Drug intelligence / Profile preview

LY3295668 erbumine + endocrine therapy

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral (LY3295668 Erbumine, Most Endocrine Therapies)
01

Overview

**LY3295668 erbumine + endocrine therapy** is a combination regimen consisting of LY3295668 erbumine, a highly selective small molecule inhibitor of **Aurora kinase A**, and one or more endocrine therapies commonly used in hormone-driven cancers (e.g., breast cancer). LY3295668 erbumine inhibits Aurora kinase A—an enzyme implicated in cell cycle regulation, tumorigenesis, and stabilization of MYCN/MYC proteins—by binding competitively and selectively at the kinase's ATP-binding site, thereby suppressing cellular proliferation and enhancing cell death in tumor cells. The rationale for combining LY3295668 erbumine with endocrine therapy is to target both cell cycle dysregulation and hormone receptor pathways, particularly in hormone-dependent cancers such as select breast malignancies[3][8][10]. Endocrine therapy typically refers to agents modulating estrogen receptor activity, such as aromatase inhibitors, selective estrogen receptor modulators (SERMs), or selective estrogen receptor degraders (SERDs).

Other names
LY3295668LY-3295668LY 3295668
02

Targets

AURKA (Aurora kinase A)

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