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| Clinical data | |
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| Other names | LY-3502970 |
| Routes of administration | Oral |
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| Pharmacokinetic data | |
| Eliminationhalf-life | 29–49 hours |
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| Chemical and physical data | |
| Formula | C48H48F2N10O5 |
| Molar mass | 882.974 g·mol−1 |
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Orforglipron (LY-3502970) is an oral, non-peptide,small-moleculeGLP-1 receptor agonist developed as aweight loss drug byEli Lilly and Company.[1] It was discovered byChugai Pharmaceutical Co., then waslicensed 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 asmall-molecule, partial GLP-1 receptor agonist affecting the activity ofcyclic adenosine monophosphate (cAMP); its effects are similar to the actions ofglucagon-like peptide-1 (GLP-1) for reducing food intake and loweringblood glucose levels.[1][3]
The results ofPhase I safety andPhase II ascending-doseclinical trials enrolling people withobesity ortype 2 diabetes were published in 2023.[4][5]
Orforglipron has ahalf-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 ofadverse events in orforglipron-treated participants was 62–89%, mostly fromgastrointestinal discomfort (44–70% with orforglipron, 18% with placebo) having mild to moderate severity.[6] The most common side effects of orforglipon arediarrhea,nausea, upset stomach, andconstipation.[1][6]
The ability of orforglipron to reduce blood sugar levels and body weight was judged favorable compared todulaglutide.[6]
In April 2025, results from aPhase III clinical trial involving 559 people with type 2 diabetes who took an oral orforglipron pill,injectabledulaglutide or aplacebo 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 ofhemoglobin A1C level by more than or equal to 1.5 percentage points, bringing them into the non-diabetic range as defined by theAmerican 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] In its press release, Lilly noted that the subjects' weight loss had not yet plateaued at the time the trial concluded, and suggested that this indicated that greater weight reduction would ultimately be achieved with extended therapy.[1]
Side effects were similar to those seen with other GLP-1 agonists, and no significant liver problems were observed.[1]