A Study of [14C]-LY3866288 in Healthy Participants

A Phase 1, Open-label, 2-part Study of the Absorption, Metabolism, and Excretion, and Absolute Bioavailability of [14C]-LY3866288 in Healthy Participants

The main purpose of this study is to evaluate how much of the study drug (LY3866288), administered as a single dose that has the radioactive substance 14C incorporated into it, passes from blood into urine, feces and expired air in healthy participants. The study will also measure how much of the study drug gets into the bloodstream when taken orally, compared to when injected directly into the vein, how its broken down, and how long it takes the body to get rid of it. The study will also evaluate the safety and tolerability of LY3866288.The study is conducted in two parts. The study is expected to last approximately 68 days.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: [14C]-LY3866288; Drug: [14C]-LY3866288; Drug: LY3866288

• Study Type: Interventional
• Enrollment (Actual): 15
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Wisconsin
    • Madison, Wisconsin, United States, 53704
      • Fortrea Clinical Research Unit

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• Male and female participants who are overtly healthy determined by medical history, physical examination, 12-lead ECGs, vital signs measurements, and clinical laboratory evaluations at screening and/or check-in by the investigator
• Have Body mass index between 18.0 and 32.0 kg/m^2 (kilograms per meter squared)
• Male participants who are infertile via bilateral orchiectomy or vasectomy
• Female participants (non-childbearing potential only for Part A) who follow standard contraceptive methods

Exclusion Criteria:

• Female participants who are lactating or pregnant
• Have history of alcohol and/or drug abuse within 2 years prior to screening
• Have history or presence of any diseases or conditions of clinical significance by the Investigator (or designee) and/or Sponsor
• Have history of significant hypersensitivity, intolerance, or allergy to any drug compound, food, or other substance, unless approved by the investigator

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: N/A
• Interventional Model: Parallel Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Part A: [14C]-LY3866288; Single dose of [¹⁴C]-LY3866288 administered orally.	Drug: [14C]-LY3866288; Administered orally.; Drug: [14C]-LY3866288; Administered IV.
Experimental: Part B: LY3866288 + [14C]-LY3866288; Single dose of LY3866288 administered orally followed by a single dose of [¹⁴C]-LY3866288 administered intravenously (IV).	Drug: [14C]-LY3866288; Administered orally.; Drug: [14C]-LY3866288; Administered IV.; Drug: LY3866288; Administered orally.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Part A, Fraction of [14C]-LY3866288 Dose Excreted in Urine (Feur) Expressed as a Percentage of the Total Radioactive Dose Administered	Predose up to Day 21 postdose
Part A, Fraction of Dose [14C]-LY3866288 Excreted in Feces Expressed as a Percentage of the Total Radioactive Dose Administered	Predose up to Day 21 postdose
Part B, Absolute Bioavailability (Fabs) of LY3866288	Predose up to Day 9 postdose

Secondary Outcome Measures

Outcome Measure	Time Frame
Part A: Pharmacokinetics (PK): Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-∞) of LY3866288 in Plasma Following a Single Oral Dose of [14C]-LY3866288	Predose up to Day 7 postdose
Part A: Pharmacokinetics (PK): Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-∞) of Total Radioactivity in Plasma and Whole Blood Following a Single Oral Dose of [14C]-LY3866288	Predose up to Day 21 postdose
Part A: PK: Maximum Observed Plasma Concentration (Cmax) of LY3866288 in Plasma Following a Single Oral Dose of [14C]-LY3866288	Predose up to Day 7 postdose
Part A: PK: Maximum Observed Plasma Concentration (Cmax) of Total Radioactivity in Plasma and Whole Blood Following a Single Oral Dose of [14C]-LY3866288	Predose up to Day 21 postdose
Part A: PK: Ratio of AUC0-inf of Plasma LY3866288 to AUC0-inf of Plasma Total Radioactivity	Predose up to Day 21 postdose
Part A: PK: Ratio of AUC0-inf of Whole Blood Total Radioactivity to AUC0-inf of Plasma Total Radioactivity	Predose up to Day 21 postdose
Part B: PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-∞) of LY3866288 in Plasma	Predose up to Day 9 postdose
Part B: PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-∞) of [14C]-LY3866288 in Plasma	Predose up to Day 9 postdose
Part B: PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-∞) of Total Radioactivity in Plasma	Predose up to Day 9 postdose
Part B: PK: Maximum Observed Plasma Concentration (Cmax) of LY3866288 in Plasma	Predose up to Day 9 postdose
Part B: PK: Maximum Observed Plasma Concentration (Cmax) of [14C]-LY3866288 in Plasma	Predose up to Day 9 postdose
Part B: PK: Maximum Observed Plasma Concentration (Cmax) of Total Radioactivity in Plasma	Predose up to Day 9 postdose

Collaborators and Investigators

• Sponsor: Eli Lilly and Company
• Investigators: Study Director: 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 record dates

Study Major Dates

• Study Start (Actual): October 28, 2024
• Primary Completion (Actual): January 3, 2025
• Study Completion (Actual): January 3, 2025

Study Registration Dates

• First Submitted: October 15, 2024
• First Submitted That Met QC Criteria: October 15, 2024
• First Posted (Actual): October 16, 2024

Study Record Updates

• Last Update Posted (Actual): March 25, 2025
• Last Update Submitted That Met QC Criteria: January 21, 2025
• Last Verified: January 1, 2025

More Information

Terms related to this study

• Keywords: Bioavailability; ADME; Disposition; Radioactive
• Other Study ID Numbers: 18885 (Stanford IRB); J4G-OX-JZVB (Other Identifier: Eli Lilly and Company)

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No