PMID-37369232 – Orforglipron Phase 2 Type 2 Diabetes

PMID-37369232 – Orforglipron Phase 2 Type 2 Diabetes

Frias JP, Hsia S, Engel SS, et al. Efficacy and safety of oral orforglipron in patients with type 2 diabetes: a multicentre, randomised, dose-response, phase 2 study. Lancet. 2023;402(10400):472-483.

Quick Reference

Property Value
PMID 37369232
DOI 10.1016/S0140-6736(23)01302-8
Year 2023
Journal The Lancet
Study Type RCT (Phase 2, dose-response)
Evidence Level II
Sample n=383 adults with type 2 diabetes (569 screened)
Peptide(s) Studied Orforglipron

Key Findings

  • At week 26, mean HbA1c change with orforglipron was up to -2.10% (-1.67% placebo-adjusted) vs. -0.43% with placebo
  • Dulaglutide 1.5 mg comparator arm achieved -1.10% HbA1c reduction
  • Body weight change at week 26 was up to -10.1 kg with orforglipron vs. -2.2 kg (placebo) and -3.9 kg (dulaglutide)
  • 352 of 383 (92%) participants completed the study; 303 (79%) completed 26 weeks of treatment
  • Dose-dependent HbA1c reductions across 3, 12, 24, 36, and 45 mg dose groups
  • Treatment-emergent adverse events occurred in 62-89% of orforglipron-treated participants
  • GI events (44-70% with orforglipron) were predominantly mild-to-moderate
  • No significant hepatic or renal safety signals

Study Design

Phase 2, multicentre, randomised, double-blind, placebo-controlled, dose-response study with an open-label dulaglutide 1.5 mg comparator arm. Adults with T2D (HbA1c 7.0-10.5%) on metformin or without background therapy were randomized to orforglipron (3, 12, 24, 36, or 45 mg daily), placebo, or open-label dulaglutide 1.5 mg weekly for 26 weeks. Primary endpoint was HbA1c change from baseline at week 26.

Limitations

  • Phase 2 dose-finding design (not powered for clinical endpoints)
  • Open-label dulaglutide arm introduces potential bias
  • 26-week treatment duration limits long-term conclusions
  • Higher doses had higher GI adverse event rates
  • Small sample sizes per dose group

Clinical Relevance

This Lancet publication demonstrated that oral orforglipron achieves glycemic control and weight loss superior to injectable dulaglutide 1.5 mg. The -2.10% HbA1c reduction and -10.1 kg weight loss with a once-daily oral pill rival or exceed many injectable GLP-1 RAs. For the peptide therapy landscape, orforglipron represents the leading edge of oral non-peptide GLP-1 RA development. Practitioners must understand this competitive landscape: if Phase 3 (ATTAIN program) confirms these results, the therapeutic paradigm for GLP-1-based treatment could shift substantially from injection to oral administration. NOTE: Orforglipron is a small molecule, NOT a peptide.

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