BetterLife Pharma Provides Scientific Update of Mechanism of Action of BETR-001 in Treatment of Psychiatric Disorders

Rhea-AI Summary

BetterLife Pharma has presented promising preclinical data for BETR-001, its proprietary non-hallucinogenic compound for treating psychiatric disorders. The drug shows a breakthrough mechanism by selectively activating the 5HT2A receptor to 60%, staying below the 70% hallucination threshold, unlike LSD which activates it to 90%. Key advantages include: no 5HT2B receptor activation (improving cardiac safety), no tolerance development allowing daily dosing, and potential for at-home administration as a non-controlled substance. The company has secured USPTO patent protection and completed most IND-enabling studies, with human trials projected to begin in H1 2026. BETR-001's unique properties position it as a potential new paradigm for treating depression, anxiety, and PTSD.

Positive

• Preclinical data shows promising therapeutic effects without hallucinogenic side effects
• Unique 5HT2A receptor activation mechanism (60%) stays below hallucination threshold (70%)
• No cardiac safety concerns due to lack of 5HT2B receptor activation
• Patent protection secured from USPTO
• Allows daily dosing without tolerance development
• Potential for at-home administration as non-controlled substance
• Most IND-enabling studies completed

Negative

• Human trials not yet started, projected for H1 2026
• Still in early development stages with only preclinical data available

VANCOUVER, British Columbia, May 14, 2025 (GLOBE NEWSWIRE) -- BetterLife Pharma Inc. (“BetterLife” or the “Company”) (CSE: BETR / OTCQB : BETRF / FRA: NPAU), an emerging biotech company focused on the development of BETR-001, a non-hallucinogenic neuroplastogen in the treatment of psychiatric and neurological disorders, recently presented a scientific update at Bloom Burton Conference on May 5, 2025 in Toronto, Canada.

BetterLife reported that its proprietary compound, BETR-001, is showing very promising preclinical data of its breakthrough ability to provide therapeutic effect in depression/anxiety animal models. Current methods of treating depression/anxiety primarily focus on increasing the level of one of the three neurotransmitters: serotonin, norepinephrine and/or dopamine in the brain. Each neurotransmitter has different receptor targets, and each receptor performs different functions. Current treatments are usually reuptake inhibitors such as SSRIs (selective serotonin reuptake inhibitors) and by increasing the amount of a neurotransmitter, all its receptors are activated. What is needed are new treatments that activate the neuroreceptors themselves, and more importantly, only selective subsets of these receptors.

The therapeutic effects of BETR-001 seen in preclinical models are primarily driven by its activation (agonism) of serotonin’s 5HT2A receptor. Not only does BETR-001 activate the 5HT2A receptor, which plays a key role in depression/anxiety, this activation is via a mechanism that allows for a highly efficacious therapeutic effect without hallucinogenic side effects. This stands in contrast to other potent 5HT2A activators, such as LSD, psilocybin and other psychedelics. BetterLife has reported on the details of BETR-001 activation of the 5HT2A receptor previously (Lewis et al., Cell Reports, 2023). Recently studies have shown that the activation of the 5HT2A receptor above 70% leads to hallucination (Wallach et al., Nature Communications, 2023). Ideally, a therapeutic agent should activate 5HT2A but stay below the 70% threshold. BETR-001 fulfills this parameter perfectly: activating 5HT2A maximally to 60%, unlike LSD, which activates 5HT2A to near 90%. This is shown in our 5HT2A receptor activation data below, where the X-axis is an increasing amount of the drug, and the Y axis is the percentage activation of the 5HT2A receptor. The drugs tested are 5-HT (the parent serotonin), LSD and BETR-001.

TABLE: BETR-001 5HT2A Receptor Activation Data

BetterLife believes that BETR-001’s novel mechanism of action provides a new paradigm for treatment of psychiatric disorders such as depression, anxiety and PTSD. It activates the 5HT2A receptor partially but stays below the hallucination threshold. In addition, unlike LSD, psilocybin, MDMA and other such agents BETR-001 is not an activator of the 5HT2B receptor. Activation of 5HT2B has been linked to cardiac safety. The neuroreceptor selectivity of BETR-001 in this regard is another of its key advantages over other competitor agents. An additional benefit of BETR-001 is that repeated dosing does not induce tolerance, unlike classic agents like LSD. This allows daily administration if needed. Furthermore, the lack of hallucinations with BETR-001 means it is a non-controlled substance and patient self-administration at home is possible. Finally, an overarching property of BETR-001 is that it is a very potent neuroplastogen.

