PCI-27483

PCI-27483 is a reversible, selective small-molecule inhibitor of activated factor VII (factor VIIa), a serine protease that becomes active upon binding to tissue factor (TF) and forms the FVIIa/TF complex. This complex activates intracellular signaling pathways, including those mediated by protease activated receptor 2 (PAR2), which are implicated in tumor cell proliferation, angiogenesis, and metastasis—especially in tumors overexpressing TF. By inhibiting FVIIa within the FVIIa/TF complex, PCI‑27483 blocks PAR2-mediated signal transduction and may suppress tumor growth and spread as well as reduce thrombotic complications associated with cancer. The drug also inhibits both extrinsic and intrinsic coagulation cascades, providing antithrombotic effects. Preclinical studies demonstrated significant inhibition of tumor growth in animal models of pancreatic cancer; clinical trials have focused on advanced pancreatic cancer patients receiving gemcitabine[2][3][6][8]. The compound was originally developed by Celera Corporation, later licensed to Pharmacyclics (acquired by AbbVie), with Novo Nordisk obtaining rights for non-oncology indications[3][7].

Other names

UNII-6073LCU8U9UNII6073LCU8U9UNII 6073LCU8U9