fasted conditions on Day 1 and Day 5 and in fed state after participants ate a standard breakfast without respect to dosing time on Day 2 to Day 4
2
Part B MAD: 250 mg LY3526318
Participants received 250 mg LY3526318 administered orally under fasted conditions on Day 1 and Day 5 and in fed state after participants ate a standard breakfast without respect to dosing time on Day 2 to Day 4.
6
Total16

Baseline characteristics

CharacteristicPart A SAD: Sequence P1-L2-L3-L4TotalPart B MAD: 250 mg LY3526318Part B MAD: PlaceboPart A: L1-L2-L3-P4Part A SAD: L1-L2-P3-L4Part A SAD: L1-P1-L3-L4
Age, Continuous52 years
STANDARD_DEVIATION 4
40 years
STANDARD_DEVIATION 16.57
35 years
STANDARD_DEVIATION 21
31 years
STANDARD_DEVIATION 14
43 years
STANDARD_DEVIATION 13
59 years
STANDARD_DEVIATION 3
31 years
STANDARD_DEVIATION 11
Ethnicity (NIH/OMB)
Hispanic or Latino
0 Participants1 Participants0 Participants0 Participants0 Participants1 Participants0 Participants
Ethnicity (NIH/OMB)
Not Hispanic or Latino
2 Participants15 Participants6 Participants2 Participants2 Participants1 Participants2 Participants
Ethnicity (NIH/OMB)
Unknown or Not Reported
0 Participants0 Participants0 Participants0 Participants0 Participants0 Participants0 Participants
Race (NIH/OMB)
American Indian or Alaska Native
0 Participants1 Participants0 Participants0 Participants0 Participants0 Participants1 Participants
Race (NIH/OMB)
Asian
0 Participants1 Participants0 Participants1 Participants0 Participants0 Participants0 Participants
Race (NIH/OMB)
Black or African American
0 Participants0 Participants0 Participants0 Participants0 Participants0 Participants0 Participants
Race (NIH/OMB)
More than one race
0 Participants1 Participants0 Participants0 Participants0 Participants1 Participants0 Participants
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
0 Participants0 Participants0 Participants0 Participants0 Participants0 Participants0 Participants
Race (NIH/OMB)
Unknown or Not Reported
0 Participants0 Participants0 Participants0 Participants0 Participants0 Participants0 Participants
Race (NIH/OMB)
White
2 Participants13 Participants6 Participants1 Participants2 Participants1 Participants1 Participants
Region of Enrollment
Netherlands
2 Participants16 Participants6 Participants2 Participants2 Participants2 Participants2 Participants
Sex: Female, Male
Female
1 Participants10 Participants4 Participants2 Participants1 Participants1 Participants1 Participants
Sex: Female, Male
Male
1 Participants6 Participants2 Participants0 Participants1 Participants1 Participants1 Participants

Adverse events

Event typeEG000
affected / at risk
EG001
affected / at risk
EG002
affected / at risk
EG003
affected / at risk
EG004
affected / at risk
EG005
affected / at risk
EG006
affected / at risk
EG007
affected / at risk
EG008
affected / at risk
deaths
Total, all-cause mortality
0 / 20 / 20 / 40 / 60 / 60 / 60 / 60 / 20 / 6
other
Total, other adverse events
1 / 21 / 22 / 44 / 61 / 62 / 62 / 61 / 24 / 6
serious
Total, serious adverse events
0 / 20 / 20 / 40 / 60 / 60 / 60 / 60 / 20 / 6

Outcome results

Primary

Part A - SAD, Pharmacokinetics (PK): Area Under the Concentration Time Curve From Time 0 to Infinity (AUC 0-∞) of LY3526318

Area Under the Concentration Time Curve From Time 0 to Infinity (AUC 0-∞) of LY3526318

Time frame: Predose,1, 2, 4, 6, 8,12, 24, 48, 72, 96 hours post-dose

Population: Part A - SAD: All participants who received at least one dose of study drug and had evaluable PK data.

