Lexaria Bioscience Corp. has announced the completion of dosing in its human pilot study #3, which investigates an orally dosed, DehydraTECH-processed version of tirzepatide, a dual-action glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) receptor agonist. The study, conducted in nine healthy volunteers, marks a significant step toward developing an oral alternative to injectable GLP-1 receptor agonists currently dominating the market.
The trial evaluated the tolerability, pharmacokinetic (PK) profile, and impact on blood sugar control of DehydraTECH-processed tirzepatide, using Zepbound® as the tirzepatide input material. The seven-day dosing phase, completed on November 16th, involved subjects receiving either oral DehydraTECH-processed tirzepatide capsules or a single injected dose of tirzepatide in a randomized, cross-over design.
Safety and Tolerability
Notably, no serious adverse events were observed during the dosing visits. This is a key consideration for Lexaria, which aims to create a well-tolerated oral version of Eli Lilly’s tirzepatide products, currently available only as injectables.
Market Context and Potential
Tirzepatide, marketed as Zepbound® and Mounjaro® by Eli Lilly, is projected to generate approximately $15 billion in revenue in 2024. Clinical data has demonstrated tirzepatide's efficacy in reducing the risk of progression to type 2 diabetes by 94% over three years and achieving an average body weight reduction of 23% maintained over the same period.
Lexaria's previous studies with DehydraTECH-processed semaglutide (Rybelsus®, Ozempic®, and Wegovy®) have shown improved absorption rates, reduced blood sugar, and fewer adverse events compared to Rybelsus® tablets alone. Semaglutide and tirzepatide currently account for over 90% of revenue in the GLP-1/GIP receptor agonist market.
Study Design
The DehydraTECH-tirzepatide test articles were formulated using Zepbound® and administered under fasted conditions. The oral formulation was dosed at 20 mg tirzepatide daily for seven days, while the injectable Zepbound® formulation was administered as a single 2.5 mg dose. Blood samples were collected at multiple time points over 24 hours on the first day of each treatment phase, with additional samples taken daily for the following seven days. Standardized meals were provided to the test subjects at specific times after dosing.
Anticipated Results
Lexaria anticipates data analysis in December, with results expected in January 2025. The company hopes to demonstrate meaningful absorption rates of oral tirzepatide, which could transform the treatment landscape for type 2 diabetes and obesity.
