Tideglusib


Tideglusib is a potent, selective and irreversible small molecule non-ATP-competitive glycogen synthase kinase 3 inhibitor.

Other GSK inhibitors

There are few classes of GSK-inhibitors, including lithium
, the small peptide L803mts10, and members
of the thiazolidinedione family, containing non-competitive
inhibitors of GSK-3, such as TDZD-8 or
Tideglusib®, the latter having an
irreversible inhibitory effect on GSK-3. The
inhibition of the GSK-3 pathways through distinct mechanisms has
been associated with a wide range of adverse reactions, ranging
from mild, such as vertigo—or diarrhea —to
very severe, such as hypoglycemia—or tumorigenesis. The use of Tideglusib specifically was associated with
mild-moderate adverse reactions, which included transient increases
in serum creatine kinase, ALT—or gGT—diarrhea, nausea, cough,
fatigue, and headache. In a phase-IIa clinical
trial, the treatment was discontinued in 35% of all the active subjects,
mainly due to adverse reactions.

Potential applications

Tideglusib is under investigation for multiple applications: