^
    6ms
    A Study of Temodar With Abexinostat (PCI-24781) for Patients With Recurrent Glioma (clinicaltrials.gov)
    P1, N=18, Recruiting, University of Nebraska | Trial completion date: Jun 2027 --> Mar 2027 | Trial primary completion date: Feb 2025 --> Mar 2026
    Trial completion date • Trial primary completion date
    |
    temozolomide • abexinostat (CG-781)
    7ms
    Abexinostat and Ibrutinib in Diffuse Large B-cell Lymphoma and Mantle Cell Lymphoma (clinicaltrials.gov)
    P1, N=15, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Trial completion date: May 2024 --> May 2025 | Trial primary completion date: May 2024 --> May 2025
    Trial completion date • Trial primary completion date
    |
    BCL6 (B-cell CLL/lymphoma 6) • IRF4 (Interferon regulatory factor 4) • MME (Membrane Metalloendopeptidase)
    |
    Imbruvica (ibrutinib) • abexinostat (CG-781)
    9ms
    Abexinostat in Combination With Pembrolizumab in Patients With Advanced Solid Tumor Malignancies (clinicaltrials.gov)
    P1, N=35, Completed, Rahul Aggarwal | Active, not recruiting --> Completed | Phase classification: P1b --> P1
    Trial completion • Phase classification • Combination therapy • Metastases
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR
    |
    Keytruda (pembrolizumab) • abexinostat (CG-781)
    11ms
    A Clinical Study to Evaluate Pharmacokinetics, Safety, and Tolerability of Abexinostat in Chinese Patients (clinicaltrials.gov)
    P1/2, N=12, Active, not recruiting, Xynomic Pharmaceuticals, Inc. | Recruiting --> Active, not recruiting | N=25 --> 12 | Trial completion date: Dec 2023 --> Jun 2024
    Enrollment closed • Enrollment change • Trial completion date
    |
    abexinostat (CG-781)
    11ms
    FORERUNNER: Study of Abexinostat in Patients With Relapsed or Refractory Follicular Lymphoma (clinicaltrials.gov)
    P2, N=139, Active, not recruiting, Xynomic Pharmaceuticals, Inc. | Trial completion date: Dec 2023 --> Dec 2025 | Trial primary completion date: Dec 2023 --> Dec 2024
    Trial completion date • Trial primary completion date
    |
    abexinostat (CG-781)
    11ms
    A Study of Pazopanib With or Without Abexinostat in Patients With Locally Advanced or Metastatic Renal Cell Carcinoma (RENAVIV) (clinicaltrials.gov)
    P3, N=413, Recruiting, Xynomic Pharmaceuticals, Inc. | Trial completion date: Jun 2023 --> Jun 2025 | Trial primary completion date: Jun 2023 --> Dec 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    pazopanib • abexinostat (CG-781)
    11ms
    Study to Evaluate Efficacy and Safety of Oral Abexinostat in Patients With Relapsed or Refractory Diffuse Large B-cell Lymphoma (DLBCL) (clinicaltrials.gov)
    P2, N=170, Recruiting, Xynomic Pharmaceuticals, Inc. | Trial completion date: May 2024 --> May 2025 | Trial primary completion date: May 2024 --> Dec 2024
    Trial completion date • Trial primary completion date
    |
    abexinostat (CG-781)
    11ms
    A Multi-Center Phase 2 Study to Evaluate Efficacy and Safety of Oral Abexinostat as Monotherapy in Patients With Relapsed or Refractory Follicular Lymphoma (clinicaltrials.gov)
    P2, N=96, Recruiting, Xynomic Pharmaceuticals, Inc. | Trial completion date: Jun 2023 --> Sep 2024 | Trial primary completion date: Jun 2023 --> Feb 2024
