The trial was conducted in 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.
In the recently completed study, PCI-27483 increased the INR with minimal intra-subject variation and a half-life of 10 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 two to three, the target window for treatment and prevention of thromboembolic events.
David Loury, vice president of development at Pharmacyclics, said: PCI-27483 is expected to have a dual effect of inhibiting tumor growth and decreasing the incidence of venous thromboembolic events in patients with cancer. We’re diligently working to move PCI-27483 through clinical development, as evidenced by our early completion of the Phase I trial. We believe that this compound has unique potential for cancer patients.