Mechanism Of Action:
Abemaciclib demonstrates high selectivity in inhibiting CDK4 and CDK6 with potent activity in the low nanomolar range. By inhibiting the phosphorylation of Rb, it induces a G1 cell cycle arrest and effectively hinders cell proliferation. Importantly, abemaciclib’s activity is specifically targeted towards Rb-proficient cells.
Indication:
Breast Cancer
When used alongside an aromatase inhibitor or tamoxifen, abemaciclib is indicated for adjuvant treatment in adults with hormone receptor-positive, human epidermal growth factor receptor type 2 (HER2)-negative, node-positive, early-stage breast cancer. This therapy is specifically recommended for individuals at high risk of recurrence, whose Ki-67 score (determined by an FDA-approved test) is equal to or exceeds 20%.
For the initial treatment of hormone receptor-positive, HER2-negative advanced or metastatic breast cancer in postmenopausal women and men, abemaciclib is administered in combination with an aromatase inhibitor such as anastrozole or letrozole.
Abemaciclib, in combination with fulvestrant, is utilized for the treatment of hormone receptor-positive, HER2-negative advanced or metastatic breast cancer in adults who have experienced disease progression following prior endocrine therapy.
Abemaciclib is employed as a monotherapy for the treatment of hormone receptor-positive, HER2-negative advanced or metastatic breast cancer in adults who have undergone disease progression following endocrine therapy and prior chemotherapy for metastatic disease.
