Drug intelligence / Profile preview

exemestane + goserelin + palbociclib

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

Overview

This is a combination regimen consisting of three drugs—exemestane, goserelin, and palbociclib—used primarily in the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) metastatic or advanced breast cancer in premenopausal women. - **Exemestane** is an aromatase inhibitor that blocks estrogen synthesis, reducing estrogen levels and thus limiting the growth stimulus for HR+ breast cancer cells. - **Goserelin** is a gonadotropin-releasing hormone (GnRH) agonist that suppresses ovarian function, leading to decreased production of estrogen from the ovaries—a necessary step for effective use of aromatase inhibitors in premenopausal women. - **Palbociclib** is a selective cyclin-dependent kinase 4/6 (CDK4/6) inhibitor that blocks cell cycle progression from G1 to S phase, thereby inhibiting proliferation of cancer cells. The combination has demonstrated improved progression-free survival compared to chemotherapy with capecitabine or endocrine therapy alone in clinical trials involving premenopausal patients with HR+/HER2- metastatic breast cancer[6][7]. The regimen requires careful monitoring due to risks such as neutropenia and other hematologic toxicities.

02

Targets

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

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