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Editorial

Sobetirome: the past, present and questions about the future

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Bibliography

References 2 and 3 are recent reviews of emerging therapies for dyslipidemia.

  • Baxter JD, Webb P. Thyroid hormone mimetics: potential applications in atherosclerosis, obesity and type 2 diabetes. Nat Rev 2009;8:308-20
  • Scanlan TS. Sobetirome: a case history of bench-to-clinic drug discovery and development. Heart Fail Rev 2010;15:177-82

State of the art review on Sobetirome action from the creator of the compound.

  • Tancevski I, Demetz E, Eller P. Sobetirome: a selective thyromimetic for the treatment of dyslipidemia. Recent Pat Cardiovasc Drug Discov 2011;6:16-19

Good recent review on Sobetirome.

  • Bernal J, Guadaño-Ferraz A, Morte B . Thyroid hormone transporters-functions and clinical implications. Nat Rev Endocrinol 2015;11:406-17
  • Lin JZ, MartagÓn AJ , Hsueh WA, et al. Thyroid hormone receptor agonists reduce serum cholesterol independent of the LDL receptor. Endocrinology 2012;153:6136-44

Highlights the importance of non-low density lipoprotein (LDL) receptor dependent pathways in thyroid hormone (TH)-dependent cholesterol reabsorption; key for TH receptor (TR)-based therapies.

  • Berkenstam A , Kristensen J, MellstrÖm K, et al. The thyroid hormone mimetic compound KB2115 lowers plasma LDL cholesterol and stimulates bile acid synthesis without cardiac effects in humans. Proc Natl Acad Sci USA 2008;105:663-7
  • Ladenson PW, Kristensen JD, Ridgway EC, et al. Use of the thyroid hormone analogue eprotirome in statin-treated dyslipidemia. N Engl J Med 2010;362:906-16
  • Sjouke B, Langslet G, Ceska R, et al. Eprotirome in patients with familial hypercholesterolaemia (the AKKA trial): a randomised, double-blind, placebo-controlled phase 3 study. Lancet Diabetes Endocrinol 2014;2:455-63
  • Angelin B, Kristensen JD, Eriksson M, et al. Reductions in serum levels of LDL cholesterol, apolipoprotein B, triglycerides and lipoprotein(a) in hypercholesterolaemic patients treated with the liver-selective thyroid hormone receptor agonist eprotirome. J Intern Med 2015;277:331-42
  • Takahashi N, Asano Y, Maeda K, Watanabe N. In vivo evaluation of 1-benzyl-4-aminoindole-based thyroid hormone receptor beta agonists: importance of liver selectivity in drug discovery. Biol Pharm Bull 2014;37:1103-8
  • Williams GR. Thyroid hormone actions in cartilage and bone. Eur Thyroid J 2013;2:3-13
  • Scanlan T, Hartley M, Placzek A, Righi M. Use of Sobetirome in the Treatment of X-linked Adrenoleukodystrophy. WO178892; 2014
  • MartagÓn AJ , Lin JZ, Cimini SL, et al. The amelioration of hepatic steatosis by thyroid hormone receptor agonists is insufficient to restore insulin sensitivity in Ob/Ob mice. PLoS One 2015;10:e0122987
  • Mousa SA, Lin HY, Tang HY, et al. Modulation of angiogenesis by thyroid hormone and hormone analogues: implications for cancer management. Angiogenesis 2014;17:463-9

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