Orforglipron ( LY3502970 ), a novel, oral non‐peptide glucagon‐like peptide‐1 receptor agonist: A Phase 1a, blinded, placebo‐controlled, randomized, single‐ and multiple‐ascending‐dose study in healthy participants
Authors' conclusion
Orforglipron's long half-life (25-68 hours) allows once-daily oral dosing, without water and food restrictions. Orforglipron had a pharmacodynamic and safety profile similar to that of injectable GLP-1RAs, which supports continued clinical development.
Study context
- Population
- Healthy adults aged 18 to 65 years, BMI 20 to 40 kg/m², HbA1c 47.5 mmol/mol (<6.5%)32 Part A, 60 Part B
- Participants
- 92 adults
- Comparison
- Oral orforglipron vs placebo
- Primary endpoint
- Safety, tolerability, pharmacokinetics and pharmacodynamics of single and multiple doses
Methodological detailsPhase 1a, double-blind, placebo-controlled, single- and multiple-ascending-dose
- Phase 1a
- Double-blind
- Placebo-controlled
- Single- and multiple-ascending-dose
Primary result
As reported in the abstract
Pharmacokinetics: mean t1/2
Mean t1/2 after single dose (0.3-6 mg)
24.6 to 35.3 hours
Mean t1/2 on Day 28 (2-24 mg)
48.1 to 67.5 hours
Further findings
| Outcome | Placebo | P value |
|---|---|---|
| Body weight reduction · 4 weeksOrforglipron vs Placebo | 2.4 kg | P < 0.05 |
- Body weight reduction: Orforglipron up to 5.4 kg
Fasting glucose and gastric emptying
- Orforglipron decreased fasting glucose across Days 1 to 28
- Gastric emptying delayed on Day 28
Safety
- Most common adverse events were gastrointestinal tract-related
Original publication
Orforglipron ( LY3502970 ), a novel, oral non‐peptide glucagon‐like peptide‐1 receptor agonist: A Phase 1a, blinded, placebo‐controlled, randomized, single‐ and multiple‐ascending‐dose study in healthy participants. Diabetes Obes Metab. Published 21 June 2023. doi:10.
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