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    DRUG CLASS:

    MAT2A inhibitor

    Related drugs:
    16d
    S095035 as a Single Agent and in Combination in Adult Participants With Advanced or Metastatic Solid Tumors With Deletion of MTAP (clinicaltrials.gov)
    P1/2, N=60, Active, not recruiting, Servier Bio-Innovation LLC | N=342 --> 60 | Trial completion date: Oct 2031 --> May 2027 | Trial primary completion date: Oct 2031 --> May 2027 | Recruiting --> Active, not recruiting
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date • First-in-human
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    CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • MTAP (Methylthioadenosine Phosphorylase)
    |
    CDKN2A deletion • MTAP deletion • IDH wild-type
    |
    vopimetostat (TNG462)
    30d
    An Investigational Study of BG-89894 Tablets in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=29, Terminated, BeOne Medicines | Active, not recruiting --> Terminated; The study was discontinued following an internal decision by the sponsor
    Trial termination
    |
    MTAP (Methylthioadenosine Phosphorylase)
    1m
    The Combination of Methionine Adenosyltransferase 2A (MAT2A) Inhibitor AG-270 and Recombinant Methioninase Is Not Cancer-selective in a Co-culture Model of Colon Cancer Cells and Normal Fibroblasts. (PubMed, Cancer Diagn Progn)
    In contrast, rMETase combined with numerous first-line chemotherapeutic drugs acted selectively and synergistically against cancer cells while sparing normal cells, including co-culture models. The present results suggest that AG-270 may have limited potential as an anticancer agent.
    Journal
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    MAT2A (Methionine Adenosyltransferase 2A)
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    ONCase (recombinant methionine α, γ-lyase) • S095033
    1m
    S095035 as a Single Agent and in Combination in Adult Participants With Advanced or Metastatic Solid Tumors With Deletion of MTAP (clinicaltrials.gov)
    P1/2, N=342, Recruiting, Servier Bio-Innovation LLC | Active, not recruiting --> Recruiting | N=104 --> 342
    Enrollment open • Enrollment change • First-in-human
    |
    CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • MTAP (Methylthioadenosine Phosphorylase)
    |
    CDKN2A deletion • MTAP deletion • IDH wild-type
    |
    vopimetostat (TNG462)
    1m
    A Phase I Study of SY-9453 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=122, Recruiting, Shouyao Holdings (Beijing) Co. LTD | Not yet recruiting --> Recruiting
    Enrollment open
    |
    MTAP (Methylthioadenosine Phosphorylase)
    2ms
    S095035 as a Single Agent and in Combination in Adult Participants With Advanced or Metastatic Solid Tumors With Deletion of MTAP (clinicaltrials.gov)
    P1/2, N=104, Active, not recruiting, Servier Bio-Innovation LLC | Recruiting --> Active, not recruiting
    Enrollment closed • First-in-human
    |
    CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • MTAP (Methylthioadenosine Phosphorylase)
    |
    CDKN2A deletion • MTAP deletion • IDH wild-type
    |
    vopimetostat (TNG462)
    2ms
    Design and Discovery of Pyridazinone-Based MAT2A Inhibitors Targeting MTAP-Deficient Cancers. (PubMed, J Med Chem)
    Herein, we report the design and optimization of a novel series of pyridazinone-based MAT2A inhibitors via a ring-opening strategy from AGI-41998...Mechanically, treatment with 33 markedly reduced SAM and sDMA levels both in vitro and in vivo. Collectively, these results establish pyridazinone as a privileged scaffold for MAT2A inhibition and identify compound 33 as a compelling lead for further preclinical development.
    Journal
    |
    MTAP (Methylthioadenosine Phosphorylase) • MAT2A (Methionine Adenosyltransferase 2A)
    |
    MTAP deletion
    2ms
    IDE397-001: Study of IDE397 in Participants With Solid Tumors Harboring MTAP Deletion (clinicaltrials.gov)
    P1, N=169, Active, not recruiting, IDEAYA Biosciences | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    MTAP (Methylthioadenosine Phosphorylase)
    |
    MTAP deletion
    |
    Trodelvy (sacituzumab govitecan-hziy) • IDE397
    2ms
    An Investigational Study of BG-89894 Tablets in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=29, Active, not recruiting, BeOne Medicines | Recruiting --> Active, not recruiting | N=140 --> 29 | Trial completion date: Dec 2028 --> Apr 2026
    Enrollment closed • Enrollment change • Trial completion date
    |
    MTAP (Methylthioadenosine Phosphorylase)
    3ms
    A Phase I Study of SY-9453 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=122, Not yet recruiting, Shouyao Holdings (Beijing) Co. LTD
    New P1 trial
    |
    MTAP (Methylthioadenosine Phosphorylase)
    4ms
    CL1-95035-001: A study of S095035 as a single agent and in combination in adult participants with advanced or metastatic solid tumors with deletion of MTAP (2025-521249-25-00)
    P1/2, N=118, Recruiting, Institut De Recherches Internationales Servier IRIS
    New P1/2 trial
    |
    MTAP (Methylthioadenosine Phosphorylase)
    |
    MTAP deletion • IDH wild-type
    |
    vopimetostat (TNG462)
    4ms
    Lack of Cancer Specificity of Methionine Adenosyltransferase 2A (MAT2A) Inhibitor AG-270 in Combination With Recombinant Methioninase In Vitro. (PubMed, Anticancer Res)
    AG-270 showed lack of cancer specificity in combination with rMETase when tested on both cancer and normal cells. The present results contrast with numerous chemotherapy agents, which in combination with rMETase are synergistic on cancer cells but not on normal cells. The present findings suggest that MAT2A inhibition affects crucial metabolic pathways in normal as well as cancer cell types and thus AG-270 may not be suitable as a cancer-specific therapeutic strategy.
    Preclinical • Journal
    |
    MAT2A (Methionine Adenosyltransferase 2A)
    |
    ONCase (recombinant methionine α, γ-lyase) • S095033