BioCentury
ARTICLE | Distillery Therapeutics

Autoimmune disease

April 10, 2018 10:50 PM UTC

In vitro and mouse studies identified a tetrahydrocarboline-based HDAC6 inhibitor that could help treat arthritis. Chemical synthesis and in vitro activity assays of tetrahydrocarboline analogs yielded a compound that inhibited HDAC6 with a Ki of 0.7 nM and 250- to 2,600-fold greater selectivity over other HDAC types. In a mouse model of collagen-induced arthritis, the compound decreased disease severity scores, paw thickness, and synovial inflammation, cellular invasion, degradation of cartilage and bone erosion in joints and increased body weight compared with vehicle. Next steps could include testing the compound in additional models of arthritis.

Celgene Corp. has the HDAC6 inhibitor ricolinostat (ACY-1215) in Phase II testing for multiple myeloma (MM) and Phase I/II testing for lymphoma. Celgene and Regenacy Pharmaceuticals LLC also have the compound in preclinical testing for chemotherapy-induced peripheral neuropathy (CIPN)...

BCIQ Company Profiles

University of Regensburg

BCIQ Target Profiles

Histone deacetylase 6 (HDAC6)