    Trial completion date • Trial primary completion date • Epigenetic controller
    |
    abexinostat (CG-781)
    12ms
    Pazopanib in Combination With PCI-24781 in Patients With Metastatic Solid Tumors (clinicaltrials.gov)
    P1, N=90, Active, not recruiting, Pamela Munster | Recruiting --> Active, not recruiting
    Enrollment closed • Combination therapy • Metastases
    |
    pazopanib • abexinostat (CG-781)
    1year
    A Study of Temodar With Abexinostat (PCI-24781) for Patients With Recurrent Glioma (clinicaltrials.gov)
    P1, N=18, Recruiting, University of Nebraska | Trial completion date: Jun 2026 --> Jun 2027 | Trial primary completion date: Feb 2024 --> Feb 2025
    Trial completion date • Trial primary completion date
    |
    temozolomide • abexinostat (CG-781)
    over1year
    Study to Evaluate Efficacy and Safety of Oral Abexinostat in Patients With Relapsed or Refractory Diffuse Large B-cell Lymphoma (DLBCL) (clinicaltrials.gov)
    P2, N=170, Recruiting, Xynomic Pharmaceuticals, Inc. | Trial completion date: May 2023 --> May 2024 | Trial primary completion date: May 2023 --> May 2024
    Trial completion date • Trial primary completion date
    |
    abexinostat (CG-781)
    over1year
    A Study of Temodar With PCI-24781 for Patients With Recurrent Glioma (clinicaltrials.gov)
    P1, N=18, Recruiting, University of Nebraska | Not yet recruiting --> Recruiting | Trial completion date: Sep 2026 --> Jun 2026 | Trial primary completion date: May 2024 --> Feb 2024
    Enrollment open • Trial completion date • Trial primary completion date
    |
    temozolomide • abexinostat (CG-781)
    over1year
    Abexinostat and Ibrutinib in Diffuse Large B-cell Lymphoma and Mantle Cell Lymphoma (clinicaltrials.gov)
    P1, N=15, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Phase classification: P1/2 --> P1
    Phase classification
    |
    BCL6 (B-cell CLL/lymphoma 6) • IRF4 (Interferon regulatory factor 4) • MME (Membrane Metalloendopeptidase)
    |
    Imbruvica (ibrutinib) • abexinostat (CG-781)
    2years
    Integrating High-Throughput Dynamic BH3 Profiling and Molecular Phenotyping to Identify Therapeutic Vulnerabilities in CLL (ASH 2022)
    Despite recent advances in chronic lymphocytic leukemia (CLL) therapy, such as the use of targeted agents including, Bruton's tyrosine kinase (BTK) inhibitor ibrutinib and the potent BCL-2 antagonist venetoclax, this disease remains incurable for most patients, who are refractory or become resistant to the novel agents...Other drugs that demonstrated high priming included navitoclax (BCL-XL/BCL-2), nutlin-3 (MDM2), abexinostat (HDAC), gandotinib (JAK2), duvelisib (PI3K δ/γ), idelalisib (PI3Kδ) and cerdulatinib (SYK/JAK)...First, we found that IGHV-mutated CLLs (M-CLLs) became more primed to apoptosis than IGHV-unmutated CLLs (U-CLLs) across the panel of drugs (p<0.001, paired t-test) and significantly in response to fludarabine and umbralisib (FDR<0.1, t-test)...EC-i, associated with the intermediate methylation subtype of CLL, was the most resistant EC to ibrutinib but was very sensitive to navitoclax, more than to any other drug. Altogether, we present a framework that links ex-vivo drug response with molecular features including expression subtypes to highlight new therapeutic opportunities in CLL.
    IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • JAK2 (Janus kinase 2) • CD19 (CD19 Molecule) • IGH (Immunoglobulin Heavy Locus) • BCL2L1 (BCL2-like 1) • PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • CD5 (CD5 Molecule) • IL10 (Interleukin 10) • SYK (Spleen tyrosine kinase)
    |
    IGH mutation • IL10 overexpression • TS 12
    |
    Venclexta (venetoclax) • Imbruvica (ibrutinib) • Zydelig (idelalisib) • Copiktra (duvelisib) • navitoclax (ABT 263) • Ukoniq (umbralisib) • fludarabine IV • abexinostat (CG-781) • cerdulatinib (ALXN2075) • Nutlin-3 • gandotinib (LY 2784544)
    over2years
    Abexinostat and Ibrutinib in Diffuse Large B-cell Lymphoma and Mantle Cell Lymphoma (clinicaltrials.gov)
    P1/2, N=15, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Recruiting --> Active, not recruiting | N=40 --> 15
    Enrollment closed • Enrollment change
    |
    BCL6 (B-cell CLL/lymphoma 6) • IRF4 (Interferon regulatory factor 4) • MME (Membrane Metalloendopeptidase)
    |
    Imbruvica (ibrutinib) • abexinostat (CG-781)
    over2years
    Abexinostat and Ibrutinib in Diffuse Large B-cell Lymphoma and Mantle Cell Lymphoma (clinicaltrials.gov)
    P1/2, N=40, Recruiting, Memorial Sloan Kettering Cancer Center | Trial completion date: May 2023 --> May 2024 | Trial primary completion date: May 2023 --> May 2024
    Trial completion date • Trial primary completion date
    |
    BCL6 (B-cell CLL/lymphoma 6) • IRF4 (Interferon regulatory factor 4) • MME (Membrane Metalloendopeptidase)
    |
    Imbruvica (ibrutinib) • abexinostat (CG-781)
    over2years
    Abexinostat in Combination With Pembrolizumab in Patients With Advanced Solid Tumor Malignancies (clinicaltrials.gov)
    P1b, N=35, Active, not recruiting, Rahul Aggarwal | Recruiting --> Active, not recruiting | Trial completion date: May 2023 --> Nov 2023 | Trial primary completion date: May 2023 --> Nov 2023
    Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR
    |
    Keytruda (pembrolizumab) • abexinostat (CG-781)
    over2years
    Abexinostat and Ibrutinib in Diffuse Large B-cell Lymphoma and Mantle Cell Lymphoma (clinicaltrials.gov)
    P1/2, N=40, Recruiting, Memorial Sloan Kettering Cancer Center | Trial completion date: May 2022 --> May 2023 | Trial primary completion date: May 2022 --> May 2023
    Trial completion date • Trial primary completion date
    |
    BCL6 (B-cell CLL/lymphoma 6) • IRF4 (Interferon regulatory factor 4) • MME (Membrane Metalloendopeptidase)
    |
    Imbruvica (ibrutinib) • abexinostat (CG-781)
    3years
    Differential gene expression-based connectivity mapping identified novel drug candidate and improved Temozolomide efficacy for Glioblastoma. (PubMed, J Exp Clin Cancer Res)
    PCI-24781 is a novel GBM-signature specific HDAC inhibitor that works synergistically with TMZ to enhance TMZ efficacy and improve GBM survival. These promising MGMT-agnostic results warrant clinical evaluation.
