Drug intelligence / Profile preview

raloxifene + exemestane

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Raloxifene + exemestane is a combination of two oral small molecule drugs used in the context of breast cancer prevention and treatment in postmenopausal women. Raloxifene is a second-generation selective estrogen receptor modulator (SERM) that acts as an estrogen agonist on bone and an antagonist on breast and uterine tissue, reducing the incidence of breast cancer by blocking estrogenic stimulation in these tissues. Exemestane is a steroidal aromatase inhibitor that suppresses estrogen synthesis by irreversibly inhibiting the aromatase enzyme, thereby lowering circulating estrogen levels. The rationale for combining these agents is to achieve complete estrogen blockade—raloxifene blocks the action of residual estrogens at the receptor level while exemestane reduces overall estrogen production. This combination has been studied for safety and tolerability in postmenopausal women with a history of hormone receptor-negative breast cancer[1][2][5][6].

Other names
exemestane and raloxifene
02

Targets

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

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