Drug intelligence / Profile preview

abemaciclib + anastrozole + degarelix

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

Overview

This is a combination therapy consisting of three drugs—abemaciclib, anastrozole, and degarelix—used in clinical research for the treatment of hormone receptor–positive (HR+), HER2-negative breast cancer, particularly in men. - **Abemaciclib** is a small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression and inhibits tumor cell proliferation. - **Anastrozole** is a nonsteroidal aromatase inhibitor that reduces estrogen production by inhibiting the aromatase enzyme, thereby decreasing growth stimulation in estrogen receptor–positive tumors. - **Degarelix** is a gonadotropin-releasing hormone (GnRH) antagonist that rapidly suppresses testosterone production by blocking GnRH receptors in the pituitary gland; this further reduces androgen-driven tumor growth. This triple combination aims to maximize endocrine suppression and cell cycle inhibition to improve outcomes for patients with HR+/HER2- breast cancer. It is being studied as neoadjuvant therapy (pre-surgical) for male breast cancer as part of phase II clinical trials such as ETHAN[1][2][6].

02

Targets

CDK4 (Cyclin-dependent kinase 4)GnRHR (Gonadotropin-releasing hormone receptor)CDK6 (Cyclin-dependent kinase 6)CYP19A1 (Aromatase)

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