Researchers from Bridgebio Pharma Inc. recently presented BBO-10203, a first-in-class, orally bioavailable, covalent small-molecule candidate designed to inhibit RAS-driven PI3Kα activity without affecting glucose metabolism.
Haisco Pharmaceutical Group Co. Ltd. has synthesized poly(ADP-ribose) polymerase 1 (PARP-1; ARTD1) inhibitors reported to be useful for the treatment of cancer.
Researchers from Blueprint Medicines Corp. presented data from a study that aimed to assess the effects of combining cyclin-dependent kinase 2 (CDK2) inhibitor BLU-222 with CDK4/6 inhibitors, such as palbociclib or ribociclib, to overcome CDK4/6 inhibitor resistance in HR-positive/HER2-negative breast cancer.
Synnovation Therapeutics Inc. has synthesized phosphatidylinositol 3-kinase α (PI3Kα) inhibitors reported to be useful for the treatment of cancer, congenital lipomatous overgrowth, vascular malformations, epidermal naevi and skeletal abnormalities and PIK3CA-related overgrowth spectrum (PROS).
Phosphoinositide 3-kinase (PI3K) is a key cell cycle pathway regulator involved in tumor growth and development. PI3Kα mutations in p110α subunit, H1047R and E542K/E545K are found in patients with several cancer types, including breast cancer and are targeted by approved drugs such as Piqray (alpelisib, Novartis AG).
Researchers from Insilico Medicine Inc. reported on ISM-5043, a novel KAT6A inhibitor aimed to be used for the treatment of refractory ER+ breast cancer.
Isozymes that are overexpressed in cancer and key in some metabolic processes are potential therapeutic targets. Previous studies found that phosphoenolpyruvate carboxykinase 2 (PCK2) is required by cancer cells for maintaining high metabolic activity and proliferation in some cancer types, but no small-molecule PCK2 inhibitors currently exist.
South Korean artificial intelligence software developer Lunit Inc. plans to acquire Volpara Health Technologies Ltd. for $193 million (AUD 292 million) by mid-2024, taking a global leap to the U.S. market and becoming an AI-based platform health care firm.
The inhibition of cyclin-dependent kinase 4 (CDK4) and CDK6 is a useful strategy to treat hormone receptor (HR)+/HER2+ breast cancer, but patients may develop resistance through different mechanisms. As reported at the recent San Antonio Breast Cancer Symposium, researchers from Biotheryx Inc. have synthesized a new CDK4/6 degrader – BTX-9341 – to address the problem of therapeutic resistance in breast cancer.
