Journal article
Abstract A177: Phase 1, dose-escalation, safety, pharmacokinetic and pharmacodynamic study of single agent PF-03758309, an oral PAK inhibitor, in patients with advanced solid tumors.
Lee S Rosen, Todd A Blumenkopf, Aurora Breazna, Sheree Darang, Jorge D Gallo, Jonathan Goldman, Diane Wang, Linda Mileshkin, S Gail Eckhardt
Molecular Cancer Therapeutics | American Association for Cancer Research (AACR) | Published : 2011
Abstract
Abstract Background: P21 activated kinase (PAK), a family of serine-threonine kinases, is a downstream effector of the Rho family and functions as a signaling node for various oncogenic pathways. The capability to transform cell cultures and the consistent anti tumor response associated with PAK inhibition in preclinical studies has raised the interest of PAK as a potential target for oncology. PAK consists in 6 isoforms divided into 2 subgroups. PAK isoforms 1 and 4 have been more frequently related to cancer biology. PF309 is a potent ATP-competitive inh of PAK1, 4, 5 and 6. Methods: Adult pts with advanced solid tumors were enrolled in a Ph 1 single agent dos..
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