Plexxikon Preclinical Data Shows Dramatic Improvement in Key Symptoms of PKD -- Polycystic Kidney Disease Message Board

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Subject: Plexxikon Preclinical Data Shows Dramatic Improvement in Key Symptoms of PKD

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Date Posted: 18:58:32 05/21/08 Wed

http://biz.yahoo.com/bw/080521/20080521006149.html?.v=1

BERKELEY, Calif.--(BUSINESS WIRE)--Plexxikon Inc. today announced data from preclinical studies of Polycystic Kidney Disease (PKD) demonstrating significantly reduced kidney disease following treatment with Plexxikon’s novel drug candidate. Plexxikon’s novel small molecule kinase inhibitor is a highly selective and potent inhibitor of Raf kinase, a critical mediator of PKD pathology. These data were recently presented at the ISN Forefronts Symposium on Polycystic Kidney Disease in Montreal, Canada by Stefan Somlo, M.D., CNH Long Professor of Internal Medicine and Genetics and Chief of Nephrology at the Yale University School of Medicine.

“The degree to which this compound slowed progression of the kidney disease in preclinical models with early onset aggressive polycystic kidney disease was very dramatic, demonstrating the promise of this agent as a candidate therapy for patients with this disease,” stated Dr. Somlo. “There are currently no treatments for PKD, which is an inherited disease of the kidneys and other organs that often becomes manifest between the ages of 30 and 40 and eventually leads to kidney failure in a significant proportion of affected individuals.”

“Plexxikon’s PKD drug candidate is another example of the highly selective kinase inhibitors we are developing at Plexxikon, a prerequisite for a compound to be useful in treating a chronic disease such as PKD, and we are pleased to see such strong preclinical data in polycystic kidney disease and safety in GLP toxicology studies,” stated K. Peter Hirth, Ph.D., chief executive officer of Plexxikon. “We look forward to initiating a Phase 1 clinical trial for this novel drug candidate in 2008.”

In the preclinical study of Plexxikon’s PKD drug candidate, doses of the drug candidate were administered orally daily for 14 days. A marked reduction in kidney cyst burden was observed in the treatment group compared to vehicle treated mice. Levels of blood urea nitrogen (BUN), an indicator of kidney function, were also significantly improved in the drug-treated groups compared with the vehicle-treated group, suggesting that improved renal function accompanied reduced cyst growth in treated animals.

Using its proprietary Scaffold-Based Drug Discovery™ platform, Plexxikon has identified a portfolio of unique compounds that selectively block Raf-dependent cells, leaving healthy cells unharmed since Raf activity is differentially regulated in those cells. The co-crystallography platform enabled scientists at Plexxikon to determine the exact location where such inhibitors selectively bind to the kinase active site.

Plexxikon’s family of Raf kinase inhibitors selectively target a unique binding site of the protein, minimizing the common side effects seen from other less selective kinase inhibitors. In several different systems, Plexxikon’s Raf inhibitor blocks proliferation of dysfunctional cells, without detectable affects on healthy cells. Interestingly, our drug candidate is highly selective for the PKD indication, with no detectable inhibition of cancer cell line growth – including no activity in cancers bearing the important B-RafV600E oncogene.

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><a rel=nofollow target=_blank >href="http://biz.yahoo.com/bw/080521/20080521006149.htm >l?.v=1">http://biz.yahoo.com/bw/080521/20080521006149.h >tml?.v=1</a> > >BERKELEY, Calif.--(BUSINESS WIRE)--Plexxikon Inc. >today announced data from preclinical studies of >Polycystic Kidney Disease (PKD) demonstrating >significantly reduced kidney disease following >treatment with Plexxikon’s novel drug candidate. >Plexxikon’s novel small molecule kinase inhibitor is a >highly selective and potent inhibitor of Raf kinase, a >critical mediator of PKD pathology. These data were >recently presented at the ISN Forefronts Symposium on >Polycystic Kidney Disease in Montreal, Canada by >Stefan Somlo, M.D., CNH Long Professor of Internal >Medicine and Genetics and Chief of Nephrology at the >Yale University School of Medicine. > >“The degree to which this compound slowed progression >of the kidney disease in preclinical models with early >onset aggressive polycystic kidney disease was very >dramatic, demonstrating the promise of this agent as a >candidate therapy for patients with this disease,” >stated Dr. Somlo. “There are currently no treatments >for PKD, which is an inherited disease of the kidneys >and other organs that often becomes manifest between >the ages of 30 and 40 and eventually leads to kidney >failure in a significant proportion of affected >individuals.” > >“Plexxikon’s PKD drug candidate is another example of >the highly selective kinase inhibitors we are >developing at Plexxikon, a prerequisite for a compound >to be useful in treating a chronic disease such as >PKD, and we are pleased to see such strong preclinical >data in polycystic kidney disease and safety in GLP >toxicology studies,” stated K. Peter Hirth, Ph.D., >chief executive officer of Plexxikon. “We look forward >to initiating a Phase 1 clinical trial for this novel >drug candidate in 2008.” > >In the preclinical study of Plexxikon’s PKD drug >candidate, doses of the drug candidate were >administered orally daily for 14 days. A marked >reduction in kidney cyst burden was observed in the >treatment group compared to vehicle treated mice. >Levels of blood urea nitrogen (BUN), an indicator of >kidney function, were also significantly improved in >the drug-treated groups compared with the >vehicle-treated group, suggesting that improved renal >function accompanied reduced cyst growth in treated >animals. > >Using its proprietary Scaffold-Based Drug Discovery™ >platform, Plexxikon has identified a portfolio of >unique compounds that selectively block Raf-dependent >cells, leaving healthy cells unharmed since Raf >activity is differentially regulated in those cells. >The co-crystallography platform enabled scientists at >Plexxikon to determine the exact location where such >inhibitors selectively bind to the kinase active site. > >Plexxikon’s family of Raf kinase inhibitors >selectively target a unique binding site of the >protein, minimizing the common side effects seen from >other less selective kinase inhibitors. In several >different systems, Plexxikon’s Raf inhibitor blocks >proliferation of dysfunctional cells, without >detectable affects on healthy cells. Interestingly, >our drug candidate is highly selective for the PKD >indication, with no detectable inhibition of cancer >cell line growth – including no activity in cancers >bearing the important B-RafV600E oncogene.
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