Drug intelligence / Profile preview

NTS-105

Development stage
Unknown
Lead developer
NeuroTrauma Sciences
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

NTS-105 is a neuroactive steroid small molecule being developed by NeuroTrauma Sciences for the treatment of acute ischemic stroke (AIS), chronic stroke, and traumatic brain injury (TBI). It is the active metabolite of the prodrug NTS-104, which is administered intravenously and rapidly converts to NTS-105 in the plasma. NTS-105 is designed to cross the blood-brain barrier and reach pharmacologic concentrations in the brain, where it modulates multiple nuclear receptors. Specifically, it acts as a full antagonist at the androgen receptor, a partial agonist at progesterone receptor B, and a full antagonist at the mineralocorticoid receptor. This multi-targeted mechanism provides neuroprotection through anti-inflammatory, anti-apoptotic, and anti-edema activities, as demonstrated in preclinical models of brain injury and stroke.

Other names
active metabolite of NTS-104
02

Targets

MR (Mineralocorticoid receptor)AR (Adrenergic receptors)RB1 (Retinoblastoma-associated Protein)

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