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    DRUG CLASS:

    CDK9 inhibitor

    Related drugs:
    15d
    Integrin-binding sialoprotein as an extracellular matrix-associated independent prognostic biomarker in glioma. (PubMed, BMC Cancer)
    IBSP represents an independent prognostic biomarker associated with adverse outcomes in glioma. These findings provide insight into the molecular mechanisms underlying IBSP-associated glioma progression and highlight potential therapeutic targets that may contribute to improved clinical outcomes in patients with glioma.
    Journal
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    SLC16A3 (Solute Carrier Family 16 Member 3) • CASP4 (Caspase 4) • KYNU (Kynureninase) • SIGLEC9 (Sialic Acid Binding Ig Like Lectin 9)
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    alvocidib (DSP-2033) • dinaciclib (MK-7965)
    15d
    Inhibition of RNA polymerase II-activating CDK9 and CDK12/13, but not of cell cycle relevant CDKs, induces apoptosis by downregulating the short-lived Bcl-2 proteins Mcl1 and Bfl1/A1. (PubMed, Cell Death Dis)
    Only inhibition of CDK9 (by AZD4573 and atuveciclib) or of CDK12/13 (by SR4835 and THZ531)-which target the transcriptional elongation of RNA polymerase II (RNAPII)-exerted a strong apoptotic potential. Because Bcl-2 only inhibits Bax, but not Bak, AZD4573 and SR4835 were able to induce apoptosis in Jurkat cells overexpressing Bcl-2. As tumor cells frequently upregulate Bcl-2, inhibitors of CDK9 and CDK12/13 represent promising anticancer drugs.
    Journal • IO biomarker
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    BCL2 (B-cell CLL/lymphoma 2) • MCL1 (Myeloid cell leukemia 1) • CDK4 (Cyclin-dependent kinase 4) • BCL2L1 (BCL2-like 1) • CDK12 (Cyclin dependent kinase 12) • CDK7 (Cyclin Dependent Kinase 7) • CDK9 (Cyclin Dependent Kinase 9) • CDK1 (Cyclin-dependent kinase 1) • CDC73 (Cell Division Cycle 73)
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    zemirciclib (AZD4573) • atuveciclib (BAY 1143572)
    22d
    IRST204.09: A Phase II, Open-Label Randomized Study of Intravenous Tambiciclib in Combination with the Standard of care Venetoclax and Azacitidine in Patients with Newly Diagnosed AML Who Failed to Achieve at Least MLFS After the First Two Cycles of Treatment with Venetoclax and Azacitidine Alone (2025-524308-31-00)
    P1/2, N=40, Not yet recruiting, Istituto Romagnolo Per Lo Studio Dei Tumori Dino Amadori IRST S.r.l., IIS La Fe
    New P1/2 trial
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    Venclexta (venetoclax) • azacitidine • tambiciclib (SLS009)
    1m
    Cyclin-dependent kinase-9 and oxidative phosphorylation inhibition overcome ibrutinib resistance in mantle cell lymphoma. (PubMed, Cancer Res Commun)
    OxPhos inhibitor IACS-010759 demonstrated synergy with AZD4573 in vitro. Thus, CDK9 inhibition exhibits activity in ibrutinib-resistant MCL and can be further enhanced by co-targeting of OxPhos.
    Journal
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    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MCL1 (Myeloid cell leukemia 1) • CDK9 (Cyclin Dependent Kinase 9)
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    Imbruvica (ibrutinib) • IACS-010759 • zemirciclib (AZD4573)
    2ms
    Studying TAK-243 in Patients With Advanced Cancer (clinicaltrials.gov)
    P1, N=95, Recruiting, National Cancer Institute (NCI) | Trial completion date: Apr 2026 --> Apr 2027 | Trial primary completion date: Apr 2026 --> Apr 2027
    Trial completion date • Trial primary completion date
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    TAK-243
    2ms
    Investigation of the Inhibitory Effects and Underlying Mechanisms of Vitexin Derivatives Targeting CDK1 in HCT Colorectal Cancer Cells. (PubMed, Chem Biol Drug Des)
    Molecular docking reveals strong binding affinity between M3 and CDK1 (Docking score -10.127), and molecular dynamics simulations confirm the stability of the M3-CDK1 complex with inhibitory effects comparable to flavopiridol (FP). Furthermore, M3 downregulates CDK1/cyclin B expression in HCT-116 cells (IC₅₀ = 9.83 ± 2.65 μM). M3 may suppress HCT-116 cell proliferation by targeting CDK1/cyclin B and inducing G₂/M phase arrest.