BetterLife has been granted a composition of matter patent on BETR-001 by the USPTO (BetterLife press release January 14, 2025). BetterLife has had its BETR-001 pre-IND meeting with the FDA and has completed most of the required IND-enabling studies. The BETR-001 IND filing and start of human trials are projected for H1 2026. BetterLife is considering the development of BETR-001 for treatment of various psychiatric and neurological disorders.

About BetterLife Pharma 

BetterLife Pharma Inc. is an emerging biotechnology company primarily focused on developing and commercializing two compounds, BETR-001 and BETR-002, to treat neuro-psychiatric and neurological disorders.

BETR-001, which is in preclinical and IND-enabling studies, is a non-hallucinogenic neuroplastogen. BETR-001 is a non-controlled substance. BETR-001 will be developed for the treatment of various psychiatric and neurological disorders. BETR-001 pending patent, for composition and method of use, covers treatment of major depressive disorder, anxiety disorder and neuropathic pain and other neuro-psychiatric and neurological disorders. 

BETR-002, which is in preclinical and IND-enabling studies, is based on honokiol, the active anxiolytic ingredient of magnolia bark. BetterLife’s pending method of use and formulations patent covers treatment of anxiety-related disorders including benzodiazepine dependency. 

BetterLife also owns a drug candidate for the treatment of viral infections and is in the process of seeking strategic alternatives for further development.

For further information, please visit BetterLife Pharma.

Contact

David Melles, Investor Relations Manager 
Email: David.Melles@blifepharma.com
Phone: 1-778-887-1928 

Cautionary Note Regarding Forward-Looking Statements

No securities exchange has reviewed nor accepts responsibility for the adequacy or accuracy of the content of this news release. This news release contains forward-looking statements relating to product development, licensing, commercialization and regulatory compliance issues and other statements that are not historical facts. Forward-looking statements are often identified by terms such as “will”, “may”, “should”, “anticipate”, “expects” and similar expressions. All statements other than statements of historical fact, included in this release are forward-looking statements that involve risks and uncertainties. There can be no assurance that such statements will prove to be accurate and actual results and future events could differ materially from those anticipated in such statements. Important factors that could cause actual results to differ materially from the Company’s expectations include the failure to satisfy the conditions of the relevant securities exchange(s) and other risks detailed from time to time in the filings made by the Company with securities regulations. The reader is cautioned that assumptions used in the preparation of any forward-looking information may prove to be incorrect. Events or circumstances may cause actual results to differ materially from those predicted, as a result of numerous known and unknown risks, uncertainties, and other factors, many of which are beyond the control of the Company. The reader is cautioned not to place undue reliance on any forward-looking information. Such information, although considered reasonable by management at the time of preparation, may prove to be incorrect and actual results may differ materially from those anticipated. Forward-looking statements contained in this news release are expressly qualified by this cautionary statement. The forward-looking statements contained in this news release are made as of the date of this news release and the Company will update or revise publicly any of the included forward-looking statements as expressly required by applicable law.

An infographic accompanying this announcement is available at https://www.globenewswire.com/NewsRoom/AttachmentNg/82d32974-a4a8-4dd3-b49a-fddeea51dd9c

FAQ

What is BETR-001 and how does it work for treating psychiatric disorders?

BETR-001 is a non-hallucinogenic neuroplastogen that selectively activates the 5HT2A receptor to 60%, staying below the 70% hallucination threshold. This mechanism allows therapeutic effects for depression/anxiety without hallucinogenic side effects.

When will BETRF start human trials for BETR-001?

BetterLife Pharma plans to file IND and begin human trials for BETR-001 in the first half of 2026.

What advantages does BETR-001 have over traditional psychiatric medications?

BETR-001 offers several advantages: no hallucinogenic effects, no cardiac safety concerns, no tolerance development allowing daily dosing, and potential for at-home administration as a non-controlled substance.

How is BETR-001 different from psychedelics like LSD and psilocybin?

Unlike LSD and psilocybin, BETR-001 activates the 5HT2A receptor only to 60% (vs. LSD's 90%), avoiding hallucinations. It also doesn't activate the 5HT2B receptor, improving cardiac safety.

What psychiatric conditions could BETR-001 potentially treat?

BETR-001 is being developed for the treatment of various psychiatric disorders, including depression, anxiety, and PTSD.