ArmMeasureValue (GEOMETRIC_MEAN)Dispersion
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part A - SAD, Pharmacokinetics (PK): Area Under the Concentration Time Curve From Time 0 to Infinity (AUC 0-∞) of LY3526318147978 nanograms*hours per milliliter (ng*h/mL)Geometric Coefficient of Variation 37.5
Part A - SAD: 250 mg LY3526318 Fed (High Fat Meal)Part A - SAD, Pharmacokinetics (PK): Area Under the Concentration Time Curve From Time 0 to Infinity (AUC 0-∞) of LY3526318131271 nanograms*hours per milliliter (ng*h/mL)Geometric Coefficient of Variation 61.8
Part A - SAD: 250 mg LY3526318 FastedPart A - SAD, Pharmacokinetics (PK): Area Under the Concentration Time Curve From Time 0 to Infinity (AUC 0-∞) of LY3526318137814 nanograms*hours per milliliter (ng*h/mL)Geometric Coefficient of Variation 58.6
Part A - SAD: 100 mg LY3526318 FastedPart A - SAD, Pharmacokinetics (PK): Area Under the Concentration Time Curve From Time 0 to Infinity (AUC 0-∞) of LY352631876902 nanograms*hours per milliliter (ng*h/mL)Geometric Coefficient of Variation 56.1
Primary

Part A - SAD, PK: Maximum Observed Drug Concentration (Cmax) of LY3526318

Part A - SAD, PK: Maximum Observed Drug Concentration (Cmax) of LY3526318

Time frame: Predose,1, 2, 4, 6, 8,12, 24, 48, 72, 96 hours post-dose

Population: Part A - SAD: All participants who received at least one dose of study drug and had evaluable PK data.

ArmMeasureValue (GEOMETRIC_MEAN)Dispersion
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part A - SAD, PK: Maximum Observed Drug Concentration (Cmax) of LY352631812406 nanograms per milliliter (ng/mL)Geometric Coefficient of Variation 26.4
Part A - SAD: 250 mg LY3526318 Fed (High Fat Meal)Part A - SAD, PK: Maximum Observed Drug Concentration (Cmax) of LY35263186199 nanograms per milliliter (ng/mL)Geometric Coefficient of Variation 61.4
Part A - SAD: 250 mg LY3526318 FastedPart A - SAD, PK: Maximum Observed Drug Concentration (Cmax) of LY35263189544 nanograms per milliliter (ng/mL)Geometric Coefficient of Variation 26.8
Part A - SAD: 100 mg LY3526318 FastedPart A - SAD, PK: Maximum Observed Drug Concentration (Cmax) of LY35263185441 nanograms per milliliter (ng/mL)Geometric Coefficient of Variation 49.9
Primary

Part B - MAD, PK: Area Under the Concentration Time Curve From Time Zero to the End of the Dosing Interval, Tau (AUC[0-tau ]) of LY3526318

Part B - MAD, PK: Area Under the Concentration Time Curve From Time Zero to the End of the Dosing Interval, Tau (AUC\[0-tau \]) of LY3526318

Time frame: Day 5: Predose,1, 2, 4, 6, 8,12, 24 hours post dose

Population: Part B - MAD: All participants who received at least one dose of study drug and had evaluable PK data.

ArmMeasureValue (GEOMETRIC_MEAN)Dispersion
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part B - MAD, PK: Area Under the Concentration Time Curve From Time Zero to the End of the Dosing Interval, Tau (AUC[0-tau ]) of LY352631889614 ng*h/mLGeometric Coefficient of Variation 19.7
Primary

Part B - MAD, PK: Maximum Observed Drug Concentration (Cmax) of LY3526318

Part B - MAD, PK: Maximum Observed Drug Concentration (Cmax) of LY3526318

Time frame: Day 5: Predose,1, 2, 4, 6, 8,12, 24 hours post dose

Population: Part B - MAD: All participants who received at least one dose of study drug and had evaluable PK data.

ArmMeasureValue (GEOMETRIC_MEAN)Dispersion
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part B - MAD, PK: Maximum Observed Drug Concentration (Cmax) of LY352631810717 nanograms per milliliter (ng/mL)Geometric Coefficient of Variation 35.1
Secondary

Part A, Effect of a Meal on Pharmacokinetics of LY3526318: Area Under the Concentration Time Curve From Time 0 to Infinity (AUC 0-∞)

Part A, Effect of a meal on pharmacokinetics of LY3526318: Area under the concentration time curve from time 0 to infinity (AUC 0-∞)

Time frame: Predose,1, 2, 4, 6, 8,12, 24, 48, 72, 96 hours post-dose

Population: Part A, SAD: All participants who received 250 mg LY3526318 and had evaluable PK data.

