Sobetirome: A selective thyromimetic for the treatment of dyslipidemia

Recent Patents on Cardiovascular Drug Discovery

Volumn 6, Issue 1, 2011, Pages 16-19

  Tancevski, Ivan ^a   Demetz, Egon ^a   Eller, Philipp ^a  

^a INNSBRUCK MEDICAL UNIVERSITY   (Austria)

Author keywords

Atherosclerosis; Bile acids; Gc 1; LDL cholesterol; Reverse cholesterol transport; Triglycerides

Indexed keywords

BILE ACID; CHOLESTEROL; EPROTIROME; HORMONE RECEPTOR STIMULATING AGENT; KB 141; KB 495; LIOTHYRONINE; LOW DENSITY LIPOPROTEIN CHOLESTEROL; LOW DENSITY LIPOPROTEIN RECEPTOR; MB 07811; SOBETIROME; T 0681; THYROMIMETIC AGENT; TRIACYLGLYCEROL; UNCLASSIFIED DRUG; VERY LOW DENSITY LIPOPROTEIN; VIA 3196;

ARTICLE; BILE SECRETION; CHOLESTEROL BLOOD LEVEL; CHOLESTEROL TRANSPORT; CLINICAL TRIAL (TOPIC); DOSE RESPONSE; DRUG EFFICACY; DRUG MECHANISM; DRUG TOLERABILITY; DYSLIPIDEMIA; HUMAN; NONHUMAN; PHASE 1 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; PROTEIN INDUCTION; TRIACYLGLYCEROL BLOOD LEVEL;

ACETIC ACIDS; ANIMALS; BILE ACIDS AND SALTS; BIOLOGICAL MARKERS; CHOLESTEROL; DYSLIPIDEMIAS; HUMANS; HYPOLIPIDEMIC AGENTS; LIVER; MOLECULAR MIMICRY; PHENOLS; RECEPTORS, LDL; THYROID HORMONES; TREATMENT OUTCOME; TRIGLYCERIDES;

EID: 79551673577     PISSN: 15748901     EISSN: None     Source Type: Journal    
DOI: 10.2174/157489011794578473     Document Type: Article

References (41)

