Trial results for a Phase 1 study of Orforglipron (LY3502970) in healthy participants were posted on ClinicalTrials.gov on 2026-05-27. The study evaluated the pharmacokinetics of the drug, reporting a geometric mean absolute bioavailability of 77%.
Trial design
The completed Phase 1 study (NCT06085482) enrolled 10 healthy participants. The main purpose was to evaluate the pharmacokinetics of LY3502970, specifically how much of the drug and its radioactive form [14C]-LY3502970 gets into the bloodstream, how it is broken down, and its elimination time from the body. The study duration for each participant was approximately 9 weeks.
Key results
The study measured several pharmacokinetic parameters for LY3502970 and [14C]-LY3502970 in healthy participants:
- Absolute Bioavailability of LY3502970: 77% (Geometric Coefficient of Variation: 27%).
- Area Under the Curve (AUC [0-∞]) of Total Radioactivity in Plasma: 3.71 nanogram equivalent*hour per milliliter (Geometric Coefficient of Variation: 29%).
- AUC [0-∞] of [14C]-LY3502970 in Plasma: 2.91 nanogram equivalent*hour per milliliter (Geometric Coefficient of Variation: 19%).
- AUC [0-∞] of LY3502970 in Plasma: 108 nanogram*hour per milliliter (Geometric Coefficient of Variation: 35%).
- Maximum Concentration (Cmax) of Total Radioactivity in Plasma: 2.10 nanogram equivalent per milliliter (Geometric Coefficient of Variation: 59%).
- Cmax of [14C]-LY3502970 in Plasma: 2.08 nanogram equivalent per milliliter (Geometric Coefficient of Variation: 53%).
- Cmax of LY3502970 in Plasma: 5.43 nanogram per milliliter (Geometric Coefficient of Variation: 42%).
What this means
The results from this Phase 1 study provide initial pharmacokinetic data for Orforglipron in healthy individuals. The observed absolute bioavailability of 77% indicates a significant proportion of the orally administered drug reaches systemic circulation, which is a key factor for an oral therapeutic. The detailed measurements of AUC and Cmax for both the parent drug and total radioactivity offer insights into its absorption, distribution, metabolism, and excretion profile. This foundational pharmacokinetic understanding is crucial for guiding further clinical development, including dose selection and regimen design for future studies in patient populations.
Source
The information for these trial results was obtained from ClinicalTrials.gov, a public database of clinical studies. The results for the study NCT06085482, titled "A Phase I Study of LY3502970 in Healthy Participants", were posted on 2026-05-27 on clinicaltrials.gov.