ArmMeasureGroupValue (NUMBER)
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part A, Effect of a Meal on Pharmacokinetics of LY3526318: Area Under the Concentration Time Curve From Time 0 to Infinity (AUC 0-∞)Ratio of Fed Light Breakfast/ Fasted1.1341 unitless
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part A, Effect of a Meal on Pharmacokinetics of LY3526318: Area Under the Concentration Time Curve From Time 0 to Infinity (AUC 0-∞)Ratio of Fed High Fat Meal/ Fasted0.8454 unitless
Secondary

Part A, Effect of a Meal on Pharmacokinetics of LY3526318: Maximum Concentration (Cmax)

Part A, Effect of a meal on pharmacokinetics of LY3526318: Maximum Concentration (Cmax)

Time frame: Predose,1, 2, 4, 6, 8,12, 24, 48, 72, 96 hours post-dose

Population: Part A, SAD: All participants who received 250 mg LY3526318 and had evaluable PK data.

ArmMeasureGroupValue (NUMBER)
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part A, Effect of a Meal on Pharmacokinetics of LY3526318: Maximum Concentration (Cmax)Ratio of Fed Light Breakfast/ Fasted1.2768 unitless
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part A, Effect of a Meal on Pharmacokinetics of LY3526318: Maximum Concentration (Cmax)Ratio of Fed High Fat Meal/ Fasted0.6195 unitless
Secondary

Part A, Effect of a Meal on Pharmacokinetics of LY3526318: Time at Maximal Concentration (Tmax)

Part A, Effect of a Meal on Pharmacokinetics of LY3526318: Time at Maximal Concentration (Tmax)

Time frame: Predose,1, 2, 4, 6, 8,12, 24, 48, 72, 96 hours post-dose

Population: Part A, SAD: All participants who received 250 mg LY3526318 and had evaluable PK data

ArmMeasureGroupValue (NUMBER)
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part A, Effect of a Meal on Pharmacokinetics of LY3526318: Time at Maximal Concentration (Tmax)Fed Light Breakfast - Fasted0.00 hours
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part A, Effect of a Meal on Pharmacokinetics of LY3526318: Time at Maximal Concentration (Tmax)Fed High Fat Meal - Fasted0.03 hours
Secondary

Part A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

A TEAE started on or after the date and time of the first dose of study drug administered in this study, or started prior to the study drug administration but worsened after the study drug started. Clinically significant events were defined as SAEs and other non-serious adverse events (AEs). A summary of SAEs and other non-serious AEs is located in the Reported Adverse Events module.

Time frame: Single oral dose to up to 11 days of follow-up

Population: Part A, SAD: All participants who received at least one dose of study drug.

ArmMeasureGroupValue (COUNT_OF_PARTICIPANTS)
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)TEAEs2 Participants
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)SAEs0 Participants
Part A - SAD: 250 mg LY3526318 Fed (High Fat Meal)Part A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)TEAEs1 Participants
Part A - SAD: 250 mg LY3526318 Fed (High Fat Meal)Part A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)SAEs0 Participants
Part A - SAD: 250 mg LY3526318 FastedPart A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)TEAEs1 Participants
Part A - SAD: 250 mg LY3526318 FastedPart A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)SAEs0 Participants
Part A - SAD: 100 mg LY3526318 FastedPart A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)TEAEs2 Participants
Part A - SAD: 100 mg LY3526318 FastedPart A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)SAEs0 Participants
Part A - SAD: 250 mg LY3526318 FastedPart A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)SAEs0 Participants
Part A - SAD: 250 mg LY3526318 FastedPart A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)TEAEs2 Participants
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)TEAEs4 Participants
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)SAEs0 Participants
Part A - SAD: 250 mg LY3526318 Fed (High Fat Meal)Part A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)SAEs0 Participants
Part A - SAD: 250 mg LY3526318 Fed (High Fat Meal)Part A, SAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)TEAEs1 Participants
Secondary

Part B, MAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

A TEAE started on or after the date and time of the first dose of study drug administered in this study, or started prior to the study drug administration but worsened after the study drug started. Clinically significant events were defined as SAEs and other non-serious adverse events (AEs). A summary of SAEs and other non-serious AEs is located in the Reported Adverse Events module.

Time frame: Up to 14 days following first dose

Population: Part B, MAD: All participants who received at least one dose of study drug.

ArmMeasureGroupValue (COUNT_OF_PARTICIPANTS)
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part B, MAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)TEAEs1 Participants
Part A - SAD: 250 mg LY3526318 Fed (Light Breakfast)Part B, MAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)SAEs0 Participants
Part A - SAD: 250 mg LY3526318 Fed (High Fat Meal)Part B, MAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)TEAEs4 Participants
Part A - SAD: 250 mg LY3526318 Fed (High Fat Meal)Part B, MAD: Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)SAEs0 Participants

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026