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.
Simcere Zaiming Pharmaceutical Co. Ltd. has synthesized antibody-drug conjugates (ADC) comprising humanized monoclonal antibodies targeting CDH6 covalently linked to a camptothecin analogue through a linker.
Breast cancer patients receiving aromatase inhibitors as antihormone therapy are at major risk of cardiovascular disease. Previous observations suggest that, since estrogen biosynthesis is regulated by aromatase and aldosterone biosynthesis is modulated by aldosterone synthase, a dual inhibitor could have anticancer efficacy while reducing cardiovascular risks in breast cancer patients.
Injecting a combination of cisplatin and vinblastine – engineered by way of the company’s Dfuserx platform – turned out to be just the ticket for early stage breast cancer in the phase II study called Invincible conducted by Intensity Therapeutics Inc. Shares of the Shelton, Conn.-based firm (NASDAQ:INTS) closed Dec. 8 at $6.88, up $2.68, or 63%, having traded as high as $11.44, thanks to Wall Street’s satisfaction with the data testing INT230-6, which emerged during the San Antonio Breast Cancer Symposium.
While early stage and involving a relatively small patient population, the interim phase Ib readout from the combination cohort testing estrogen receptor (ER)-targeting candidate vepdegestrant in combination with CDK4/6 inhibitor Ibrance (palbociclib) in heavily pretreated patients with ER-positive/HER2-negative breast cancer was impressive enough to prompt partners Arvinas Inc. and Pfizer Inc. to expand development work on the program. The results also struck a chord on the Street, with shares of Arvinas (NASDAQ:ARVN) gaining 31% on the day.