1. Mason RL, Hunt HM, Hurxthal L. Blood cholesterol values in hyperthyroidism and hypothyroidism. N Engl J Med 1930; 203: 1273-1278.
2. Jorgensen EC. Thyromimetics and antithyroid drugs. Berger's Med Chem 1979; Part 3: 103-145.
3. The Coronary Drug Project. Findings leading to further modifications of its protocol with respect to dextrothyroxine. The coronary drug project research group. JAMA 1972; 220(7): 996-1008.
4. Baxter JD, Dillmann WH, West BL, Huber R, Furlow JD, Fletterick RJ, et al. Selective modulation of thyroid hormone receptor action. J Steroid Biochem Mol Biol 2001; 76(1-5): 31-42.
5. Young WF, Jr., Gorman CA, Jiang NS, Machacek D, Hay ID. L-Thyroxine contamination of pharmaceutical D-thyroxine: probable cause of therapeutic effect. Clin Pharmacol Ther 1984; 36(6): 781-787.
6. Sap J, Munoz A, Damm K, Goldberg Y, Ghysdael J, Leutz A, et al. The c-Erb-A protein is a high-affinity receptor for thyroid hormone. Nature 1986; 324(6098): 635-640.
7. Weinberger C, Thompson CC, Ong ES, Lebo R, Gruol DJ, Evans RM. The c-Erb-A gene encodes a thyroid hormone receptor. Nature 1986; 324(6098): 641-646.
8. Apriletti JW, Ribeiro RC, Wagner RL, Feng W, Webb P, Kushner PJ, et al. Molecular and structural biology of thyroid hormone receptors. Clin Exp Pharmacol Physiol Suppl 1998; 25: S2-S11.
9. Lazar MA. Thyroid hormone receptors: multiple forms, multiple possibilities. Endocr Rev 1993; 14(2): 184-193.
10. Weiss RE, Murata Y, Cua K, Hayashi Y, Seo H, Refetoff S. Thyroid hormone action on liver, heart, and energy expenditure in thyroid hormone receptor beta-deficient mice. Endocrinology 1998; 139(12): 4945-4952.
11. Gullberg H, Rudling M, Salto C, Forrest D, Angelin B, Vennstrom B. Requirement for thyroid hormone receptor beta in T3 regulation of cholesterol metabolism in mice. Mol Endocrinol 2002; 16(8): 1767-1777.
12. Johansson C, Vennstrom B, Thoren P. Evidence that decreased heart rate in thyroid hormone receptor-alpha1-deficient mice is an intrinsic defect. Am J Physiol 1998; 275(2 Pt 2): R640-R646.
13. Gloss B, Trost S, Bluhm W, Swanson E, Clark R, Winkfein R, et al. Cardiac ion channel expression and contractile function in mice with deletion of thyroid hormone receptor alpha or beta. Endocrinology 2001; 142(2): 544-550.
14. Baxter JD, Webb P. Thyroid hormone mimetics: Potential applications in atherosclerosis, obesity and type 2 diabetes. Nat Rev Drug Discov 2009; 8(4): 308-320.
15. Scanlan TS. Sobetirome: a case history of bench-to-clinic drug discovery and development. Heart Fail Rev 2010; 15(2): 177-182.
16. Scanlan, T.S., Chiellini, G., Yoshihara, H., Apriletti, J., Baxter,J.D., Ribeiro, R.C.J. Selective thyroid hormone analogues. US005883294 (1999).
17. Scanlan, T.S., Yoshihara, H.A.I., Chiellini, G., Mitchison, T.J. Thyroid hormone analogues and methods for their preparation. US006107517 (2000).
18. Morkin, E., Bucalo, L.R., Goldman, S. Administration of 3,5-Diiodothyropropionic acid for stimulating weight loss, and/or lowering triglyceride levels, and/or treatment of metabolic syndrome. US20100249235 (2010).
19. Mousa, S.A., Davis, F.B., Davis, P.J. Thyroid hormone analogs and methods of use. US007785632 (2010).
20. Bleicher L, Aparicio R, Nunes FM, Martinez L, Dias GSM, Figueira AC, et al. Structural basis of GC-1 selectivity for thyroid hormone receptor isoforms. BMC Struct Biol 2008; 8: 8.
21. Trost SU, Swanson E, Gloss B, Wang-Iverson DB, Zhang H, Volodarsky T, et al. The thyroid hormone receptor-beta-selectiveagonist GC-1 differentially affects plasma lipids and cardiac activity. Endocrinology 2000; 141(9): 3057-3064.
22. Baxter JD, Webb P, Grover G, Scanlan TS. Selective activation of thyroid hormone signaling pathways by GC-1: A new approach tocontrolling cholesterol and body weight. Trends Endocrinol Metab 2004; 15(4): 154-157.
23. Grover GJ, Egan DM, Sleph PG, Beehler BC, Chiellini G, Nguyen NH, et al. Effects of the thyroid hormone receptor agonist GC-1 on metabolic rate and cholesterol in rats and primates: selective actions relative to 3,5,3'-triiodo-L-thyronine. Endocrinology 2004; 145(4): 1656-1661.
24. Bakker O, Hudig F, Meijssen S, Wiersinga WM. Effects of triiodothyronine and amiodarone on the promoter of the human LDL receptor gene. Biochem Biophys Res Commun 1998; 249(2): 517-521.
25. Salter AM, Hayashi R, Al-Seeni M, Brown NF, Bruce J, Sorensen O, et al. Effects of hypothyroidism and high-fat feeding on mRNA concentrations for the low-density-lipoprotein receptor and on acyl-CoA: Cholesterol acyltransferase activities in rat liver. Biochem J 1991; 276 (Pt 3): 825-832.
26. Staels B, Van Tol A, Chan L, Will H, Verhoeven G, Auwerx J. Alterations in thyroid status modulate apolipoprotein, hepatic triglyceride lipase, and low density lipoprotein receptor in rats. Endocrinology 1990; 127(3): 1144-1152.
27. Johansson L, Rudling M, Scanlan TS, Lundasen T, Webb P, Baxter J, et al. Selective thyroid receptor modulation by GC-1 reduces serum lipids and stimulates steps of reverse cholesterol transport in euthyroid mice. Proc Natl Acad Sci USA 2005; 102(29): 10297-10302.
28. Tancevski I, Demetz E, Eller P, Duwensee K, Hoefer J, Heim C, et al. The liver-selective thyromimetic T-0681 influences reverse cholesterol transport and atherosclerosis development in mice. PLoS One 2010; 5(1): e8722.
29. Tancevski I, Wehinger A, Demetz E, Hoefer J, Eller P, Huber E, et al. The thyromimetic T-0681 protects from atherosclerosis. J Lipid Res 2009; 50(5): 938-944.
30. Erion MD, Cable EE, Ito BR, Jiang H, Fujitaki JM, Finn PD, et al. Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. Proc Natl Acad Sci USA 2007; 104(39): 15490-15495.
31. Billheimer, J.T., Rader, D.J. Method for in vivo measurement of reverse cholesterol transport. WO2009158328 (2009).
32. Hellerstein, M.K. Methods for measuring cholesterol metabolism and transport. US20060251576 (2006).
33. Saxena, U., Pillarisetti, S., Khanna, I. Compositions and methods to enhance reverse cholesterol transport. WO2007143724 (2007).
34. Duffy D, Rader DJ. Emerging therapies targeting high-density lipoprotein metabolism and reverse cholesterol transport. Circulation 2006; 113(8): 1140-1150.
35. Cuchel M, Rader DJ. Macrophage reverse cholesterol transport: key to the regression of atherosclerosis? Circulation 2006; 113(21): 2548-2555.
36. Wang X, Rader DJ. Molecular regulation of macrophage reverse cholesterol transport. Curr Opin Cardiol 2007; 22(4): 368-372.
37. Tancevski I, Eller P, Patsch JR, Ritsch A. The resurgence of thyromimetics as lipid-modifying agents. Curr Opin Investig Drugs 2009; 10(9): 912-918.
38. Nilsson L-M, Rehnmark S, Davoodpour P, Larsson L, Parini P. Thyroid hormone receptor modulation reduces the atherosclerotic process through increased reverse cholesterol transport. Arterioscler Thromb Vasc Biol Annu Conf 2009; 29: P325.
39. Taub R, Grimsby J, Larigan JD, Pietranico S, Dvorozniak M, Conde-Knape K. VIA-3196, a liver-directed thyroid beta agonist for treating cardiometabolic disease. Circ Suppl 2009; 120: S1095.
40. Ladenson PW, Kristensen JD, Ridgway EC, Olsson AG, Carlsson B, Klein I, et al. Use of the thyroid hormone analogue eprotirome in statin-treated dyslipidemia. N Engl J Med 2010; 362(10): 906-916.
41. Tancevski I, Wehinger A, Demetz E, Eller P, Duwensee K, Huber J, et al. Reduced plasma high-density lipoprotein cholesterol in hyperthyroid mice coincides with decreased hepatic adenosine 5'-triphosphate-binding cassette transporter 1 expression. Endocrinology 2008; 149(7): 3708-12.