BioZapetite delivers orforglipron (6 mg), a first-in-class oral, small-molecule GLP-1 receptor agonist designed for investigational use. Unlike peptide GLP-1 agonists, orforglipron is orally bioavailable without fasting or water restrictions and demonstrates robust pharmacology in glucose and weight regulation.
Together, its mechanisms are designed to:
- Promote glucose disposal & insulin sensitivity by enhancing glucose-dependent insulin secretion, suppressing glucagon, and improving post-prandial glucose control [1][3].
- Drive weight reduction & appetite control through central satiety signaling, slowed gastric emptying, and consistent reductions in caloric intake [1][2].
- Improve lipid & cardiometabolic health via secondary benefits of weight loss, including reductions in blood pressure, triglycerides, and waist circumference [1][3].
- Provide oral dosing convenience with a ~29–49 h half-life supporting once-daily use and no need for co-formulated absorption enhancers [4][6].
- Exhibit a safety profile consistent with injectable GLP-1 medicines, dominated by mild-to-moderate GI events during dose titration, with no hepatic safety signal in Phase 3 readouts [3][5].
These complementary mechanisms make BioZapetite a promising candidate for research in weight regulation, glycemic control, and cardiometabolic health.
BioZapetite Structure
| Ingredient | Dose (per capsule) | Key Actions |
| Orforglipron | 6 mg | Non-peptide GLP-1R agonist; enhances insulin secretion, ↓glucagon, ↓appetite, slows gastric emptying; t½ ~29–49 h; oral bioavailability without fasting/water restrictions [1][3][4][6] |
Research Areas
- Appetite Regulation & Body Weight
- Glucose Disposal & Glycemic Control
- Cardiometabolic Risk Reduction
- Oral Small-Molecule Incretin Pharmacology
Translational Safety & GI Tolerability
Glucose Disposal & Glycemic Control
In a 26-week multicentre trial in type 2 diabetes (n=383), orforglipron reduced HbA1c up to –2.10% and body weight by –10.1 kg, significantly outperforming placebo and matching/exceeding dulaglutide at higher doses [3]. A 12-week Phase 1b trial reported HbA1c reductions of –1.5% to –1.8% with up to –5.8 kg weight loss [4].
Appetite & Weight Regulation
In a 36-week obesity study, orforglipron produced –9.4% to –14.7% weight reduction vs –2.3% with placebo, with 46–75% of participants achieving ≥10% weight loss depending on dose [1][2]. Improvements were observed in all prespecified cardiometabolic measures, including waist circumference, blood pressure, and lipid markers.
Oral Pharmacology & PK
Unlike oral peptide GLP-1 formulations, orforglipron does not require an absorption enhancer or fasting. AUC and Cmax decrease ~18–24% with food, but this is not clinically significant [6]. Half-life ~29–49 h supports once-daily dosing [4].
Safety & Tolerability
Across Phase 2 and Phase 3 programs, the safety profile was consistent with injectable GLP-1 RAs. GI events (nausea, diarrhea, dyspepsia, vomiting) were most common and dose-related, occurring mainly during titration [3][5]. In Phase 3 (ACHIEVE-1), discontinuations due to AEs were 4–8% vs 1% with placebo, and no hepatic safety signals were detected [5].
References
- Wharton S, et al. NEJM 2023. Orforglipron in obesity: –9.4% to –14.7% weight loss at 36 weeks; improvements in cardiometabolic measures. https://pubmed.ncbi.nlm.nih.gov/37351564/
- Wharton S, et al. NEJM 2023. Dose-dependent weight loss (–8.6% to –12.6% at 26 weeks) in obesity without diabetes. https://pubmed.ncbi.nlm.nih.gov/37351564/
- Frias JP, et al. Lancet 2023. Phase 2 T2D: HbA1c ↓ up to –2.10%; weight ↓ up to –10.1 kg; greater efficacy than dulaglutide at high dose. https://cardiometabolicforum.com/publications/99
- Pratt E, et al. Diabetes Obes Metab 2023. Phase 1b: HbA1c –1.5% to –1.8%, weight loss –5.8 kg; t½ ~29–49 h. https://pubmed.ncbi.nlm.nih.gov/37264711/
- Lilly Press Release 2025. Phase 3 ACHIEVE-1: HbA1c ↓ –1.3% to –1.6%; weight ↓ –7.9%; GI AEs dose-related; no hepatic signal. https://www.prnewswire.com/news-releases/lillys-oral-glp-1-orforglipron-demonstrated-statistically-significant-efficacy-results-and-a-safety-profile-consistent-with-injectable-glp-1-medicines-in-successful-phase-3-trial-302430985.html
- Ma X, et al. Diabetes Therapy 2024. Food-effect PK: AUC/Cmax ↓ ~18–24% fed vs fasted; overall well-tolerated; no SAEs. https://link.springer.com/article/10.1007/s13300-024-01554-1
Note: BioZapetite is supplied strictly for investigational research use only. It is not approved or intended for diagnostic, therapeutic, or in vivo applications in humans or animals.
