sampleoral GLP-1
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This product is sold strictly for in lab conditions (in vitro) research purposes. Not approved for human consumption.
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Orforglipron
Oral GLP-1 Receptor Agonist | FDA-Approved for Weight Loss
In short
Orally bioavailable small molecule and GLP-1 receptor agonist studied in clinical models of metabolic control.
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Orforglipron is a non-peptide small molecule that functions as a GLP-1 receptor agonist. At the molecular level, it binds to these receptors to activate specific signaling pathways, stimulating insulin secretion and delaying gastric emptying while minimizing receptor desensitization. The compound is widely studied in in vitro and animal models to evaluate its high oral bioavailability and extended half-life. While it is known commercially as the approved medication Foundayo, the product provided here is strictly research-grade and is not a drug for human consumption.
Research reagent for laboratory use only. Not a medicine. For medical questions, consult a physician.
Scientific review
Written by
Калина Тодорова
Magister Pharmaciae, MSc Pharmacy
Reviewed by
Борис Маринов
MSc Biochemistry & Molecular Biology
Reviewed on
Orforglipron (brand name Foundayo) is an FDA-approved oral, non-peptide GLP-1 receptor agonist and the first small-molecule GLP-1 approved for weight management. Approved April 2026 under the FDA's National Priority Voucher program, Foundayo can be taken once daily at any time without food or water restrictions. Clinical trials demonstrated up to 11.1% weight loss (24.9 lbs) at 72 weeks with the highest approved dose (17.2mg) and robust glycemic control (HbA1c reductions of 1.3-1.6%). Developed by Chugai Pharmaceutical and marketed by Eli Lilly. Available in 0.8mg, 2.5mg, 5.5mg, 9mg, 14.5mg, and 17.2mg tablets.
First oral GLP-1 small-molecule (Eli Lilly) 9.4-14.7% weight loss (Phase 2 NEJM 2023) Non-peptide → orally bioavailable Biased agonist - improved side-effect profile
Small-molecule GLP-1 receptor agonist with biased signaling - preferentially activates G protein/cAMP pathways (enhancing insulin secretion, suppressing glucagon, delaying gastric emptying, reducing appetite) while minimizing receptor desensitization. 79.1% oral bioavailability with 29-49 hour half-life supporting once-daily dosing.
FDA-approved based on ATTAIN-1 trial: 17.2mg dose achieved 11.1% weight loss (24.9 lbs) at 72 weeks in non-diabetic adults with obesity. 9mg achieved 8.3% (18.9 lbs), 5.5mg achieved 7.4% (17.2 lbs). First oral small-molecule GLP-1 approved for weight management.
ATTAIN-2 Phase 3 trial showed 9.6% weight loss (21.2 lbs) with 17.2mg in patients with both obesity and diabetes. 9mg achieved 7% (15.9 lbs), 5.5mg achieved 5.1% (11.7 lbs).
Significant improvements in waist circumference, systolic blood pressure (8-12 mmHg reductions), triglycerides (-20-30%), and non-HDL cholesterol across Phase 3 trials. Comprehensive metabolic syndrome reversal.
Among 1,127 ATTAIN-1 participants with prediabetes at baseline, up to 91% achieved near-normal blood sugar levels vs 42% with placebo, demonstrating diabetes prevention potential.
Dosing
The typical regimens you'll see in the published research - for reference when planning in vitro or in vivo experiments. Not medical advice.
Disclaimer
These are regimens discussed in the research literature, not medical advice. Consult a healthcare provider before use.
Timing
Any time of day, with or without food, with or without water
BOXED WARNING: May cause thyroid C-cell tumors including medullary thyroid carcinoma (MTC). Contraindicated in patients with personal/family history of MTC or Multiple Endocrine Neoplasia syndrome type 2 (MEN 2)
Start at 0.8mg daily, titrate to 2.5mg after 30 days, then 5.5mg after 60 days - gradual titration minimizes GI side effects
Do not use with other receptor agonist medicines
Monitor for signs of acute pancreatitis (severe, persistent abdominal pain with or without nausea/vomiting) - stop taking Foundayo immediately if suspected
Common side effects: nausea, constipation, diarrhea, vomiting, indigestion, abdominal pain, headache, bloating, fatigue, belching, heartburn, gas, and hair loss
May cause dehydration leading to kidney problems - drink fluids to reduce risk, especially with nausea/vomiting/diarrhea
May affect oral contraceptive efficacy - use alternative birth control for 30 days after starting and after each dose increase
May require adjustment of insulin or sulfonylurea doses to prevent low blood sugar (hypoglycemia)
Not safe during pregnancy (may harm unborn baby) or breastfeeding - pregnancy exposure registry available at 1-800-LillyRx
Gallbladder problems reported - monitor for upper abdominal pain, fever, jaundice, or clay-colored stools
Tell healthcare providers you take Foundayo before any surgery or procedure using anesthesia (aspiration risk)
If doses missed for 7+ consecutive days, contact healthcare provider about how to restart treatment
References
Links to peer-reviewed publications on PubMed, cited in the peptide's scientific profile.
ATTAIN-1 Phase 3 Trial (Obesity) - 2025
3,127 adults with obesity without diabetes | 72-week study | FDA-approved doses: 5.5mg, 9mg, 17.2mg daily
Highest approved dose (17.2mg) achieved 11.1% weight loss (24.9 lbs) vs 2.1% placebo. 9mg achieved 8.3% (18.9 lbs), 5.5mg achieved 7.4% (17.2 lbs). First oral small-molecule GLP-1 to complete Phase 3. Significant improvements in waist circumference, blood pressure, triglycerides, and non-HDL cholesterol.
ATTAIN-2 Phase 3 Trial (Obesity + T2DM) - 2025
1,613 adults with obesity and type 2 diabetes | 72-week study | FDA-approved doses: 5.5mg, 9mg, 17.2mg daily
Highest approved dose (17.2mg) achieved 9.6% weight loss (21.2 lbs). 9mg achieved 7% (15.9 lbs), 5.5mg achieved 5.1% (11.7 lbs). Demonstrated efficacy extends to patients with comorbid diabetes and obesity.
ACHIEVE-1 Phase 3 Trial (Type 2 Diabetes) - 2025
559 adults with T2DM | 40-week study | 3mg, 12mg, 36mg daily doses
All doses significantly reduced HbA1c by 1.3-1.6% from 8.0% baseline vs 0.4% placebo. 76.2% achieved HbA1c <7%, 66.0% achieved ≤6.5%. 36mg dose produced 7.9% weight loss (16 lbs). First oral GLP-1 with no food/water restrictions to complete Phase 3.
Phase 2 Obesity Study - 2023
272 adults with obesity | 36-week study | Multiple dose escalations to 45mg
Achieved up to 14.7% mean weight reduction at 36 weeks with 45mg dose. Established dose-response relationship and optimal dosing ranges for Phase 3 development.
Phase 2 Type 2 Diabetes Study - 2023
Adult T2DM patients | 26-week study | Doses 3-45mg vs placebo and dulaglutide 1.5mg comparator
Demonstrated superior HbA1c reduction and body weight reduction compared to injectable dulaglutide across multiple dose levels, establishing proof-of-concept for oral efficacy matching injectables.
Phase 1 Safety and Pharmacokinetics Studies - 2023
92 healthy adults | Single and multiple ascending dose studies
Established 79.1% oral bioavailability, 29-49 hour half-life supporting once-daily dosing, and safety profile consistent with GLP-1 class. Confirmed no food effect on absorption, allowing unrestricted dosing.
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