Portola Pharmaceuticals commences Phase 1 trial of PRT062607 for chronic inflammatory diseases

Portola Pharmaceuticals, Inc. today announced that it has initiated its first in human Phase 1 trial in healthy volunteers of PRT062607, a novel, oral Syk-specific kinase inhibitor in development to treat chronic inflammatory diseases, including rheumatoid arthritis (RA), and certain cancers, including non-Hodgkin's lymphoma and chronic lymphocytic leukemia. In preclinical in vivo models of RA, PRT062607 was shown to reduce inflammation in a dose-dependent manner.

PRT062607 is Portola's lead compound discovered from an extensive kinase chemistry effort that has led to the development of potent, oral inhibitors of Spleen Tyrosine Kinase (Syk) and Janus Kinase (JAK).  Syk and JAK play key roles in signaling pathways that modulate inflammation and certain cancers.  PRT062607 has been shown to be a highly specific inhibitor of Syk in a broad panel of in vitro kinase and cellular assays.

"Because of its key role as a mediator in a number of important signaling pathways, specific, low-level Syk inhibition may be ideal for the management of chronic inflammatory diseases, such as RA, and may be better tolerated than less selective kinase inhibitors," said Daniel D. Gretler, M.D., chief medical officer of Portola.  "The initiation of the Phase 1 trial of PRT062607 is an important milestone toward our goal of developing safe and efficacious oral drugs for rheumatoid arthritis and other chronic inflammatory diseases."

The ascending, single-dose Phase 1 study is assessing the safety, pharmacokinetics and pharmcodynamics of oral PRT062607 in up to 48 healthy individuals. The trial is being conducted at a single U.K. site.  It is expected to be completed in the second half of 2010.

SOURCE Portola Pharmaceuticals, Inc.