This week in therapeutics

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Cancer

Pancreatic cancer

K-Ras; 3-phosphoinositide-dependent protein kinase-1 (PDPK1)

Mouse studies suggest inhibiting PDPK1 could help prevent mutant K-Ras-driven pancreatic ductal adenocarcinomas (PDACs). In the epithelial cells of K-ras mutant mice, Pdpk1 inactivation prevented acinar-to-ductal development of premalignant pancreatic intraepithelial neoplasias and PDACs. The mice also had higher median survival than K-ras mutant mice expressing functional Pdpk1. Next steps could include testing clinical-stage PDK1 inhibitors in mouse models for PDAC.
Arno Therapeutics Inc.'s AR-12, a small molecule PDPK1 inhibitor that blocks the phosphoinositide 3-kinase (PI3K) and protein kinase B (PKB; PKBA; AKT; AKT1) pathway, is in Phase I testing to treat solid tumors and lymphoma.

SciBX 6(11); doi:10.1038/scibx.2013.264
Published online March 21, 2013

Patent and licensing status unavailable

Eser, S. et al. Cancer Cell; published online Feb. 28, 2013;
doi:10.1016/j.ccr.2013.01.023
Contact: Dieter Saur, Technical University Munich, Munich, Germany
e-mail:
dieter.saur@lrz.tum.de