    Journal
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    CDK1 (Cyclin-dependent kinase 1)
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    alvocidib (DSP-2033)
    3ms
    Dual-Targeting Cuproptosis and Mitophagy via a Flavopiridol-Copper Nanoplatform Potentiates Immunotherapy Against Uveal Melanoma. (PubMed, Adv Sci (Weinh))
    This work establishes cuproptosis induction via NP@Fla-Cu as a transformative strategy against UM, effectively addressing challenges in tumor selectivity and off-target toxicity. The dual functionality of flavopiridol as a copper ionophore and mitophagy activator provides a promising combinatorial approach to overcome therapy resistance in immunosuppressive malignancies.
    Journal • Tumor mutational burden • IO biomarker
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    TMB (Tumor Mutational Burden) • CD8 (cluster of differentiation 8)
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    TMB-L
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    alvocidib (DSP-2033)
    3ms
    A Study of Voruciclib Alone or in Combination With Venetoclax in Subjects With B-Cell Malignancies or AML (clinicaltrials.gov)
    P1, N=84, Terminated, MEI Pharma, Inc. | Recruiting --> Terminated; Business reasons, not related to safety or efficacy results.
    Trial termination
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    Venclexta (venetoclax) • voruciclib (ME-522)
    3ms
    GFH009X2101: Study of SLS009 (Formerly GFH009) a Potent Highly Selective CDK9 Inhibitor in Patients With Hematologic Malignancies and High-Risk Newly Diagnosed AML (clinicaltrials.gov)
    P1/2, N=160, Recruiting, Sellas Life Sciences Group | Trial completion date: Dec 2025 --> Dec 2027 | Trial primary completion date: Dec 2025 --> Dec 2026
    Trial completion date • Trial primary completion date
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    PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • FLT3 (Fms-related tyrosine kinase 3) • IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2) • NPM1 (Nucleophosmin 1) • SF3B1 (Splicing Factor 3b Subunit 1) • ASXL1 (ASXL Transcriptional Regulator 1) • SRSF2 (Serine and arginine rich splicing factor 2) • BCOR (BCL6 Corepressor) • U2AF1 (U2 Small Nuclear RNA Auxiliary Factor 1) • STAG2 (Stromal Antigen 2) • DDX41 (DEAD-Box Helicase 41) • ZRSR2 (Zinc Finger CCCH-Type, RNA Binding Motif And Serine/Arginine Rich 2)
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    TP53 mutation • KRAS mutation • FLT3-ITD mutation • Chr del(17p) • IDH1 mutation • IDH2 mutation • FLT3 mutation • TP53 wild-type • NPM1 mutation • KRAS wild-type • Chr del(11q) • ASXL1 mutation • SF3B1 mutation • EZH2 mutation • NRAS wild-type • SRSF2 mutation • IDH wild-type
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    Venclexta (venetoclax) • azacitidine • tambiciclib (SLS009)
    3ms
    Structure-Based Discovery of HS34: A Highly Selective and Orally Bioavailable CDK9 Inhibitor for Triple-Negative Breast Cancer. (PubMed, J Med Chem)
    In cellular assays, HS34 displayed potent antiproliferative activity against TNBC cells, outperforming the reference inhibitor KB-0742...Furthermore, HS34 exhibits favorable DMPK properties, including high oral bioavailability and metabolic stability, which align with the significant antitumor efficacy observed in an orally treated xenograft model. Collectively, these findings establish HS34 as a selective CDK9 inhibitor and demonstrate that exploiting target-specific conformational features offers an effective strategy for kinase selectivity.
    Journal
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    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MCL1 (Myeloid cell leukemia 1)
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    istisociclib (KB-0742)
    3ms
    Use of Small-Molecule Inhibitors of CILK1 and AURKA as Cilia-Promoting Drugs to Decelerate Medulloblastoma Cell Replication. (PubMed, Biomedicines)
    The results demonstrated the potential of using cilia-promoting drugs, such as Alvocidib and Alisertib, to suppress cancer cell replication. Additionally, it shows the massive benefits of integrating accessible large language models to conduct sweeping, rapid, and accurate literature searches.
    Journal
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    AURKA (Aurora kinase A)
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    alisertib (MLN8237) • alvocidib (DSP-2033)
    4ms
    Study of VIP152, Venetoclax, and Prednisone (VVIP) in Relapsed/Refractory Lymphoid Malignancies (clinicaltrials.gov)
    P1/2, N=8, Completed, National Cancer Institute (NCI) | Active, not recruiting --> Completed
    Trial completion
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    ALK (Anaplastic lymphoma kinase) • BCL2 (B-cell CLL/lymphoma 2)
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    Venclexta (venetoclax) • enitociclib (VIP152)