Curis Hedgehog and Beyond --plus multi-targeting cancer inhibitors

Discovery of 7-(4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDC-101) as a Potent Multi-Acting HDAC, EGFR, and HER2 Inhibitor for the Treatment of Cancer.

http://pubs.acs.org/doi/full/10.1021/jm901453q

By incorporating histone deacetylase (HDAC) inhibitory functionality into the pharmacophore of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) inhibitors, we synthesized a novel series of compounds with potent, multiacting HDAC, EGFR, and HER2 inhibition and identified 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide 8 (CUDC-101) as a drug ...

CUDC-101 is a molecule that can target 3 different and novel cancer pathways at once. This allows patients to take a single doses instead of having to take multiple agents at once or at various times. The intent of this design is for network disruption.

• Efficacy dose ranges are above 150mg/m2
• About double the half life in tumors when compared to plasma

What does CUDC-101 Target? (EGFR, HDAC, HER2)

EGFR (Epidermal growth factor receptor) ...