Lyndra Therapeutics Presents Preclinical Data on Once-Weekly Oral Buprenorphine Treatment, LYN-013, in Development for Opioid Use Disorder

Data demonstrate LYN-013 delivered sustained buprenorphine drug levels over one-week dosing period and showed sustained suppression of opioid self-administration in an animal model

Results suggest that LYN-013 has potential to provide a new, weekly oral treatment option for opioid use disorder

WATERTOWN, Mass.–(BUSINESS WIRE)–Lyndra Therapeutics, a clinical-stage biotechnology company working to make daily pills a thing of the past, today announced results from a preclinical study on LYN-013, the company’s oral, ultra-long-acting, extended-release (ER) buprenorphine capsule, in development for the weekly treatment of opioid use disorder (OUD). 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 (CPDD) 83^rd Annual Scientific Virtual Meeting.

“We are encouraged by the possibility of providing not just the first oral buprenorphine treatment, but to provide it as a weekly dosing option, which has the potential to be a game-changer for the two million people in the U.S. with opioid use disorder that currently face a lack of therapeutic options, limited access to approved prescribers, and strict therapeutic regimes,” said Dr. Patricia Hurter, Chief Executive Officer of Lyndra Therapeutics. “These promising results, and the strong Phase 2 clinical proof-of-concept data from our lead program, a weekly oral risperidone treatment for people with schizophrenia that is moving into pivotal clinical trials, add to our momentum as our platform moves into the commercialization phase.”

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 (NIH), as part of the Helping to End Addiction Long-term Initiative, or NIH HEAL Initiative.

“NIDA, and other agencies within the U.S. federal government, have called for new treatment strategies for OUD to help address the current opioid crisis, including new formulations of existing medications to improve access, adherence and reduce diversion,” said Dr. Richard Scranton, Chief Medical Officer of Lyndra Therapeutics. “Our OUD programs, which include the development of once-weekly oral formulations of both buprenorphine and levomethadone, have the potential to not only provide improved pharmacologic options to patients but also decrease the burden of disease associated with daily medication and support an improved quality of life.”

About LYN-013 Preclinical Study

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 (n=12), while pharmacological effects of multiple dose levels of LYN-013 were assessed in an opioid self-administration model in non-opioid-dependent NHPs (n=6) and compared with buprenorphine delivered via continuous intravenous and intragastric infusion.

Key findings from the study include:

• Once-weekly oral buprenorphine (LYN-013) demonstrated sustained plasma buprenorphine concentrations for more than one week.
• Oral administration of LYN-013 suppressed intravenous fentanyl self-administration and was maintained for approximately seven days, with maximal suppression occurring within 48 hours, and return to baseline by 13 days.
• LYN-013 was retained in the stomach for at least 7 days following oral administration.

About Opioid Use Disorder

Opioid use disorder (OUD) is a national crisis that has major public health implications, affecting approximately two million people in the U.S. Overdose deaths involving opioids claimed 500,000 lives from 1999-2019, and these numbers have risen further during the ongoing COVID-19 pandemic.¹ 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 U.S. in the 12 months ending in November 2020 – the highest number of overdose deaths ever recorded in a 12-month period.¹ 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.

About Lyndra Therapeutics

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 & Melinda Gates Foundation and the NIH. For more information, visit the Company’s website at www.lyndra.com.

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.

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¹ Centers for Disease Control and Prevention. Provisional Drug Overdose Death Counts. https://www.cdc.gov/nchs/nvss/vsrr/drug-overdose-data.htm. Accessed June 22, 2021.

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