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KAI Pharmaceuticals Inc. intends to use proceeds from a $17 million Series A financing to develop therapeutics that selectively modulate protein kinase C.

Located in South San Francisco, KAI is a privately held company formed in August following a $500,000 investment made by Skyline Ventures. The company's science is based on the work of Daria Mochly-Rosen, chair of the department of molecular pharmacology at Stanford University, who discovered a method of making the approach to modulating protein kinase C (PKC) more specific.

"She discovered that PKC is not one enzyme, but at least 10 different isozymes in the body," Paul Auerbach, KAI's chief operating officer, told BioWorld Today. "Furthermore, she figured out how each of these moves within cells during certain activities, such that she was able to come up with specific peptides that are composed of short chains of amino acids to either block individually each of these specific isozymes or activate them."

Already, the company's six staff members are working on two compounds. The lead candidate, a delta protein kinase C antagonist, is designed to prevent reperfusion injury associated with acute heart attack. That peptide appears to migrate during reperfusion and block the binding of the delta PKC at the mitochondria.

"The effect of that in animals, so far, has been to create a dramatic and astounding decrease in the size of the heart attack - if we squirt this down the coronary artery of an animal at the moment of reperfusion," Auerbach said.

In animal studies, Auerbach said the compound appears to diminish heart attack size by 70 percent to 80 percent. "It also appears to have the same effect in the central nervous system, so the implication for that would be that it might be efficacious in stroke as well," he said.

KAI expects the delta PKC to enter human trials in 2004. The $17 million raised in the Series A round is expected to hold the company over until late 2005.

Beyond that, KAI is working on a second drug designed as a prophylactic agent in patients at risk for ischemic injury. Preclinical studies with that compound also suggest activity in both cardiac and neurological ischemia.

The Series A was led by Skyline Ventures, of Palo Alto, Calif., and included Delphi Ventures and InterWest Partners, both of Menlo Park, Calif.; and InterSouth Partners, of Research Triangle Park, N.C.

KAI expects to increase its staff by 10 to 15 people over the next year.

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