avatrombopag is an approved drug (FDA (2018), EMA (2019))
Compound class:
Synthetic organic
Comment: Avatrombopag is a second generation, small molecule, orally administered thrombopoietin receptor agonist [1]. It was discovered through its ability to mimic the action of endogenous thrombopoietin which is the primary physiological regulator of normal platelet production. The pharmacokinetics, pharmacodynamics, pharmacogenomics, safety, and tolerability of avatrombopag were reported by Nomoto et al. in 2017 [2].
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Bioactivity Comments |
Avatrombopag dose-dependently promotes the proliferative activity of human thrombopoietin receptor‐expressing Ba/F3 cells. The EC50 for this action is 3.3 nM [1]. The maximum proliferative capacity of avatrombopag was equivalent to that of recombinant human thrombopoietin. |
Selectivity at catalytic receptors | ||||||||||||||||||||||||||||||||||
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