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    DRUG:

    LY3405105

    i
    Other names: LY-3405105, LY3405105
    Associations

    News

    Trials
    Company:
    Eli Lilly
    Drug class:
    CDK7 inhibitor
    Related drugs:
    Associations

    News

    Trials
    10ms
    A Phase I Dose-Escalation Study of LY3405105, a Covalent Inhibitor of Cyclin-Dependent Kinase 7, Administered to Patients With Advanced Solid Tumors. (PubMed, Oncologist)
    The MTD of LY3405105 monotherapy was 20 mg QD. The most common toxicities were gastrointestinal adverse events, myelosuppression, fatigue, and asthenia. Limited clinical activity was observed in this phase I trial, and there are no plans for further development.
    P1 data • Journal • Metastases
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    CDK7 (Cyclin Dependent Kinase 7)
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    LY3405105
    1year
    Discovery of XNW9015, a potent, selective, and CNS-penetrating covalent inhibitor of CDK7 with excellent in vivo antitumor activities (AACR 2023)
    In the Palbociclib-resistant breast cancer cell line MCF-7, XNW9015 exhibited antiproliferative activity, with an IC50 of 81nM, while neither Palbociclib nor Fulvestrant can inhibit the cell viability...XNW9015 exhibited superior rodent pharmacokinetic characteristics when compared to LY3405105 (Eli Lilly and Company, WO2019099298)...In summary, XNW9015 has demonstrated potent in vitro and in vivo antitumor effects, favorable pharmacokinetic and toxicological properties. XNW9015 has become a potential clinical candidate for cancer therapeutics, both as monotherapies and in combination settings.
    Preclinical
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    CDK12 (Cyclin dependent kinase 12) • CDK2 (Cyclin-dependent kinase 2) • CDK7 (Cyclin Dependent Kinase 7) • CDK9 (Cyclin Dependent Kinase 9) • CDK1 (Cyclin-dependent kinase 1)
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    Ibrance (palbociclib) • fulvestrant • LY3405105 • XNW9015
    over2years
    A Study of LY3405105 in Participants With Advanced Cancer (clinicaltrials.gov)
    P1a/1b, N=54, Terminated, Eli Lilly and Company | Completed --> Terminated; The study was terminated for lack of sufficient efficacy.
    Clinical • Trial termination
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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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    SMARCB1 mutation
    |
    LY3405105
    3years
    A Study of LY3405105 in Participants With Advanced Cancer (clinicaltrials.gov)
    P1a/1b, N=55, Completed, Eli Lilly and Company | Active, not recruiting --> Completed | N=180 --> 55 | Trial completion date: Jun 2021 --> Feb 2021
    Clinical • Trial completion • Enrollment change • Trial completion date
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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)
    |
    SMARCB1 mutation
    |
    LY3405105
    over3years
    A Study of LY3405105 in Participants With Advanced Cancer (clinicaltrials.gov)
    P1a/1b, N=180, Active, not recruiting, Eli Lilly and Company | Recruiting --> Active, not recruiting
    Clinical • Enrollment closed
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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)
    |
    SMARCB1 mutation
    |
    LY3405105
    over3years
    A Study of LY3405105 in Participants With Advanced Cancer (clinicaltrials.gov)
    P1a/1b, N=180, Recruiting, Eli Lilly and Company | Trial completion date: May 2022 --> Jun 2021 | Trial primary completion date: May 2022 --> Jan 2021
    Clinical • Trial completion date • Trial primary completion date
    |
    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)
    |
    SMARCB1 mutation
    |
    LY3405105