Drug intelligence / Profile preview

GA-11

Development stage
Preclinical
Lead developer
Apeejay Stya University
Modality
Small Molecules
Administration
Oral
01

Overview

GA-11 is a novel small molecule tamoxifen analog developed as a potential therapeutic agent for breast cancer, including estrogen receptor-positive (ER+) and triple-negative breast cancer (TNBC). Chemically, GA-11 contains a methoxy group in place of the N,N-dimethylethyl functionality of tamoxifen, along with an additional polar amine group, which improves its drug-likeness and predicted oral bioavailability. In preclinical studies, GA-11 demonstrated non-selective cytotoxicity against both ER+ (MCF-7) and triple-negative (MDA-MB-231) breast cancer cell lines, showing significantly higher potency than tamoxifen while remaining non-toxic to normal cells. Additionally, GA-11 has been shown to inhibit the expression of proteins associated with adhesion, migration, and metastasis, such as MMP-9, c-Myc, and Caveolin-1, and to suppress the migration and invasion of breast cancer cells.

02

Targets

MMP9 (Matrix metalloproteinase-9)ESR1 (ERα)CAV1 (Caveolin-1)ESR2 (ERβ)MYC (MYC proto-oncogene protein)

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