Factor VIIa Inhibitor Program

Factor VII Close close Factor VIICoagulation Factors V, VII, X and II are substances in blood essential to the normal clotting process.is a blood protein Close close Protein

A class of molecules (including enzymes, antibodies, or structural proteins) that are built from amino acid components to perform a wide range of functions in the cell.

involved in clotting. Many types of cancer (such as lung, breast, pancreatic, colorectal, gastric and others) express high levels of a cell surface protein known as Tissue Factor Close close

Tissue Factor

A protein that initiates one pathway leading to blood coagulation.

(TF). After binding to TF, Factor VII becomes activated and triggers a host of pathologic processes in the tumor Close close

TumorAn abnormal growth of cells that may be the result of cancer.microenvironment that facilitate the growth, invasion and spread of many cancers. Activation of Factor VII (Factor VIIa) Close close

Factor VIIa, Factor IXa, Factor Xa, Factor XI

A series of coagulation factors that circulate outside the blood stream and in the environment surrounding tumors.

by TF also leads to the high incidence of thromboembolic Close close

thromboembolic

The formation and dislodging of a clot (thrombus) within a blood vessel that is then carried via blood stream to plug another vessel in the lungs (pulmonary embolism), brain (stroke), gastrointestinal tract, kidneys, or leg. Treatment often involves anticoagulants (blood thinners), aspirin, or vasodilators (drugs that relax and widen vessels).

complications seen in cancer patients.

PCI-27483 is a novel first-in-class small molecule inhibitor, which selectively targets the Factor VIIa/TF complex. Inhibitors of this complex may reduce tumor growth and metastases as well as the incidence of venous thromboembolism. Close close thromboembolism

Thromboembolic complications are a leading cause of death in patients with cancer and anticoagulant treatment has been shown to improve survival in a variety of cancers (Klerk et al. J Clin Onc. 2005).

Animation of PCI-27483 Effects on Cell Signaling

Patents

PCI-27483 as a compound, in pharmaceutical compositions, and in uses for treating a variety of diseases is covered by US patent applications (issued and pending) and PCT national phase patent applications in 14 other jurisdictions, including Europe, Canada, Japan, China, India, South Korea, Australia and Brazil. Projected coverage is through at least 2024 (without including patent term extensions in the various territories).

Partnering

Pharmacyclics is seeking a partner to develop PCI-27483. We believe this unique drug may be competitively positioned for significant partnership following the successful achievement of further clinical milestones.