Drug intelligence / Profile preview

abemaciclib + nonsteroidal aromatase inhibitor

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Abemaciclib + nonsteroidal aromatase inhibitor is a **combination therapy** used in the treatment of hormone receptor-positive, human epidermal growth factor receptor 2-negative (HR+, HER2-) breast cancer, both in advanced/metastatic and early (adjuvant) settings[1][2][3][4]. **Abemaciclib** is a selective, orally bioavailable inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which prevents phosphorylation of the retinoblastoma protein (Rb), resulting in G1 cell cycle arrest and inhibition of cancer cell proliferation. **Nonsteroidal aromatase inhibitors** (letrozole, anastrozole) inhibit the aromatase enzyme, reducing estrogen synthesis, thus depriving HR+ breast cancers of estrogen-driven growth signals. The combination increases antitumor activity and has shown improved progression-free survival and invasive disease-free survival in clinical trials, especially in high-risk early breast cancer populations. Common adverse effects include diarrhea, fatigue, neutropenia, nausea, and hepatotoxicity[1][2][3][4][5].

Brand names
Verzenio + Arimidex + Femara
Other names
abemaciclib plus NSAIabemaciclib + letrozoleabemaciclib + anastrozoleabemaciclib plus nonsteroidal aromatase inhibitor
02

Targets

CYP19A1 (Aromatase)CDK1 (Cyclin-dependent kinase 1)Cyclin-dependent kinase 2/cyclin A/E complexCDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)

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