Synonyms: Mulpleta® | S-888711 | S888711
lusutrombopag is an approved drug (Japan (2015), FDA (2018), EMA (2019))
Compound class:
Synthetic organic
Comment: Lusutrombopag is an orally bioavailable, nonpeptidyl, small molecule thrombopoietin (TPO) receptor agonist [3] that was developed by Shionogi in Japan. It was the second TPO receptor agonist to receive FDA approval in 2018 (avatrombopag was the first).
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Bioactivity Comments |
Lusutrombopag is selective for the human TPO receptor, and does not activate the mouse TPO receptor [3]. It promotes proliferation of Ba/F3-hMpl cells with an EC50 of 84 nM via activation of the same signal transduction pathways as native human TPO. Incubation of HuBM-CD34-positive cells with lusutrombopag for 12 days in vitro promotes megakaryocytic colony formation, which is indicative of enhanced platelet formation. |
Selectivity at catalytic receptors | ||||||||||||||||||||||||||||||||||
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