^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    DRUG CLASS:

    MAT2A inhibitor

    Related drugs:
    23h
    Study of ISM3412 in Participants With Locally Advanced/Metastatic Solid Tumors (clinicaltrials.gov)
    P1/2, N=114, Recruiting, InSilico Medicine Hong Kong Limited | Phase classification: P1 --> P1/2 | N=80 --> 114
    Phase classification • Enrollment change • First-in-human
    |
    MTAP (Methylthioadenosine Phosphorylase)
    |
    MTAP deletion
    24d
    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
    |
    CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • MTAP (Methylthioadenosine Phosphorylase)
    |
    CDKN2A deletion • MTAP deletion • IDH wild-type
    |
    vopimetostat (TNG462)
    1m
    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)
    2ms
    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
    |
    MAT2A (Methionine Adenosyltransferase 2A)
    |
    ONCase (recombinant methionine α, γ-lyase) • S095033
    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=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)
    2ms
    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
    3ms
    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)