Composition comprising a benzoate salt of 5-methoxy-N,N-dimethyltryptamine

Inventors

FEILDING-MELLEN, Cosmo • Mason, Timothy

Assignees

Beckley Psytech Ltd

Abstract

A composition comprising a pharmaceutically effective amount of a pharmaceutically acceptable benzoate salt of 5-methoxy-N,N-dimethyltryptamine (5MeODMT).

Core Innovation

The disclosed subject matter provides pharmaceutically acceptable benzoate salts of 5-methoxy-N,N-dimethyltryptamine (5MeODMT), specifically 5MeODMT benzoate, as medicaments. The active solid-state form is used in combination with pharmaceutically acceptable carriers or excipients, including formulations intended for nasal delivery, and is presented as an alternative to 5MeODMT hydrochloride (HCl salt).

A stated problem addressed by the disclosure is mucosal irritation and reduced mucosal delivery associated with existing 5MeODMT salt forms. The disclosure reports reduced mucosal irritation in slug mucosal irritation assays and higher cumulative permeation across ovine nasal epithelium for the benzoate relative to the hydrochloride salt, supporting development of the benzoate medicament for intranasal administration.

The disclosure emphasizes solid-state and stability characterization for 5MeODMT benzoate. It describes a crystalline form characterized by XRPD crystalline Pattern A with peaks at 17.5°, 17.7°, and 21.0° 2θ±0.1° as measured with an x-ray wavelength of 1.5406 Å, and reports DSC/TGA/DVS characterization showing benzoate stability relative to the HCl salt, including lower moisture uptake and higher shelf-life potential.

The disclosed medicament and formulation concepts include nasal delivery using powder dosage forms, including nasal inhalation/powder and intranasal liquid delivery, and a nasal delivery device comprising powder. The disclosure includes preclinical safety and pharmacokinetic/toxicokinetic data for intranasal dosing, including respiratory/cardiovascular observations, hERG potassium channel inhibition in vitro, and toxicology studies in rats and dogs, together with genotoxicity/compatibility characterization supporting development.

Claims Coverage

The independent claims comprise three distinct inventive areas: (1) a pharmaceutical composition containing 5-MeO-DMT benzoate with pharmaceutically acceptable carriers or excipients, (2) a nasal delivery device including a powder containing 5-MeO-DMT benzoate and carriers/excipients, and (3) a method of treating depression via intranasal administration of 5-MeO-DMT benzoate. Across these independent claim sets, the coverage includes formulation concepts, device implementation, and a treatment method, with dependent claims adding excipient categories, particle-size constraints, and an XRPD-defined crystalline form.

Overall claim coverage extends from composition to nasal device and to intranasal treatment of depression, anchored by 5-MeO-DMT benzoate. Dependent claim refinements further define excipient categories, intranasal formulation, powder particle size/distribution metrics, unit-dose dry powder inhaler configuration, and a crystalline 5-MeO-DMT benzoate form defined by specific XRPD peak positions at an x-ray wavelength of 1.5406 Å.

Stated Advantages

Documented Applications