Pharmacyclics Announces Completion of Phase 1 Clinical Trial of Factor VIIa Inhibitor...( SUNNYVALE Calif. Nov. 25 /- Pharmacyc...),Health

SUNNYVALE, Calif., Nov. 25 /PRNewswire-FirstCall/ -- Pharmacyclics, Inc. (Nasdaq: PCYC) today announced that the company has completed a Phase 1 clinical trial with PCI-27483, the company's novel, first-in-class small-molecule Factor VIIa inhibitor. The trial was conducted in sixteen (16) healthy volunteers to evaluate the safety and pharmacologic effect of PCI-27483. A single administration of PCI-27483 resulted in a linear dose response in the International Normalized Ratio (INR), a routine laboratory test used to assess the level of anticoagulation (blood-thinning).

"Single doses of PCI-27483 reliably and quickly achieved therapeutic levels of anticoagulation without adverse effects in this initial trial," said James Lowder, M.D., Vice President, Clinical Development for Pharmacyclics. "The ability to achieve precise levels of anticoagulation that can be readily measured differentiates PCI-27483 from other available anticoagulants. The Factor VIIa: tissue factor complex, the pharmacologic target of PCI-27483, has been implicated both in the progression of solid tumors and the increased incidence of venous thromboembolic events observed in many malignancies. Up-regulation of tissue factor expression is observed in pancreatic, lung, and breast cancer, and is associated with a worsened prognosis."

In the recently completed study, PCI-27483 increased the INR with minimal intra-subject variation and a half-life of ten hours. At the highest subcutaneous dose of PCI-27483 evaluated, a mean (+/-standard error) peak INR of 2.72 (+/- 0.24) was achieved one to two hours post-dosing. The trial further established doses of PCI-27483, which upon repeated dosing are expected to maintain the INR in the range of 2.0 to 3.0, the target window for treatment and prevention of thromboembolic events (i.e., formation of blood clots).