Shenogen Pharma Group Ltd. has identified proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN)-binding moiety coupled to an estrogen receptor α (ER-α; ESR1)-targeting moiety through a linker reported to be useful for the treatment of cancer, infections, immunological disorders, diabetes, inflammatory and cardiovascular disorders.
Daiichi Sankyo Co. Ltd.’s trophoblast cell surface antigen 2 (Trop2)-directed antibody-drug conjugate (ADC), datopotamab deruxtecan (dato-dxd), has been approved in Japan for treating adults with hormone receptor (HR)-positive, HER2-negative unresectable or recurrent breast cancer after prior chemotherapy.
Radiopharm Theranostics Ltd. has been granted Belberry Human Research Ethics Committee (HREC) approval in Australia to initiate a first-in-human phase I therapeutic study of 177Lu-labeled RAD-202 (177Lu-RAD-202) for the treatment of HER2-expressing solid tumors, including breast and gastric cancers.
Beigene Co. Ltd. has presented data on a CDK4 selective inhibitor, BGB-43395, for the potential treatment of this cancer type and which would reduce the neutropenia associated with CDK6 inhibition.
In tumoral cells, the modulation of the G1/S phases of cell cycle is destabilized by amplification and high expression of cyclin E (CCNE) or by mutation or loss of retinoblastoma 1 (RB1) gene. Cancer cells meeting these characteristics have been sown to be highly sensitive to cyclin-dependent kinase 2 (CDK2) depletion.
Ideaya Biosciences Inc. has nominated IDE-251, a dual KAT6/7 inhibitor targeting 8p11 amplification tumors in breast and lung cancers, as a development candidate. IDE-251 is an equipotent, highly selective, small-molecule dual inhibitor of KAT6 and -7, both of which have been shown to support cancer cell survival.
