Thyromimetic
Appearance
Thyromimeticdrugs are synthetic agonists of thethyroid hormone receptor's isoforms TR α1, TRα2, TRβ1, or TRβ2, mimicking some or all of the effects of endogenously producedthyroid hormonesthat regulatemetabolism.[1][2]Some thyromimetic drugs are selective for various of these receptors over others, enabling more targeted effects and reducing toxicity. Thyromimetics selective for TRβ—includingeprotirome,[3]sobetirome,[4]resmetirom,[5]and theprodrugVK2809—have been investigated for the treatment ofnon-alcoholic fatty liver disease,dyslipidemia,and other metabolic and neurodegenerative diseases.[3]
References
[edit]- ^Unnikrishnan, A. G.; Baruah, Manash; Kalra, Sanjay (December 2012)."Thyromimetics: What does the future hold?".Indian Journal of Endocrinology and Metabolism.16(Suppl 2): S159–S161.doi:10.4103/2230-8210.104029.ISSN2230-8210.PMC3603016.PMID23565368.
- ^Devereaux, Jordan; Ferrara, Skylar J.; Scanlan, Thomas S. (2018). "Quantification of Thyromimetic Sobetirome Concentration in Biological Tissue Samples".Thyroid Hormone Nuclear Receptor.Methods in Molecular Biology. Vol. 1801. Springer. pp. 193–206.doi:10.1007/978-1-4939-7902-8_16.ISBN978-1-4939-7901-1.
- ^abSaponaro, Federica; Sestito, Simona; Runfola, Massimiliano; Rapposelli, Simona; Chiellini, Grazia (2020)."Selective Thyroid Hormone Receptor-Beta (TRβ) Agonists: New Perspectives for the Treatment of Metabolic and Neurodegenerative Disorders".Frontiers in Medicine.7:331.doi:10.3389/fmed.2020.00331.ISSN2296-858X.PMC7363807.PMID32733906.
- ^Tancevski, Ivan; Demetz, Egon; Eller, Philipp (1 January 2011)."Sobetirome: A Selective Thyromimetic for the Treatment of Dyslipidemia".Recent Patents on Cardiovascular Drug Discovery.6(1): 16–19.doi:10.2174/157489011794578473.
- ^Alkhouri, Naim (1 February 2020)."Thyromimetics as emerging therapeutic agents for nonalcoholic steatohepatitis: rationale for the development of resmetirom (MGL-3196)".Expert Opinion on Investigational Drugs.29(2): 99–101.doi:10.1080/13543784.2020.1708899.ISSN1354-3784.
Further reading
[edit]- Yehuda-Shnaidman, Einav; Kalderon, Bella; Bar-Tana, Jacob (2014)."Thyroid Hormone, Thyromimetics, and Metabolic Efficiency".Endocrine Reviews.35(1): 35–58.doi:10.1210/er.2013-1006.