This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Cancer

Histone deacetylase 6 (HDAC6); histone deacetylase 8 (HDAC8)

In vitro studies suggest dual inhibition of HDAC6 and HDAC8 could help treat cancer. Inhibition of HDAC6 or HDAC8 has been shown to promote cancer cell death. In a panel of HDACs, BRD73954 selectively inhibited HDAC6 and HDAC8 with nanomolar IC50 values. Next steps include testing BRD73954 in models for neuroblastoma and using the compound to identify substrates for HDAC6 and HDAC8.
Acetylon Pharmaceuticals Inc.'s rocilinostat, an oral selective HDAC6 inhibitor, is in Phase I/II testing to treat multiple myeloma.

At least three other companies have compounds that inhibit HDAC6 or HDAC8 in preclinical development to treat various cancers or inflammation.

SciBX 6(23); doi:10.1038/scibx.2013.572
Published online June 13, 2013

Patent application filed; available for licensing

Olson, D.E. et al. J. Med. Chem.; published online May 14, 2013;
doi:10.1021/jm400390r
Contact: Edward Holson, Broad Institute of MIT and Harvard, Cambridge, Mass.
e-mail:
edholson@broadinstitute.org