NTS-104 TRIS

NTS-104 TRIS is a novel, water-soluble prodrug that rapidly converts in plasma to the neuroactive steroid NTS-105. Upon administration, NTS-105 crosses the blood-brain barrier and exerts neuroprotective effects by modulating nuclear hormone receptors. Specifically, it acts as a full antagonist at the androgen receptor and mineralocorticoid receptor and as a partial agonist at cellular progesterone receptor B. These actions result in potent anti-inflammatory, anti-apoptotic (cell death inhibition), and anti-edema activity both in the brain and systemically. Preclinical studies have demonstrated that administration of NTS-104 after ischemic stroke or traumatic brain injury improves functional outcomes and reduces lesion volume. The drug also induces time- and dose-dependent changes in biomarkers such as reductions in IL-6, VEGF, ICAM-1, IL‑1β, MCP‑1, RAGE, GM-CSF (inflammatory mediators), with an elevation of galectin‑1[1][4][5][6][8]. Developed for acute neurological injuries like stroke and traumatic brain injury (TBI), it is currently being evaluated for safety and pharmacokinetics in Phase 1 clinical trials[3].