Eli Lilly's Oral Small-Molecule GLP-1R Agonist Orforglipron Granted IND Approval in China for Weight Management

On June 28, the CDE website showed that Eli Lilly's once-daily oral small molecule GLP-1R agonist LY3502970 capsule (Orforglipron) obtained tacit approval for clinical trial application for weight loss.

LY3502970 capsule is a novel, highly effective, orally administered non-peptide GLP-1R agonist, initially developed by Chugai. In September 2018, Eli Lilly and Company reached an agreement with Chugai to obtain global development and commercialization rights for LY3502970.

On June 23, Eli Lilly and Company announced the detailed data from the Phase II clinical trial of Orforglipron in obese patients without type 2 diabetes (average baseline weight of 109 kg). The study has been published in The New England Journal of Medicine.

The results showed that at Week 26, all dose groups of Orforglipron (12mg, 24mg, 36mg, or 45mg) achieved statistically significant dose-dependent weight loss, ranging from 8.6% (9.0kg) to 12.6% (13.3kg), compared to 2.0% (2.1kg) in the placebo group, reaching the primary endpoint.

By the 36th week, patients in all dose groups continued to experience weight loss, ranging from 9.4% (9.8 kg) to 14.7% (15.4 kg), compared to 2.3% (2.4 kg) in the placebo group.

The study also met all key secondary endpoints. The proportion of patients with ≥5% weight loss in the four dose groups (12mg, 24mg, 36mg, or 45mg) was 72%, 90%, 92%, and 90%, respectively, compared to 24% in the placebo group; the proportion of patients with ≥10% weight loss was 47%, 62%, 75%, and 69%, respectively, compared to only 9% in the placebo group. Additionally, the BMI of participants in the four groups decreased from baseline by 3.4, 4.7, 5.0, and 5.5 kg/m², respectively (compared to 0.9 kg/m² in the placebo group); waist circumference decreased from baseline by 9.6 cm, 11.2 cm, 10.6 cm, and 13.6 cm, respectively (compared to 4 cm in the placebo group).

Orforglipron's safety is similar to other incretin-based treatments. Gastrointestinal side effects are the most commonly reported adverse events, generally mild to moderate in severity, and typically occur during dose escalation.

Currently, Eli Lilly has initiated three Phase III clinical trials for Orforglipron, including: a comparison with insulin glargine (personalized dosage, once daily) for obese or overweight patients with type 2 diabetes who have an increased cardiovascular risk (NCT05803421), a comparison with placebo for the treatment of adult obesity or overweight patients with weight-related comorbidities (NCT05869903), and a comparison with placebo for the treatment of obese or overweight adult patients with type 2 diabetes (NCT05872620).

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