TSI Initiates Phase 1 Study of New-Generation Thrombolytic, TS01

- Novel Mechanism of TS01 Promotes Enhanced Safety and Efficacy

CAMBRIDGE, Massachusetts, Oct. 2, 2012 /PRNewswire/ -- Thrombolytic Science International (TSI) today announced the initiation of a Phase 1 study of TS01, a new-generation clot-dissolving therapy intended for the treatment of acute ischemic stroke. This first-in-man randomized, double-blind, placebo-controlled study will assess the overall safety and tolerability of TS01 in healthy adults. TS01 selectively targets occlusive clots that cause strokes and spares hemostatic clots (good clots), resulting in a superior safety profile and greatly reduced risk of intra-cranial hemorrhage. TS01 is based on a mutant form of pro-urokinase, a natural thrombolytic.

"Current treatment options for patients who suffer acute ischemic strokes are extremely limited. Moving our novel clot-busting therapy into the clinic is a significant milestone for these patients and for TSI," said Alexis Wallace, chief executive officer of TSI. "Because TS01 is an entirely new approach to thrombolysis, we expect its improved safety and clot-dissolving efficacy to fundamentally alter the treatment paradigm for patients with acute stroke."

The study will be conducted at the Centre for Human Drug Research in The Netherlands. The trial will enroll between 50 and 70 healthy males. Subjects will receive ascending doses of mutant prourokinase or placebo, preceded, or not, by a bolus of a specific inhibitor called C1-esterase inhibitor or a C1-esterase inhibitor-placebo. Systemic plasminogen activation, changes in coagulation and ex-vivo lytic activity will be assessed.

For more information on this trial see clinicaltrials.gov.

About Stroke

Each year, strokes affect 15 million people worldwide. In the United States, it is the leading cause of long-term disability and the fourth-leading cause of death, costing the healthcare system in excess of $73 billion each year. Approximately 90 percent of all strokes are caused by blood clots (acute ischemic stroke), for which there is still no satisfactory clot-dissolving treatment. Because of the short treatment time-window, suboptimal efficacy of current therapy and the risk of intra-cranial hemorrhage, only about 5% of stroke patients are treated with a clot-dissolving drug.

About TS01

TS01 is a proprietary new-generation, clot-dissolving therapy intended to treat patients with acute ischemic stroke. TS01 is composed of a patented, rationally-designed mutant of native pro-urokinase and a pre-administered specific inhibitor which together, uniquely enhance thrombolytic specificity thereby improving safety and efficacy. TS01 selectively targets occlusive clots that cause ischemic strokes and spares hemostatic clots (good clots), resulting in a superior safety profile and greatly reduced risk of intra-cranial hemorrhage compared to current therapies. It is expected that because the dose of TS01 is not limited by the risk of bleeding complications, TS01 will be delivered at a maximally effective dose.

About TSI

TSI is a privately-held vascular medicine and biotechnology company currently developing a new-generation clot-dissolving therapy with the first novel mechanism of action in 20 years for stroke and other thrombotic diseases. TSI's technology is based upon pioneering earlier work on pro-urokinase (proUK) by its cofounders. The primary component of TSI's thrombolytic therapy is a rationally designed mutant of proUK.

For more information, please visit tsillc.net.