Drug intelligence / Profile preview

genistein

Development stage
Phase 3
Lead developer
Humanetics
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Genistein is a naturally occurring isoflavone and phytoestrogen primarily found in soybeans and other legumes. It acts as a selective estrogen receptor modulator (SERM) with both estrogenic and anti-estrogenic effects. Genistein exhibits antineoplastic activity by binding to and inhibiting protein-tyrosine kinases, disrupting signal transduction pathways essential for cell growth and proliferation[1][2]. It also inhibits topoisomerase-II (DNA topoisomerases, type II), induces G2 phase cell cycle arrest, promotes apoptosis in cancer cells, and modulates multiple signaling pathways including PI3K/Akt/HIF-1α, NF-κB, MAPK/ERK1/2, Wnt/β-catenin[6]. Genistein has demonstrated antioxidant, anti-inflammatory[5], antibacterial, antiviral activities as well as beneficial effects on cardiovascular health by interacting with nuclear estrogen receptors to alter gene transcription[2][4]. Additionally, it has anthelmintic properties effective against certain parasitic worms by inhibiting glycolytic enzymes in the parasites[2][7]. Genistein is under investigation for use in cancer prevention/treatment (notably breast cancer), cardiovascular disease prevention in postmenopausal women[4], diabetes management via modulation of glucose metabolism[2], osteoporosis prevention[5], and as an anti-inflammatory agent.

Brand names
Bonistein
Other names
4',5,7-trihydroxyisoflavone7-hydroxy-3-(4-hydroxyphenyl)chromen-4-one
02

Targets

TOP2A (DNA topoisomerase II)ESR1 (ERα)ESR2 (ERβ)GPER1 (G protein-coupled estrogen receptor 1)PTK (Protein-Tyrosine Kinase)

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