Oral bofanglutide shows sub-2% bioavailability but clean safety in Phase 1
A Chinese healthy-volunteer study found the SNAC-formulated oral GLP-1 well tolerated with only grade 1 GI side effects, though absorption stayed under 1.5% across doses.
Executive Summary
- An oral formulation of the GLP-1 receptor agonist bofanglutide produced measurable, dose-dependent drug exposure in a healthy-volunteer study, while absorption relative to an injected dose remained low across all tested doses.
- Tolerability tracked what has become the expected profile for this drug class: mild gastrointestinal side effects and no severe events, whether the drug was given as a single dose or repeated daily.
- A longer post-dose fasting period nearly doubled how much drug reached the bloodstream during repeated dosing, pointing to dosing conditions as a variable that could matter as much as the dose itself.
- The results support continuing to study once-daily oral dosing for type 2 diabetes and excess weight, without yet establishing whether the achieved exposure translates into a therapeutic effect.
The design: two-part Phase 1 study
The study evaluated oral bofanglutide, co-formulated with sodium N-(8- amino) caprylate (SNAC), an excipient designed to help large peptide molecules cross the gut lining. Part A enrolled 44 participants to receive single doses of oral bofanglutide at 30, 60, or 90 mg, or a 0.6 mg subcutaneous injection as a comparator. Part B enrolled 48 participants to take once-daily oral doses for 14 days, starting at 30 mg and stepping up to 60 mg, with participants fasting for either 30 or 60 minutes after dosing. The primary measures were safety, tolerability, relative bioavailability against the injected comparator, and pharmacokinetics and pharmacodynamics. SafetySafety, tolerability, relative bioavailability, pharmacokinetics, and pharmacodynamics of single and multiple doses of the novel oral bofanglutide in healthy Chinese participants.Jul 13, 2026
The exposure data
Single-dose relative bioavailability measured 0.56% at the 30 and 60 mg oral doses and 1.31% at 90 mg, versus the subcutaneous injection. Peak plasma concentration rose from 40.95 to 254.47 ng/mL and total drug exposure (AUC) rose from 3,980.76 to 28,180.67 h·ng/mL as the oral dose increased, a dose-dependent pattern consistent with absorption scaling with dose even at these low bioavailability levels. In the multiple-dose cohort, extending the post-dose fast from 30 to 60 minutes roughly doubled exposure, with apparent bioavailability at 9.22% versus 4.88%. SafetySafety, tolerability, relative bioavailability, pharmacokinetics, and pharmacodynamics of single and multiple doses of the novel oral bofanglutide in healthy Chinese participants.Jul 13, 2026
The safety profile
Most treatment-related adverse events tied to oral bofanglutide were grade 1 gastrointestinal events, and the study recorded no serious adverse events and no severe hypoglycemia across either the single-dose or 14-day repeated-dose cohorts. That profile held across the full oral dose range tested, from 30 mg up to 60 mg in the multiple-dose arm. SafetySafety, tolerability, relative bioavailability, pharmacokinetics, and pharmacodynamics of single and multiple doses of the novel oral bofanglutide in healthy Chinese participants.Jul 13, 2026
What the data support
The authors concluded that oral bofanglutide was safe and well tolerated and that its pharmacokinetic and pharmacodynamic profile supports further investigation of once-daily oral dosing for type 2 diabetes and overweight or obesity. The bioavailability figures establish that the SNAC formulation delivers dose-dependent systemic exposure from an oral tablet, the threshold question for any oral peptide program, without this abstract reporting whether that exposure level produced a glucose-lowering or weight effect. SafetySafety, tolerability, relative bioavailability, pharmacokinetics, and pharmacodynamics of single and multiple doses of the novel oral bofanglutide in healthy Chinese participants.Jul 13, 2026
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