Drug intelligence / Profile preview

butolame

Development stage
Preclinical
Modality
Small Molecules
01

Overview

Butolame is a synthetic 17β-aminoestrogen (17β-AE) and an analog of 17β-estradiol (E2). It is characterized by the presence of a butyl group at the 17β position of the estrogen steroid skeleton. Butolame is being investigated as a potential candidate for hormone replacement therapy (HRT) in menopausal women. Research indicates that butolame interacts with the G-protein-coupled receptor for estrogen (GPER1), also known as GPR30, which is involved in various neoplasms. Unlike estradiol and its analog prolame, butolame has demonstrated a safer pharmacological profile in preclinical studies, as it does not appear to stimulate the proliferation of breast (MCF-7) or cervical (SIHA) cancer cells. Furthermore, butolame has been shown to reduce the phosphorylation of the oncoprotein c-fos in certain cancer cell lines, suggesting a distinct signaling mechanism that may avoid the proliferative risks associated with traditional estrogen therapies.

Other names
17β-aminoestrogen17β-AEN-butyl-1,3,5(10)-estratrien-3-ol-17β-amine
02

Targets

GPER1 (G protein-coupled estrogen receptor 1)

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