Drug intelligence / Profile preview

E7090 + exemestane

Development stage
Unknown
Lead developer
Eisai
Modality
Small Molecules
Administration
Oral
01

Overview

E7090 + exemestane is an investigational combination therapy comprising E7090 (tasurgratinib), a selective small molecule inhibitor of fibroblast growth factor receptor 1–3 (FGFR1–3), and exemestane, a steroidal aromatase inhibitor. E7090 targets FGFR-dependent tumor growth and signaling, while exemestane irreversibly inhibits aromatase, blocking estrogen synthesis and thereby suppressing estrogen receptor-mediated tumor proliferation. The combination is being developed for the treatment of estrogen receptor positive (ER+), human epidermal growth factor receptor 2 negative (HER2−), recurrent or metastatic breast cancer, particularly in patients who have received prior CDK4/6 inhibitor therapy[1][2][5]. Preclinical and clinical studies have shown this combination has manageable safety and tolerability, with preliminary evidence of antitumor activity in FGFR-driven and HR+/HER2− advanced breast cancer after CDK4/6 inhibitor exposure[2]. The developers and trial sponsor is Eisai.

Brand names
Aromasin
Other names
tasurgratinibexemestane
02

Targets

FGFR4 (Fibroblast growth factor receptor 4)ESR1 (ERα)CYP19A1 (Aromatase)FGFR3 (Fibroblast growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)

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