Full-Life Technologies Ltd. has received IND clearance by the FDA, allowing it to conduct clinical trials of 225Ac-FL-020, its PSMA-targeted radiopharmaceutical for the treatment of metastatic castration-resistant prostate cancer.
E1A binding protein (EP300) and CREB binding protein (CBP) are two closely related histone acetyltransferases (HATs), the mutations in which are related to several cancers. In the current study, researchers from Daiichi Sankyo Co. Ltd. aimed to develop orally available small molecule EP300/CBP HAT inhibitors with antitumor activity.
Eikon Therapeutics Inc. has received IND clearance from the FDA to initiate phase I studies with IMP-1734, a highly selective poly(ADP-ribose) polymerase 1 (PARP-1) inhibitor developed in partnership with Impact Therapeutics Inc.
Researchers from the University of Texas System presented preclinical data for MC-1-F2, a direct small molecule inhibitor of forkhead box protein C2 (FOXC2). The candidate has previously shown activity in breast cancer cell lines, and the current study aimed to assess its efficacy in castration-resistant prostate cancer (CRPC).
The Shanghai Institute of Materia Medica of the Chinese Academy of Sciences has described androgen receptor antagonists and/or androgen receptor degradation inducers reported to be useful for the treatment of gastrointestinal disorders, osteoporosis and SARS-CoV-2 infection (COVID-19), as well as breast and castration-resistant prostate cancer.
Researchers from Peking University (PKU) recently presented the discovery and preclinical evaluation of a novel small-molecule inhibitor of pan-αv integrin, C19-9-21, being developed for the treatment of prostate cancer.
Researchers from Arvinas Inc. and affiliated organizations presented the discovery and preclinical evaluation of ARV-766, a novel androgen receptor (AR) degrading proteolysis targeting chimera (PROTAC), being developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC).
As prostate cancer progresses, tumors lose the androgen receptor (AR) on which initial treatment is based. Oftentimes, such patients also lose expression prostate-specific membrane antigen (PSMA), which is the target of approved agent Pluvicto (lutetium (177Lu) vipivotide tetraxetan; Novartis AG) as well as a number of experimental drugs. Such patients can no longer benefit from either androgen- or PSMA-directed therapy.
New understanding of how prostate cancer adapts to the stress of androgen receptor targeted drugs and becomes castrate-resistant, points to a lesser-studied family of lipid kinases as playing a pivotal role in this process. The findings indicate that specific inhibition of one isoform of these phosphatidylinositol-5-phosphate-4-kinases (PI5P4K) could provide a route to prevent cancer cells altering their metabolism and becoming resistant to androgen deprivation.
