Plexxikon has pursued a number of drug targets for the treatment of cardiovascular and renal disease, including polycystic kidney disease, hypertension and atherosclerosis.

Polycystic Kidney Disease

Plexxikon is developing novel, oral kinase inhibitors for the treatment of polycystic kidney disease (PKD), a debilitating, genetic disease that leads to loss of kidney function. There is currently no treatment for PKD. This disease affects 600,000 patients in the U.S. and 12.5 million patients worldwide.

Plexxikon's compounds are highly selective, potent inhibitors of Raf kinase, a critical mediator of PKD pathology. Compelling efficacy has been demonstrated in multiple preclinical models of PKD, including effects on cyst size and renal function.

Hypertension

Plexxikon has utilized its Scaffold-Based Drug Discovery Platform™ to identify non-peptidic inhibitors of renin, a validated drug target for hypertension. A number of scaffold candidates have been identified as well as very low-molecular weight leads.

Developing non-peptidic renin compounds with good oral availability has been a longstanding challenge for the industry. An advantage of Plexxikon's approach is the generally smaller size of Plexxikon's drug candidates, which often translates into more attractive pharmaceutical properties.