Terran Biosciences' Four Patent Applications Cover Improved Versions Of Classic Empathogens

Terran Biosciences, the NY-based biotech platform that develops transformational therapeutics announced the publication of four international PCT patent applications covering novel compounds and potentially improved versions of the empathogens methylone (also called bk-MDMA or MDMC), ethylone, MDEA (aka MDE), MDAI, and MBDB. 

The company works towards developing distinct therapeutic options tailored to specific patient needs, so that for instance patients with the most severe forms of PTSD may benefit from the most powerful empathogens such as MDMA and MDEA, while patients with milder forms of PTSD, anxiety or depression may benefit from medicines such as MDAI or MBDB. Empathogens are compounds that increase feelings of empathy.

While MDMA has been the most studied one, related compound methylone invented by renowned chemists Alexander Shulgin and Peyton Jacob III has been described as efficacious in treating PTSD through inducing a milder sensorial experience than the former.

Results on which the patent applications are based:

• Racemic methylone did not follow a classic dose-dependent pattern but rather produced an increase in anxiety at lower doses, yet when dose was increased the effects were reversed and the drug acted as an effective anxiolytic, confirming that a sufficient dose level must be reached for a therapeutic effect while low doses may produce unwanted side effects (animal models.)

• Methylone’s components, R-methylone and S-methylone, were mimicked by the company in a manner that both compounds are enantiomerically pure and that way their respective salts and polymorphs can be characterized to explore potential advantages. So far, comparisons between racemic methylone, R-methylone and S-methylone showed that while S-methylone was more potent than R-methylone at producing therapeutic effects, it also produced the anxiety increase at lower doses. Pure R-methylone did not induce any anxiety but rather reduced it in a consistent dose-dependent manner (animal models.)

• MDEA, MDAI and MBDB have been designed in novel deuterated forms with optimized pharmacokinetics (preclinical models.) MDEA has been previously described as being a potential alternative to MDMA with similar potency and ability to create strong empathogenic effects with fewer reported side effects, while MDAI and MBDB are described as very mild empathogens potentially more suitable for at-home use in the outpatient setting. 

• MDEA and MBDB exist as a racemic mixture of the R and S forms, such as methylone, and also have been shown to not follow a typical dose-dependent response and produce increased anxiety at low doses. This time, enantiomerically pure forms showed advantages differently: in the case of MDEA, the S-MDEA form relieved anxiety in a classic dose-dependent manner while the R-MDEA form increased anxiety at low doses and reduced it at high ones; and for MBDB, pure S-MBDB reduced anxiety with a potentially greater therapeutic index than racemic MBDB or R-MBDB (animal studies).

• Terran’s discoveries include novel deuterated forms, enantiomerically pure forms, as well as novel salts, polymorphs and co-crystals of racemic methylone, R-methylone and S-methylone, a body of work that spans several years and their publication, following that of DMT and ibogaine-based novel compounds last week, “unveils one of the most comprehensive novel empathogen development programs in the industry to date” as stated by the company.

Photo: Benzinga edit with photo by cottonbro and Chokniti Khongchum on Pexels.