Development

Eli Lilly's orforglipron set for approval filing in diabetes after positive Phase III results

Eli Lilly (NYSE: LLY) reported that orforglipron (Foundayo) met its primary cardiovascular safety endpoint in the Phase III ACHIEVE-4 trial, demonstrating non-inferiority in risk of major adverse cardiovascular events (MACE) in patients with type 2 diabetes. Lilly says the data will support an FDA submission for the type 2 diabetes indication by end of Q2 2026.

Trial specifics

ACHIEVE-4 (NCT05803421) is a Phase III, event-driven, randomized, open-label trial enrolling adults with type 2 diabetes and overweight or obesity at increased cardiovascular risk, which randomized 2,749 participants across 15 countries.

The primary endpoint — time to first occurrence of MACE-4, encompassing cardiovascular death, heart attack, stroke, or hospitalization for unstable chest pain — showed a hazard ratio of 0.84 (95% CI: 0.59 to 1.20) for orforglipron versus insulin glargine, satisfying the prespecified non-inferiority margin. On the narrower MACE-3 composite, the hazard ratio was 0.77 (95% CI: 0.52 to 1.13). Neither endpoint reached nominal statistical superiority. In a pre-specified but multiplicity-uncontrolled analysis, all-cause mortality was 57% lower with orforglipron (HR: 0.43; 95% CI: 0.25 to 0.75; nominal p = 0.002), a finding that warrants cautious interpretation but is likely to feature prominently in regulatory discussions. On glycemic and weight endpoints, orforglipron produced a 1.6% reduction in A1C from a mean baseline of 8.22% at 52 weeks versus 1.0% for insulin glargine, and an 8.8% reduction in body weight compared to a 1.7% gain in the insulin glargine arm.

The safety profile was consistent with the GLP-1 receptor agonist class. Nausea, vomiting, diarrhea, decreased appetite, and constipation were the most common adverse events. Approximately 10.6% of orforglipron patients discontinued treatment due to adverse events over the 52-week minimum treatment period. A pre-specified analysis of drug-induced liver injury found no hepatic safety signal, consistent with earlier trials in the ACHIEVE and ATTAIN programs.

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Strategic context

Orforglipron is a non-peptide small molecule that activates the GLP-1 receptor — a pharmacologically distinct approach from the peptide-based GLP-1 agonists that currently dominate the cardiometabolic market. Unlike injectable agents such as semaglutide (Ozempic) or dulaglutide (Trulicity), or even oral semaglutide (Rybelsus), orforglipron can be taken at any time of day without food or water restrictions. The small-molecule format also carries manufacturing advantages — chemical synthesis rather than biological production eliminates cold-chain requirements and may reduce cost of goods over time.

Insulin glargine remains the standard intensification step when oral antidiabetics fail to achieve glycemic targets, and there is no currently approved oral GLP-1 agonist with demonstrated non-inferiority to basal insulin on cardiovascular outcomes. The ACHIEVE-4 data now provide that evidence for orforglipron, while simultaneously showing superior glycemic control and substantial weight reduction. The directionality of the data positions orforglipron as a potential oral alternative to insulin initiation in overweight or obese patients with type 2 diabetes who carry cardiovascular risk.


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