Safety, tolerability, and pharmacokinetics of oral Ketamir-2, a novel selective NMDA receptor antagonist: results of a first-in-human Phase 1 study

This preprint reports a first-in-human, randomised, double-blind, placebo-controlled Phase I trial of oral Ketamir-2 in 57 healthy adults. Single doses of 50–600 mg and daily doses of 150–600 mg for five days produced dose-related exposure without serious adverse events or a meaningful psychotomimetic signal. The study assessed short-term safety and pharmacokinetics; it did not establish pain relief or superiority to ketamine.