Arena says it will advance cardiovascular agonist APD791 to preclinical studies

By E. Janene Geiss

Philadelphia, Dec. 29 - Arena Pharmaceuticals, Inc. said Thursday that it is advancing APD791 into preclinical development from its cardiovascular research program and expects to begin clinical development in about a year.

APD791 is a selective inverse agonist of the 5-HT2A serotonin receptor. By selectively inhibiting the activation of 5-HT2A serotonin receptors found on platelets and vascular smooth muscle, Arena said it believes that APD791 may reduce the risk of arterial thrombosis and conditions such as acute coronary syndrome, heart attack and stroke, according to a company news release.

"APD791 represents a potential new approach to reducing the risk of arterial thromboembolic disease, a public health problem with significant mortality and morbidity," Jack Lief, Arena's president and chief executive officer, said in the release.

"The advancement of this program further demonstrates Arena's ability to sustain the growth and diversification of its pipeline," Lief said in the release.

Stimulation of the 5-HT2A serotonin receptor on platelets and vascular smooth muscle is thought by Arena to play an important role in the cascade of events leading to arterial thromboembolic diseases.

Normally, when a platelet is activated by one of a number of clotting and aggregating factors, such as thrombin or collagen, the platelet releases serotonin, which enhances platelet aggregation and promotes vasoconstriction and intimal hyperplasia, or thickening of the vessel wall, officials said.

APD791, discovered by Arena, is a novel and orally bioavailable selective inverse agonist of the 5-HT2A serotonin receptor.

By a blockade of the 5-HT2A receptor on platelets and other cardiovascular tissues, APD791 may inhibit platelet aggregation, vasoconstriction and intimal hyperplasia, thereby reducing the risk of arterial thrombosis, officials said.

Preclinical studies indicate that APD791 potentially has an improved therapeutic index over currently marketed anti-platelet drugs, officials said.

Arena said it believes the potential improvement is due to a separation of antithrombotic activity from the increased bleeding that may be seen as a treatment effect of these currently marketed drugs.

Arena is a San Diego clinical-stage biopharmaceutical company focusing on development and commercialization of small molecule drugs in four major therapeutic areas including metabolic, cardiovascular, inflammatory and central nervous system diseases.

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