BetterLife Obtains Positive In Vivo Oral Bioavailability, Food Effect & Pharmacokinetics Data for BETR-001

BetterLife Pharma Inc. recently announced it has obtained positive results from an in vivo oral bioavailability and food-effect pharmacokinetic (PK) study on BETR-001 in beagle dogs. BETR-001 (2-bromo-LSD, formerly TD-0148A) is a non-hallucinogenic derivative of lysergic acid diethylamide (LSD). Previous published studies have not included any data on PK for BETR-001. It was also unknown if presence of food would affect the bioavailability of orally administered BETR-001. The current study conducted by contract research organization, Nucro-Technics (Scarborough, ON, Canada), demonstrated the following key results after a single dose of oral BETR-001 (capsule) administered to beagle dogs:

• No significant difference was observed in bioavailability and total exposure of BETR-001 in PK profile of fed versus fasted beagle dogs.
• Oral bioavailability (%F), defined as the fraction of oral administered drug that reaches systemic circulation, was calculated to be 61% and 63% for fasted and fed states, respectively (no significant difference).
• The maximum systemic concentration (C_max) of BETR-001 after a single oral dose was reached at 0.5 hr (T_max), suggesting a quick uptake of the drug into the systemic circulation. The drug was detectable in systemic circulation eight hours post oral dose with an elimination rate constant (K_el) of 0.4 per hour, pointing to the fraction of drug eliminated per unit of time.

The findings demonstrate that oral administration of a single dose of BETR-001 can reach the therapeutic range in the systemic circulation. The PK elimination constant (K_el) of 0.4 per hour for BETR-001 indicates a low probability of toxicity as a result of drug accumulation in the systemic circulation.

“We are very pleased with the results of the first oral PK study for BETR-001 drug manufactured by BetterLife’s patented synthesis and formulation process. Although 2-bromo-LSD has been tested in rodents and human studies in the past, this is the first study to characterize its PK profile in vivo”, said BetterLife’s Chief Executive Officer, Dr. Ahmad Doroudian. “These data, together with the ongoing IND-enabling nonclinical toxicology studies, will support the filing of BETR-001’s IND application with the FDA and initiation of human clinical trials in H2 2022.”

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 (formerly TD-0148A), which is in preclinical and IND-enabling studies, is a non-hallucinogenic and non-controlled LSD derivative in development and it is unique in that it is unregulated and therefore can be self-administered. BetterLife’s synthesis patent for BETR-001 eliminates regulatory hurdles and its pending patent for composition and method of use covers treatment of depression, cluster headaches, post-traumatic stress disorder and other neuro-psychiatric and neurological disorders.

BETR-002 (formerly TD-010), 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 such as COVID-19 and is in the process of seeking strategic alternatives for further development. For further information, visit BetterLife Pharma.