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Study of Oral LY3410738 in Patients With Advanced Hematologic Malignancies With IDH1 or IDH2 Mutations

Phase 1
Active, not recruiting
Conditions
Myelodysplastic Syndrome (MDS)
Myeloproliferative Neoplasms (MPNs)
Acute Myeloid Leukemia (AML)
Chronic Myelomonocytic Leukemia (CMML)
Interventions
Registration Number
NCT04603001
Lead Sponsor
Eli Lilly and Company
Brief Summary

This is an open-label, multi-center Phase 1 study of LY3410738, an oral, covalent isocitrate dehydrogenase (IDH) inhibitor, in patients with IDH1 and/or IDH2-mutant advanced hematologic malignancies who may have received standard therapy

Detailed Description

This study includes 2 parts: dose escalation and dose expansion. The dose escalation will enroll eligible patients with select IDH-mutant advanced hematologic malignancies. Once the maximum tolerated dose (MTD) and/or recommended Phase 2 dose (RP2D) of LY3410738 is established, the dose expansion will begin and enroll into 5 cohorts to further evaluate safety and clinical activity

Recruitment & Eligibility

Status
ACTIVE_NOT_RECRUITING
Sex
All
Target Recruitment
260
Inclusion Criteria
  • Advanced IDH mutant hematologic malignancy including:

    -- For Dose Escalation Arm C and Dose Expansion Cohort 5:

    • Patients with newly diagnosed AML who are 75 years or older or have comorbidities that preclude the use of intensive chemotherapy
    • Patients with R/R AML (US only)
  • Patients must have received prior therapy

  • Blasts at least 5% in bone marrow.

  • Patients must have a qualifying IDH1 R132, IDH2 R140 or IDH2 R172 mutation

  • Eastern Cooperative Oncology Group (ECOG) 0 to 2

  • Adequate organ function

  • Ability to swallow capsules or tablets

  • Ability to comply with outpatient treatment, laboratory monitoring, and required clinic visits for the duration of study participation

  • Willingness of men and women of reproductive potential to observe conventional and effective birth control for the duration of treatment and for 3 months following the last dose of study treatment.

Exclusion Criteria
  • Investigational agent or anticancer therapy within 2 weeks or 5 half-lives, whichever is shorter; or investigational monoclonal antibody within 4 weeks prior to planned start of LY3410738

  • For Dose Escalation Arm C and Dose Expansion Cohort 5:

    • Prior venetoclax treatment is not allowed.
    • Patients are allowed to receive up to 1 cycle of single agent azacitidine or azacitidine plus venetoclax while waiting for results of locally obtained molecular profiling, including IDH1/IDH2 mutational status, prior to starting on study.
  • Major surgery within 4 weeks prior to planned start of LY3410738.

  • Active, uncontrolled clinically significant systemic bacterial, viral, fungal or parasitic infection or an unexplained fever > 38.5ÂșC during Screening or on the first day of study drug administration.

  • Another concurrent malignancy requiring active therapy.

  • Active central nervous system involvement

  • Any unresolved toxicities from prior therapy greater than CTCAE v5.0 Grade 2 at the time of starting study treatment except for alopecia.

  • History of hematopoietic stem cell transplant (HSCT) or chimeric antigen receptor T-cell (CAR-T) therapy within 60 days of the first dose of LY3410738.

  • Clinically significant cardiovascular disease

  • Active hepatitis B virus (HBV)

  • Active hepatitis C virus (HCV)

  • Clinically significant active malabsorption syndrome or other condition likely to affect gastrointestinal (GI) absorption of the study drug

  • Current treatment with certain strong cytochrome P450 3A4 (CYP3A4) inhibitors or inducers and/or P- glycoprotein (P-gp) inhibitor, with the exception of patients being treated with allowed antifungal inhibitors of CYP3A4

  • Treatment with proton pump inhibitor (PPIs) within 7 days of starting LY3410738

  • Any serious underlying medical or psychiatric condition (e.g. alcohol or drug abuse), dementia or altered mental status or any issue that would impair the ability of the patient to understand informed consent or that in the opinion of the Investigator would contraindicate the patient's participation in the study or confound the results of the study

  • Known human immunodeficiency virus (HIV), excluded due to potential drug-drug interactions between antiretroviral medications and LY3410738

  • Pregnancy, lactation or plan to breastfeeding during the study or within 90 days of the last dose of study intervention

  • Known hypersensitivity to any of the components of LY3410738 or its formulation

