Orforglipron Phase 1 Trial Posts Safety and Pharmacokinetic Results

Trial results for a Phase 1 study of Orforglipron (LY3502970) in healthy overweight and obese participants were posted on ClinicalTrials.gov on 2026-05-26. The study evaluated the safety, tolerability, and pharmacokinetics of the drug, reporting treatment-emergent adverse events in 20, 21, and 16 participants across three cohorts, respectively.

Background

The study investigated LY3502970 (Orforglipron) in healthy overweight and obese participants. The primary objectives were to assess the safety and tolerability of the drug, as well as to characterize its pharmacokinetics, including how it is absorbed, distributed, metabolized, and eliminated by the body. Blood tests were conducted to measure the concentration of LY3502970 in the bloodstream over time.

Trial design

The completed Phase 1 study (NCT05313802) enrolled 72 participants who were healthy, overweight, or obese. The trial's main purpose was to evaluate the safety and tolerability of LY3502970, and to measure its pharmacokinetics in these participants. The study duration was up to 42 days, excluding the screening period. Participants were divided into three cohorts, each receiving LY3502970.

Key results

The trial reported safety and pharmacokinetic data:

• Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Event(s) (SAEs) considered related to study drug administration:
  • LY3502970 Cohort 1: 20 participants
  • LY3502970 Cohort 2: 21 participants
  • LY3502970 Cohort 3: 16 participants
• Pharmacokinetics (PK) on Day 1:
  • Area Under the Concentration Versus Time Curve (AUC[0-tlast]):
    • Cohort 1: Geometric Mean 117 nanogram hour per milliliter (ng*h/mL) (Geometric Coefficient of Variation: 39)
    • Cohort 2: Geometric Mean 66.1 nanogram hour per milliliter (ng*h/mL) (Geometric Coefficient of Variation: 25)
    • Cohort 3: Geometric Mean 66.9 nanogram hour per milliliter (ng*h/mL) (Geometric Coefficient of Variation: 30)
  • Maximum Observed Concentration (Cmax):
    • Cohort 1: Geometric Mean 8.40 nanograms per milliliter (ng/mL) (Geometric Coefficient of Variation: 41)
    • Cohort 2: Geometric Mean 4.97 nanograms per milliliter (ng/mL) (Geometric Coefficient of Variation: 25)
    • Cohort 3: Geometric Mean 5.00 nanograms per milliliter (ng/mL) (Geometric Coefficient of Variation: 34)
  • Time to Maximum Observed Concentration (Tmax):
    • Cohort 1: Median 7.03 hours
    • Cohort 2: Median 6.00 hours
    • Cohort 3: Median 6.00 hours

  What this means

  The posted results from this Phase 1 study provide initial insights into the safety, tolerability, and pharmacokinetic profile of Orforglipron (LY3502970) in healthy overweight and obese participants. The data on treatment-emergent adverse events across the three cohorts, with 20, 21, and 16 participants experiencing such events, offers an early look at the drug's safety signals. Furthermore, the detailed pharmacokinetic measurements, including AUC, Cmax, and Tmax values, are crucial for understanding the drug's absorption and exposure in the body. These foundational data points will inform the design of subsequent clinical trials, helping to determine appropriate dosing strategies and further evaluate the drug's potential in relevant therapeutic areas.

  Source

  The information regarding these trial results was obtained from ClinicalTrials.gov, a public database of clinical studies. The results for the study NCT05313802, titled "A Study of LY3502970 in Healthy Overweight and Obese Participants", were posted on 2026-05-26 on clinicaltrials.gov.