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Tested

Tested: Orforglipron 6mg × 100 Tabs
Lab: Analiza Białek
Date: October 2026
Result: 5.91 mg per tablet (6 mg label)
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GLP-1 Oral

Orforglipron

First oral small-molecule GLP-1 agonist. Not a peptide - no absorption problems. Phase-3 positive and close to approval.

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At a glance

Orforglipron by the numbers

The key figures from our lexicon.

Full lexicon entry

Class

GLP-1 agonist

small molecule, oral

Half-life

long

dosed daily

Use

Oral

in mg/day

Sizes

2 sizes

6mg/90tabs, 6mg/100tabs

What studies show

1
Orforglipron, an oral small-molecule GLP-1 agonist, in early type 2 diabetes (phase 3) (opens in a new tab)NEJM, 2025

The source in the lexicon

For research and educational purposes only. Values from the TPD lexicon, sources linked there.

Knowledge

Everything about Orforglipron

Description

Orforglipron is the first orally available small-molecule agonist of the GLP-1 receptor that has successfully completed Phase 3 studies. Unlike classical oral peptide variants, Orforglipron is not a peptide but a small chemical compound. This eliminates the absorption problems peptides have in the gastrointestinal tract.

Per study reports Orforglipron activates the GLP-1 receptor with similar selectivity and potency as Semaglutide, but with two decisive advantages: first, oral bioavailability without absorption enhancers; second, no restrictions on fasting intake or water limits. Orforglipron is simply swallowed daily, with or without food.

The substance was originally discovered by Chugai Pharmaceutical and licensed to Eli Lilly in 2018. In the landmark ATTAIN-1 study (Phase 3, 2025) subjects under 36mg Orforglipron achieved 11.2% weight loss over 72 weeks - comparable with Wegovy, but as a convenient oral tablet.

In the parallel ACHIEVE study in type-2 diabetes, Orforglipron significantly lowered glycated hemoglobin (HbA1c) over 40 weeks. Global approval applications were submitted at the end of 2025, market approval expected for 2026.

Pharmacokinetically orally bioavailable with excellent bioavailability. Half-life allows once-daily dosing. Safety profile consistent with the GLP-1 class: gastrointestinal effects at start, subside with titration.

You can order Orforglipron as oral tablets in one bottle, 6mg per tablet with 90 or 100 tablets and 12mg per tablet with 100 tablets.

This information is for research and educational purposes only. No medical recommendations.

Risks & Safety

As an oral small-molecule agonist, Orforglipron activates the same GLP-1 receptor as the peptide compounds, so the documented safety profile is correspondingly consistent with the GLP-1 class and shaped by gastrointestinal effects.

Observed in studies and user reports:

Gastrointestinal effects: nausea, vomiting, diarrhea and constipation are the most commonly documented observations, particularly at the start. In the Phase 3 studies they subside with titration. Slow titration reduces the incidence.
Appetite and fluids: the reduced appetite can lead to decreased food and fluid intake. The literature describes an elevated risk of dehydration.
Muscle mass and gallbladder: weight loss involves a portion of muscle mass alongside fat mass. Gallbladder issues during rapid weight loss are documented for the GLP-1 class.
Class signals: as with other GLP-1 agonists, the literature discusses rare safety signals such as pancreatitis.
Limited long-term data: Orforglipron has completed the Phase 3 studies but is a very new compound. Data beyond the study periods are lacking.

Monitoring via bloodwork is recommended. This classification does not replace medical advice. Risk and responsibility for any actual use lie entirely with the buyer.

Studies

Orforglipron, an Oral Small-Molecule GLP-1 Receptor Agonist for Obesity Treatment (ATTAIN-1) - NEJM 2025: Phase 3 gold-standard obesity study.
Orforglipron, an Oral Small-Molecule GLP-1 Receptor Agonist, in Early Type 2 Diabetes (ACHIEVE-1) - NEJM 2025, Rosenstock et al: Phase 3 trial, all three doses significantly lowered HbA1c over 40 weeks versus placebo.
Orforglipron for treatment of obesity in people with type 2 diabetes (ATTAIN-2) - Lancet 2025: Co-morbidity obesity + diabetes study.

