Bicycle radionuclide conjugates (BRCs) have been developed as a unique radiotheranostic modality for imaging and targeting of proteins overexpressed by tumors, and they possess favorable drug-like properties allowing for effective delivery of radioisotopes. Researchers from Bicycletx Ltd. recently presented a new BRC that targets ephrin type-A receptor 2 (EphA2), named BCY-18469.
Carbonic anhydrase IX (CAIX) is a transmembrane protein involved in cell proliferation and transformation that is expressed in clear-cell renal cell carcinoma (ccRCC), colorectal cancer (CRC), and other hypoxic tumor types, but has low expression in healthy tissues.
Lipids are “very diverse, but also vastly understudied,” Anne Brunet told the audience at the recent meeting on Aging Research and Drug Discovery. Advances in the ability to predict protein structures have fueled a much better understanding of the human proteome and its estimated 20,000 members. The lipidome is much larger, numbering maybe 100,000 total. And what those lipids do remains much more fuzzy. “Very little is known about their function, and especially their function during aging,” Brunet said. Slowly, however, technological advances are enabling researchers to understand the roles of lipids as well.
Pancreatic ductal adenocarcinoma (PDAC) is an exocrine pancreatic cancer with a poor prognosis and limited treatment options. There is a strong demand for new treatment strategies to overcome these challenges.
At the recent ERS meeting, researchers from Hilung Inc. and Ube Corp. presented preclinical data for the novel lysophospholipid LPA1 receptor antagonist, HL-001, being developed for the treatment of idiopathic pulmonary fibrosis (IPF).
Senescence of lung epithelial tissue translates into fibrinolysis reduction and loss of tissue repair, both drivers of pulmonary fibrotic diseases. Researchers from Tokushima University reported on the effect of ARV-825, a BRD4 degrader, as an antifibrotic agent in lung fibrosis.
It has been previously demonstrated that glypican-3 (GPC3) is differentially expressed in hepatocellular carcinomas (HCC), making it a promising target for radiopharmaceutical therapy to treat HCC. At the ongoing meeting of the European Association of Nuclear Medicine in Vienna, researchers from Rayzebio Inc. and Peptidream Inc. presented the preclinical characterization of a novel proprietary peptide binder of GPC3, RAYZ-8009.
Osimertinib is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor with documented efficacy in non-small-cell lung cancer. However, in most cases, patients develop resistance to this treatment by mechanisms that are not clear in half of the cases. Researchers from Shanghai Pulmonary Hospital presented data on BC-3448, a bispecific antibody targeting EGFR and CD3 aimed to recruit T cells to tumors with high EGFR expression leading to T cell-driven tumor cell killing. The compound presents a stronger binding affinity for EGFR than for CD3 to avoid the development of cytokine release syndrome, which is a safety issue common in CD3-based bispecific antibodies.
Researchers from Beijing Inno Medicine Co. Ltd. recently reported preclinical data for the novel liposome encapsulated rosuvastatin calcium candidate, YN-001, being developed for the treatment of atherosclerosis.
Conjugated oligoelectrolytes (COEs) have recently emerged as potential broad-spectrum antibiotics with promising selectivity that is irrespective of metabolic state, including dormant and biofilm-associated bacteria. Researchers from National University of Singapore, University of California Santa Barbara, and Walter Reed Army Institute of Research have sought to identify novel cationic antimicrobial COE candidates.