    Clinical • Journal • BRCA Biomarker
    |
    BRCA1 (Breast cancer 1, early onset) • PTEN (Phosphatase and tensin homolog) • MGMT (6-O-methylguanine-DNA methyltransferase) • RAD51 (RAD51 Homolog A) • CHEK1 (Checkpoint kinase 1) • HDAC2 (Histone deacetylase 2) • HDAC1 (Histone Deacetylase 1) • HDAC11 (Histone Deacetylase 11) • GFAP (Glial Fibrillary Acidic Protein)
    |
    temozolomide • Zolinza (vorinostat) • abexinostat (CG-781)
    over3years
    A Phase 1b Dose Escalation/Expansion Study of Abexinostat in Combination With Pembrolizumab in Patients With Advanced Solid Tumor Malignancies (clinicaltrials.gov)
    P1b, N=42, Recruiting, Rahul Aggarwal | Trial primary completion date: Feb 2022 --> May 2023 | Trial completion date: Apr 2022 --> May 2023
    Clinical • Trial completion date • Trial primary completion date • Combination therapy
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR
    |
    Keytruda (pembrolizumab) • abexinostat (CG-781)
    over3years
    Abexinostat, Palbociclib, and Fulvestrant for the Treatment of Breast or Gynecologic Cancer (clinicaltrials.gov)
    P1, N=0, Withdrawn, Pamela Munster | N=70 --> 0 | Not yet recruiting --> Withdrawn
    Clinical • Enrollment change • Trial withdrawal
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER positive • HER-2 amplification • HER-2 negative
    |
    Ibrance (palbociclib) • fulvestrant • abexinostat (CG-781)
    almost4years
    The histone deacetylase inhibitor PCI-24781 impairs calcium influx and inhibits proliferation and metastasis in breast cancer. (PubMed, Theranostics)
    We have demonstrated that PCI-24781 is an effective anti-tumor therapeutic agent that targets calcium signaling by activating RGS2. This study also provides a novel perspective into the use of HDAC inhibitors for cancer therapy.
    Journal
    |
    RGS2 (Regulator Of G Protein Signaling 2)
    |
    abexinostat (CG-781)
    4years
    Abexinostat, Palbociclib, and Fulvestrant for the Treatment of Breast or Gynecologic Cancer (clinicaltrials.gov)
    P1, N=70, Not yet recruiting, Pamela Munster | Trial completion date: Jan 2022 --> Jun 2025 | Trial primary completion date: Oct 2021 --> Jun 2025
    Clinical • Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER positive • HER-2 amplification • HER-2 negative
    |
    Ibrance (palbociclib) • fulvestrant • abexinostat (CG-781)
    over4years
    Abexinostat, Palbociclib, and Fulvestrant for the Treatment of Breast or Gynecologic Cancer (clinicaltrials.gov)
    P1, N=70, Not yet recruiting, Pamela Munster
    Clinical • New P1 trial
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER positive • HER-2 amplification • HER-2 negative
    |
    Ibrance (palbociclib) • fulvestrant • abexinostat (CG-781)
    over4years
    Histone deacetylase 1 regulates the malignancy of oral cancer cells via miR-154-5p/PCNA axis. (PubMed, Biol Chem)
    Targeted inhibition of HDAC1 via its specific inhibitor PCI24781 or siRNA can inhibit the proliferation of OSCC cells and increase their sensitivity to the chemo-sensitivity such as doxorubicin (Dox) treatment. Results showed that HDAC1 can negative regulate the expression of miR-154-5p, inhibitor of miR-154-5p can attenuate PCI24781 treatment decreased PCNA expression and cell proliferation. Collectively, our present study suggested that HDAC1 can promote the growth and progression of OSCC via regulation of miR-154-5p/PCNA signals.
    Journal
    |
    PCNA (Proliferating cell nuclear antigen)
    |
    doxorubicin hydrochloride • abexinostat (CG-781)
    over5years
    Abexinostat and Ibrutinib in Diffuse Large B-cell Lymphoma and Mantle Cell Lymphoma (clinicaltrials.gov)
    P1/2; N=40; Recruiting; Sponsor: Memorial Sloan Kettering Cancer Center; Not yet recruiting --> Recruiting
    Enrollment open
    |
    BCL6 (B-cell CLL/lymphoma 6) • MME (Membrane Metalloendopeptidase)
    |
    Imbruvica (ibrutinib) • abexinostat (CG-781)
    over5years
    Abexinostat and Ibrutinib in Diffuse Large B-cell Lymphoma and Mantle Cell Lymphoma (clinicaltrials.gov)
    P1/2; N=40; Not yet recruiting; Sponsor: Memorial Sloan Kettering Cancer Center
    New P1/2 trial
    |
    BCL6 (B-cell CLL/lymphoma 6) • MME (Membrane Metalloendopeptidase)
    |
    Imbruvica (ibrutinib) • abexinostat (CG-781)