Phase 1: First-in-Human Single and Multiple Ascending Dose Study of Retatrutide
NCT04042896 · Eli Lilly
- Phase
- Phase 1
- Enrollment
- 120 participants
- Est. completion
- Completed 2021
- Sponsor
- Eli Lilly
Background
The first-in-human Phase 1 study established the safety, tolerability, and pharmacokinetic profile of retatrutide (LY3437943) in healthy adults and adults with type 2 diabetes. Single ascending dose (SAD) and multiple ascending dose (MAD) cohorts were evaluated. The study confirmed once-weekly dosing was pharmacokinetically supported and identified the dose range for Phase 2 development.
Key result
Retatrutide demonstrated acceptable safety and tolerability across dose levels. Half-life supported once-weekly dosing. Dose-dependent reductions in body weight and glucose were observed. Results informed Phase 2 dose selection (1 mg, 4 mg, 8 mg, 12 mg).
Primary endpoint
Safety, tolerability, and pharmacokinetics of single and multiple ascending doses
Secondary endpoints
- Maximum tolerated dose
- Pharmacokinetic parameters (Cmax, AUC, t½)
- Pharmacodynamic effects (glucose, insulin, glucagon)
- Immunogenicity
Population
Healthy adults and adults with type 2 diabetes, n=~120
Intervention
Retatrutide single doses (0.1–6 mg) or multiple weekly doses (0.5–6 mg) SC vs. placebo; no dose escalation protocol in Phase 1
Inclusion criteria
Healthy adults 18–65 years (SAD cohorts); adults with type 2 diabetes on stable metformin (MAD cohorts); BMI 23–40 kg/m²
Exclusion criteria
Personal or family history of medullary thyroid carcinoma or MEN2; significant hepatic, renal, or cardiovascular disease; use of insulin or GLP-1 agonists
Trial information sourced from ClinicalTrials.gov and published literature. TryTrutide is not affiliated with Eli Lilly or any trial site. This is not medical advice.