Drug intelligence / Profile preview

Ketamir-2

Development stage
Phase 1
Lead developer
MIRA Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Topical
01

Overview

Ketamir-2 is a novel oral analog of ketamine developed by MIRA Pharmaceuticals for the treatment of neuropathic pain and neuropsychiatric disorders, including major depressive disorder (MDD), treatment-resistant depression (TRD), and major depressive disorder with suicidal ideation (MDD-SI). Unlike traditional ketamine, Ketamir-2 is designed to selectively inhibit the NMDA receptor at the PCP-binding site with 30–50 times lower affinity than ketamine, which reduces dissociative and psychotomimetic side effects. It does not interact with opioid receptors or other neurotransmitter systems affected by traditional ketamine. Preclinical studies have shown that Ketamir-2 provides superior efficacy in neuropathic pain models compared to gabapentin and pregabalin, normalizing pain thresholds without inducing hyperlocomotor activity or sedation. The drug demonstrates high oral bioavailability (~80%), prolonged therapeutic effect due to its active metabolite Nor-Ketamir-2, and is not a substrate for P-glycoprotein, allowing better brain penetration. It is being developed as both an oral and topical formulation for targeted delivery. The DEA has determined that Ketamir-2 is not a controlled substance.

Other names
ketamir
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)

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