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    DRUG:

    pidnarulex (CX-5461)

    i
    Other names: CX-5461
    Company:
    Senhwa Biosci
    Drug class:
    RNA polymerase 1 inhibitor
    Related drugs:
    9d
    Testing the Effectiveness of the Anti-cancer Drug Pidnarulex (CX-5461), in Combination With Another Anti-cancer Drug Cemiplimab (REGN2810), in Treating Refractory Microsatellite Stable Colorectal Cancer (clinicaltrials.gov)
    P1/2, N=86, Recruiting, National Cancer Institute (NCI) | Not yet recruiting --> Recruiting | Initiation date: Mar 2026 --> Dec 2026
    Enrollment open • Trial initiation date
    |
    MSI (Microsatellite instability) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • FBXW7 (F-Box And WD Repeat Domain Containing 7)
    |
    Libtayo (cemiplimab-rwlc) • pidnarulex (CX-5461)
    2ms
    RNA polymerase I inhibitor CX-5461 suppresses cervical cancer cell growth by inducing DNA damage and mitotic catastrophe and enhances cisplatin sensitivity. (PubMed, Biochem Pharmacol)
    When combined with cisplatin, CX-5461 enhances the sensitivity of cervical cancer cells to this chemotherapeutic agent. In conclusion, CX-5461 demonstrates potential therapeutic value for cervical cancer, particularly as a new strategy for patients with primary or platinum-resistant disease.
    Journal
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    CDK1 (Cyclin-dependent kinase 1) • CCNB1 (Cyclin B1)
    |
    cisplatin • pidnarulex (CX-5461)
    2ms
    TFEB confers resistance against the chemotherapeutic agent CX-5461. (PubMed, Autophagy Rep)
    Interfering with TFEB improved the sensitivity of cancer cells to both CX-5461 and gemcitabine. Our findings suggest that TFEB provides broad protection against the stress caused by chemotherapeutic drugs, representing a promising target for intercepting chemoresistance and improving the efficacy of anticancer agents.
    Journal
    |
    TFEB (Transcription Factor EB 2)
    |
    gemcitabine • pidnarulex (CX-5461)
    3ms
    Testing the Safety of Anti-Cancer Drug, CX-5461 (Pidnarulex), in Treating Lymphoma With Specific Changes in the MYC Gene (clinicaltrials.gov)
    P1/2, N=50, Recruiting, National Cancer Institute (NCI) | Not yet recruiting --> Recruiting | Trial completion date: Sep 2027 --> Jan 2030 | Initiation date: Mar 2026 --> Oct 2026 | Trial primary completion date: Sep 2027 --> Jan 2030
    Enrollment open • Trial completion date • Trial initiation date • Trial primary completion date
    |
    BCL2 (B-cell CLL/lymphoma 2) • BCL6 (B-cell CLL/lymphoma 6)
    |
    pidnarulex (CX-5461)
    3ms
    Testing the Safety of the Combination of Anti-Cancer Drugs CX-5461 (Pidnarulex) and Trastuzumab Deruxtecan (T-DXd) for Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Solid Tumors and Breast Cancer (clinicaltrials.gov)
    P1, N=36, Recruiting, National Cancer Institute (NCI) | Not yet recruiting --> Recruiting | Initiation date: Mar 2026 --> Oct 2026
    Enrollment open • Trial initiation date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    HER-2 positive
    |
    Enhertu (fam-trastuzumab deruxtecan-nxki) • pidnarulex (CX-5461)
    3ms
    Testing the Safety of the Combination of Anti-Cancer Drugs CX-5461 (Pidnarulex) and Trastuzumab Deruxtecan (T-DXd) for Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Solid Tumors and Breast Cancer (clinicaltrials.gov)
    P1, N=36, Not yet recruiting, National Cancer Institute (NCI) | Trial completion date: Mar 2027 --> Jan 2028 | Trial primary completion date: Mar 2027 --> Jan 2028
    Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    HER-2 positive
