PharmaceuticalSmall-moleculeOral GLP-1 receptor agonist
Lotiglipron
Also known as PF-07081532
Discontinued once-daily oral small-molecule GLP-1 receptor agonist from Pfizer, halted after elevated liver enzymes were observed in trial participants.
01 Overview
Lotiglipron (PF-07081532) was an oral, once-daily small-molecule GLP-1 receptor agonist developed by Pfizer as a convenient alternative to injectable peptides. It reached Phase 2 development for obesity and type 2 diabetes.
In 2023 Pfizer discontinued the compound after observing elevated liver transaminases in some participants, choosing to focus its oral GLP-1 efforts elsewhere. Human data are limited and the compound is no longer in development.
02 Mechanism
Orally active small-molecule GLP-1 receptor agonist stimulating insulin secretion and reducing appetite.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Trial dose | 80–200 mg/day | Oral | Approximate Phase 2 exploratory doses; programme discontinued |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Weight lossEarly weight-loss signal in Phase 2 before discontinuation. | Modest, dose-dependent | Clinical | |
| Glucose loweringExpected GLP-1 glycaemic effect in early trials. | Reduced fasting glucose/HbA1c | Clinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Elevated liver enzymesTransaminase elevations that led to discontinuation of the drug. | Severe | Uncommon | Clinical | |
| Gastrointestinal effectsNausea typical of oral GLP-1 agonists. | Moderate | Common | Clinical |
06 Legal status
United States
Investigational
Discontinued; never approved · as of Jan 2026
07 References
Pfizer discontinues lotiglipron (PF-07081532) after liver enzyme elevationsPfizer announcement, 2023
08 Discussion0 comments
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This page is reference information, not medical advice. Doses and protocols are documented as they appear in the clinical literature and in practice — describing them is not a recommendation to use them. Countermeasures listed here are not a substitute for a physician. Legal status varies by jurisdiction and changes.