Tideglusib

Tideglusib (NP-12, NP031112) is a potent, selective and irreversible small molecule non-ATP-competitive glycogen synthase kinase 3 (GSK-3) inhibitor.
Other GSK inhibitors.
There are few classes of GSK-inhibitors, including lithium
(Martinez et al., 2011), the small peptide L803mts10, and members
of the thiazolidinedione family, containing non-competitive
inhibitors of GSK-3, such as TDZD-8 (Shapira et al., 2007) or
Tideglusib® (Noscira, Madrid, and Spain), the latter having an
irreversible inhibitory effect on GSK-3 (del Ser et al., 2013). 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 (del Ser et al., 2013)—to
very severe, such as hypoglycemia—or tumorigenesis (Martinez
et al., 2011). 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 (del Ser et al., 2013). In a phase-IIa clinical
trial, the treatment was discontinued in 35% of all the active subjects,
mainly due to adverse reactions (del Ser et al., 2013).
Potential applications.
Tideglusib is under investigation for multiple applications: