Drug intelligence / Profile preview

abemaciclib + fulvestrant

Development stage
Phase 4
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Abemaciclib + fulvestrant is a combination therapy used to treat hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer, particularly in patients whose disease has progressed following endocrine therapy. Abemaciclib is an oral small molecule inhibitor of cyclin-dependent kinase 4 (CDK4) and cyclin-dependent kinase 6 (CDK6), which are key regulators of cell cycle progression from the G1 to S phase. By inhibiting CDK4/6, abemaciclib prevents phosphorylation of the retinoblastoma protein, leading to cell cycle arrest and inhibition of cancer cell proliferation. Fulvestrant is an estrogen receptor antagonist that binds competitively to estrogen receptors and accelerates their degradation, thereby blocking estrogen signaling required for tumor growth in HR+ breast cancers. The combination has demonstrated improved progression-free survival compared with fulvestrant alone in clinical trials[1][5][8].

Other names
Abemaciclib plus fulvestrantAbemaciclib + Fulvestrant
02

Targets

CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)ER (Estrogen receptor)

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