^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    DRUG CLASS:

    CDK2 inhibitor

    Related drugs:
    3d
    INCB123667-305: Phase 3 Study of INCB123667 Versus Investigator's Choice of Chemotherapy in Platinum Resistant Ovarian Cancer With Cyclin E1 Overexpression (2025-522748-42-00)
    P2/3, N=108, Not yet recruiting, Incyte Corp.
    New P2/3 trial • Platinum resistant
    |
    FOLR1 ( Folate receptor alpha )
    |
    FOLR1 expression
    |
    gemcitabine • paclitaxel • pegylated liposomal doxorubicin • topotecan
    3d
    CGVV858A12101: Study of GVV858 as a single agent or in combination with endocrine therapy in patients with HR+/HER2- breast cancer and other advanced solid tumors (2025-521911-38-00)
    P1/2, N=26, Not yet recruiting, Novartis Pharma AG
    New P1/2 trial
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    fulvestrant • letrozole • goserelin acetate • leuprolide acetate for depot suspension
    9d
    PF-07104091 as a Single Agent and in Combination Therapy (clinicaltrials.gov)
    P2, N=157, Active, not recruiting, Pfizer | Trial completion date: Mar 2026 --> Dec 2026 | Trial primary completion date: Mar 2026 --> Dec 2026
    Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive • HR positive • HER-2 negative • HR positive + HER-2 negative
    |
    Ibrance (palbociclib) • fulvestrant • letrozole • tegtociclib (PF-07104091)
    9d
    Study of ZE94-0605 in Patients With Advanced Solid Tumors, With Dose Expansion Cohorts. (clinicaltrials.gov)
    P1, N=60, Not yet recruiting, Eilean Therapeutics
    New P1 trial
    |
    CCNE1 (Cyclin E1)
    16d
    MAESTRA 1: A Study of INCB123667 in Participants With Platinum-Resistant Ovarian Cancer With Cyclin E1 Overexpression (clinicaltrials.gov)
    P2, N=160, Recruiting, Incyte Corporation
    Trial initiation date • Platinum resistant
    |
    FOLR1 ( Folate receptor alpha )
    21d
    INX-315-01: Open-Label Study to Evaluate the Safety, Tolerability, PK, and Efficacy of INX-315 in Patients With Advanced Cancer (clinicaltrials.gov)
    P1/2, N=150, Recruiting, Incyclix Bio | Trial completion date: Jun 2026 --> Sep 2027 | Trial primary completion date: Dec 2025 --> Jul 2027
    Trial completion date • Trial primary completion date • First-in-human
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    Verzenio (abemaciclib) • fulvestrant • INX-315
    2ms
    CYCAD-1: A First-in-human Dose Escalation and Expansion Study to Evaluate the Safety, and Tolerability of AZD8421 Alone or in Combination in Participants With Selected Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
    P1/2, N=564, Recruiting, AstraZeneca | Trial completion date: Aug 2026 --> Aug 2027 | Trial primary completion date: Aug 2026 --> Aug 2027
    Trial completion date • Trial primary completion date • First-in-human
    |
    Ibrance (palbociclib) • Verzenio (abemaciclib) • Kisqali (ribociclib) • camizestrant (AZD9833)
    2ms
    INCB123667-203: Phase 2 Study of INCB123667 in Platinum-Resistant Ovarian Cancer With Cyclin E1 Overexpression (2025-521513-14-00)
    P1/2, N=29, Recruiting, Incyte Corp.
    New P1/2 trial • Platinum resistant
    |
    CCNE1 (Cyclin E1) • FOLR1 ( Folate receptor alpha )
    |
    FOLR1 expression
    3ms
    Pro-Tumorigenic Roles of Cyclin Dependent Kinase 2 and its Associated Cyclins in Cholangiocarcinoma Progression under High Glucose Condition. (PubMed, Arch Med Res)
    CCA cells with upregulated CDK2 and its cyclin partners in HG were more sensitive to tagtociclib at a higher dose. Cyclin E and cyclin A also regulated CCA metastasis by controlling epithelial-mesenchymal transition. Targeting CDK2 and its associated cyclins in CCA cells demonstrated therapeutic potential that requires further translational and clinical verification.
    Journal
    |
    CCNA2 (Cyclin A2) • CDK2 (Cyclin-dependent kinase 2)
    |
    tegtociclib (PF-07104091)
    3ms
    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, Recruiting, Incyte Corporation | Not yet recruiting --> Recruiting
    Enrollment open • Platinum resistant
    |
    FOLR1 ( Folate receptor alpha )
    |
    gemcitabine • paclitaxel • pegylated liposomal doxorubicin • topotecan
    3ms
    CDK2 inhibitor BLU-222 synergizes with CDK4/6 inhibitors in drug resistant breast cancers through p21/p27 induction. (PubMed, Nat Commun)
    In vivo, combining BLU-222 with palbociclib or ribociclib produced significant antitumor activity across eight resistant models, driving durable tumor regression and prolonged survival. CRISPR knockout of p21 or p27 in palbociclib-resistant cells eliminated this synergy. Further, RNA sequencing revealed that combination treatment upregulated senescence and interferon pathways, providing mechanistic insight into the observed therapeutic synergy.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
    |
    HR positive • HER-2 negative • HR positive + HER-2 negative
    |
    Ibrance (palbociclib) • Kisqali (ribociclib) • cirtociclib (BLU-222)
    3ms
    CYCAD-1: A First-in-human Dose Escalation and Expansion Study to Evaluate the Safety, and Tolerability of AZD8421 Alone or in Combination in Participants With Selected Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
    P1/2, N=564, Recruiting, AstraZeneca | N=348 --> 564
    Enrollment change • First-in-human
    |
    Ibrance (palbociclib) • Verzenio (abemaciclib) • Kisqali (ribociclib) • camizestrant (AZD9833)