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    DRUG CLASS:

    MERTK inhibitor

    Related drugs:
    8d
    MRX-2843 and Osimertinib for the Treatment of Advanced EGFR Mutant Non-small Cell Lung Cancer (clinicaltrials.gov)
    P1, N=69, Recruiting, Emory University | Trial primary completion date: Dec 2025 --> Dec 2026
    Trial primary completion date
    |
    EGFR mutation
    |
    Tagrisso (osimertinib) • MRX2843
    27d
    ONO-7475-03: Study of ONO-7475 in Combination With Osimertinib in EGFR Gene Mutation-positive Non-small Cell Lung Cancer (clinicaltrials.gov)
    P1, N=78, Completed, Ono Pharmaceutical Co. Ltd | Active, not recruiting --> Completed | Trial completion date: Apr 2026 --> Jun 2025 | Trial primary completion date: Apr 2026 --> Jun 2025
    Trial completion • Trial completion date • Trial primary completion date
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • EGFR L858R • EGFR exon 19 deletion
    |
    Tagrisso (osimertinib) • tamnorzatinib (ONO-7475)
    1m
    Design, synthesis, and Lead optimization of novel Quinazoline-based FLT3 inhibitors with potent anti-acute myelogenous leukemia activity. (PubMed, Bioorg Med Chem Lett)
    Guided by a scaffold-hopping strategy based on G-749 (denfivontinib), a series of quinazoline-based derivatives was designed and synthesized to explore structure-activity relationships (SAR)...Mechanism studies indicated that W4 induced G0/G1 cell cycle arrest and apoptosis, accompanied by a reduction in intracellular reactive oxygen species levels and a loss of mitochondrial membrane potential. Collectively, these results identified W4 as a potent FLT3 inhibitor and provided valuable SAR insights for further scaffold optimization.
    Journal
    |
    FLT3 (Fms-related tyrosine kinase 3) • KIT (KIT proto-oncogene, receptor tyrosine kinase)
    |
    FLT3 mutation
    |
    denfivontinib (SKI-G-801)
    1m
    KEYNOTE-D35: Oral Axl/Mer/CSF1R Selective Tyrosine Kinase Inhibitor Q702 in Combination With Pembrolizumab in Patients With Selected Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=120, Active, not recruiting, Qurient Co., Ltd. | Recruiting --> Active, not recruiting | Trial completion date: Jun 2026 --> Mar 2028 | Trial primary completion date: Oct 2025 --> Dec 2027
    Enrollment closed • Trial completion date • Trial primary completion date
    |
    Keytruda (pembrolizumab) • adrixetinib (Q702)
    1m
    Defective Single-Site Nanozymes with Exposed Unsaturated Cu-N2 Sites for Antitumor Immunotherapy via Innate Immune-Checkpoint Blockade. (PubMed, J Am Chem Soc)
    Herein, we develop an MRX-2843 (MerTK inhibitor) and Mn2+ codelivered defective metal-organic framework (copper-2,3,6,7,10,11-hexaiminotriphenylene (Cu-HITP))-based single-site nanozyme (Ir@D-Cu-HITP-MMP) for antitumor immunotherapy via innate immune-checkpoint blockade...This synergizes with Mn2+ to enhance the stimulator of interferon genes (STING) activation, triggering robust immune responses. Overall, Ir@D-Cu-HITP-MMP demonstrates potent antitumor effects by activating powerful innate and adaptive immune responses.
    Journal • Checkpoint inhibition • IO biomarker
    |
    MERTK (MER Proto-Oncogene, Tyrosine Kinase) • STING (stimulator of interferon response cGAMP interactor 1)
    |
    MRX2843
    2ms
    QRNT-012: Study of Q702 in Subjects with Relapsed or Refractory Chronic Graft-versus-Host Disease (cGVHD) (2025-522680-14-00)
    P1, N=16, Recruiting, Qurient Co. Ltd.
    New P1 trial
    |
    adrixetinib (Q702)
    2ms
    MERTK inhibition cooperates with immunomodulatory cyclophosphamide to induce CXCL9⁺ monocyte-macrophage programming and durable anti-tumor immunity in triple negative breast cancer. (PubMed, bioRxiv)
    Combining CTX with the next generation MERTK-selective inhibitor UNC2371 (MRX-2843) drives complete remissions in both models, but durable long-term responses occurred selectively in the basal-like subtype model. Suppressive myeloid programing limits effective adaptive immune engagement in TNBC usually resulting in ICB treatment resistance and tumor recurrence. This study identifies a therapeutically actionable myeloid interferon checkpoint in which MERTK inhibition stabilizes CXCL9⁺ monocyte-macrophage programming to promote CD4⁺ T cell dependent immune memory and durable tumor control in basal-like TNBC.
    Journal
    |
    MERTK (MER Proto-Oncogene, Tyrosine Kinase) • CXCL9 (Chemokine (C-X-C motif) ligand 9) • CD4 (CD4 Molecule) • IRF1 (Interferon Regulatory Factor 1) • SOCS1 (Suppressor Of Cytokine Signaling 1) • STAT1 (Signal Transducer And Activator Of Transcription 1) • CXCR3 (C-X-C Motif Chemokine Receptor 3) • IRF7 (Interferon Regulatory Factor 7)
    |
    cyclophosphamide • MRX2843
    3ms
    Pharmacokinetic and Safety Study of MRX-2843 in Adults With Relapsed/Refractory Advanced and/or Metastatic Solid Tumors (clinicaltrials.gov)
    P1, N=42, Completed, Meryx, Inc. | Active, not recruiting --> Completed | Trial completion date: Apr 2025 --> Dec 2025 | Trial primary completion date: Feb 2025 --> Dec 2025
    Trial completion • Trial completion date • Trial primary completion date • First-in-human
    |
    MRX2843
    3ms
    Pharmacokinetic and Safety Study of MRX-2843 in Adolescents and Adults With Relapsed/Refractory AML, ALL, or MPAL (clinicaltrials.gov)
    P1, N=50, Recruiting, Meryx, Inc. | Trial completion date: Mar 2026 --> Sep 2026 | Trial primary completion date: Dec 2025 --> Jul 2026
    Trial completion date • Trial primary completion date
    |
    MRX2843
    3ms
    A Study to Evaluate Adrixetinib (Q702) in Adults With Active Chronic Graft-Versus-Host Disease (clinicaltrials.gov)
    P1, N=18, Recruiting, Qurient Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    adrixetinib (Q702)
    3ms
    Oral Axl/Mer/CSF1R Selective Tyrosine Kinase Inhibitor in Patients With Advanced Solid Tumor (clinicaltrials.gov)
    P1, N=51, Completed, Qurient Co., Ltd. | Active, not recruiting --> Completed | N=78 --> 51 | Trial completion date: Feb 2025 --> Dec 2025 | Trial primary completion date: Dec 2024 --> Dec 2025
    Trial completion • Enrollment change • Trial completion date • Trial primary completion date
    |
    adrixetinib (Q702)
    4ms
    Anexelekto (Axl)/Mer inhibitor tamnorzatinib in patients with relapsed/refractory acute myeloid leukaemia: Results from a phase I (monotherapy) and phase II (combination with venetoclax) clinical study. (PubMed, Acta Haematol)
    Tamnorzatinib alone and in combination with venetoclax was safe and well tolerated but failed to induce robust clinical efficacy in R/R AML.
    P1 data • P2 data • Journal
    |
    AXL (AXL Receptor Tyrosine Kinase) • MERTK (MER Proto-Oncogene, Tyrosine Kinase)
    |
    Venclexta (venetoclax) • tamnorzatinib (ONO-7475)