Drug intelligence / Profile preview

goserelin + letrozole + palbociclib

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

Overview

This is a combination regimen consisting of three drugs—goserelin, letrozole, and palbociclib—used primarily for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. - **Goserelin** is a luteinizing hormone-releasing hormone (LHRH) agonist that suppresses ovarian function and reduces estrogen production in premenopausal or perimenopausal women. - **Letrozole** is an aromatase inhibitor that blocks the conversion of androgens to estrogens, further lowering estrogen levels. - **Palbociclib** is a selective cyclin-dependent kinase 4/6 (CDK4/6) inhibitor that arrests cell cycle progression in cancer cells by blocking phosphorylation of retinoblastoma protein, thereby inhibiting proliferation of HR+ breast cancer cells. This combination is indicated for use in premenopausal or perimenopausal women with HR+, HER2- metastatic breast cancer. Goserelin provides ovarian suppression to allow effective use of aromatase inhibitors like letrozole; palbociclib adds targeted inhibition of cell cycle progression to enhance antitumor efficacy[1][3][4][7].

Other names
palbociclib + letrozole + goserelin
02

Targets

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

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