Peptide Library / Detail
Orforglipron
Half-life
Approximately 20-30 hours
Delivery
Oral administration (tablet or capsule)
Dosage
—
Research Use Only
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Description
Orforglipron is an oral, small-molecule GLP-1 receptor agonist under development for the treatment of obesity and type 2 diabetes. Unlike traditional peptide-based GLP-1 agonists that require injection, orforglipron is taken orally, offering improved convenience and patient compliance. It represents a novel class of non-peptide compounds that activate the GLP-1 receptor to regulate glucose metabolism and reduce body weight.
Usage
Orforglipron is administered orally once daily in investigational trials. Clinical studies have evaluated doses ranging from 12 mg to 45 mg daily, with dose escalation protocols used to improve tolerability. The medication is typically taken at the same time each day, with or without food. Current research protocols involve gradual dose titration over several weeks to minimize gastrointestinal side effects.
Mechanism of Action
Orforglipron binds to and activates the GLP-1 (glucagon-like peptide-1) receptor, mimicking the action of endogenous GLP-1 hormone. This activation stimulates glucose-dependent insulin secretion, suppresses glucagon release, slows gastric emptying, and reduces appetite through central nervous system pathways. As a non-peptide small molecule, it offers oral bioavailability while maintaining receptor selectivity and agonist activity comparable to peptide-based GLP-1 receptor agonists.
Benefits(6)
- Significant weight reduction in patients with obesity (up to 14.7% body weight loss)
- Improved glycemic control and HbA1c reduction in type 2 diabetes patients
- Oral administration providing greater convenience compared to injectable GLP-1 agonists
- Reduction in fasting plasma glucose and postprandial glucose levels
- Potential cardiovascular and renal protective effects similar to other GLP-1 receptor agonists
- Decreased appetite and caloric intake through centrally-mediated satiety pathways
Side Effects(8)
- Nausea (most common, occurring in 40-60% of patients)
- Vomiting and gastrointestinal disturbances
- Diarrhea or constipation
- Abdominal pain and dyspepsia
- Decreased appetite beyond therapeutic intent
- Potential increase in heart rate
- Dizziness or headache
- Possible risk of pancreatitis (monitoring required)