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    DRUG:

    methoxyamine (TRC102)

    i
    Other names: TRC102, TRC-102
    Associations

    News

    Trials
    Company:
    Tracon Pharma
    Drug class:
    DNA excision repair inhibitor
    Associations

    News

    Trials
    9ms
    NCI-2021-14403: Testing the Addition of an Anti-Cancer Drug, TRC102, to the Usual Chemotherapy Treatment (Pemetrexed, Cisplatin or Carboplatin) During Radiation Therapy for Stage III Non-Squamous Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=42, Recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2025 --> Jun 2027 | Trial primary completion date: Dec 2025 --> Jun 2027
    Trial completion date • Trial primary completion date
    |
    CD4 (CD4 Molecule)
    |
    cisplatin • carboplatin • Imfinzi (durvalumab) • pemetrexed • methoxyamine (TRC102)
    over1year
    Base-excision repair pathway regulates transcription-replication conflicts in pancreatic ductal adenocarcinoma. (PubMed, Cell Rep)
    Co-treatment with ATR inhibitor (VX970) and BER inhibitor (methoxyamine) at clinically relevant doses synergistically enhanced DNA damage and reduced cell proliferation in PDAC cells. The study provides mechanistic insights into the regulation of TRCs in PDAC by the BER pathway, which has biologic and therapeutic implications.
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
    |
    berzosertib (M6620) • methoxyamine (TRC102)
    over1year
    Evaluating the Base Excision Repair Inhibitor TRC102 and Temozolomide for patients with Recurrent Glioblastoma in the Phase 2 Adult Brain Tumor Consortium Trial BERT. (PubMed, Clin Cancer Res)
    These findings confirm safety and feasibility of TRC102+TMZ for rGBM patients. They also warrant further evaluation of combination therapy in biomarker-enriched trials enrolling GBM patients with baseline hyperactivated DDR pathways.
    P2 data • Journal
    |
    PCNA (Proliferating cell nuclear antigen)
    |
    Avastin (bevacizumab) • temozolomide • methoxyamine (TRC102)
    almost2years
    Methoxyamine, Cisplatin, and Pemetrexed Disodium in Treating Patients With Advanced Solid Tumors or Mesothelioma That Cannot Be Removed by Surgery or Mesothelioma That Is Refractory to Pemetrexed Disodium and Cisplatin or Carboplatin (clinicaltrials.gov)
    P1/2, N=30, Active, not recruiting, National Cancer Institute (NCI) | Phase classification: P2 --> P1/2
    Phase classification • Combination therapy • Surgery • Metastases
    |
    cisplatin • carboplatin • pemetrexed • methoxyamine (TRC102)
    almost2years
    Testing the Addition of an Anti-Cancer Drug, TRC102, to the Usual Chemotherapy Treatment (Pemetrexed, Cisplatin or Carboplatin) During Radiation Therapy for Stage III Non-Squamous Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=42, Recruiting, National Cancer Institute (NCI) | N=78 --> 42
    Enrollment change • Combination therapy
    |
    CD4 (CD4 Molecule)
    |
    cisplatin • carboplatin • Imfinzi (durvalumab) • pemetrexed • Pemfexy (pemetrexed) • methoxyamine (TRC102)
    over2years
    Exceptional Responders to Base Excision Repair (BER) Inhibition for Recurrent Glioblastoma Display Enrichment for DNA Damage Response Pathways: RNA Sequencing Analysis from a Multicenter Trial (SNO 2023)
    TRC102 (methoxyamine), a small molecule DNA base-excision repair (BER) inhibitor, reverses temozolomide (TMZ) resistance in preclinical glioma models...If sufficient activity was identified, arm 2 was planned in bevacizumab-refractory patients... rGBM patients with elevated levels of MPG and DDR molecular signature may have impaired BER and respond better to TRC102+TMZ.
    Clinical
    |
