TNX-4900

TNX-4900 is a highly selective small-molecule Sigma-1 receptor antagonist developed as a non-opioid approach to treating chronic neuropathic pain. The compound binds the human Sigma-1 receptor with nanomolar affinity (Ki = 7.5 nM) and demonstrates greater than 100-fold selectivity over the Sigma-2 receptor. It exhibits high blood-brain barrier penetration and favorable pharmacokinetic properties including oral bioavailability of approximately 28%. In preclinical models of diabetic and chemotherapy-induced neuropathic pain, TNX-4900 produced significant and durable reductions in pain behaviors following both acute and chronic dosing without evidence of tolerance development or motor impairment. The compound was developed through a structure-based drug design program at Rutgers University using computer-aided and AI-driven approaches.