Discover and read the best of Twitter Threads about #tarloxotinib

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#ESMO20 Happy to share the first results of RAIN-701, a phase II study of #tarloxotinib in patients with NSCLC harboring an #EGFR exon 20 insertion or an activating #HER2 mutation and any solid tumor with an #NRG1 or ERBB gene fusion. #LCSM @OncoAlert
#ESMO20 Tarlox is given as an inactive prodrug that embeds in the cell membrane. Only when it encounters hypoxia does it undergo single electron reduction to fragment to a cell permeable, pan-HER, irreversible TKI with subnanomolar potency at EGFR, HER2 and HER4. @OncoAlert #LCSM
#ESMO20 Top right shows the IC50 of Tarloxotinib-E in human cell lines, bottom right corroborate with additional mutations in BAF3 models. Note the differential target inhibition for Tarlox-E with a lower IC50 for #HER2 than EGFR and the lowest IC50 for #NRG1 fusions. #LCSM
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