Category Archives: Rational Drug Design

Genspera G-202 – anti-cancer hand grenade

Genspera is a company developing novel prodrugs for the treatment of cancer.  In a phase 2 study in patients with hepatocellular carcinoma who have failed treatment with Nexavar (sorafenib), a tyrosine kinase inhibitor that blocks KIT, FLT-3 RET, raf, VEGFR1-3, and PDGF kinases, a doubling of time to progression was seen in patients taking G-202. Continue reading

Ras – targeting the “undruggable”

The Ras onogene has been studied for 30 years, with over 40,000 scientific articles published on it.  However, an inhibitor of the mutated form of Ras has not been able to be developed.  So, researchers have developed downstream blockers of the Ras cascade – MEK inhibitors and Raf inhibitors, for example.  But why can’t a molecule that blocks mutated Ras be identified? Continue reading

Precision Medicine: SWOG Lung-MAP study – unique public/private collaboration

Using genomics to take-on advanced non-small cell lung cancer, the Southwest Oncology Group announced the start of a master protocol that will screen patients for optimal eligibility into one of five clinical trials with experimental drugs… Continue reading