Tirilazad mesylate, a novel 21 -aminosteroid derivative, has been marketed in
Austria for the intravenous treatment of subarachnoid hemorrhage (SAH) in male
patients. Studies have indicated involvement of lipid peroxidation and/or lipid
hydrolysis in the genesis of SAH-initiated microvascular damage and prolonged
vasospasm of the large cerebral vessels. Tirilazad mesylate is a highly lipophilic
compound that localizes to the cell membrane. It is a potent inhibitor of lipid
peroxidation induced by oxygen free radicals, purely through a mechanism similar to
vitamin E by scavenging lipid peroxyl radicals, and is a stabilizer of biological
membranes. Tirilazad mesylate has been demonstrated to have a positive effect in
reducing symptomatic vasospasm, cerebral infarction, and neurological dysfunction.
Clinically, it is reportedly effective in reducing mortality in male SAH patients relative to
the control group. The title compound is also reportedly in clinical trials for ischemic
stroke, spinal cord injury, and for non-systemic ocular applications. Little or no
behavioral and physiological side effects have been reported.
