Alexa

September Fall Special Edition 2021

A Global Leader in Enhancing the Speed and Efficiency of Orally-Delivered Fat-Soluble Active Molecules and Drugs: Lexaria Bioscience

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“Lexaria’s DehydraTECH™ is clinically demonstrated to significantly increase bioavailability for fat soluble drugs.”

Lexaria Bioscience Corp. is a Kelowna-based global innovator in drug delivery platforms. It began work in the fields of enhanced delivery of active ingredients and drugs, in 2014. However, the company was incorporated in 2004.

To highlight and further understand what Lexaria stands for and seeks to explore in this segment, I sat down with Chris Bunka, who serves as the company’s Chief Executive Officer.

Below is an excerpt.

Q. How does Lexaria Bioscience’s proprietary drug delivery technology, DehydraTECH™, improve APIs' entry into the bloodstream? And to what drugs and active ingredients this technology can be applied?

In May 2016, we commenced out­licensing our patented DehydraTECH™ technology for improved delivery of bioactive compounds that promote healthy ingestion methods, lower overall dosing, and higher effectiveness in active molecule delivery.

DehydraTECH™ improves the way active pharmaceutical ingredients (APIs) enter the bloodstream by promoting healthier oral ingestion methods and increasing the effectiveness of fat-soluble active molecules, thereby lowering overall dosing. This technology can be applied to many different ingestible product formats, including foods, beverages, oral suspensions, tablets, and capsules.

Besides, DehydraTECH has repeatedly demonstrated with cannabinoids and nicotine the ability to increase bio-absorption by up to 5-10x, reduce the time of onset from 1-2 hours to minutes, and mask unwanted tastes, and is planned to be further evaluated for orally administered bioactive molecules, including anti-virals, cannabinoids, vitamins, non-steroidal anti-inflammatory drugs (NSAIDs), and nicotine. We, at Lexaria, have licensed DehydraTECH to multiple companies, including a world-leading tobacco producer for the development of smokeless, oral-based nicotine products and for use in industries that produce cannabinoid beverages edibles and oral products. In addition, we operate a licensed in-house research laboratory and hold a robust intellectual property portfolio with 19 patents granted and over 50 patent applications pending around the world.

Q. Please walk us through your R&D programs?

Lexaria relies on applied R&D programs to generate confirmatory results and data evidencing improved drug delivery characteristics that enable pursuit of commercial opportunities and/or corporate relationships. As such, we consider advancing these applied R&D studies to be a vital early step towards our goal of establishing commercial relationships with potential industry partners to utilize DehydraTECH within our existing product lines or in the development of new product lines.

Q. VIRAL-A20-2 — A tolerability and pharmacokinetic or ‘PK’ study in animals using antiviral drugs remdesivir and ebastine.

Animal dosing and all in-life procedures and sample analysis have been completed, but data analysis is underway with a view to reporting soon. There were four groups of 10 animals dosed to determine if DehydraTECH-enhanced remdesivir and ebastine were well tolerated and enabled improved overall quantity of drug delivery (Area Under the Curve or AUC) relative to non-enhanced controls as Lexaria has successfully evidenced for other antiviral drugs. Lexaria hopes to build on recently announced positive findings from its VIRAL-C21-3 study that evidenced effective inhibition of the COVID-19 SARS-CoV-2 virus using these DehydraTECH-enhanced compounds in an in vitro screening assay.

Q. VIRAL-A20-3 — An additional tolerability and PK study in animals evaluating AUC for 3 other antiviral drugs.

Animal dosing and all in-life procedures have been completed and sample analyses is ongoing. There were six groups of 10 animals dosed in this study examining tolerability and quantity of drug delivery for three other antiviral drugs of interest with potential utility against the COVID-19 SARS-CoV-2 virus.

Q. VIRAL-MC21-1 — A molecular characterization (MC) study being performed by Canada's National Research Council.

In this study, Nuclear Magnetic Resonance (NMR) and Liquid Chromatography-High

Resolution Mass Spectrometry (LC-HRMS) are being applied to five DehydraTECH-enhanced antiviral drug formulations currently being investigated by the company in studies VIRAL-A20-2 and VIRAL-A20-3. Molecular characterization is an important step in determining whether Lexaria’s DehydraTECH technology alters the underlying drugs to a degree significant enough to result in formation of a covalently bonded new molecular entity (NME). NMEs are generally subjected to more involved regulatory examination and approval processes than non-NMEs. Lexaria has previously reported findings evidencing that NME formation did not occur following DehydraTECH formulation with other substances of interest such as nicotine and cannabidiol (CBD).

Q. HYPER-A21-1 and HYPER-A21-2 — Follow on blood pressure testing in animals pursuant to previously reported successful PK study findings.

