Pharmacopeia initiates early stage trial

PS433540 is the only dual-acting angiotensin and endothelin receptor antagonist (DARA) compound in development and it possesses two clinically validated mechanisms of action in a single compound.

The compound works by selectively blocking the action of two potent vasoconstrictor and mitogenic agents, angiotensin II (AII) and endothelin 1 (ET1), at their respective receptors.

There is considerable preclinical data suggesting that compared to either agent alone, simultaneously blocking the actions of both AII and ET1 may provide significantly improved treatment options for several cardiovascular diseases.

In addition, studies to date have demonstrated PS433540 to be safe and well tolerated in preclinical studies with a pharmacokinetic profile consistent with an expected once-daily oral dosing in humans.

The objective of this phase I study is to evaluate the compound's preliminary safety and tolerability. In addition clinical investigators will also evaluate dose-related pharmacokinetics.