Indications
Abemaciclib is a kinase inhibitor. It is used together with endocrine therapy (tamoxifen or an aromatase inhibitor) as adjuvant treatment in adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, node-positive, early breast cancer. These patients must be at high risk of recurrence and have a Ki-67 score ≥20%, as determined by an FDA approved test. Abezino is a kinase inhibitor as well, and its uses are the following. It is given with endocrine therapy (tamoxifen or an aromatase inhibitor) for the adjuvant treatment of adult patients with HR-positive, HER2-negative, node-positive, early breast cancer at high risk of recurrence and a Ki-67 score ≥20%, as determined by an FDA approved test. It is used in combination with an aromatase inhibitor as initial endocrine-based therapy for postmenopausal women, and men, with HR-positive, HER2-negative advanced or metastatic breast cancer. Combined with fulvestrant, it is used for adult patients with HR-positive, HER2-negative advanced or metastatic breast cancer whose disease has progressed following endocrine therapy. It can also be used on its own (as monotherapy) for adult patients with HR-positive, HER2-negative advanced or metastatic breast cancer with disease progression following endocrine therapy and prior chemotherapy in the metastatic setting.
⚠️ Always consult a registered physician before taking any medicine.
Pharmacology
Abemaciclib blocks two enzymes called cyclin-dependent kinases 4 and 6 (CDK4 and CDK6). These kinases switch on when they bind to D-cyclins. In estrogen receptor-positive (ER+) breast cancer cell lines, cyclin D1 and CDK4/6 drive phosphorylation of the retinoblastoma protein (Rb), and this pushes the cell cycle forward and makes the cells multiply.
In vitro, continuous exposure to abemaciclib inhibited Rb phosphorylation. It also stopped cells from moving from G1 into S phase of the cell cycle, and this led to senescence and apoptosis. In breast cancer xenograft models, abemaciclib given daily without interruption, either as a single agent or together with antiestrogens, reduced tumor size.
Pregnancy & Breastfeeding
Abemaciclib can harm an unborn baby if a pregnant woman takes it. This is based on animal studies and on how the medicine works. In pregnant rats, giving abemaciclib during the period when the organs form caused malformations (teratogenicity) and lower fetal weight. The mother's exposure in those studies was similar to the exposure seen in people at the maximum recommended human dose, measured by area under the curve (AUC).
Pregnant women should be told about the possible risk to the baby. Women who could become pregnant should use effective contraception while they are on Abemaciclib and for 3 weeks after the last dose.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Dosage Reference
⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.
Side Effects & Interactions
Side Effects
No side-effect data recorded yet.