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DRUG:

DS-2087b

i
Other names: DS-2087b, DS 2087b, DS2087b
Associations
Trials
Company:
Daiichi Sankyo
Drug class:
HER2 exon 20 mutation inhibitor
Associations
Trials
2ms
Evaluation of interspecies differences in DS-2087b-induced gastrointestinal toxicity using mouse and monkey intestinal organoids. (PubMed, Toxicol Lett)
In the transcriptomic analysis, expression of stem- and Paneth-cell marker genes was markedly decreased in the monkey small intestinal organoids. In conclusion, the intestinal organoids are valuable in vivo-in vitro translation of drug-induced GI toxicity and the changes in specific cell-type composition induced by DS-2087b may be important factors for contributing the interspecies differences.
Preclinical • Journal
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HER-2 (Human epidermal growth factor receptor 2)
|
DS-2087b
over5years
[VIRTUAL] Preclinical evaluation of DS-2087b, a novel and selective inhibitor of EGFR/HER2 exon 20 insertions (ESMO 2020)
Methods We evaluated the inhibitory effects of DS-2087b and poziotinib, an investigational tyrosine kinase inhibitor against Ba/F3 cells harboring WT EGFR and against EGFR/HER2 ex20ins mutations, including EGFR V769_D770 insertion ASV (EGFR ins.ASV); EGFR D770_N771 insertion SVD (EGFR ins.SVD); and HER2 A775_G776 insertion YVMA (HER2 ins.YVMA). Legal entity responsible for the study: Yuki Abe. Funding: Daiichi Sankyo Company, Limited.
Preclinical
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EGFR (Epidermal growth factor receptor)
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HER-2 mutation • EGFR exon 20 insertion • HER-2 exon 20 insertion • EGFR exon 20 mutation • HER-2 A775
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Pozenveo (poziotinib) • DS-2087b