As a drug candidate of thrombocytopenia, Lusutrombopag (S-888711) is in Phase III clinical trial stage right now. It is been proven that Lusutrombopag (S-888711) is excellent property in safety and efficacy by clinical trials. In this meeting, we will present in detail about the history of drug discovery of Lusutrombopag.Because Lusutrombopag (S-888711) acts specifically to human TPO receptor, we prepared TPOR-Ki/Shi mice expressing a mouse-human chimeric TPOR for evaluating the efficacy. This TPOR-Ki/Shi mice worked very well as an evaluation model of drug efficacy, so we were able to select Lusutrombopag from many candidate compounds. In this meeting, we will present the results of the efficacy in TPOR-Ki/Shi mice of Lusutrombopag and the similar drug (Eltrombopag).

Discovery and biological evaluation of Lusutrombopag (S-888711) as a novel nonpeptide drug candidate for thrombocytopenia

247th National Meeting (2014)

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