Researchers from Scorpion Therapeutics Inc. presented the discovery and preclinical evaluation of a novel mutant-selective, allosteric phosphoinositide 3-kinase α (PI3Kα) inhibitor, STX-478. In vitro, STX-478 showed mutant selectivity, as it selectively inhibited the viability of cell lines with mutations in the PIK3CA kinase domain and helical domain.
Trastuzumab deruxtecan (DS-8201a) is an antibody-drug conjugate used for the treatment of metastatic HER2+ breast cancer that is refractory to anti-HER2 therapy such as T-DM1, however, there is a lack of knowledge on acquired or innate resistance to the drug.
Researchers from Kbluebio Inc. and affiliated organizations recently reported the discovery and preclinical evaluation of a novel prohibitin-2 (PHB2) ligand as a potential candidate for the treatment of multiple myeloma (MM).
Approximately 20,000 patients diagnosed with non-Hodgkin lymphomas died in 2022 despite current treatments; 30-40% of these cases involved diffuse large B-cell lymphoma (DLBCL). Monoallelic mutations in histone acetyltransferases (HATs) occur in over 39% of germinal center DLBCLs. Activation of intact wild-type alleles offers an opportunity to overcome the mutated allele.
Cyclin-dependent kinase 4 (CDK4) and CDK6 inhibitors, in combination with letrozole or fulvestrant, have been approved for treating hormone receptor-positive breast cancer. Even though the therapy shows benefits in some patients, resistance develops in other treated patients.
Triple-negative breast cancer (TNBC) has a diverse etiology, with high unmet clinical needs. Researchers from Tavotek Biotherapeutics (Hong Kong) Ltd. presented data on TAVO-412, a trispecific EGFR/cMET/VEGF (2:1:1 binding arm ratio) antibody for the potential treatment of TNBC.
Researchers from Hangzhou Healzen Therapeutics Co. Ltd. and Biopolar Hongye (Nantong) Pharmaceutical Co. Ltd. presented the discovery and preclinical characterization of a next-generation Bcl-2 inhibitor, HZ-L105, being developed for the treatment of hematological cancers.
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