    |
    Enhertu (fam-trastuzumab deruxtecan-nxki) • pidnarulex (CX-5461)
    4ms
    Testing the Safety of Anti-Cancer Drug, CX-5461 (Pidnarulex), in Treating Lymphoma With Specific Changes in the MYC Gene (clinicaltrials.gov)
    P1/2, N=50, Not yet recruiting, National Cancer Institute (NCI) | Initiation date: Dec 2025 --> Mar 2026
    Trial initiation date
    |
    BCL2 (B-cell CLL/lymphoma 2)
    |
    pidnarulex (CX-5461)
    4ms
    Testing the Effectiveness of the Anti-cancer Drug Pidnarulex (CX-5461) in Combination With Another Anti-cancer Drug Cemiplimab (REGN2810), in Treating Refractory Microsatellite Stable Colorectal Cancer (clinicaltrials.gov)
    P1/2, N=86, Not yet recruiting, National Cancer Institute (NCI) | Initiation date: Dec 2025 --> Mar 2026
    Trial initiation date
    |
    Libtayo (cemiplimab-rwlc) • pidnarulex (CX-5461)
    4ms
    Testing the Safety of the Combination of Anti-Cancer Drugs CX-5461 (Pidnarulex) and Trastuzumab Deruxtecan (T-DXd) for Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Solid Tumors and Breast Cancer (clinicaltrials.gov)
    P1, N=36, Not yet recruiting, National Cancer Institute (NCI) | Initiation date: Dec 2025 --> Mar 2026
    Trial initiation date
    |
    Enhertu (fam-trastuzumab deruxtecan-nxki) • pidnarulex (CX-5461)
    5ms
    Targeting RNA polymerase I to boost natural killer cell anticancer activity in multiple myeloma. (PubMed, Cell Death Dis)
    Our study examined two "first-in-class" RNA Pol I inhibitors, CX-5461 and BMH-21, which differentially regulate NK cell-activating and inhibitory ligand expression in MM. This effect was modulated by Lenalidomide and Panobinostat. Moreover, RNA Pol I inhibition enhanced Daratumumab-mediated antibody-dependent cellular cytotoxicity (ADCC) of NK cells against MM, uncovering novel immuno-mediated antitumor mechanisms.
    Journal
    |
    IFNG (Interferon, gamma) • TNFA (Tumor Necrosis Factor-Alpha) • HLA-E (Major Histocompatibility Complex, Class I, E)
    |
    lenalidomide • Darzalex (daratumumab) • Farydak (panobinostat) • pidnarulex (CX-5461)
    5ms
    Reply to: The chemotherapeutic drug CX-5461 is a potent mutagen in cultured human cells. (PubMed, medRxiv)
    This is particularly important given that several clinical trials, including a Phase Ib study of CX-5461 in patients with solid tumours [ NCT04890613 ] and a National Cancer Institute sponsored Phase I trial [ NCT06606990 ] are currently enrolling patients. These ongoing and planned clinical efforts highlight both the therapeutic promise of CX-5461 and the importance of evaluating this agent within rigorous and clinically relevant frameworks.
    Journal • Tumor mutational burden
    |
    TMB (Tumor Mutational Burden)
    |
    pidnarulex (CX-5461)
    6ms
    High-throughput combination screening of Pidnarulex and other G-quadruplex ligands in multi-cell type tumor spheroids. (PubMed, SLAS Discov)
    To investigate the therapeutic potential of three G4 ligands-pidnarulex, APTO-253, and BRACO-19-a high-throughput drug combination screen was conducted in thirty-one multi-cell type tumor spheroids derived from patient tumors and established cancer cell lines. Brightfield imaging corroborated enhanced spheroid growth suppression from synergistic combinations. These findings underscore the context-dependent activity of G4 ligands and support the use of integrated functional and imaging-based approaches to characterize potential therapeutic combinations in physiologically relevant 3D cancer models.
    Journal
    |
    PIM1 (Pim-1 Proto-Oncogene)
    |
    pidnarulex (CX-5461) • APTO-253