Eltrombopag | Small molecule thrombopoietin agonist

Eltrombopag (496775-61-2) is a novel, orally active, small molecule human thrombopoietin receptor (TPO-R) agonist, EC₅₀=0.27 μM.^1,2 Maintains human hematopoietic stem and progenitor cells under inflammatory conditions.³ Promotes DNA repair in human hematopoietic stem and progenitor cells.⁴ Acts as a powerful chelator of cellular and extracellular iron(III).⁵ Stimulates hematopoietic stem cells via a TPO-R-independent mechanism involving iron chelation.⁶

References/Citations
1) Xie et al. (2018), Pharmacological characterization of hetrombopag, a novel orally active human thrombopoietin receptor agonist; J. Cell. Mol. Med., 22 5367
2) Erickson-Miller et al. (2008), Preclinical activity of eltrombopag (SB-497115), an oral, nonpeptide thrombopoietin receptor agonist; Stem Cells, 27 424
3) Alvarado et al. (2019), Eltrombopag maintains human hematopoietic stem and progenitor cells under inflammatory conditions mediated by IFN-γ; Blood, 133 2043
4) Guenther et al. (2019), Eltrombopag promotes DNA repair in human hematopoietic stem and progenitor cells; Exp. Hematol. 73 1
5) Vlachodimitropoulou et al. (2017), Eltrombopag: a powerful chelator of cellular or extracellular iron (II) alone or combined with a second chelator; Blood, 130 1923
6) Kao et al. (2018), Thrombopoietin receptor-independent stimulation of hematopoietic stem cells by eltrombopag; Science Transl. Med., 10 eaas9563