To Investigate the Effect of Retatrutide (LY3437943) on Metoprolol Pharmacokinetics in Healthy Participants

A Phase 1, Open-label, Single-arm Study to Investigate the Effect of Retatrutide on Metoprolol Pharmacokinetics in Healthy Participants

The purpose of this study J1I-MC-GZQE is to measure the effect of retatrutide on the pharmacokinetics (PK) of metoprolol in healthy participants.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Metoprolol; Drug: Retatrutide

• Study Type: Interventional
• Enrollment (Actual): 30
• Phase: Phase 1

Contacts and Locations

Study Locations

• Singapore
  • Singapore, Singapore, 138623
    • Lilly Centre for Clinical Pharmacology

Participation Criteria

Eligibility Criteria

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

Description

Inclusion Criteria:

• Are overtly healthy as determined by medical evaluation including medical history, physical examination, laboratory tests, and vital signs
• Have a body mass index (BMI) within the range 22.0 to 35.0 kilogram per square meter (kg/m2) (inclusive) at screening

Exclusion Criteria:

• Have history of diabetes (except gestational diabetes) or current diagnosis of diabetes (any form), or have glycated hemoglobin (HbA1c) greater than or equal to (≥) 6.5% (48 millimole/mole (mmol/mol)
• Have a mean supine screening pulse rate of less than 45 or greater than 100 beats per minute (bpm) from 2 assessments. If a repeat measurement (mean of 2 assessments) shows values within the range of 45 to 100 bpm, the participant may be included in the trial
• Have significant history of or current cardiovascular, respiratory, hepatic, renal, GI, endocrine, hematological, or neurological disorders capable of significantly altering the absorption, metabolism, or elimination of drugs; of constituting a risk when taking the study drug; or of interfering with the interpretation of data
• Had any of the following cardiovascular conditions prior to screening: acute myocardial infarction, cerebrovascular accident, unstable angina, or hospitalization due to congestive heart failure

Study Plan

How is the study designed?

Design Details

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

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Retatrutide; In period 1, participants will be administered a singe oral dose of metoprolol followed by a 1-week washout before retatrutide subcutaneous (SC) injection is given in period 2, followed by a second dose of metoprolol.	Drug: Metoprolol; Administered orally; Drug: Retatrutide; Administered subcutaneously (SC); Other Names: LY3437943

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Pharmacokinetics (PK): Area Under Concentration From Time Zero to Infinity (AUC[0-∞]) of Metoprolol	PK: AUC (0-∞) of Metoprolol	Day 1 to Day 3
Pharmacokinetics (PK): AUC (0-∞) of Metoprolol with Retatrutide	PK: AUC (0-∞) of Metoprolol with Retatrutide	Day 9 to Day 11
PK: Maximum Concentration (Cmax) of Metoprolol	PK: Cmax of Metoprolol	Day 1 to Day 3
PK: Cmax of Metoprolol with Retatrutide	PK: Cmax of Metoprolol with Retatrutide	Day 9 to Day 11

Secondary Outcome Measures

Outcome Measure	Time Frame
Number of Participants with an Incidence of Treatment Emergent Adverse Events TEAEs (TEAEs)	Baseline to Day 44

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): February 3, 2025
• Primary Completion (Actual): April 15, 2025
• Study Completion (Actual): April 15, 2025

Study Registration Dates

• First Submitted: January 31, 2025
• First Submitted That Met QC Criteria: January 31, 2025
• First Posted (Actual): February 5, 2025

Study Record Updates

• Last Update Posted (Estimated): June 5, 2025
• Last Update Submitted That Met QC Criteria: June 4, 2025
• Last Verified: June 1, 2025

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Autonomic Agents; Peripheral Nervous System Agents; Neurotransmitter Agents; Anti-Arrhythmia Agents; Adrenergic Agents; Antihypertensive Agents; Sympatholytics; Adrenergic beta-1 Receptor Antagonists; Adrenergic beta-Antagonists; Adrenergic Antagonists; Metoprolol
• Other Study ID Numbers: 27303; J1I-MC-GZQE (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: No
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No