Drug intelligence / Profile preview

STIR-101

Development stage
Unknown
Lead developer
Stir Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

STIR-101 is a proprietary oral formulation of low-dose naltrexone (LDN) being developed by STIR Pharma for the treatment of persistent post-viral symptoms, including Chronic Fatigue Syndrome (ME/CFS) and Long COVID (PASC). While naltrexone is traditionally used at higher doses as an opioid antagonist for addiction, at low doses (typically 1-5 mg), it is hypothesized to exert immunomodulatory and anti-inflammatory effects. Its mechanism of action involves the antagonism of Toll-like receptor 4 (TLR4) on microglia, which reduces the production of pro-inflammatory cytokines and neuroinflammation, as well as transiently blocking opioid receptors to induce an up-regulation of endogenous endorphins and opioid receptors. STIR-101 is currently being evaluated in a Phase 2 randomized controlled trial in New Zealand to assess its safety and efficacy in improving fatigue and functional capacity in patients with post-viral syndromes.

Other names
low-dose naltrexoneLDN
02

Targets

TLR4 (Toll-like receptor 4)

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