This week in therapeutics




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3-Phosphoinositide-dependent protein kinase-1 (PDPK1); BRAF

Studies in patient tumor samples and mice suggest PDPK1 inhibitors could help treat melanoma. In human primary and metastatic melanoma tumors, PDPK1 levels were higher than those in normal tissue. In mouse models of Braf-mutant melanoma, Pdpk1 knockout increased survival and decreased primary tumor growth and lung metastases compared with normal Pdpk1 expression. In this model, a small molecule PDPK1 inhibitor decreased tumor growth and metastasis compared with vehicle. Next steps include identifying human melanomas that might respond to PDPK1 inhibitors.
Arno Therapeutics Inc. has AR-12 (OSU-0312), a small molecule PDPK1 inhibitor, in Phase I testing to treat lymphoma and solid tumors.
Phusis Therapeutics Inc. has PHT-427, a small molecule inhibitor of protein kinase B (PKB; PKBA; AKT; AKT1) mRNA and PDPK1, in preclinical development to treat cancer.

SciBX 6(40); doi:10.1038/scibx.2013.1124
Published online Oct. 17, 2013

Patented by the Sanford-Burnham Medical Research Institute; licensing status undisclosed

Scortegagna, M. et al. Oncogene; published online Sept. 16, 2013;
Contact: Ze'ev A. Ronai, Sanford-Burnham Medical Research Institute,
La Jolla, Calif.