Trial results for a Phase 1 study of Orforglipron (LY3502970) in healthy participants were posted on ClinicalTrials.gov on 2026-05-26. The study evaluated the pharmacokinetics and safety of multiple doses, showing a geometric mean maximum observed concentration (Cmax) of 80.5 ng/mL in the fasted state compared to 67.5 ng/mL in the fed state after a 16 mg dose.
Background
This study investigated LY3502970, also known as Orforglipron, in healthy participants. The primary objective was to characterize the pharmacokinetics of the drug, specifically how it is absorbed, distributed, metabolized, and excreted, in both fed and fasted conditions. The study also aimed to assess the safety and tolerability of multiple doses of LY3502970.
Trial design
The completed Phase 1 study (NCT05110794) enrolled 34 healthy participants. The trial's main purpose was to conduct blood tests to measure the concentration of LY3502970 in the bloodstream and to understand its handling and elimination by the body in both fed and fasted states. Additionally, the study evaluated the safety and tolerability of LY3502970 in these participants over a duration of up to 49 days.
Key results
Pharmacokinetic results for a 16 mg dose of LY3502970 were reported:
- The geometric mean maximum observed concentration (Cmax) was 80.5 ng/mL with a geometric coefficient of variation of 64% in the fasted state.
- In the fed state, the geometric mean Cmax was 67.5 ng/mL with a geometric coefficient of variation of 40%.
- The geometric mean area under the concentration-time curve from 0 to 24 hours (AUC0-24) was 1200 ng*hour/mL with a geometric coefficient of variation of 58% in the fasted state.
- In the fed state, the geometric mean AUC0-24 was 1050 ng*hour/mL with a geometric coefficient of variation of 40%.
- The median time to maximum observed concentration (Tmax) was 8.0 hours in the fasted state.
- The median Tmax was 8.00 hours in the fed state.
What this means
The Phase 1 pharmacokinetic results indicate that food intake influences the absorption of Orforglipron (LY3502970). Both the maximum observed concentration (Cmax) and overall exposure (AUC0-24) were lower in the fed state compared to the fasted state. For instance, geometric mean Cmax was 80.5 ng/mL fasted versus 67.5 ng/mL fed, and AUC0-24 was 1200 ng*hour/mL fasted versus 1050 ng*hour/mL fed. This suggests food may reduce the extent of Orforglipron's absorption. The median time to maximum concentration (Tmax) was consistent at 8.0 hours for both conditions. These findings are important for determining optimal dosing and administration instructions for future clinical development.
Source
The information regarding these trial results was obtained from ClinicalTrials.gov, a public database of clinical studies. The results for the study NCT05110794, titled "A Multiple-Dose Study of LY3502970 in Healthy Participants", were posted on 2026-05-26 on clinicaltrials.gov.