Mutations in the PIK3CA gene are present in about 4% to 36% of cancers such as breast, ovarian, endometrial and colorectal cancer, among others.

Changchun Genescience Pharmaceuticals Co. Ltd. has reported GSC-000829, a novel and selective FGFR2/FGFR3 inhibitor being developed for the potential treatment of cancer.

Targeted protein degradation has gained attention in recent years due to its potential to hit proteins that are difficult to engage with conventional small molecules. Pin1 is an enzyme associated with tumor formation overexpressed in pancreatic cancer cells or cancer-associated fibroblasts in particular.

MBT-C101 is a selective, potentially first-in-class potent HSP90 chaperone-mediated degrader of PI3Kα, for the treatment of breast cancer. It was developed by Magicbullet Therapeutics Inc. using the company’s Chaperone-mediated Degrader (CM-Degrader) platform.

NTS-071 is a novel orally bioavailable p53 Y220C reactivator recently discovered and characterized by Nutshell Therapeutics Inc.

Activin receptor-like kinase 5 (ALK5) is a member of the transforming growth factor-β (TGF-β) family associated with tumor development and progression that impacts cancer immune response within the tumor microenvironment.

Nimbus Therapeutics LLC reported the identification of an allosteric, potent, selective, highly efficacious and noncovalent Werner syndrome helicase (WRN) inhibitor, NTX-452, for the potential treatment of microsatellite instability high (MSI-H) tumors.

Nodus Oncology Ltd. presented the discovery of NODX-010, a potent poly(ADP-ribose) glycohydrolase (PARG) inhibitor being developed for the potential treatment of cancer, including tumors resistant to PARP inhibitors.