MIRA Pharmaceuticals Unveils Ketamir-2's Principal Metabolite: Nor-Ketamir - a Longer-Acting, Brain Penetrating and Selective Compound Acting on the NMDA PCP Receptor

This breakthrough in bioavailability and formulation showcases the potential for advanced, at home neurological treatments.

MIAMI, FL / ACCESSWIRE / August 12, 2024 / MIRA Pharmaceuticals, Inc. (NASDAQ:MIRA), or MIRA Pharmaceuticals, a leading pre-clinical-stage pharmaceutical company unveiled new preclinical data providing further insights into the mechanism of action of its innovative drug candidate, Ketamir-2's principal metabolite, Nor-Ketamir-2. This data indicates that similar to Ketamir-2, its principal metabolite, Nor-Ketamir-2 selectively interacts with a low affinity at the NMDA PCP site with high selectivity and lack of activity on the glutamate NMDA site, opiate and other sites. Additionally, a new salt, Ketamir-2 Pamoate and associated formulation, were developed to potentially enhance pharmacokinetics and improve brain penetration, achieving higher plasma and brain levels with longer half-life, with nearly 100 percent oral bioavailability of Nor-Ketamir-2.

Traditional ketamine, while effective, suffers from very low oral bioavailability (less than 30%) and poses significant safety concerns due to its interaction with multiple NMDA and other receptor sites. This often necessitates intravenous or intranasal administration, which limits its practicality for at-home use. In contrast, Ketamir-2 and its principal metabolite, Nor-Ketamir-2, demonstrate superior selectivity and bioavailability in preclinical studies. Upon oral absorption, the body efficiently metabolizes Ketamir-2 into Nor-Ketamir-2, leading to sustained plasma residence and brain penetration and extended therapeutic efficacy, making it a promising candidate for at-home treatment.

The development of the Ketamir-2 Pamoate with a new formulation is particularly significant. This new formulation enhances pharmacokinetics, ensuring that the body effectively absorbs and utilizes both Ketamir-2 and Nor-Ketamir-2. With Nor-Ketamir-2 achieving near 100 percent oral bioavailability, the drug can maintain higher levels in the bloodstream for extended periods, allowing for sustained therapeutic action and potentially reducing the frequency of dosing.

Summary of Key Findings:

Enhanced Bioavailability: The new Pamoate salt and formulation brings Nor-Ketamir-2's bioavailability close to 100%, a significant improvement over traditional ketamine's less than 30% oral bioavailability.

Sustained Brain Penetration: The extended half-life and elevated levels of Nor-Ketamir-2 observed in preclinical studies suggest prolonged therapeutic effects, which are essential for effective at-home treatment.