Researchers from Totus Medicines Inc. presented preclinical data for the potent and selective covalent inhibitor of phosphoinositide 3-kinase α (PI3Kα), TOS-358, which is being developed for the treatment of cancer.
Researchers from Black Diamond Therapeutics Inc. presented the discovery and preclinical characterization of a novel brain-penetrant BRAF class I/II/III mutation inhibitor, BDTX-4933.
Researchers from Aligos Therapeutics Inc. have described the discovery of novel liver-targeted oral PD-L1 small-molecule inhibitors for the treatment of chronic hepatitis B and liver cancers.
CD39 has an essential role in converting extracellular adenosine triphosphate (ATP; pro-inflammatory) into adenosine monophosphate (AMP; anti-inflammatory). Preventing the action of CD39 in the tumor microenvironment would increase levels of ATP, causing myeloid cell activation and improvement of tumor control.
Investigators working at University of Texas Health Science Center, Houston, have discovered that the ubiquitin ligase UBR2 is up-regulated and sufficient for targeting the myosin heavy chain protein for the degradation characteristic of cancer cachexia. UBR2 knockout or pharmacological inhibition could prevent cachexia in mice. Confirmatory observations were noted in cancer cachexia patient-derived tissues.
Immutep Ltd.’s lead immunotherapy candidate eftilagimod (IMP-321, efti) met the primary endpoint in its phase II trial evaluating the combination of efti and Merck & Co. Inc.’s Keytruda (pembrolizumab) as first-line treatment of non-small-cell lung cancer (NSCLC), reporting final data that show an overall response rate of 40.4%.
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