    MGMT (6-O-methylguanine-DNA methyltransferase) • PCNA (Proliferating cell nuclear antigen)
    |
    MGMT expression
    |
    Avastin (bevacizumab) • temozolomide • methoxyamine (TRC102)
    over2years
    Exceptional Responders to Base Excision Repair (BER) Inhibition for Recurrent Glioblastoma Display Enrichment for DNA Damage Response Pathways: RNA Sequencing Analysis from a Multicenter Trial (SNO 2023)
    TRC102 (methoxyamine), a small molecule DNA base-excision repair (BER) inhibitor, reverses temozolomide (TMZ) resistance in preclinical glioma models...If sufficient activity was identified, arm 2 was planned in bevacizumab-refractory patients... rGBM patients with elevated levels of MPG and DDR molecular signature may have impaired BER and respond better to TRC102+TMZ.
    Clinical
    |
    MGMT (6-O-methylguanine-DNA methyltransferase) • PCNA (Proliferating cell nuclear antigen)
    |
    MGMT expression
    |
    Avastin (bevacizumab) • temozolomide • methoxyamine (TRC102)
    over2years
    Methoxyamine, Cisplatin, and Pemetrexed Disodium in Treating Patients With Advanced Solid Tumors or Mesothelioma That Cannot Be Removed by Surgery or Mesothelioma That Is Refractory to Pemetrexed Disodium and Cisplatin or Carboplatin (clinicaltrials.gov)
    P2, N=30, Active, not recruiting, National Cancer Institute (NCI) | N=58 --> 30 | Trial completion date: Dec 2023 --> Oct 2024 | Trial primary completion date: Dec 2023 --> Dec 2022
    Enrollment change • Trial completion date • Trial primary completion date • Combination therapy • Surgery • Metastases
    |
    cisplatin • carboplatin • pemetrexed • methoxyamine (TRC102)
    over2years
    Methoxyamine, Cisplatin, and Pemetrexed Disodium in Treating Patients With Advanced Solid Tumors or Mesothelioma That Cannot Be Removed by Surgery or Mesothelioma That Is Refractory to Pemetrexed Disodium and Cisplatin or Carboplatin (clinicaltrials.gov)
    P2, N=58, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2022 --> Dec 2023 | Trial primary completion date: Dec 2022 --> Dec 2023
    Trial completion date • Trial primary completion date • Combination therapy • Surgery • Metastases
    |
    cisplatin • carboplatin • pemetrexed • methoxyamine (TRC102)
    over2years
    TRC102 and Temozolomide for Relapsed Solid Tumors and Lymphomas (clinicaltrials.gov)
    P1/2, N=93, Completed, National Cancer Institute (NCI) | Recruiting --> Completed | N=140 --> 93 | Trial completion date: Feb 2024 --> Aug 2023 | Trial primary completion date: Feb 2024 --> Aug 2023
    Trial completion • Enrollment change • Trial completion date • Trial primary completion date • Combination therapy
    |
    temozolomide • methoxyamine (TRC102)
    over2years
    Identifying the Reactive Metabolites of Tyrosine Kinase Inhibitor Pexidartinib In Vitro Using LC-MS-Based Metabolomic Approaches. (PubMed, Chem Res Toxicol)
    In the current study, the metabolic activation of PEX was investigated in human/mouse liver microsomes (HLM/MLM) and primary human hepatocytes (PHH) using glutathione (GSH) and methoxyamine (NHOMe) as trapping reagents. CYP3A4 and CYP3A5 were identified as the primary enzymes responsible for the formation of these adducts using recombinant human P450s and CYP3A chemical inhibitor ketoconazole. Overall, our studies suggested that PEX metabolism can produce reactive metabolites mediated by CYP3A, and the association of the reactive metabolites with PEX hepatotoxicity needs to be further studied.
    Preclinical • Journal • Metabolomic study
    |
    CSF1R (Colony stimulating factor 1 receptor) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • CYP3A5 (Cytochrome P450 Family 3 Subfamily A Member 5)
    |
    Turalio (pexidartinib) • methoxyamine (TRC102)