Sustained Action of Imapextide, A Glucagon-Like Peptide-1 Receptor Antagonist, in Healthy Volunteers
Authors' conclusion
Imapextide was generally well tolerated in HVs. PK findings supported weekly dosing. PD showed consistent effects on GLP-1 levels, supporting a potential role for imapextide in modulating PBH pathophysiology.
Study context
- Population
- Healthy adult volunteers32 SAD, 23 MAD, 14 drug-drug interactions (DDIs)
- Participants
- 69 volunteers
- Comparison
- Subcutaneous imapextide vs placebo
- Primary endpoint
- Safety/tolerability (TEAEs)
Methodological details3-part, double-blind, placebo-controlled, single and multiple ascending doses, randomized 3:1
- 3-part
- Double-blind
- Placebo-controlled
- Single and multiple ascending doses
- Randomized 3:1
Primary result
As reported in the abstract
TEAE rates with imapextide across cohorts
TEAE rate range, SAD
33.3% to 50.0%
TEAE rate range, MAD
33.3% to 100%
TEAE rate, DDIs
14.3%
Further findings
Pharmacokinetics (PK)
- Median tmax
- 24-48 hours
- Mean t1/2
- ∼90 hours
- Exposure dose proportional
Pharmacodynamics (PD) during MMTT (MAD)
- Imapextide increased GLP-1 concentrations at early time points; effects on other glycemic parameters variable
DDIs
- Minimal nonclinically relevant DDIs with rosuvastatin
- Imapextide slightly accelerated gastric emptying
Safety
- TEAE rate range, SAD
- 33.3% to 50.0%
- TEAE rate range, MAD
- 33.3% to 100%
- TEAE rate, DDIs
- 14.3%
- Most common TEAEs: injection site erythema (SAD, MAD) and injection site swelling (MAD)
Original publication
Sustained Action of Imapextide, A Glucagon-Like Peptide-1 Receptor Antagonist, in Healthy Volunteers. J Clin Endocrinol Metab. Published 24 December 2025. doi:10.
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