ABSTRACT
Tirilazad mesylate is effective in many animal models of acute neurologic disorders. Tirilazad mesylate was selected as an optimal example of this class for clinical development. Tirilazad mesylate is a very lipophilic compound with a calculated log octanol/water partition coefficient of 8. It distributes preferentially to the lipid bilayer of cells, where it exerts organizational effects on the lipid bilayer while positioning its antioxidant heterocycle directly into the bilayer. Tirilazad mesylate has been evaluated in many models of injury to the central nervous system: head and spinal cord injury, ischemia, and hemorrhagic stroke. Weir and co-workers demonstrated the effects of tirilazad mesylate in a primate model of chronic subarachnoid hemorrhage-induced vasospasm in a double-blind, placebo-controlled trial. Tirilazad mesylate is being tested clinically in head and spinal cord injury patients and in ischemic and hemorrhagic stroke patients at multiple centers in the US, Canada, Europe, Australia, and Japan.
