Drug intelligence / Profile preview

everolimus + imlunestrant

Development stage
Phase 1
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

everolimus + imlunestrant is an investigational oral combination therapy for advanced or metastatic breast cancer. Everolimus is a small molecule inhibitor of the mammalian target of rapamycin (mTOR), while imlunestrant is a next-generation, oral selective estrogen receptor degrader (SERD) that targets and degrades the estrogen receptor, including in tumors with ESR1 mutations. The combination aims to overcome resistance to endocrine therapies by simultaneously inhibiting mTOR signaling and degrading the estrogen receptor, thereby suppressing tumor cell proliferation in hormone receptor–positive, HER2-negative breast cancer. Clinical studies have shown that this combination demonstrates antitumor activity and manageable safety in patients previously treated with CDK4/6 inhibitors and other endocrine therapies[1][5][6][8].

02

Targets

ESR1 (ERα)Mechanistic target of rapamycin complex 1

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