The advent of antibody-drug conjugates (ADCs) changed targeted cancer therapy by enabling the delivery of cytotoxic agents to cancer cells. Topoisomerase I inhibitors are commonly used as payloads in TROP2-directed ADCs, but they are linked to toxicity and emerging resistance. Degrader-antibody conjugates (DACs) go beyond conventional cytotoxic payloads by combining antigen targeting and selective protein degradation.
Jiangsu Hengrui Pharmaceuticals Co. Ltd. and Shanghai Hengrui Pharmaceutical Co. Ltd. have identified new BCL6 degradation inducers potentially useful for the treatment of autoimmune disease and cancer.
Shanghai Helioson Pharmaceutical Co. Ltd. has patented molecular glue degraders comprising cereblon (CRBN) binding agents acting as proto-oncogene Vav (VAV1) degradation inducers found to be potentially useful for the treatment of autoimmune disease and cancer.
Researchers from Zhejiang University of Technology and collaborators presented the discovery and preclinical characterization of YSA-64, a novel RBM39 degrader, in cancer models.
Kymera Therapeutics has developed KT-579, a potent and selective IRF5 degrader as a novel approach for treating systemic lupus erythematosus (SLE) and Sjögren disease.
Amphista Therapeutics Ltd. has obtained IND clearance from the FDA for AMX-883, an orally bioavailable degrader of BRD9, for the treatment of acute myeloid leukemia (AML). A phase I trial in patients with relapsed or refractory AML and high-risk myelodysplastic syndrome is expected to begin in the second half of this year.
Researchers from Jiangsu Hengrui Pharmaceuticals Co. Ltd. and Shanghai Hengrui Pharmaceutical Co. Ltd. have reported molecular glue degraders acting as proto-oncogene Vav (VAV1) degradation inducers found to be potentially useful for the treatment of cancer, inflammatory disorders and autoimmune diseases.
Synnovation Therapeutics Inc. has discovered new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin-protein ligases binding moiety coupled to nuclear factor erythroid 2-related factor 2 (NFE2L2; NRF2)-targeting moiety potentially useful for the treatment of cancer.
Treeline Biosciences Inc. has patented new tetrahydroisoquinoline heterobifunctional proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to a Bcl-2-like protein 1 (Bcl-xl; Bcl-X; BCL2L1)-targeting moiety potentially useful for the treatment of cancer.
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