Therapeutics: Catechol-O-methyl-transferase (COMT)

In vitro studies identified a thiazolidinedione-based COMT inhibitor that could help treat PD. Directed structure-based drug design and in vitro testing identified a thiazolidinedione analog that inhibited the activity of human COMT with greater potency than the COMT inhibitors Tasmar tolcapone and Comtan entacapone (IC50 values of 54 nM, 127 nM and 386 nM, respectively). In a human liver cell line, the compound induced less mitochondrial toxicity than Tasmar and induced toxicity comparable to Comtan. Next steps include testing the inhibitor in PD models.

Roche markets Tasmar to treat PD...