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    DRUG CLASS:

    CDK2 inhibitor

    Related drugs:
    2d
    CDK2 inhibition enhances CDK4/6 inhibitor antitumor activity in comprehensive breast cancer PDX model screen. (PubMed, NPJ Breast Cancer)
    Early clinical data demonstrated activity of BLU-222, a potent and selective CDK2 inhibitor, both as monotherapy (CCNE1 amplified) and in combination with ribociclib and fulvestrant in patients with HR+/HER2- breast cancer. These findings provide evidence that CDK2i combined with CDK4/6i can address multiple known mechanisms of resistance to CDK4/6i, enhancing antitumor responses in preclinical breast cancer models.
    Journal
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    HER-2 (Human epidermal growth factor receptor 2) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • RB1 (RB Transcriptional Corepressor 1) • CCND1 (Cyclin D1) • CCNE1 (Cyclin E1)
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    HR positive • HER-2 negative
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    Kisqali (ribociclib) • fulvestrant • cirtociclib (BLU-222)
    7d
    (VELA) Study of BLU-222 in Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=50, Terminated, Blueprint Medicines Corporation | Phase classification: P1/2 --> P1 | N=366 --> 50 | Trial completion date: Sep 2026 --> Jul 2025 | Active, not recruiting --> Terminated | Trial primary completion date: Nov 2025 --> Jul 2025; This trial was terminated prior to the initiation of Phase 2 for reasons not due to safety concerns.
    Phase classification • Enrollment change • Trial completion date • Trial termination • Trial primary completion date
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    HER-2 (Human epidermal growth factor receptor 2) • CCNE1 (Cyclin E1)
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    HER-2 negative
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    carboplatin • Kisqali (ribociclib) • fulvestrant • cirtociclib (BLU-222)
    9d
    FN-1501 Synergistically Enhances Almonertinib Efficacy in EGFR-TKI-Resistant Lung Adenocarcinoma through Ferroptosis Induction. (PubMed, Anticancer Agents Med Chem)
    FN-1501 exhibits significant antitumor activity and, when combined with Alm, effectively reverses EGFR-TKI resistance by inducing ferroptosis, highlighting its potential for clinical application.
    Journal
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    NCOA4 (Nuclear Receptor Coactivator 4)
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    Ameile (aumolertinib) • FN-1501
    30d
    Dual CDK and MEK Inhibition potentiates CD8+ T cell-mediated antitumor immunity by inducing pyroptotic cell death in high-mutational head and neck cancer. (PubMed, J Exp Clin Cancer Res)
    Our findings indicate that the combination of AZD5438 and PD0325901 holds therapeutic potential for the treatment of HPV (-) HNSCC, particularly in tumors with a high mutational burden. By targeting complementary pathways, this combination may improve treatment outcomes in this aggressive cancer subtype.
    Journal • Tumor mutational burden
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    TMB (Tumor Mutational Burden) • CD8 (cluster of differentiation 8) • CASP8 (Caspase 8) • GSDME (Gasdermin E)
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    TMB-H
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    Gomekli (mirdametinib)
    1m
    A Study to Evaluate the Effect of Food on the Single-Dose Pharmacokinetics and a Drug-Drug Interaction Evaluation of Itraconazole and Rifampin on INCB123667 When Administered Orally to Healthy Adult Participants (clinicaltrials.gov)
    P1, N=51, Recruiting, Incyte Corporation | Completed --> Recruiting | N=15 --> 51 | Trial completion date: May 2025 --> Mar 2026 | Trial primary completion date: May 2025 --> Feb 2026
    Enrollment open • Enrollment change • Trial completion date • Trial primary completion date
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    itraconazole • rifampicin
    1m
    BG-68501-101: A Study to Examine the Safety of Different Doses of BG-68501 Given to Participants With Advanced-Stage Tumors (clinicaltrials.gov)
    P1, N=258, Recruiting, BeiGene | Trial completion date: Feb 2028 --> Jul 2028
    Trial completion date
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    fulvestrant
    1m
    INCB123667-103: Study Assessing the Mass Balance, Pharmacokinetics, and Metabolite Profiles of a Single Oral Dose of [14C]-INCB123667 in Healthy Male Participants (clinicaltrials.gov)
    P1, N=9, Recruiting, Incyte Corporation | Not yet recruiting --> Recruiting
    Enrollment open
    2ms
    Study Assessing the Mass Balance, Pharmacokinetics, and Metabolite Profiles of a Single Oral Dose of [14C]-INCB123667 in Healthy Male Participants (clinicaltrials.gov)
    P1, N=9, Not yet recruiting, Incyte Corporation
    New P1 trial
    2ms
    MAESTRA 2: Study to Evaluate INCB123667 Versus Investigator's Choice of Chemotherapy in Participants With Platinum-Resistant Ovarian Cancer With Cyclin E1 Overexpression (clinicaltrials.gov)
    P3, N=466, Not yet recruiting, Incyte Corporation
    New P3 trial • Platinum resistant
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    gemcitabine • paclitaxel • pegylated liposomal doxorubicin • topotecan
    2ms
    Design, synthesis, and activity evaluation of selective CDK9 inhibitors containing indazole fragments. (PubMed, Bioorg Chem)
    This study designed and synthesized two series (A and B) of 28 unreported compounds based on rational structural modification of the lead compound AZD5438...Mechanistic studies demonstrated that B11 induces apoptosis in HCT116 cells by elevating intracellular ROS levels through suppression of anti-apoptotic protein expression and activating the caspase-3 pathway. In conclusion, compound B11 may serve as a novel selective CDK9 inhibitor worthy of further development for colorectal cancer treatment.
    Journal
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    CASP3 (Caspase 3)
    2ms
    NKT3447-101: A Study With NKT3447 for Adults With Advanced/Metastatic Solid Tumors (clinicaltrials.gov)
    P1, N=23, Terminated, NiKang Therapeutics, Inc. | N=90 --> 23 | Trial completion date: Mar 2027 --> Apr 2025 | Active, not recruiting --> Terminated | Trial primary completion date: Nov 2025 --> Apr 2025; This study was terminated as a result of Sponsor portfolio reprioritization.
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date • First-in-human
    3ms
    Study of AVZO-023 as a Single Agent and in Combination With AVZO-021, and/or Endocrine Therapy in Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=380, Recruiting, Avenzo Therapeutics, Inc. | Not yet recruiting --> Recruiting
    Enrollment open
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    fulvestrant • letrozole • AVZO-021