Working to Improve the World’s Best Selling Anesthetic

We're building a diverse pharmaceutical product pipeline that addresses serious chronic and acute neurodegenerative disorders. AQUAVAN
® Injection is an important addition to this franchise, which may offer advantages over traditional anesthetic agents.

The Need:
Propofol is an intravenous drug widely used to anesthetize or sedate patients undergoing surgery or other diagnostic or medical procedures. Sales of propofol in 1999 were in excess of $750 million -- making it the world's best selling anesthetic agent. Despite its commercial success, propofol has been associated with various side effects. These include: cardiovascular side effects (such as reduced heart rate and decreased blood pressure), depressed respiration, elevated blood lipid levels, pain at the site of injection, and a potential for bacterial contamination that could lead to infection. Many of these side effects result from the product's formulation, which is an oil-based emulsion.

The News:
The newest addition to Guilford’s pharmaceutical pipeline, AQUAVAN
® Injection is a novel, water-soluble pro-drug of propofol that is rapidly converted in the body into propofol after intravenous administration. Because of its solubility in water, Guilford believes that AQUAVAN® Injection could have significant advantages over a lipid-based formulation. These may include potentially fewer side effects such as: cardiovascular side effects, elevated blood lipid levels (hyperlipidemia), increased ease of use, improved stability, reduced risk of bacterial contamination and pain upon injection.

® Injection is formulated in a clear aqueous solution that does not require a lipid (oil-based) emulsion for its administration. In preclinical studies, AQUAVAN® Injection produced rapid and effective anesthesia and sedation at doses that were not associated with cardiovascular or other side effects.

The Background:
® Injection is an important addition to Guilford's neurological product pipeline. Under the terms of an agreement with ProQuest Pharmaceuticals Inc., Guilford acquired exclusive worldwide rights to develop and commercialize AQUAVAN® Injection, as well as rights to other potential pro-drugs of propofol for other indications. Under the agreement, Guilford acquired an equity position in ProQuest. In exchange, ProQuest received $1 million in cash and will be eligible for milestone payments - if the product progresses through clinical development, and royalty payments on any future product sales.

The Development Strategy:
® Injection is a pro-drug of a successful commercial product, Guilford believes that the development timeline for AQUAVAN® Injection may be shorter than with a new chemical entity.

The Status:
In 2002, Guilford began a U.S. Phase II clinical trial of AQUAVAN® Injection in approximately 200 patients undergoing colonoscopy procedures. A second phase II clinical trial was begun in Europe in patients undergoing coronary artery bypass surgery. The goal of these studies is to assess the safety and efficacy AQUAVAN® Injection in the conscious sedation and cardiac surgery setting. Results from these studies should be available in late 2003.

Copyright© 2001 Guilford Pharmaceuticals Inc.
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