Researchers from Cogent Biosciences Inc. have reported the discovery and preclinical characterization of CGT-4255, a novel EGFR-sparing, ErbB2 inhibitor with activity against oncogenic ErbB2 mutations.
It is known that CD19-directed CAR T-cell therapy is useful in the treatment of large B-cell lymphoma, but about 60% of patients relapse after treatment, and about 30% of these are CD19-negative patients with poor survival. Sana Biotechnology Inc. is developing a hypoimmune CD22-directed CAR T-cell therapy, named SC-262, for the potential treatment of large B-cell lymphoma.
Phosphoinositide 3-kinase (PI3K) is a key cell cycle pathway regulator involved in tumor growth and development. PI3Kα mutations in p110α subunit, H1047R and E542K/E545K are found in patients with several cancer types, including breast cancer and are targeted by approved drugs such as Piqray (alpelisib, Novartis AG).
Researchers from Insilico Medicine Inc. reported on ISM-5043, a novel KAT6A inhibitor aimed to be used for the treatment of refractory ER+ breast cancer.
Researchers from Engrail Therapeutics Inc. presented preclinical data for the novel D2/3 receptor antagonist ENX-104, being developed for the treatment of depression.
The KCNC1 gene encodes the voltage-gated potassium channel subunit KV3.1, and variants in this gene have been previously linked to developmental and epileptic encephalopathy (DEE).
A sustained antiplatelet effect plus target selectivity are the two major requirements for developing new antithrombotic therapies. Increasing the levels of cAMP in the platelets by the action of a prostacyclin receptor (PTGIR) agonist is a possible approach for this purpose. Researchers from the University of Michigan have presented preclinical data on their PTGIR agonist CS-585, which has shown higher blood stability, as a potential therapeutic for thrombosis.
Isozymes that are overexpressed in cancer and key in some metabolic processes are potential therapeutic targets. Previous studies found that phosphoenolpyruvate carboxykinase 2 (PCK2) is required by cancer cells for maintaining high metabolic activity and proliferation in some cancer types, but no small-molecule PCK2 inhibitors currently exist.
Previous studies with mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) inhibitors have demonstrated their potential as antitumor agents across several tumor models when administered alone or in combination with standard treatments.
Researchers from Weill Cornell Medicine and Scenic Biotech BV presented promising preclinical data on SC-2882, a first-in-class specific glutaminyl-peptide cyclotransferase-like (QPCTL) inhibitor that induces secondary proteolytic degradation of the monocyte chemo attractants CCL2 and CCL7 and inactivation of the “don’t-eat-me” signal CD47, as a novel therapeutic for diffuse large B-cell lymphoma (DLBCL).
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