Small molecule
PubChem CID 137319706
Orforglipron
Foundayo
- Mechanism of action
- GLP-1 receptor agonist (non-peptide, oral)
- In plain language
- A small-molecule pill, not an injection, that switches on the same brain receptor as the body's natural appetite hormone, GLP-1, reducing hunger and slowing digestion to drive steady weight loss.
- How it works
- Orforglipron is a non-peptide small molecule that binds to and activates the human GLP-1 receptor -- unlike earlier GLP-1 agonists such as semaglutide and liraglutide, which are injectable peptide analogs of the native hormone. GLP-1 receptors are present in brain regions that regulate appetite and caloric intake; in animal studies, orforglipron distributed to and activated neurons in these appetite-regulating regions. The resulting decrease in food intake, together with a delay in gastric emptying that is largest after the first dose and diminishes over time, drives sustained reduction in body weight, with proportionally greater loss of fat mass than lean mass. Because it is a conventional small molecule rather than a peptide, it does not require the injection delivery that GLP-1 peptide analogs do, and is taken as a once-daily tablet at any time of day, with or without food.
- Therapeutic applications
- Per FDA-approved labeling, orforglipron (Foundayo) is indicated in combination with a reduced-calorie diet and increased physical activity to reduce excess body weight and maintain weight reduction long term in adults with obesity, or adults with overweight in the presence of at least one weight-related comorbid condition. Concomitant use with another GLP-1 receptor agonist is not recommended.
- Class
- Small molecule
- Therapeutic area
- Metabolic / Weight Management
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