Drug intelligence / Profile preview

axp107-11

Development stage
Phase 2
Lead developer
Axcentua
Modality
Small Molecules
Administration
Oral
01

Overview

AXP107-11 is a novel, multi-component crystalline salt form of the naturally occurring isoflavone genistein, developed to improve its physiochemical properties and oral bioavailability compared to natural genistein. It acts primarily by binding to and modulating nuclear estrogen receptors (ERα/ESR1) as well as activating the G-protein-coupled estrogen receptor 1 (GPER1). These mechanisms are believed to sensitize tumor cells and their microenvironment to chemotherapy, particularly gemcitabine. AXP107-11 has been investigated in phase Ib/IIa clinical trials for advanced or metastatic pancreatic cancer, both as monotherapy and in combination with gemcitabine. The drug demonstrated a favorable safety profile with no dose-limiting toxicities observed in early-phase studies. Preclinical data indicate that AXP107-11 can synergistically enhance the antiproliferative effects of gemcitabine on pancreatic cancer cells[1][2][3][4][6][8].

Other names
crystalline genistein formulationgenistein sodium dihydrate
02

Targets

GPER1 (G protein-coupled estrogen receptor 1)ESR1 (ERα)

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