Dosing

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Frequently asked

Sources for every answer: lexicon entry

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How does Orforglipron differ from semaglutide as a tablet?

Semaglutide is a peptide and is poorly absorbed in the stomach, which is why a strict fasting rule applies. Orforglipron is a small molecule that acts on the same GLP-1 receptor. With food the absorbed amount was only about 18 to 24 percent lower in two studies, half-life and time to peak stayed the same. The US prescribing information states no clinically relevant food effect.

Is Orforglipron approved?

Yes, in the US since 1 April 2026 for long-term weight reduction in adults with obesity or with overweight and at least one related condition. Applications were under review in the EU, Japan and Canada in 2026, also for type 2 diabetes. The approved tablets have different strengths than the capsules used in the trials, so the numbers are not directly comparable.

How much did weight drop in the trials?

In the phase 3 trial with 3,127 adults without diabetes weight fell by 7.5, 8.4 and 11.2 percent over 72 weeks depending on the level, by 2.1 percent on placebo. In the highest level 54.6 percent lost at least a tenth of their weight and 18.4 percent at least a fifth. With type 2 diabetes the loss was 5.1 to 9.6 percent. Waist size, systolic blood pressure and blood lipids improved.

How does it perform in type 2 diabetes?

In early type 2 diabetes HbA1c fell by 1.24 to 1.48 percentage points over 40 weeks, by 0.41 on placebo. There were no severe hypoglycaemias. In a 52-week head-to-head trial both tested Orforglipron levels lowered HbA1c more than both levels of oral semaglutide, 1.91 against 1.47 percentage points comparing the higher levels.

Which side effects were seen?

Mainly gastrointestinal complaints such as nausea, constipation, diarrhoea and vomiting, mostly mild to moderate and mainly during dose escalation. Compared with oral semaglutide 58 to 59 percent had such complaints against 37 to 45 percent. 9 to 10 percent stopped against 4 to 5 percent. Pulse rose by up to 4.7 beats per minute on average.

Why is one tablet a day enough?

Orforglipron stays in the blood for a long time. In the first human study the half-life after several weeks was 48 to 68 hours, the US prescribing information gives 29 to 49 hours. A steady level is reached after about a week. It is broken down mainly in the liver via CYP3A4, so interactions with drugs that slow down or speed up this enzyme matter.

Does it help to keep weight off after injection therapy?

One trial tested this: people who switched to Orforglipron after 72 weeks of injected tirzepatide or semaglutide kept on average 74.7 and 79.3 percent of their previous loss after one year, 49.2 and 37.6 percent on placebo. There was no arm that continued the injection and the trial ran for one year only.

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Tirzepatide Oral

Peptides · GLP-1 Oral GLP-1 Oral

1 size

36 EUR

Important - Oral GLP-1 Compounds

Three oral GLP-1 options available: Orforglipron (non-peptide, normal tablet absorption), Semaglutide Oral (peptide + SNAC absorption enhancer) and Tirzepatide Oral (peptide, GLP-1/GIP dual agonist, experimental).
Orforglipron has noticeably better bioavailability and can be taken with or without food - the practical advantage over peptide-based oral GLP-1.
Semaglutide Oral has ~1% bioavailability and MUST be taken fasted in the morning with minimal water, then nothing to eat or drink for 30 minutes.
Oral Semaglutide 14mg daily roughly corresponds to injectable Semaglutide 1mg per week in terms of effect.
Orforglipron Phase 3 studies (ATTAIN/ACHIEVE) demonstrate effective weight loss and HbA1c reduction at doses up to 45mg/day.
Tirzepatide Oral is the most experimental option: dual agonist (GLP-1 + GIP) like injectable Tirze, but as a peptide with bioavailability under 5% and a low 500mcg dose - thin data on the oral route.
Not a GLP-1, but an oral weight-loss alternative: Tesofensine is a monoamine reuptake inhibitor (appetite suppressant), found in the fat-burner section.

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