Related Experiment Video

Updated: Jan 10, 2026

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
08:45

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors

Published on: July 17, 2020

6.6K

First-of-Its-Kind PPARG Inhibitor Shows Compelling Activity

    Cancer Discovery
    |November 25, 2025
    PubMed

    Insights

    A new drug, FX-909, targeting the PPARG protein, effectively shrank tumors in patients with advanced urothelial carcinoma. The drug may also reduce immune suppression by modulating T cells and cytokines.

    Area of Science:

    • Oncology
    • Immunology

    Background:

    • Advanced urothelial carcinoma often overexpresses the protein PPARG.
    • PPARG plays a role in immune suppression within the tumor microenvironment.

    Purpose of the Study:

    • To evaluate the efficacy of FX-909, a novel PPARG inhibitor, in patients with advanced urothelial carcinoma.
    • To explore the drug's impact on the tumor immune microenvironment.

    Main Methods:

    • Clinical trial administering FX-909 to patients with advanced urothelial carcinoma.
    • Analysis of tumor shrinkage and immune markers (CD4+ T cells, chemokines, cytokines) in responding patients.

    Main Results:

    • FX-909 treatment resulted in tumor shrinkage in most patients with high PPARG expression.
    • Responding patients showed elevated CD4+ T cells, chemokines, and cytokines.
    • These immune changes suggest FX-909 may overcome PPARG-mediated immune suppression.

    Conclusions:

    • FX-909 demonstrates significant anti-tumor activity in advanced urothelial carcinoma.
    • The drug's mechanism may involve the modulation of the tumor immune microenvironment.
    • FX-909 represents a potential therapeutic strategy for urothelial carcinoma by targeting PPARG and immune suppression.

    More Related Videos

    Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts10:27

    Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts

    Published on: July 25, 2020

    7.8K
    Utilizing 18F-FDG PET/CT Imaging and Quantitative Histology to Measure Dynamic Changes in the Glucose Metabolism in Mouse Models of Lung Cancer06:51

    Utilizing 18F-FDG PET/CT Imaging and Quantitative Histology to Measure Dynamic Changes in the Glucose Metabolism in Mouse Models of Lung Cancer

    Published on: July 21, 2018

    18.5K

    Related Concept Videos

    Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

    Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

    Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
    These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
    443
    Dipeptidyl Peptidase 4 Inhibitors01:23

    Dipeptidyl Peptidase 4 Inhibitors

    Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
    566