Drug intelligence / Profile preview

exemestane + leuprolide + palbociclib

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

Overview

Exemestane + leuprolide + palbociclib is a three-drug combination regimen used primarily in the treatment of hormone receptor-positive, HER2-negative metastatic breast cancer in premenopausal women. Exemestane is a steroidal aromatase inhibitor that suppresses estrogen synthesis by irreversibly binding to the aromatase enzyme, thereby reducing estrogen levels and limiting tumor growth driven by estrogen signaling. Leuprolide is a gonadotropin-releasing hormone (GnRH) agonist that induces ovarian suppression, further lowering circulating estrogen levels in premenopausal patients. Palbociclib is an oral small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression from G1 to S phase, inhibiting proliferation of cancer cells dependent on this pathway. The combination has demonstrated improved progression-free survival compared to chemotherapy with capecitabine in clinical trials for premenopausal women with HR-positive/HER2-negative metastatic breast cancer[1][2][4][6].

02

Targets

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

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