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For research and educational purposes only. Not intended for human consumption.

Orforglipron

Extensively Studied
Updated Dec 2025

Oral Small-Molecule GLP-1 Receptor Agonist | Weight Loss & Diabetes

Oral
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36-45mg daily
Once daily
Oral
N/A - Oral tablet
Continuous
Typical duration
Room
Storage

Overview

What is Orforglipron?

Orforglipron is a novel oral non-peptide GLP-1 receptor agonist in Phase 3 clinical trials for obesity and type 2 diabetes. Unlike injectable GLP-1 agonists, it can be taken as a daily pill without food restrictions, offering similar weight loss efficacy (up to 14.7%) with greater convenience. Developed by Eli Lilly as a potential game-changer in obesity treatment.

Key Benefits

Oral administration (no injections), no food restrictions, comparable efficacy to injectable GLP-1s, daily dosing convenience, room temperature storage.

Mechanism of Action

Orforglipron is a small molecule that activates GLP-1 receptors similarly to endogenous GLP-1, reducing appetite, increasing satiety, and improving insulin secretion in a glucose-dependent manner.

Molecular Information

~500 Da (small molecule)
Weight
0
amino acids
Non-peptide GLP-1 agonist
Type
Amino Acid Sequence:
N/A - Small molecule compound
* First-in-class oral non-peptide GLP-1 receptor agonist

Pharmacokinetics

Peak
4-6 hours
Half-life
~30 hours
Cleared
~6 days
100%50%0%0h6h12h18h24h
Peak
Half-life
Cleared
Phase 3 trial data

Research Indications

Obesity Without Diabetes

Up to 14.7% weight loss at 36 weeks in Phase 2 trials.

Obesity With Type 2 Diabetes

Significant weight loss in diabetic patients.

Cardiometabolic Improvement

Improvements in cardiovascular risk factors.

Research Protocols

Disclaimer: Orforglipron is in Phase 3 clinical trials and not yet FDA approved. Protocols are based on clinical trial data.

GoalDoseFrequencyRoute
Obesity (Phase 3 dose)36-45mg dailyOnce dailyOral
Diabetes (Phase 3 dose)36-45mg dailyOnce dailyOral
Dose Escalation3mg → 6mg → 12mg → 24mg → 36mg → 45mgWeekly increasesOral

Timing: Take at the same time each day. No food restrictions - can be taken with or without food.

Peptide Interactions

How to Reconstitute

Important: Always use bacteriostatic water (BAC). Sterile technique is essential.

1

No reconstitution needed - oral tablet

2

Take at the same time each day

3

Can be taken with or without food

4

Swallow whole with water

5

Do not crush, split, or chew tablets

6

Store at room temperature

Dosing Calculator

Calculate your injection volume with visual dosing guide

FINAL CONCENTRATION
2.50mg/mL
Each milliliter contains 2.50 mg of peptide
VISUAL REFERENCE (RESEARCH USE ONLY)

To obtain 250 mcg from this solution:

Draw 0.10 mL=10 units

(1 mL = 100 units on any insulin syringe)

0102030405060708090100
00.10.20.30.40.50.60.70.80.91.0
0.10 mL
10 units

Draw to this mark for 250 mcg

This calculator is for research purposes only. Always verify calculations and consult protocols.

Quality Indicators

Oral convenience

No injections required - daily tablet.

No food restrictions

Can be taken any time without fasting.

Not yet approved

Currently in Phase 3 trials - FDA approval pending.

GI side effects

Nausea and vomiting common during dose escalation.

What to Expect

  • Week 1-2: GI adaptation, appetite suppression begins
  • Week 4-8: Noticeable weight loss (2-5%)
  • Week 12-24: Significant weight loss (8-12%)
  • Week 24-36: Maximum weight loss achieved (up to 14.7%)

Side Effects & Safety

Side Effects

  • Most common: nausea (40-50%), vomiting, diarrhea
  • GI side effects typically mild-moderate and diminish over time
  • Dose escalation protocol minimizes side effects
  • Similar safety profile to injectable GLP-1s
  • Not recommended during pregnancy

When to Stop

  • Severe persistent nausea/vomiting
  • Signs of pancreatitis
  • Allergic reactions
  • As directed by healthcare provider

References

2 Studies

ACHIEVE-1 Phase 2 Obesity Trial

Human | Up to 45mg daily | 36 weeks | 14.7% weight loss at highest dose

Demonstrated oral GLP-1 can achieve weight loss comparable to injectables.

ACHIEVE-2 Phase 2 Diabetes Trial

Human | Various doses | 26 weeks | Significant HbA1c reduction

Showed glycemic efficacy in type 2 diabetes patients.

Quick Start Guide

Typical Dose
36-45mg daily (after escalation)
How Often
Once daily at the same time
Where to Inject
N/A - Oral tablet taken with water
Timing
Any time of day, with or without food
Effects Timeline
Appetite reduction: 1-2 weeks; Significant weight loss: 4-12 weeks; Full effect: 24-36 weeks
Storage
Room temperature, protect from moisture
Cycle Length
Continuous treatment
Break Between
Not applicable - continuous therapy

Research Disclaimer

Orforglipron is sold for laboratory research purposes only and is not intended for human or animal consumption. The information provided on this page is compiled from published research, veterinary studies, and anecdotal reports for educational purposes. This content does not constitute medical advice, diagnosis, or treatment recommendations. Any research involving Orforglipron must comply with all applicable local, state, and federal regulations. BioInfinity Lab makes no claims regarding the safety or efficacy of Orforglipron for any purpose. Consult qualified professionals for any research applications.