Pharmacyclics' Factor VIIa Program

Pharmacyclics has developed a small molecule inhibitor of Factor VIIa. PCI-27483 will initially be studied for the treatment of thrombotic complications of cancer and as an anti-cancer agent. Pharmacyclics initiated a Phase 1 trial with PCI-27483 and plans to complete enrollment and evaluation of a Phase 1 trial in the fourth quarter of calendar 2008.

In preclinical studies, PCI-27483 has demonstrated the ability to selectively inhibit Factor VIIa when it is complexed with a protein called tissue factor (TF). In cancer, the Factor VIIa:TF complex is found in abundance in lung, breast, pancreatic, gastric and colon tumors, and triggers a host of physiologic processes that facilitate angiogenesis, tumor growth, and invasion. Animal models suggest that inhibitors of Factor VIIa may block tumor growth and metastases.