Tideglusib
| |
| |
Identifiers | |
---|---|
| |
CAS Number | |
PubChem CID | |
ChemSpider | |
Chemical and physical data | |
Formula | C19H14N2O2S |
Molar mass | 334.392 g/mol |
3D model (JSmol) | |
| |
|
Tideglusib (NP-12, NP031112) is a potent, selective and irreversible[1] small molecule non-ATP-competitive glycogen synthase kinase 3 (GSK-3) inhibitor.
Potential applications
Tideglusib is under investigation for multiple applications:
- Alzheimer's disease and progressive supranuclear palsy. As of 2017 it was undergoing Phase IIa[2] and IIb clinical trials.[3][4][5][6] The first trial to be published (in English) was Phase II and demonstrated that tideglusib was well tolerated, except for some moderate, asymptomatic, fully reversible increases in liver enzymes.[4]
- Tooth repair mechanisms that promotes dentine reinforcement of a sponge structure until the sponge biodegrades, leaving a solid dentine structure. In 2016, the results of animal studies were reported in which 0.14 mm holes in mouse teeth were permanently filled.[7]
- Tideglusib is being studied in Phase II clinical trials as a treatment for congenital/juvenile-onset myotonic muscular dystrophy type I.[8]
References
- ↑ Domínguez, JM; Fuertes, A; Orozco, L; del Monte-Millán, M; Delgado, E; Medina, M (January 2012). "Evidence for Irreversible Inhibition of Glycogen Synthase Kinase-3 by Tideglusib" (PDF). The Journal of Biological Chemistry. 287 (2): 893–904. doi:10.1074/jbc.M111.306472. PMC 3256883. PMID 22102280.
- ↑ Teodoro Del Ser (2010). "Phase IIa clinical trial on Alzheimer's disease with NP12, a GSK3 inhibitor". Alzheimer's & Dementia. 6 (4): S147. doi:10.1016/j.jalz.2010.05.455.
- ↑ Eldar-Finkelman, H; Martinez, A (2011). "GSK-3 Inhibitors: Preclinical and Clinical Focus on CNS". Frontiers in Molecular Neuroscience. 4: 32. doi:10.3389/fnmol.2011.00032. PMC 3204427. PMID 22065134.
- 1 2 Del Ser, T; Steinwachs, KC; Gertz, HJ; Andrés, MV; Gómez-Carrillo, B; Medina, M; Vericat, JA; Redondo, P; et al. (2013). "Treatment of Alzheimer's disease with the GSK-3 inhibitor tideglusib: A pilot study". Journal of Alzheimer's Disease. 33 (1): 205–15. doi:10.3233/JAD-2012-120805. PMID 22936007.
- ↑ "FDA Grants Fast Track Status to Tideglusib (ZentylorTM) for Progressive Supranuclear Palsy". PR Newswire Europe Including UK Disclose. 10 September 2010. Retrieved 11 August 2013.
- ↑ Dominguez, JM; Fuertes, A; Orozco, L; Del Monte-Millan, M; Delgado, E; Medina, M (2011). "Evidence for Irreversible Inhibition of Glycogen Synthase Kinase-3 by Tideglusib". Journal of Biological Chemistry. 287 (2): 893–904. doi:10.1074/jbc.M111.306472. PMC 3256883. PMID 22102280.
- ↑ Gallagher, James (2017-01-09). "'Tooth repair drug' may replace fillings". BBC News. Retrieved 2017-01-09.
- ↑ "AMO-2". AMO Pharmaceuticals. Retrieved 2017-09-21.
This article is issued from
Wikipedia.
The text is licensed under Creative Commons - Attribution - Sharealike.
Additional terms may apply for the media files.