Drug intelligence / Profile preview

alpelisib + goserelin + tamoxifen

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

Overview

Alpelisib + goserelin + tamoxifen is a combination regimen used in the treatment of hormone receptor-positive (HR+), HER2-negative advanced or metastatic breast cancer, particularly in premenopausal women. Alpelisib is a selective inhibitor of the phosphatidylinositol 3-kinase alpha (PI3Kα) isoform, targeting tumors with PIK3CA mutations. Goserelin is a gonadotropin-releasing hormone (GnRH) agonist that suppresses ovarian function and reduces estrogen production. Tamoxifen is a selective estrogen receptor modulator (SERM) that antagonizes estrogen receptors on breast cancer cells. This combination aims to block both the PI3K pathway and estrogen signaling, providing dual pathway inhibition for improved efficacy in endocrine-sensitive breast cancers[1][2][4].

02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)ESR2 (ERβ)ESR1 (ERα)PIK3CA (Phosphoinositide 3-kinase alpha)

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