Drug intelligence / Profile preview

exemestane + fulvestrant

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

Overview

Exemestane + fulvestrant is a combination of two endocrine therapies used in the treatment of hormone receptor-positive (HR+) advanced or metastatic breast cancer, primarily in postmenopausal women. Exemestane is an irreversible steroidal aromatase inhibitor that reduces estrogen production by inhibiting the aromatase enzyme, thereby lowering circulating estrogen levels. Fulvestrant is a selective estrogen receptor degrader (SERD) that binds to and accelerates degradation of the estrogen receptor, blocking its activity and reducing tumor cell proliferation driven by estrogen signaling. The rationale for combining these agents lies in their complementary mechanisms—one suppresses systemic estrogen synthesis while the other directly antagonizes and degrades the receptor. Clinical studies have shown that this combination does not significantly improve clinical benefit over single-agent therapy with either drug[1][6]. Both drugs are approved individually for HR+ advanced breast cancer.

02

Targets

ESR2 (ERβ)ESR1 (ERα)CYP19A1 (Aromatase)

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