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    DRUG CLASS:

    SLC6A8 inhibitor

    Related drugs:
    4ms
    Hypoxia-Induced Creatine Uptake Reprograms Metabolism to Antagonize PARP1-Mediated Cell Death and Facilitate Tumor Progression in Hepatocellular Carcinoma. (PubMed, Cancer Res)
    The SLC6A8 inhibitor RGX-202 exerted potent antitumor activity alone and in combination with lenvatinib in patient-derived xenografts and primary HCC mouse models. Overall, this study identified intracellular creatine accumulation as a mechanism that allows hypoxic cancer cells to circumvent parthanatos and as a therapeutic target in HCC.
    Journal • PARP Biomarker
    |
    HIF1A (Hypoxia inducible factor 1, alpha subunit) • PARP1 (Poly(ADP-Ribose) Polymerase 1) • SERPINE1 (Serpin Family E Member 1)
    |
    Lenvima (lenvatinib) • ompenaclid (RGX-202)
    8ms
    RGX-202-001: A Study of RGX-202-01 (Ompenaclid) as Combination Therapy in RAS Mutant Advanced Colorectal Cancer (clinicaltrials.gov)
    P1, N=89, Completed, Inspirna, Inc. | Trial completion date: Dec 2024 --> Mar 2025 | Recruiting --> Completed | Trial primary completion date: Dec 2024 --> Mar 2025
    Trial completion • Trial completion date • Trial primary completion date
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR • RAS mutation
    |
    Avastin (bevacizumab) • 5-fluorouracil • oxaliplatin • irinotecan • leucovorin calcium • ompenaclid (RGX-202)
    9ms
    A Study to Investigate Ompenaclid Combined With FOLFIRI Plus Bevacizumab in Advanced/Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=70, Active, not recruiting, Inspirna, Inc. | Trial completion date: Dec 2026 --> Mar 2025 | Trial primary completion date: Sep 2025 --> Jan 2025
    Trial completion date • Trial primary completion date
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR • RAS mutation
    |
    Avastin (bevacizumab) • 5-fluorouracil • irinotecan • leucovorin calcium • ompenaclid (RGX-202)
    1year
    A Study to Investigate Ompenaclid Combined With FOLFIRI Plus Bevacizumab in Advanced/Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=70, Active, not recruiting, Inspirna, Inc. | Recruiting --> Active, not recruiting | Trial completion date: Aug 2028 --> Dec 2026 | Trial primary completion date: Aug 2026 --> Sep 2025
    Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR • RAS mutation
    |
    Avastin (bevacizumab) • 5-fluorouracil • irinotecan • leucovorin calcium • ompenaclid (RGX-202)
    over1year
    RGX-202-001: A Study of RGX-202-01 (Ompenaclid) as Combination Therapy in RAS Mutant Advanced Colorectal Cancer (clinicaltrials.gov)
    P1, N=108, Recruiting, Inspirna, Inc. | N=60 --> 108 | Trial primary completion date: Dec 2023 --> Dec 2024
    Enrollment change • Trial primary completion date • Combination therapy • Metastases
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR • RAS mutation
    |
    Avastin (bevacizumab) • 5-fluorouracil • oxaliplatin • irinotecan • leucovorin calcium • ompenaclid (RGX-202)
    over1year
    A Study to Investigate Ompenaclid Combined With FOLFIRI Plus Bevacizumab in Advanced/Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=70, Recruiting, Inspirna, Inc. | N=50 --> 70
    Enrollment change • Combination therapy • Metastases
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR • RAS mutation
    |
    Avastin (bevacizumab) • 5-fluorouracil • irinotecan • leucovorin calcium • ompenaclid (RGX-202)
    2years
    A Study to Investigate Ompenaclid Combined With FOLFIRI Plus Bevacizumab in Advanced/Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=50, Recruiting, Inspirna, Inc.
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR • RAS mutation
    |
    Avastin (bevacizumab) • 5-fluorouracil • oxaliplatin • irinotecan • leucovorin calcium • ompenaclid (RGX-202)
    2years
    A Study to Investigate Ompenaclid Combined With FOLFIRI Plus Bevacizumab in Advanced/Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=50, Recruiting, Inspirna, Inc. | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy • Metastases
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR • RAS mutation
    |
    Avastin (bevacizumab) • 5-fluorouracil • oxaliplatin • irinotecan • leucovorin calcium • ompenaclid (RGX-202)
    over2years
    A Study to Investigate Response to Ompenaclid Combined With FOLFIRI Plus Bevacizumab in Patients With Advanced or Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=50, Not yet recruiting, Inspirna, Inc.
    New P2 trial • Combination therapy • Metastases
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR • RAS mutation
    |
    Avastin (bevacizumab) • 5-fluorouracil • oxaliplatin • irinotecan • leucovorin calcium • ompenaclid (RGX-202)
    over2years
    Phase Ib/II study of ompenaclid (RGX-202-01), afirst-in-class oral inhibitor of the creatine transporter SLC6A8, in combination with FOLFIRI and bevacizumab (BEV) in RAS mutated (RASm) second-line (2L) advanced/metastatic colorectal cancer (mCRC) (ESMO 2023)
    Eligible pts had disease progression after a 1L oxaliplatin-containing regimen...There is a high unmet need for a safe and combinable oral pan-RASm therapy in mCRC. Recruitment of RASm pts continues and a randomized controlled trial in 2L RASm mCRC is planned.
    Clinical • P1/2 data • Combination therapy • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase) • CKB (Creatine Kinase B)
    |
    KRAS G12D • KRAS G13D • RAS mutation • KRAS G12
    |
    Avastin (bevacizumab) • 5-fluorouracil • oxaliplatin • irinotecan • leucovorin calcium • ompenaclid (RGX-202)
    over3years
    A Study of RGX-202-01 as Combination Therapy in 2nd Line RAS Mutant Advanced Colorectal Cancer (clinicaltrials.gov)
    P1, N=60, Recruiting, Inspirna, Inc. | Trial completion date: Dec 2023 --> Dec 2024 | Trial primary completion date: May 2023 --> Dec 2023
    Trial completion date • Trial primary completion date • Combination therapy
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR • RAS mutation
    |
    Avastin (bevacizumab) • 5-fluorouracil • irinotecan • leucovorin calcium • ompenaclid (RGX-202)
    over3years
    A Study of RGX-202-01 as Combination Therapy in 2nd Line RAS Mutant Advanced Colorectal Cancer (clinicaltrials.gov)
    P1, N=60, Recruiting, Inspirna, Inc. | Trial completion date: May 2022 --> Dec 2023 | Trial primary completion date: Dec 2021 --> May 2023
    Trial completion date • Trial primary completion date • Combination therapy
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR • RAS mutation
    |
    Avastin (bevacizumab) • 5-fluorouracil • irinotecan • leucovorin calcium • ompenaclid (RGX-202)