Independent · non-commercial · publishes on a quarterly cycle|Current cycle 2026 Q3
Compound Evidence InstituteEvidence synthesis · established 2023Graded assessments of compounds, trials, methods and supply
Document set current to 30 July 2026
Compound monograph · §4

Orforglipron — safety

Adverse events as reported, contraindications, warnings, and an explicit statement of what the safety evidence does not establish.

Document identifier
CEI-MN-011/4
Series
Compound monograph
Version
1.0
Published
30 Apr 2026
Last reviewed
30 Apr 2026
Next review
30 Apr 2028
Identifier
10.71829/cei.mono.11
Certainty
Moderate
Cycle
2026 Q2

§4Safety

§4.1Adverse events reported in controlled trials

Table 4. Adverse events for Orforglipron as reported in the trial safety tables the Institute holds. Percentages are of randomised participants in the stated trial and arm.

EventActive, %Comparator, %Difference, ppSource
Nausea44.09.0+35.0Phase 2 obesity (45 mg)
Vomiting25.02.0+23.0Phase 2 obesity
Constipation21.09.0+12.0Phase 2 obesity
Diarrhoea24.012.0+12.0Phase 2 obesity
Discontinuation for adverse events10.02.0+8.0Phase 2 obesity
Hepatic enzyme elevationMonitored; no consistent signal reported in phase 2
A difference column is computed by the Institute from the two reported percentages and is not itself a published figure. Confidence intervals for adverse-event differences are not reported in the contributing trials and are not constructed here.
Gastrointestinal adverse eventsProportion of participants reaching each categorical response threshold, by arm.EventActiveComparatorNausea44.0 %9.0 %Vomiting25.0 %2.0 %Constipation21.0 %9.0 %Diarrhoea24.0 %12.0 %
Figure 4. Gastrointestinal adverse events for Orforglipron as reported in the contributing safety tables. Incidences of this kind are dose- and titration-rate-dependent and attenuate with continued exposure in most but not all participants.

§4.2Contraindications

  • Not established — investigational

§4.3Warnings and precautions

  • Gastrointestinal adverse-event incidence at the higher doses studied exceeded that of approved injectable agents
  • As a small molecule with hepatic metabolism, drug-interaction potential differs materially from the peptide class and is not yet fully characterised

§4.4What this section does not establish

Related assessments: tolerability of incretin receptor agonists · acute pancreatitis · the rodent thyroid C-cell signal.[1,2]

References cited on this page

References are numbered in order of first citation in this document. Each superscript in the text links to its entry below.

  1. Wharton S, Blevins T, Connery L, Rosenstock J, Raha S, Liu R, Ma X, Mather KJ, Haupt A, Robins D, Pratt E, Kazda C, Konig M. Daily oral GLP-1 receptor agonist orforglipron for adults with obesity. New England Journal of Medicine 2023;389(10):877–888. doi:10.1056/NEJMoa2302392 · PMID 37342922
  2. Frías JP, Hsia S, Eyde S, Liu R, Ma X, Konig M, Kazda C, Mather KJ, Haupt A, Pratt E, Robins D. Efficacy and safety of oral orforglipron in patients with type 2 diabetes: a multicentre, randomised, dose-response, phase 2 study. The Lancet 2023;402(10400):472–483. doi:10.1016/S0140-6736(23)01302-8 · PMID 37369232

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