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    DRUG:

    LY3410738

    i
    Other names: LY3410738, LY 3410738, LY-3410738
    Company:
    Eli Lilly
    Drug class:
    IDH1 inhibitor, IDH2 inhibitor
    Related drugs:
    5ms
    A Study Comparing Different Formulations of LY3410738 in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=60, Completed, Eli Lilly and Company
    New P1 trial
    |
    LY3410738
    5ms
    A Study of LY3410738 in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=42, Completed, Eli Lilly and Company
    New P1 trial
    |
    LY3410738
    12ms
    Study of Oral LY3410738 in Patients With Advanced Hematologic Malignancies With IDH1 or IDH2 Mutations (clinicaltrials.gov)
    P1, N=260, Active, not recruiting, Eli Lilly and Company | Trial primary completion date: May 2024 --> Aug 2023
    Trial primary completion date • Metastases
    |
    IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2)
    |
    IDH2 mutation • IDH1 R132 • IDH2 R140 • IDH2 R172
    |
    Venclexta (venetoclax) • azacitidine • LY3410738
    12ms
    Study of LY3410738 Administered to Patients With Advanced Solid Tumors With IDH1 or IDH2 Mutations (clinicaltrials.gov)
    P1, N=200, Active, not recruiting, Eli Lilly and Company | Trial completion date: May 2023 --> May 2024 | Trial primary completion date: May 2023 --> Aug 2023
    Trial completion date • Trial primary completion date • Metastases
    |
    IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2)
    |
    IDH2 mutation • IDH1 R132 • IDH2 R140 • IDH2 R172
    |
    cisplatin • Imfinzi (durvalumab) • gemcitabine • LY3410738
    1year
    Study of Oral LY3410738 in Patients With Advanced Hematologic Malignancies With IDH1 or IDH2 Mutations (clinicaltrials.gov)
    P1, N=260, Active, not recruiting, Eli Lilly and Company | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    |
    IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2)
    |
    IDH2 mutation • IDH1 R132 • IDH2 R140 • IDH2 R172
    |
    Venclexta (venetoclax) • azacitidine • LY3410738
    1year
    Study of LY3410738 Administered to Patients With Advanced Solid Tumors With IDH1 or IDH2 Mutations (clinicaltrials.gov)
    P1, N=200, Active, not recruiting, Eli Lilly and Company | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    |
    IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2)
    |
    IDH2 mutation • IDH1 R132 • IDH2 R140 • IDH2 R172
    |
    cisplatin • Imfinzi (durvalumab) • gemcitabine • LY3410738
    over1year
    Study of LY3410738 Administered to Patients With Advanced Solid Tumors With IDH1 or IDH2 Mutations (clinicaltrials.gov)
    P1, N=200, Recruiting, Eli Lilly and Company | Trial completion date: Sep 2023 --> May 2023
    Trial completion date • Metastases
    |
    IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2)
    |
    IDH1 mutation • IDH2 mutation • IDH1 R132 • IDH2 R140 • IDH2 R172
    |
    cisplatin • Imfinzi (durvalumab) • gemcitabine • LY3410738
    over1year
    Study of Oral LY3410738 in Patients With Advanced Hematologic Malignancies With IDH1 or IDH2 Mutations (clinicaltrials.gov)
    P1, N=260, Recruiting, Eli Lilly and Company | Trial completion date: Mar 2023 --> May 2024 | Trial primary completion date: Mar 2023 --> May 2024
    Trial completion date • Trial primary completion date
    |
    IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2)
    |
    IDH2 mutation • IDH1 R132 • IDH2 R140 • IDH2 R172
    |
    Venclexta (venetoclax) • azacitidine • LY3410738
    over1year
    Secondary IDH1 resistance mutations and oncogenic IDH2 mutations cause acquired resistance to ivosidenib in cholangiocarcinoma. (PubMed, NPJ Precis Oncol)
    The irreversible mutant IDH1 inhibitor LY3410738 binds and blocks (R)-2HG production and cellular transformation by IDH1 R132H/D279N. These resistance mechanisms suggest that IDH1-mutated cholangiocarcinomas remain dependent on (R)-2HG even after prolonged ivosidenib treatment. Sequential mutant IDH inhibitor therapy should be explored as a strategy to overcome acquired resistance to mutant IDH inhibitors.
    Preclinical • Journal
    |
    IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2)
    |
    IDH1 mutation • IDH2 mutation • IDH1 R132H • IDH1 R132C • IDH1 R132
    |
    Tibsovo (ivosidenib) • LY3410738
    2years
    Study of Oral LY3410738 in Patients With Advanced Hematologic Malignancies With IDH1 or IDH2 Mutations (clinicaltrials.gov)
    P1, N=220, Recruiting, Eli Lilly and Company | Trial completion date: Sep 2023 --> Mar 2023
    Trial completion date
    |
    IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2)
    |
    IDH2 mutation • IDH1 R132 • IDH2 R140 • IDH2 R172
    |
    LY3410738
    over3years
    [VIRTUAL] A phase I study of LY3410738, a first-in-class covalent inhibitor of mutant IDH1 in cholangiocarcinoma and other advanced solid tumors. (ASCO-GI 2021)
    The primary objective for dose expansion is to assess the preliminary anti-tumor activity by ORR of LY3410738 when administered alone or in combination with cisplatin plus gemcitabine. Cohort 3 will enroll patients with advanced solid tumors who have non-measurable disease and received standard therapies. Cohort 4 will enroll CCA patients with measurable disease who are treatment naïve for advanced disease.
    P1 data
    |
    IDH1 (Isocitrate dehydrogenase (NADP(+)) 1)
    |
    IDH1 mutation
    |
    cisplatin • gemcitabine • LY3410738
    over3years
    [VIRTUAL] A Phase 1 Study of LY3410738, a First-in-Class Covalent Inhibitor of Mutant IDH in Advanced Myeloid Malignancies (Trial in Progress) (ASH 2020)
    Reversible inhibitors of IDH1 (ivosidenib) and IDH2 (enasidenib) are currently approved and achieve response rates of ~40%, with median duration of response of <1 year in the approved relapsed AML setting. Approximately 80 patients (20 patients per cohort) will be enrolled in the 4 exp cohorts. The study is planned to enroll patients in late 2020.
    P1 data • IO biomarker
    |
    IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2)
    |
    IDH1 mutation • IDH2 mutation
    |
    Tibsovo (ivosidenib) • Idhifa (enasidenib) • LY3410738
    over3years
    Study of Oral LY3410738 in Patients With Advanced Hematologic Malignancies With IDH1 or IDH2 Mutations (clinicaltrials.gov)
    P1, N=220, Recruiting, Loxo Oncology, Inc.
    Clinical • New P1 trial
    |
    IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2)
    |
    IDH2 mutation • IDH2 R140 • IDH2 R172
    |
    LY3410738
    over3years
    Study of LY3410738 Administered to Patients With Advanced Solid Tumors With IDH1 Mutations (clinicaltrials.gov)
    P1, N=180, Recruiting, Loxo Oncology, Inc.
    Clinical • New P1 trial
    |
    IDH1 (Isocitrate dehydrogenase (NADP(+)) 1)
    |
    IDH1 mutation
    |
    LY3410738