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Cohort 2LY3410738Patients with R/R AML harboring an IDH1 R132 mutation who have not received a prior IDH inhibitor.
Dose Escalation Arm B (Monotherapy)LY3410738Patients requiring a strong CYP3A4 inhibitor for active management or prevention of a lifethreatening condition, such as an azole administered to prevent invasive fungal infection.
Cohort 1LY3410738Patients with relapsed/refractory (R/R) AML harboring an IDH1 R132 mutation who have received a prior IDH inhibitor.
Cohort 3LY3410738Patients with R/R MDS, chronic myelomonocytic leukemia (CMML) or other advanced hematologic malignancy harboring an IDH1 R132 mutation.
Dose Escalation Arm C (LY3410738, Venetoclax, and Azacitidine)LY3410738Patients with no prior venetoclax therapy and not requiring a strong CYP3A4 inhibitor for active treatment within 7 days of starting LY3410738.
Cohort 4LY3410738Patients with R/R AML, MDS, CMML or other advanced hematologic malignancy harboring IDH2 mutations.
Dose Escalation Arm A (Monotherapy)LY3410738Patients not requiring a strong cytochrome P450 3A4 (CYP3A4) inhibitor.
Cohort 5LY3410738Patients with newly diagnosed AML, R/R AML, or other advanced hematologic malignancy harboring IDH1 and/or IDH2 mutations with no prior venetoclax therapy. Strong CYP3A4 inhibitor allowed but not required.
Dose Escalation Arm C (LY3410738, Venetoclax, and Azacitidine)AzacitidinePatients with no prior venetoclax therapy and not requiring a strong CYP3A4 inhibitor for active treatment within 7 days of starting LY3410738.
Dose Escalation Arm C (LY3410738, Venetoclax, and Azacitidine)VenetoclaxPatients with no prior venetoclax therapy and not requiring a strong CYP3A4 inhibitor for active treatment within 7 days of starting LY3410738.
Cohort 5VenetoclaxPatients with newly diagnosed AML, R/R AML, or other advanced hematologic malignancy harboring IDH1 and/or IDH2 mutations with no prior venetoclax therapy. Strong CYP3A4 inhibitor allowed but not required.
Cohort 5AzacitidinePatients with newly diagnosed AML, R/R AML, or other advanced hematologic malignancy harboring IDH1 and/or IDH2 mutations with no prior venetoclax therapy. Strong CYP3A4 inhibitor allowed but not required.
Primary Outcome Measures
NameTimeMethod
To determine the maximum tolerated dose (MTD)/recommended Phase 2 dose (RP2D)Up to 30 months

For Dose Escalation

To assess the activity of LY3410738 as measured by the overall response rate (ORR) per the Investigator assessmentUp to 30 months

For Dose Expansion

Secondary Outcome Measures
NameTimeMethod
To assess the activity of LY3410738 as measured by the overall response rate (ORR) per Investigator assessmentUp to 30 months

For Dose Escalation

To assess the activity of LY3410738 by Complete Remission (CR) Rate (CRR) plus partial hematologic recovery (AML patients)Up to 30 months

For Dose Expansion

To characterize the pharmacodynamic properties of LY3410738 as expressed by change in 2-HG oncometabolite levels in plasmaUp to 30 months

For Dose Escalation

To characterize the pharmacokinetics (PK) properties of LY3410738 by collecting and evaluating serum at protocol specified time pointsUp to 30 months

For Dose Expansion

To determine the safety profile and tolerability of LY3410738 including acute and chronic toxicities by collecting and evaluating adverse events and treatment emergent adverse eventsUp to 30 months

For Dose Escalation

To assess the activity of LY3410738 as measured by Best Overall Response (BOR) per Investigator assessmentUp to 30 months

For Dose Expansion

To assess the activity of LY3410738 by Duration of ResponseUp to 30 months

For Dose Expansion

To assess the activity of LY3410738 by Hematologic improvement in patients with MDSUp to 30 months

For Dose Expansion

To determine the safety profile and tolerability of LY3410738 including acute and chronic toxicities by collecting and evaluating Adverse events and treatment emergent adverse eventsUp to 30 months

For Dose Expansion

To characterize the pharmacodynamic properties of LY3410738 as expressed by change in 2-HG oncometabolite levels in plasma.Up to 30 months

For Dose Expansion

Trial Locations

Locations (37)

Roswell Park Cancer Institute

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Buffalo, New York, United States

University of Chicago Hospital

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Chicago, Illinois, United States

Massachusetts General Hospital

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Boston, Massachusetts, United States

City of Hope National Medical Center

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Duarte, California, United States

The Alfred Hospital

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Melbourne, Victoria, Australia

Cliniques universitaires Saint-Luc

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Brussels, Belgium

Jewish General Hospital

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Montréal, Quebec, Canada

Rambam Medical Center

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Haifa, Israel

National Taiwan University Hospital

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Taipei, Taiwan

Singapore General Hospital

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Singapore, Singapore

Clinico Y Provincial Barcelona

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Barcelona, Spain

Asan Medical Center

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Seoul, Seoul-teukbyeolsi [Seoul], Korea, Republic of

National University Cancer Institute

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Singapore, Singapore

Hospital Universitario La Fe de Valencia

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Valencia, Spain

Samsung Medical Center

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Seoul, Seoul-teukbyeolsi [Seoul], Korea, Republic of

Seoul National University Hospital

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Seoul, Korea, Republic of

Hospital Universitario Fundación Jiménez Díaz

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Madrid, Spain

China Medical University Hospital

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Taichung City, Taiwan

Vanderbilt University Medical Center

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Nashville, Tennessee, United States

University of California, Davis - Health Systems

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Sacramento, California, United States

H Lee Moffitt Cancer Center

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Tampa, Florida, United States

UCLA Medical Center

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Los Angeles, California, United States

Northwestern University

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Chicago, Illinois, United States

Memorial Sloan Kettering Cancer Center

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New York, New York, United States

University of North Carolina at Chapel Hill

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Chapel Hill, North Carolina, United States

Peter MacCallum Cancer Centre

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Melbourne, Victoria, Australia

University of Texas MD Anderson Cancer Center

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Houston, Texas, United States

Linear Clinical Research

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Nedlands, Western Australia, Australia

BC Cancer Vancouver

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Vancouver, British Columbia, Canada

Helsinki University Hospital - Comprehensive Cancer Center (HYKS - SyöpÀkeskus)

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Helsinki, Finland

Institut Paoli-Calmettes

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Marseille, France

Princess Margaret Hospital

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Toronto, Ontario, Canada

Hopital Saint Louis

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Paris, France

Centre hospitalier universitaire de Haut Leveque

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Pessac Cedex, France

Centre Hospitalier Lyon Sud

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Pierre Benite Cedex, France

Institut Claudius Regaud

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Toulouse cedex 9, France

Medizinische Hochschule Hanover

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Hannover, Niedersachsen, Germany

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