Abstract 1185: H3B-8800, a novel orally available SF3b modulator, shows preclinical efficacy across spliceosome mutant cancers
Sign Up to like & getrecommendations! Published in 2017 at "Cancer Research"
DOI: 10.1158/1538-7445.am2017-1185
Abstract: Genomic characterization of hematologic and solid cancers has revealed recurrent somatic mutations affecting genes encoding the RNA splicing factors SF3B1, U2AF1, SRSF2 and ZRSR2. Recent data reveal that these mutations confer an alteration of function… read more here.
Keywords: novel orally; h3b; h3b 8800; spliceosome mutant ... See more keywords
Abstract PS12-23: Development of H3B-6545, a first-in-class oral selective ER covalent antagonist (SERCA), for the treatment of ERaWTand ERaMUTbreast cancer
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DOI: 10.1158/1538-7445.sabcs20-ps12-23
Abstract: Mutations in the ligand-binding domain of estrogen receptor alpha (ERα) are detected in up to 30% of patients (pts) who have relapsed or progressed during endocrine therapy. By favoring the agonistic conformation in ERα, these… read more here.
Keywords: 6545 first; activity; cancer; h3b 6545 ... See more keywords
Phase I dose escalation of H3B-6545, a first-in-class highly Selective ERα Covalent Antagonist (SERCA), in women with ER-positive, HER2-negative breast cancer (HR+ BC).
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2019.37.15_suppl.1059
Abstract: 1059 Background: H3B-6545 inactivates both wild-type and mutant ERα by targeting cysteine 530 and enforcing a unique antagonist conformation. Methods: Women with locally advanced or metastatic HR+ BC are treated (tx) with H3B-6545 administered once… read more here.
Keywords: therapy; dose escalation; h3b 6545; h3b ... See more keywords