cilostazol indications

Oncotarget | Continuous treatment with abemaciclib leads to sustained and efficient inhibition of breast cancer cell proliferati

Worldwide, breast cancer (BC) is the second most common cancer. Pharmacologically targeting cyclin-dependent kinase 4 and 6 (CDK4 & 6) has proven to be a successful therapeutic approach in patients with estrogen receptor-positive (ER+) breast cancer.

Abemaciclib is the first FDA-approved CDK4 & 6 inhibitor (CDK4 & 6i) approved for the adjuvant treatment of HR+, HER2–, folic acid pregnancy food sources node-positive early breast cancer (EBC) at high risk of recurrence and a Ki-67 score ≥20%. Differences have been observed in both efficacy and severity of neutropenia among the available CDK4 & 6i, generating interest in a possible mechanistic explanation. In their study published in Oncotarget, researchers 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. 

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