BetterLife provides update of mechanism of action of BETR-001

BetterLife (BETRF) Pharma 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 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 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. Recently studies have shown that the activation of the 5HT2A receptor above 70% leads to hallucination. 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, LSD and BETR-001.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 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.