Licensing status

Publication and contact information

Drug platforms

Automated, high throughput, microfluidic SAR platform

An automated, microfluidic SAR platform could be used to rapidly optimize kinase inhibitors. Gleevec imatinib, a small molecule inhibitor of BCR-ABL tyrosine kinase, was subjected to repeated cycles of computer-assisted derivatization, synthesis, purification and screening using a microfluidic system. The best of the resulting compounds had about 100-fold more potent IC50 values for BCR-ABL than imatinib. The molecules also were more effective against imatinib-resistant mutant versions of the enzyme and were cell permeable. Next steps include adapting the platform for cell culture and screening against nonsoluble targets.
Gleevec is marketed by Novartis AG to treat multiple cancers.

SciBX 6(12); doi:10.1038/scibx.2013.298
Published online March 28, 2013

Platform patented; available for partnering

Desai, B. et al. J. Med. Chem.; published online Feb. 26, 2013;
Contact: Christopher N. Selway, Cyclofluidic Ltd.,
Welwyn Garden City, U.K.