Data from preclinical studies conducted to evaluate the activity of NKT-3964, a first-in-class, orally bioavailable CDK2-selective PROTAC degrader being developed for the potential treatment of cancer, were reported by Nikang Therapeutics Inc.
Two days after Monte Rosa Therapeutics Inc. signed a molecular glue degrader deal with Novartis AG, two other companies, Biogen Inc. and Neomorph Inc., are moving forward in the same space in a partnership worth up to $1.45 billion. Cambridge, Mass.-based Biogen and San Diego-based Neomorph will develop molecular glue degraders (MGDs) for priority targets in Alzheimer’s, rare neurological and immunological diseases, using Neomorph’s MGD platform to identify and validate novel small-molecule protein degraders.
Shanghai Helioson Pharmaceutical Co. Ltd. has identified molecular glue degraders acting as DNA-binding protein Ikaros (IKZF1) and/or zinc finger protein Aiolos (IKZF3) degradation inducers reported to be useful for the treatment of cancer, autoimmune disease and inflammatory disorders.
In research conducted at West China Hospital of Sichuan University and Chengdu University of Traditional Chinese Medicine, coupling of the pan-FGFR inhibitor erdafitinib with a CRBN binder led to a new series of fibroblast growth factor receptor (FGFR) degraders, with compound [I] identified as the lead candidate.
Cyclin-dependent kinases 12 and 13 (CDK12 and CDK13) are involved in the regulation of transcription elongation, DNA damage response and genomic stability balance. A few inhibitors of CDK12- and CDK13-mediated transcription have shown antiproliferative effects in the preclinical setting but have not progressed to clinical testing due to excessive toxicity.
Recursion Pharmaceuticals Inc. has gained IND clearance from the FDA for a phase I/II trial of REC-1245 in a biomarker-enriched patient population, including patients with solid tumors and lymphoma. The trial is expected to begin in the fourth quarter of this year.
B-cell lymphoma 6 (BCL6) is an essential transcriptional factor for the humoral immune response. However, genomic deregulation of BCL6 contributes to the development of different types of lymphoma such as diffuse large B-cell lymphoma (DLBCL).
A paper from Shenzhen University and affiliated organizations covers the discovery of a novel bromodomain-containing protein 4 (BRD4)-specific proteolysis-targeting chimera (PROTAC).
The University of Michigan has published details on the discovery and preclinical characterization of a new potent and selective proteolysis targeting chimera (PROTAC) degrader of BRD9, CW-3308. Synthesis and optimization of two different cereblon ligands led to the discovery of a novel series of highly potent BRD9 degraders, with CW-3308 selected as the lead candidate.
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