Pharmacopeia Announces Additional Positive Findings from Phase 1 Multiple Ascending Dose Study of PS433540 (DARA)
Monday December 3, 7:30 am ET
Results Show Statistically Significant Indications of PS433540's Potential in Treating Hypertension
PRINCETON, N.J., Dec. 3 /PRNewswire-FirstCall/ -- Pharmacopeia (Nasdaq: PCOP - News), an innovator in the discovery and development of novel small molecule therapeutics, announced today additional results from the Company's Phase 1 multiple ascending dose (MAD) study of its lead internal product candidate, PS433540 (DARA). Data demonstrated that PS433540 produced statistically significant, dose dependent increases in plasma-renin activity levels, as well as reductions in systolic and diastolic blood pressure. These findings are in addition to previously reported initial results from the MAD trial that showed all doses of PS433540 to be safe and well-tolerated. This MAD study was designed to evaluate the 14-day safety and tolerability of 50, 100, 250, 500 and 1,000 mg doses of PS433540 in healthy volunteers.
The trial's positive plasma-renin activity and blood pressure findings provide preliminary insight into the potential of PS433540 to treat hypertension. Study investigators witnessed a dose dependent increase in plasma-renin activity levels for PS433540, which was more pronounced at Day 15 than at Day 1. This observed increase in plasma-renin activity is indicative of PS433540's ability to block the angiotensin receptor, a key target in efforts to lower and control blood pressure in hypertensive patients. Furthermore, associated with the increase in plasma-renin activity levels was a decrease in both diastolic and systolic blood pressure for PS433540 of up to 15 mmHg.
"While safety and tolerability of PS433540 across a broad range of doses up to 1,000 mg are the most important results of the MAD study, we are especially pleased to see, that even in healthy normotensive volunteers, signs of the compound's potential therapeutic activity are clearly discernable. Although preliminary, these results support the potential utility of this novel compound as a new therapeutic option for patients affected by hypertension and related disorders such as diabetic nephropathy," stated Rene Belder, M.D., Pharmacopeia's Vice President of Clinical and Regulatory Affairs. "We look forward to the completion of our ongoing Phase 2a study in the first half of 2008 and hope to see the first clear demonstration of the compound's potential efficacy in hypertensive patients."
PS433540 is a dual-acting angiotensin (AII) and endothelin (ET1) receptor antagonist that is being developed as a potential treatment for hypertension and diabetic nephropathy. PS433540, the first and only DARA compound in development, possesses two clinically validated mechanisms of action in a single compound. There is considerable preclinical and initial clinical 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.
surf's up......crikey