Most results from these animal studies were released on May 6 and May 20, 2021 respectively demonstrating statistically significant gains in CBD absorption relative to controls using Lexaria's latest DehydraTECH 2.0 formulation innovations. The testing laboratory that performed this work has been engaged to perform certain follow-up work that includes monitoring of real-time animal blood pressure in response to select formulations from these PK evaluations. This work is hoped to complement Lexaria's previous human clinical study findings that have evidenced reduction in blood pressure following DehydraTECH-CBD administration. Animal dosing and in-life procedures have not yet commenced for this additional follow up work, but will be reported when developments warrant.

Q. NSAID-A21-1 — A tolerability and PK study in animals evaluating ibuprofen and naproxen.

Test articles were manufactured in April as planned, contracts were executed in early May with the animal testing laboratory performing this work, and initial animal dosing commenced the week of May 17 ahead of schedule. This work is currently underway with pilot tolerability evaluations in rodents in an effort to determine dosing that evidences superior gastrointestinal tolerability comparing Lexaria's DehydraTECH test articles to concentration-matched controls. Pending a successful outcome of the pilot tolerability investigation, formal pharmacokinetic testing will follow.

Q. Oral Nicotine: NIC-C21-1 (now NIC-A21-1) — A tolerability and PK study in animals evaluating oral nicotine.

This study has been renamed NIC-A21-1 following migration from an in vitro cell based study instead to an in vivo study in live anesthetized animals. This will allow Lexaria to perform a superior evaluation of the systemic absorption of nicotine upon oral pouch product dosing in the animals. Human oral pouch dosing of nicotine is a rapidly growing trend in several locations around the world and Lexaria believes this redesigned study will more appropriately measure outcomes. The contract has been signed with the animal testing laboratory that will be performing this work and all study test articles have been manufactured and are in the process of being shipped to the laboratory for dosing purposes. Animal dosing in this study is scheduled to commence in July ahead of the originally stated September/October dosing commencement schedule for NIC-C21-1.

Q. Could you tell us more about how Lexaria’s DehydraTECH(TM)-enabled remdesivir and ebastine effectively inhibit the COVID-19 SARS-CoV-2 virus?

Remdesivir and Ebastine processed with DehydraTECH were effective at inhibiting the COVID-19 SARS-CoV-2 virus using an in vitro screening assay in infected cells in Lexaria study VIRAL-C21-3.

The main purpose of the study was to confirm that Lexaria’s DehydraTECH formulation and processing methodology did not negate the known antiviral efficacy of these compounds before proceeding to larger, planned in vivo efficacy testing. These preliminary findings evidenced SARS-CoV-2 inhibitory performance commensurate with our expectations warranting ongoing and further investigation in animal testing.

This study used one of the most widely applied and informative predictive measures of drug efficacy to measure the half-maximal inhibitory concentration (IC50) of the drugs when formulated with DehydraTECH. This was an important step towards advancing to animal and ultimately human efficacy testing for the purpose of using DehydraTECH-processed drugs to treat COVID-19.

This study was performed using a primate cell line, VERO-E6, and conducted by a leading independent, US biosafety level-3 testing laboratory that delivers critical services to government and commercial customers. That third party laboratory was responsible for study administration, quality control, and generation of results.

Lexaria’s antiviral study program may also have benefits beyond COVID-19, including a wide range of other viral disease indications where improved oral delivery performance is needed. The combined market for antiviral drugs is projected to be over USD $66.7 billion by 2025.

2021 DehydraTECH Investigations Cumulative Market Value is Over $100 Billion

Planned pharmacokinetic studies will evaluate ability to improve quantity of drug delivered and speed with which it is delivered, in all of these areas:

  • Oral Cannabinoids: Estimated at $18.4 billion in 2021 and expected to reach $46.2 billion in 2025.
  • Antivirals: Estimated at $52.1 billion in 2021 and expected to grow to $66.7 billion by 2025.
  • Oral Mucosal Nicotine: Global smokeless tobacco product was a $13.6 billion market in 2018, forecast to grow at 7.2% per year until 2025.
  • PDE5 Inhibitors: Phosphodiesterase inhibitors with brand names such as Viagra represented a $4.4 billion market in 2014.
  • Human Hormones: Estrogen and Testosterone replacement therapies represent a $21.9 billion market.
  • Ibuprofen and Naproxen: Global NSAID sales were $15.6 billion in 2019 and projected $24.4 billion by 2027
  • Vitamin D3: Global Vitamin D3 market size was $1.1 billion in 2021, growing at 7.0% per year and expected to reach $1.7 billion in 2026.

“So far, 19 patents have been granted to Lexaria and over 50 patent applications pending around the world for technology designed for fast acting, less expensive, and more effective oral drug delivery.”