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    DRUG CLASS:

    TGM2 inhibitor

    Related drugs:
    12d
    Inhibition of TGM2 enhances cisplatin sensitivity in MSH2-deficient bladder cancer. (PubMed, Cell Death Discov)
    Accordingly, we found that the enrichment levels of transcription factor AP-1 in TGM2 promoter region were increased in MSH2-knockout BCa cells, thereby promoting the expression of TGM2 transcriptionally. This study uncovers that CDDP effectiveness depends on TGM2 levels in MSH2-deficient BCa and that the combination of CDDP with TGM2 inhibition may represent a promising therapeutic strategy for MSH2-deficient BCa patients.
    Journal
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    MSH2 (MutS Homolog 2) • TGM2 (Transglutaminase 2)
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    cisplatin
    2ms
    CEC-013/CEL: Evaluating the Efficacy and Tolerability of ZED1227 in Subjects With Non-responsive Celiac Disease (clinicaltrials.gov)
    P2, N=356, Recruiting, Dr. Falk Pharma GmbH | Active, not recruiting --> Recruiting
    Enrollment open
    6ms
    CEC-013/CEL: Evaluating the Efficacy and Tolerability of ZED1227 in Subjects With Non-responsive Celiac Disease (clinicaltrials.gov)
    P2, N=356, Active, not recruiting, Dr. Falk Pharma GmbH
    New P2 trial
    7ms
    A Study to Evaluate the Efficacy and Safety of GSK3915393 in Participants With Idiopathic Pulmonary Fibrosis (IPF) (clinicaltrials.gov)
    P2, N=158, Terminated, GlaxoSmithKline | Active, not recruiting --> Terminated; The study met futility criteria at pre-planned interim analysis, showing no clinical efficacy of the investigational drug. Based on the lack of efficacy at the interim data review, the sponsor decided to terminate the study.
    Trial termination
    9ms
    A Study to Evaluate the Efficacy and Safety of GSK3915393 in Participants With Idiopathic Pulmonary Fibrosis (IPF) (clinicaltrials.gov)
    P2, N=158, Active, not recruiting, GlaxoSmithKline | Trial completion date: Feb 2026 --> Oct 2025 | Trial primary completion date: Feb 2026 --> Oct 2025
    Trial completion date • Trial primary completion date
    9ms
    A Study to Evaluate the Efficacy and Safety of GSK3915393 in Participants With Idiopathic Pulmonary Fibrosis (IPF) (clinicaltrials.gov)
    P2, N=158, Active, not recruiting, GlaxoSmithKline | Recruiting --> Active, not recruiting
    Enrollment closed
    over1year
    A Study to Evaluate the Safety, Tolerability and Blood Levels of GSK3915393 Administered to Healthy Participants of Chinese, Japanese and European Ancestry and to Assess Effects of GSK3915393 on Nintedanib (clinicaltrials.gov)
    P1, N=50, Completed, GlaxoSmithKline | Not yet recruiting --> Completed | N=38 --> 50
    Trial completion • Enrollment change
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    nintedanib
    over1year
    A Study to Evaluate the Safety, Tolerability and Blood Levels of GSK3915393 Administered to Healthy Participants of Chinese, Japanese and European Ancestry and to Assess Effects of GSK3915393 on Nintedanib (clinicaltrials.gov)
    P1, N=38, Not yet recruiting, GlaxoSmithKline
    New P1 trial
    |
    nintedanib
    almost2years
    A Study to Evaluate the Efficacy and Safety of GSK3915393 in Participants With Idiopathic Pulmonary Fibrosis (IPF) (clinicaltrials.gov)
    P2, N=150, Recruiting, GlaxoSmithKline | Not yet recruiting --> Recruiting
    Enrollment open
    2years
    NormaliZED: Different Doses of ZED1227 vs. Placebo in NAFLD (clinicaltrials.gov)
    P2, N=186, Completed, Dr. Falk Pharma GmbH | Recruiting --> Completed
    Trial completion
    2years
    A Study to Evaluate the Efficacy and Safety of GSK3915393 in Participants With Idiopathic Pulmonary Fibrosis (IPF) (clinicaltrials.gov)
    P2, N=150, Not yet recruiting, GlaxoSmithKline
    New P2 trial
    over2years
    Discovery of novel 1H-benzo[d]imidazole-4,7-dione based transglutaminase 2 inhibitors as p53 stabilizing anticancer agents in renal cell carcinoma. (PubMed, Bioorg Chem)
    These results indicated that the inhibition of TG2 by compound 8j (MD102) could enhance p53 stabilization, thereby ultimately showing anticancer effects in RCC. Compound 8j (MD102), a novel TG2 inhibitor, can be further applied for the development of an anticancer candidate drug targeting RCC.
    Journal
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    TGM2 (Transglutaminase 2) • GLS2 (Glutaminase 2)
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    TP53 mutation • TGM2 overexpression • TGM2 expression