Phase I study of the oral GLP ‐1 receptor agonist DA ‐ 302168S : Safety, pharmacokinetics, and pharmacodynamics in healthy and overweight/obese adults
Authors' conclusion
DA-302168S demonstrates a favourable safety and PK profile, coupled with substantial, dose-dependent weight loss and metabolic benefits. These results strongly support its continued development as a promising once-daily oral therapy for obesity and type 2 diabetes.
Study context
- Population
- Healthy adults (Phase Ia, Ib) and overweight/obese adults (Phase Ic)
- Comparison
- Oral DA-302168S vs placebo
- Primary endpoint
- Safety and tolerability
Methodological detailsdouble-blind, placebo-controlled, single ascending dose, multiple ascending dose, three parts
- Double-blind
- Placebo-controlled
- Single ascending dose
- Multiple ascending dose
- Three parts
Primary result
As reported in the abstract
- DA-302168S generally well tolerated; gastrointestinal events (primarily nausea) most common AEs
Further findings
- Weight change in overweight/obese adults (Phase Ic) · 28 days — Placebo
- mean −2.90%
Pharmacokinetics (PK)
- PK dose proportional with moderate inter-individual variability across single ascending dose (SAD) and multiple ascending dose (MAD) phases
Weight change in overweight/obese adults (Phase Ic) · 28 days
- Mean weight loss with DA-302168S ranging from −5.67% to −7.26%, dose-dependent, significantly exceeding placebo
Metabolic parameters (Phase Ic)
- Significant metabolic improvements: reduced glucose fluctuations, lowered HbA1c, optimised lipid profiles
Original publication
Phase I study of the oral GLP ‐1 receptor agonist DA ‐ 302168S : Safety, pharmacokinetics, and pharmacodynamics in healthy and overweight/obese adults. Diabetes Obes Metab. Published 24 September 2025. doi:10.
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