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Tirilazad

Development stage
Phase 3
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Tirilazad is a synthetic, lipid-soluble, nonglucocorticoid 21-aminosteroid (also called a lazaroid) developed as a neuroprotective agent. Its primary mechanism of action is the inhibition of iron-dependent lipid peroxidation within cell membranes, achieved through free-radical scavenging and membrane-stabilizing properties. Tirilazad was investigated for acute neurological injuries such as subarachnoid hemorrhage, traumatic brain injury, spinal cord injury, and acute ischemic stroke. In animal models, it demonstrated neuroprotective effects by reducing oxidative damage and protecting brain tissue[5][6]. However, in clinical trials for acute ischemic stroke in humans, it failed to show benefit and was associated with increased mortality and disability[3][4][5]. The drug reached up to phase III clinical trials but has not been approved for any indication.

Brand names
Freedox
Other names
tirilazadumtirilazad [INN:BAN]tirilazadum [INN-Latin]
02

Targets

OxPL (Oxidized phospholipid)

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