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Association details:
Evidence:
Evidence Level:
Sensitive: D – Preclinical
Title:

STX-478, a Mutant-Selective, Allosteric PI3Ka Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Ka-Mutant Xenografts

Published date:
08/25/2023
Excerpt:
Here we describe STX-478, an allosteric PI3Ka inhibitor that selectively targets prevalent PI3Ka helical- and kinase-domain mutant tumors. STX-478 demonstrated robust efficacy in human tumor xenografts without causing the metabolic dysfunction observed with alpelisib. Combining STX-478 with fulvestrant and/or cyclin-dependent kinase 4/6 inhibitors was well tolerated and provided robust and durable tumor regression in ER+HER2- xenograft tumor models.
Secondary therapy:
fulvestrant
DOI:
https://doi.org/10.1158/2159-8290.CD-23-0396