Paper Abstract: Continuous Abemaciclib Treatment Leads to Breast Cancer Inhibition

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July 8, 2022

Oncotarget published this trending research paper on July 2, 2022 in Volume 13, entitled, "Continuous treatment with abemaciclib leads to sustained and efficient inhibition of breast cancer cell proliferation" by researchers from Discovery Chemistry Research and Technology, Eli Lilly and Company, Madrid, Spain; Eli Lilly and Company, Indianapolis, IN; Eli Lilly and Company, New York, NY. DOI - https://doi.org/10.18632/oncotarget.28249 Correspondence to - María José Lallena - lallena_maria_jose@lilly.com Abstract Abemaciclib is an oral, selective cyclin-dependent kinase 4 & 6 inhibitor (CDK4 & 6i), approved for hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2–) advanced breast cancer (ABC) as monotherapy for endocrine refractory disease, and with endocrine therapy (ET) for initial treatment and after progression on ET. Abemaciclib has also shown clinical activity in combination with ET in patients with high risk early BC (EBC). Here, we examined the preclinical attributes of abemaciclib and other CDK4 & 6i using biochemical and cell-based assays. In vitro, abemaciclib preferentially inhibited CDK4 kinase activity versus CDK6, resulting in inhibition of cell proliferation in a panel of BC cell lines with higher average potency than palbociclib or ribociclib. Abemaciclib showed activity regardless of HER2 amplification and phosphatidylinositol 3-kinase (PI3KCA) gene mutation status. In human bone marrow progenitor cells, abemaciclib showed lower impact on myeloid maturation than other CDK4 & 6i when tested at unbound concentrations similar to those observed in clinical trials. Continuous abemaciclib treatment provided profound inhibition of cell proliferation, and triggered senescence and apoptosis. These preclinical results support the unique efficacy and safety profile of abemaciclib observed in clinical trials. Sign up for free Altmetric alerts about this article - https://oncotarget.altmetric.com/details/email_updates?id=10.18632%2Foncotarget.28249 Press release - https://www.oncotarget.com/news/pr/oncotarget-continuous-treatment-with-abemaciclib-leads-to-sustained-and-efficient-inhibition-of-breast-cancer-cell-proliferation/ Keywords - abemaciclib, breast cancer, cell lines, CDK4/6, continuous dosing About Oncotarget Oncotarget is a peer-reviewed, open access biomedical journal covering research on all aspects of oncology. To learn more about Oncotarget, please visit https://www.oncotarget.com and connect with us: SoundCloud - https://soundcloud.com/oncotarget Facebook - https://www.facebook.com/Oncotarget/ Twitter - https://twitter.com/oncotarget Instagram - https://www.instagram.com/oncotargetjrnl/ YouTube - https://www.youtube.com/OncotargetYouTube LinkedIn - https://www.linkedin.com/company/oncotarget Pinterest - https://www.pinterest.com/oncotarget/ Reddit - https://www.reddit.com/user/Oncotarget/ Oncotarget is published by Impact Journals, LLC: https://www.ImpactJournals.com Media Contact MEDIA@IMPACTJOURNALS.COM 18009220957

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