FGFR3 genomic alterations, including S249C as the most common, are recognized oncogenic drivers in 10%-60% of bladder cancers depending on the disease stage. Onco3r Therapeutics BV recently reported the identification of a novel series of highly potent, isoform-selective small-molecule FGFR3 inhibitors.
Researchers from Eilean Therapeutics LLC and collaborators presented the discovery and characterization of a new, selective CDK2 inhibitor showing potent in vitro and in vivo activity at the 2025 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics.
At the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, researchers from Onco3r Therapeutics BV presented a novel series of selective SMARCA2 small-molecule inhibitors with a best-in-class potency and selectivity profile.
Although tricomplex pan-RAS (ON) inhibitors, such as RMC-6236, constitute a promising class of therapeutics against RAS-driven cancers, their on-target, off-tumor toxicities challenge the dosing strategy and the safety of drug combinations.
Inactivation of the tumor suppressor p53 occurs in approximately half of human cancer cases. In particular, the Y220C point mutation, which induces p53 misfolding and inactivation, is found in about 1% of solid tumors. Previous research identified a unique, druggable pocket on the p53 surface created by this mutation that constitutes a promising cancer therapeutic target.
Type I protein arginine methyltransferases (PRMTs) are an attractive target for inhibiting growth of triple-negative breast cancer. Several small-molecule inhibitors of these enzymes are in various stages of preclinical development, while clinical trials of the inhibitor GSK-3368715 had to be terminated early because of poor efficacy and toxicity.
Researchers from Prospect Therapeutics Inc. have discovered PSTA-5204, a novel oral KRAS G12D(ON) inhibitor that exhibits potent in vitro activity, strong in vivo efficacy and high selectivity over wild-type KRAS.
Aurigene Oncology Ltd. recently provided details on the discovery and preclinical characterization of AUR-243, a novel CBL-B inhibitor with a distinct therapeutic profile and best-in-class potential compared to other inhibitors. AUR-243 was described as a structurally distinct, oral small molecule demonstrating excellent potency, functional activity and superior efficacy.
Researchers at Triana Biomedicines Inc. presented the preclinical characterization of TRI-611, a CNS-penetrant molecular glue degrader targeting ALK in models of ALK fusion-positive non-small-cell lung cancer.
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