echemi logo
Product
  • Product
  • Supplier
  • Inquiry
    Home > Active Ingredient News > Urinary System > First to be confirmed: an epigenetic drug EZH2 inhibitor that treats bladder cancer by activating the immune system

    First to be confirmed: an epigenetic drug EZH2 inhibitor that treats bladder cancer by activating the immune system

    • Last Update: 2022-10-21
    • Source: Internet
    • Author: User
    Search more information of high quality chemicals, good prices and reliable suppliers, visit www.echemi.com

    Written byWang CongEditor
    Wang Duoyu typesettingWater Chengwen
    Bladder Cancer (BCa), is one of the most common malignant tumors in the urinary system, Most are transitional epithelial cell carcinomas
    .
    In foreign countries, the incidence of bladder cancer is second only to prostate cancer in male urogenital tumors, ranking second, while in China, bladder cancer ranks first
    .

    If bladder cancer is diagnosed at an early stage, the possibility of treatment is still high, the 5-year survival of patients is 77%, but the recurrence rate after bladder cancer treatment is as high as 70%, so the development of more effective anti-bladder cancer methods has become a top priority for medical workers
    .

    On October 5, 2022, researchers from Northwestern University published a paper in Science Advances: Immune activation is essential for the antitumor activity of EZH2 Research paper by Inhibition in urothelial Carcinoma.


    The study is the first to confirm that Tazemetostat, an epigenetic drug currently used to treat lymphoma and sarcoma, is able to suppress bladder cancer by activating the immune system
    。 The research team has initiated human clinical trials
    for advanced bladder cancer.


    Joshua J.
    Meeks, the corresponding author of the paper and an associate professor at Northwestern University's Feinberg School of Medicine, said this
    is the first discovery of an epigenetic drug EZH2 inhibitor — Tazemetostat actually works by activating the immune system, not just inhibiting tumor growth
    .
    The survival rate for advanced bladder cancer is extremely low, but the mechanism of action of tazecistat is different from other anticancer drugs or therapies, which is also the first application
    of epigenetic drugs in bladder cancer.

    EZH2 is a histone methyltransferase that catalyzes the trimethylation modification of histone H3 lysine 27 (H3K27me3) through its SET domain to silence downstream target genes
    .
    In many cancers, EZH2 is highly expressed and promotes cancer development and malignancy
    .
    Therefore, EZH2 is an ideal target for
    anti-cancer drugs.

    Tazecistat was developed
    by epigenetic drug development company Epizyme.
    In January 2020, the FDA approved
    Tazemetostat, the world's first EZH2 inhibitor, for the treatment of metastatic or advanced epithelioid sarcoma (ES)
    that is not suitable for surgical resection.

    Tazemustat
    EZH2 is usually overexpressed in most solid tumors and exerts a cancer-promoting effect by "locking" the tumor into a growing state, thus becoming one of
    the main genes associated with cancer.
    Some of the most common gene mutations in bladder cancer can make EZH2 more active, further promoting the development of
    bladder cancer.

    Therefore, the team tried to inhibit EZH2 gene expression in a mouse model of bladder cancer, and the results showed that after inhibition of EZH2, the tumor in the mouse model of bladder cancer was significantly shrunk and filled with immune cells
    .
    This suggests that EZH2 may also play a role
    in suppressing the immune system.
    Next, the team used Tazemetostat, a commercially available EZH2 inhibitor, to treat bladder cancer mice, and the results showed that tazemustat filled the bladders with immune cells
    .
    When using a mouse bladder cancer model without T cells
    , tazecilastat treatment was ineffective, suggesting that tazecilastat exerts anti-cancer effects
    primarily by activating the immune system.


    JoshuaJ.
    Meeks
    says tazecistat is well tolerated and can therefore be used
    in combination with other bladder cancer therapies.
    It is reported that the research team is conducting a clinical trial
    of tazeshistat treatment for patients with advanced bladder cancer.

    Link: style="letter-spacing: normal;color: rgb(136, 136, 136);font-size: 12px;" _mstmutation="1" _istranslated="1">
    open for reprinting Welcome to forward to Moments and WeChat groups 
    This article is an English version of an article which is originally in the Chinese language on echemi.com and is provided for information purposes only. This website makes no representation or warranty of any kind, either expressed or implied, as to the accuracy, completeness ownership or reliability of the article or any translations thereof. If you have any concerns or complaints relating to the article, please send an email, providing a detailed description of the concern or complaint, to service@echemi.com. A staff member will contact you within 5 working days. Once verified, infringing content will be removed immediately.

    Related Articles

    Contact Us

    The source of this page with content of products and services is from Internet, which doesn't represent ECHEMI's opinion. If you have any queries, please write to service@echemi.com. It will be replied within 5 days.

    Moreover, if you find any instances of plagiarism from the page, please send email to service@echemi.com with relevant evidence.