25 June 2021 - - US-based biotechnology company Lyndra Therapeutics has posted results from a preclinical study on LYN-013, the company's oral, ultra-long-acting, extended-release buprenorphine capsule, in development for the weekly treatment of opioid use disorder, the company said.

These data show that a single weekly dose of LYN-013 sustained drug levels of buprenorphine over the one-week dosing period and sustained suppression of opioid self-administration in an animal model.

The results of this preclinical study, evaluating the pharmacokinetics and pharmacological effects of LYN-013, were presented this week in an oral presentation at the College of Problems on Drug Dependence 83rd Annual Scientific Virtual Meeting.

LYN-013 is designed to mitigate the poor oral bioavailability of buprenorphine, an FDA-approved medication for OUD, with a novel oral dosage form designed to provide consistent target therapeutic levels of buprenorphine over the course of an entire week from a single oral capsule.

It is one of Lyndra's two Opioid Use Disorder Programs supported by the National Institute on Drug Abuse (NIDA), part of the National Institutes of Health, as part of the Helping to End Addiction Long-term Initiative, or NIH HEAL Initiative.

In this study, sponsored by Lyndra in collaboration with the New York State Psychiatric Institute, buprenorphine HCl and naloxone HCl were co-formulated and configured in an oral, ultra-long-acting, sustained release capsule, LYN-013, to release buprenorphine at a near-constant rate over a seven-day dosing period while remaining in the stomach.

LYN-013 enabled average buprenorphine doses of up to 24 mg per day over seven days from a single dose capsule.

Pharmacokinetics were evaluated in dogs, while pharmacological effects of multiple dose levels of LYN-013 were assessed in an opioid self-administration model in non-opioid-dependent NHPs and compared with buprenorphine delivered via continuous intravenous and intragastric infusion.

Opioid use disorder is a national crisis that has major public health implications, affecting approximately two m people in the US Overdose deaths involving opioids claimed 500,000 lives from 1999-2019, and these numbers have risen further during the ongoing COVID-19 pandemic.

According to provisional data from the Centers for Disease Control and Prevention, it is predicted that more than 90,000 drug overdose deaths occurred in the US in the 12 months ending in November 2020 the highest number of overdose deaths ever recorded in a 12-month period.

While there are a number of evidence-based treatments available for OUD, these medications are highly regulated, and may require daily patient visits to a specialized clinic to take medication while observed by a medical professional.

This strict therapeutic regimen presents significant challenges to ensuring patient access, adherence, and compliance, to these important treatments.

Lyndra Therapeutics is pioneering the first-ever oral, ultra-long-acting, sustained release therapies, which have the potential to fundamentally change the way people take medicine by enabling patients to take a pill once a week rather than daily.

The company's breakthrough Extended-Release Oral Capsule is designed to provide consistent drug levels for an entire week or as long as a month, from one, normal-sized capsule something no oral therapy has ever achieved before.

Lyndra's robust pipeline is made up of therapies with established and well-known safety profiles across a number of disease areas in which non-adherence is known to be a significant driver of outcomes, including schizophrenia and other central nervous system diseases, diabetes, cardiovascular disease and opioid abuse disorder, among others.

The company is also committed to advancing its platform across new chemical entities and a variety of critical global and public health opportunities alongside partners such as the Bill and Melinda Gates Foundation and the NIH.

Research reported in this announcement was supported by the National Institute on Drug Abuse through the NIH HEAL Initiative under Award Number UG3DA047709. The content is solely the responsibility of the authors and does not represent the official views of the National Institutes of Health.