Sobetirome

A case history of bench-to-clinic drug discovery and development

Research output: Contribution to journalArticle

44 Citations (Scopus)

Abstract

Sobetirome, also known as GC-1 and QRX-431, is a member of a class of compounds known as selective thyromimetics (Scanlan et al., Curr Opin Drug Discov Dev 4:614-622). These compounds are synthetic structural analogs of thyroid hormone that have tissuespecific thyroid hormone actions. Many of the compounds in this class, including sobetirome, also are subtypeselective thyroid hormone receptor (TR) agonists. Sobetirome selectively binds to and activates TRβ over TRα and this receptor selectivity led to the hypothesis that sobetirome would lower cholesterol through activation of liver TRβ without stimulating cardiac function through TRα activation in the heart. The tissue selective thyromimetic properties of sobetirome have been demonstrated in numerous animal models, which led to its clinical development as a novel cholesterol-lowering agent. This review will describe the discovery and development journey of sobetirome as a case history.

Original languageEnglish (US)
Pages (from-to)177-182
Number of pages6
JournalHeart Failure Reviews
Volume15
Issue number2
DOIs
StatePublished - Mar 2010
Externally publishedYes

Fingerprint

Drug Discovery
Thyroid Hormone Receptors
Thyroid Hormones
Cholesterol
Thyrotropin Receptors
GC 1 compound
Animal Models
Hormones
Liver
Pharmaceutical Preparations

Keywords

  • Cardiac-sparing
  • Cholesterol
  • GC-1
  • Thyroid hormone
  • Thyromimetic

ASJC Scopus subject areas

  • Cardiology and Cardiovascular Medicine

Cite this

Sobetirome : A case history of bench-to-clinic drug discovery and development. / Scanlan, Thomas (Tom).

In: Heart Failure Reviews, Vol. 15, No. 2, 03.2010, p. 177-182.

Research output: Contribution to journalArticle

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