Researchers from Birla Institute of Technology & Science, Pilani and Jadavpur University have reported novel HDAC3 inhibitors as potential candidates for the treatment of breast cancer. Synthesis and optimization of a series of pyrazino-hydrazide-based HDAC3 inhibitors led to the characterization of compound [I] as the lead candidate with potent HDAC3 inhibitory activity (IC50=14 nM) and at least 121-fold selectivity.
Cyclin-dependent kinase 7 (CDK7) regulates both cell cycle and global transcription and is a validated therapeutic target in cancer. Researchers from Shanghai Hengrui Pharmaceutical Co. Ltd. reported on the discovery and preclinical evaluation of SHR-5428, a noncovalent CDK7 inhibitor.
U3-1402/patritumab-GGFG-DXd is the first HER3-targeting antibody-drug conjugate (ADC) showing clinical efficacy in non-small-cell lung cancer. However, an elevated proportion of patients with this cancer express low levels of HER3 and are nonresponsive to this ADC. In addition, novel ADCs are needed to treat other cancer types, including colorectal cancer.
Satyarx Pharma Innovations Pvt Ltd. has disclosed novel bicyclic compounds acting as DNA repair protein RAD51 homolog 1 inhibitors reported to be useful for the treatment of cancer.
A fluorescent imaging agent developed by Vergent Bioscience Inc. enables visualization of elusive and previously undetected tumors, a phase II study presented last week at the 2023 World Conference on Lung Cancer (WCL23) demonstrated. The ability of the tumor-targeting agent, Vgt-309, to illuminate tumors could help surgeons more precisely locate tumors, better ensure clean margins and guide care decisions. In 10% of cases, the agent revealed unknown tumors in lymph nodes, which could affect which nodes are biopsied as well as when or whether a systemic therapy is recommended.
Cancer Research Technology Ltd. has disclosed proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase binding moiety covalently bonded to a mitogen-activated protein kinase 7 (MAPK7; ERK5)-targeting moiety through a linker. They are reported to be useful for the treatment of cancer.
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.
Ibex Medical Analytics Ltd. closed a $55 million series C financing round that will allow the company to expand its footprint in the U.S. to meet the increasing demand for artificial intelligence (AI)-powered diagnostic solutions. Ibex has developed the Galen platform which offers AI solutions that allow pathologists to accurately and rapidly detect and diagnose cancer. The company also reported the launch of Galen Breast HER2, a new software which will play a critical role in helping oncologists identify effective therapies for breast cancer patients.
Enliven Therapeutics Inc. has synthesized HER2 (erbB2) inhibitors, including Exon 20 insertion (Ex20Ins) mutant inhibitors, reported to be useful for the treatment of cancer.
