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![]() Above: molecular structure of orforglipron Below: 3D representation of an orforglipron molecule | |
Clinical data | |
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Other names | LY-3502970 |
Routes of administration | Oral |
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Pharmacokinetic data | |
Elimination half-life | 29–49 hours |
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Chemical and physical data | |
Formula | C48H48F2N10O5 |
Molar mass | 882.974 g·mol−1 |
3D model (JSmol) | |
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Orforglipron (LY-3502970) is an oral, non-peptide, small-molecule GLP-1 receptor agonist developed as a weight loss drug by Eli Lilly and Company. [1] It was discovered by Chugai Pharmaceutical Co., then was licensed to Lilly in 2018. [1]
Orforglipron is easier to produce than existing peptide GLP-1 agonists and is expected to be cheaper. [2]
Orforglipron is a small-molecule, partial GLP-1 receptor agonist affecting the activity of cyclic adenosine monophosphate (cAMP); its effects are similar to the actions of glucagon-like peptide-1 (GLP-1) for reducing food intake and lowering blood glucose levels. [1] [3]
The results of Phase I safety and Phase II ascending-dose clinical trials enrolling people with obesity or type 2 diabetes were published in 2023. [4] [5]
Orforglipron has a half-life of 29 to 49 hours across the doses tested and is taken once per day by mouth without food or water restrictions. [3]
Safety and dosing trials showed that the incidence of adverse events in orforglipron-treated participants was 62–89%, mostly from gastrointestinal discomfort (44–70% with orforglipron, 18% with placebo) having mild to moderate severity. [6] The most common side effects of orforglipon are diarrhea, nausea, upset stomach, and constipation. [1] [6]
The ability of orforglipron to reduce blood sugar levels and body weight was judged favorable compared to dulaglutide. [6]
In April 2025, results from a Phase III clinical trial involving 559 people with type 2 diabetes who took an oral orforglipron pill, injectable dulaglutide or a placebo daily for 40 weeks showed that orforglipron produced a reduction in blood glucose levels by 1.3 to 1.6 percentage points from a starting level of 8%. [1] [7]
More than 65% of participants taking the highest dose of orforglipron achieved a reduction of hemoglobin A1C level by more than or equal to 1.5 percentage points, bringing them into the non-diabetic range as defined by the American Diabetes Association. [1] People taking the highest dose of the pill lost 8% of their weight, or around 16 lb (7.3 kg), on average after 40 weeks. [1] [8]
Side effects were similar to those seen with other GLP-1 agonists, and no significant liver problems were observed. [1]