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    7d
    Samuraciclib for the Treatment of Patients With Resectable, Borderline Resectable, or Locally Advanced Basal Pancreatic Cancer (clinicaltrials.gov)
    P1, N=15, Not yet recruiting, University of Washington
    New P1 trial
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    GATA6 (GATA Binding Protein 6) • HMGA2 (High mobility group AT-hook 2)
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    samuraciclib (CT7001)
    11d
    A Phase 1b, Open-Label Study Of REC-617, A Selective CDK7 Inhibitor, In Patients With Metastatic Or Unresectable RB1-Negative Leiomyosarcoma After Prior Systemic Therapy (clinicaltrials.gov)
    P1, N=15, Not yet recruiting, M.D. Anderson Cancer Center
    New P1 trial
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    RB1 (RB Transcriptional Corepressor 1)
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    REC-617
    26d
    ZNF274 constrains lineage plasticity and drives intrinsic resistance to CDK7 inhibitors in pancreatic cancer. (PubMed, Nat Commun)
    HERV expression following ZNF274 loss induces a double stranded RNA response that reinforces the classical to basal subtype transition. Here, we show ZNF274 is an important epigenetic regulator of cellular plasticity and sensitivity to CDK7 inhibition, presenting a therapeutic liability of PDAC subtype transition that is actionable in the clinic.
    Journal
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    ZEB1 (Zinc Finger E-box Binding Homeobox 1)
    1m
    Structure-Guided Discovery of a Bis-Pyridyl Diamine-Based Dual CDK7/9 Inhibitor with In Vitro and In Vivo Antitumor Efficacy in Glioblastoma Multiforme. (PubMed, ACS Chem Neurosci)
    Oral administration of GNE-3511 at 20 mg/kg (twice daily) demonstrated significant anti-tumor efficacy and improved survival in both U-87 MG and T98G xenograft/orthotopic mouse models. Collectively, these findings highlight GNE-3511 as a promising lead candidate for the development of GBM therapeutics.
    Preclinical • Journal • IO biomarker
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    BCL2 (B-cell CLL/lymphoma 2) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • BIRC5 (Baculoviral IAP repeat containing 5) • CD44 (CD44 Molecule) • BMI1 (BMI1 proto-oncogene, polycomb ring finger) • CDK7 (Cyclin Dependent Kinase 7) • CDK9 (Cyclin Dependent Kinase 9) • THY1 (Thy-1 membrane glycoprotein)
    3ms
    SUMIT-ELA: A Study of Samuraciclib and Elacestrant in Participants With Metastatic or Locally Advanced HR+/HER2-negative Breast Cancer (clinicaltrials.gov)
    P1/2, N=49, Completed, Carrick Therapeutics Limited | Active, not recruiting --> Completed
    Trial completion
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • CDK4 (Cyclin-dependent kinase 4)
    |
    TP53 mutation • ER positive • HER-2 negative • ESR1 mutation • HER-2 negative + ER positive • HER-2 negative + ER positive + ESR1 mutation
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    Orserdu (elacestrant) • samuraciclib (CT7001)
    4ms
    ELUCIDATE: Study to Assess GTAEXS617 in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=230, Recruiting, Exscientia AI Ltd., a wholly owned subsidiary of Recursion Pharmaceuticals, Inc. | N=165 --> 230
    Enrollment change
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    HER-2 (Human epidermal growth factor receptor 2) • CDK4 (Cyclin-dependent kinase 4) • CDK6 (Cyclin-dependent kinase 6)
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    HR positive
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    Avastin (bevacizumab) • paclitaxel • capecitabine • fulvestrant • REC-617
    8ms
    CDK7-targeted therapy effectively disrupts cell cycle progression and oncogenic signaling in head and neck cancer. (PubMed, Signal Transduct Target Ther)
    Additionally, CDK7 knockout (KO) and selective inhibitors (YKL-5-124 and samuraciclib) demonstrated potent antitumor activity, effectively suppressing tumor growth in HNSCC patient-derived organoids (PDOs), as well as in both cell line- and patient-derived xenograft (PDX) mouse models with minimal toxicity...These findings highlight CDK7 as a promising therapeutic target for HNSCC. Our study provides strong evidence of the robust antitumor activity of CDK7-selective inhibition in disease-relevant preclinical models, strongly supporting its progression to clinical testing.
    Journal
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    CDK7 (Cyclin Dependent Kinase 7)
    |
    samuraciclib (CT7001)
    8ms
    A Study of LY3405105 in Participants With Advanced Cancer (clinicaltrials.gov)
    P1, N=54, Terminated, Eli Lilly and Company | Phase classification: P1a/1b --> P1
    Phase classification
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    ARID1A (AT-rich interaction domain 1A) • KMT2D (Lysine Methyltransferase 2D) • KMT2C (Lysine Methyltransferase 2C) • SMARCB1 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily B, Member 1) • KDM6A (Lysine Demethylase 6A) • MLL2 (Myeloid/lymphoid or mixed-lineage leukemia 2) • SMARCA2 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily A, Member 2) • SS18 (SS18 Subunit Of BAF Chromatin Remodeling Complex)
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    LY3405105
    8ms
    Functional insight into cyclin-dependent kinase (CDK)7 via chemical inhibition of the priority fungal pathogen Cryptococcus neoformans. (PubMed, mBio)
    The antifungal activity of SY-1365 was also markedly enhanced in combination with membrane-targeting antifungals. Together, our findings highlight CDK7 inhibitors as valuable tools to study CDK7 function in Cn and as potentially promising antifungals in combination with licensed antifungals.
    Journal
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    CDK7 (Cyclin Dependent Kinase 7)
    |
    SY-5609 • samuraciclib (CT7001) • mevociclib (SY-1365)
    9ms
    SUMIT-BC: A Study of Samuraciclib in Combination With Fulvestrant in Metastatic or Locally Advanced Breast Cancer in Adult Participants (clinicaltrials.gov)
    P2, N=60, Completed, Carrick Therapeutics Limited | Active, not recruiting --> Completed | Trial completion date: Dec 2025 --> Aug 2025
    Trial completion • Trial completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • CDK4 (Cyclin-dependent kinase 4)
    |
    TP53 mutation • ER positive • HER-2 negative • HER-2 negative + ER positive
    |
    fulvestrant • samuraciclib (CT7001)
    9ms
    Cell-based high-throughput screening using a target-NanoLuc fusion construct to identify molecular glue degraders of c-Myc oncoprotein. (PubMed, RSC Chem Biol)
    We verified the effectiveness of our assay by demonstrating that previously known Myc-downregulating compounds (G9 and SY-1365) were successfully identified from a library of bioactive compounds with established biological function...The self-aggregation of Myc and the dissociation of the Myc/Max dimer by C1 promoted Myc degradation. Using a target-NanoLuc fusion strategy in our novel cell-based high-throughput screening system, we identified a molecular glue-like small molecule degrader of Myc.
    Journal
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    MYC (V-myc avian myelocytomatosis viral oncogene homolog)
    |
    mevociclib (SY-1365)