Drug intelligence / Profile preview

elacestrant + exemestane

Development stage
Unknown
Lead developer
Radius Health
Modality
Small Molecules
Administration
Oral
01

Overview

elacestrant + exemestane is an investigational combination therapy being evaluated for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) metastatic breast cancer. This regimen is the focus of the Phase 2 COMBINE clinical trial, sponsored by the European Institute of Oncology. Elacestrant is an oral selective estrogen receptor degrader (SERD) that binds to estrogen receptors, inducing their degradation and inhibiting estrogen-dependent signaling. Exemestane is a steroidal aromatase inhibitor that irreversibly binds to the aromatase enzyme, preventing the conversion of androgens into estrogens. By combining these two agents, the therapy aims to achieve a more complete suppression of the estrogen signaling pathway than either agent alone, specifically targeting patients who have progressed on prior endocrine therapies but still exhibit estrogen receptor activity as confirmed by [18F]FES-PET imaging.

Other names
elacestrant and exemestaneCOMBINE trial regimen
02

Targets

ESR1 (ERα)CYP19A1 (Aromatase)

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