Lexaria Bioscience Corp. has commenced dosing in its human pilot study #3, evaluating an orally administered version of tirzepatide, the active ingredient in Zepbound® and Mounjaro®, utilizing Lexaria's DehydraTECH drug delivery technology. The study, referred to as Study GLP-1-H24-3, aims to assess the tolerability, pharmacokinetic profile, and impact on blood glucose levels of the DehydraTECH-processed tirzepatide compared to the injectable form of the drug.
The trial is enrolling up to 10 healthy volunteers. Participants will undergo two seven-day dosing phases in a cross-over design. The first phase involves daily oral administration of DehydraTECH-processed tirzepatide capsules (20mg), while the second phase involves a single injection of Zepbound® (2.5mg), with a washout period between the phases. Initial seven-day dosing phase of either an oral DehydraTECH-processed tirzepatide capsule or a single injected tirzepatide dose is scheduled to be completed on October 13th. After a multi-week washout period, the second (final) seven day dosing phase will be administered in mid-November where subjects will receive the alternate treatment condition than what was received during the initial dosing phase. Blood samples will be collected at multiple time points to evaluate tirzepatide levels and glucose control.
Tirzepatide, a dual GLP-1 and GIP receptor agonist marketed by Eli Lilly under the brand names Zepbound® and Mounjaro®, is projected to generate approximately $15 billion in revenue in 2024. Currently, tirzepatide is only available as an injectable, creating a need for more convenient oral formulations.
Lexaria's DehydraTECH technology has previously demonstrated improved absorption rates and reduced adverse events with semaglutide, another GLP-1 receptor agonist, compared to the oral formulation Rybelsus®. The company hopes to replicate these findings with tirzepatide, potentially offering a more patient-friendly alternative to injections. No serious adverse events have been observed thus far during this initial dosing phase.
Many design characteristics of the Study, also referred to as Study GLP-1-H24-3, are similar to Lexaria’s initial GLP-1 human pilot study #1. The DehydraTECH-tirzepatide test articles were compound formulated using Zepbound®, strictly for research purposes, dosed to the subjects under fasted conditions. The Study is designed to measure tolerability and side effects, blood levels of tirzepatide, and blood glucose levels. The DehydraTECH-tirzepatide composition was formulated at a strength of 20 mg tirzepatide to be administered orally daily for seven days. The Zepbound® formulation has a strength of 2.5 mg tirzepatide to be administered once via injection with the subject monitored over the same seven day duration applicable with the oral DehydraTECH-tirzepatide condition. Blood samples will be taken multiple times during the first 12 hours post dosing on the first day of each treatment phase, with a final blood draw taken 24 hours after dosing; and, a standardized meal will be fed to the test subjects at a point in time after dosing. Single blood samples will also be taken daily on each of the second through eighth days following commencement of dosing. Up to ten healthy subjects are expected to be dosed with each test article following a randomized, cross over study design across two study phases.
