The objective of this study was to evaluate the compound's preliminary safety and tolerability by treating six separate groups of healthy volunteers. In addition to safety and tolerability, dose-related pharmacokinetics were also evaluated.
Data from the single ascending dose study indicated that the product known as PS433540 was well tolerated at all six doses administered. In addition, study findings suggested that the compound possesses linear pharmacokinetics and a half-life that is consistent with once daily administration.
PS433540 works by selectively blocking the action of two potent vasoconstrictor and mitogenic agents, angiotensin II (AII) and endothelin 1 (ET1), at their respective receptors. Preclinical data suggests that, compared to either mechanism alone, simultaneously blocking the actions of both AII and ET1 may provide improved treatment options for several cardiovascular diseases.
Phamacopeia's phase I program for PS433540 is comprised of multiple studies. In addition to this trial, other planned studies include a multiple ascending dose study to further evaluate safety, as well as an angiotensin challenge study and an endothelin challenge study. Pharmacopeia expects the entire phase I program to be complete in late 2007, with a phase II trial beginning in the first half of 2008.