First in Human Study of Ziftomenib in Relapsed or Refractory Acute Myeloid Leukemia

NCT ID: NCT04067336

Last Updated: 2025-11-10

Study Results

Results pending

The study team has not published outcome measurements, participant flow, or safety data for this trial yet. Check back later for updates.

Basic Information

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Recruitment Status

RECRUITING

Clinical Phase

PHASE1/PHASE2

Total Enrollment

263 participants

Study Classification

INTERVENTIONAL

Study Start Date

2019-09-12

Study Completion Date

2028-10-16

Brief Summary

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In this trial, ziftomenib, a menin-MLL(KMT2A) inhibitor, will be tested in patients for the first time. The trial includes a Main Study and four sub-studies. In the Main Study (including Phase 1a, Phase 1b, and Phase 2 portions), ziftomenib will be evaluated in patients with relapsed or refractory (R/R) acute myeloid leukemia (AML). The main study has completed enrollment.

In Sub-studies 1 and 2, the effects of taking ziftomenib and other common drugs at the same time will be investigated in AML patients. In Sub-study 3, ziftomenib will be evaluated in patients with R/R acute lymphoblastic leukemia (ALL). In Sub-study 4, ziftomenib will be evaluated in patients with R/R AML with certain genetic mutations.

Detailed Description

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This first-in-human (FIH), open-label study will assess ziftomenib, a menin-MLL(KMT2A) inhibitor, in patients with relapsed or refractory (R/R) acute myeloid leukemia (AML). The trial includes a Main Study and four sub-studies.

The Main Study is a Phase 1/2 dose-escalation and dose-validation/expansion study to assess ziftomenib in patients with R/R AML. The dose-escalation part of the study (Phase 1a) will determine the maximum tolerated dose (MTD) and/or the recommended Phase 2 dose (RP2D). The dose-validation/expansion part of the study (Phase 1b) will determine the safety, tolerability, and minimal biologically effective dose (MBED) of ziftomenib in biomarker-specific dosing cohorts from among doses that demonstrated early biological activity and are determined to be safe in the dose-escalation phase. The Phase 2 portion of the study will determine the safety, tolerability, and anti-leukemia activity of ziftomenib in patients with nucleophosmin 1-mutant (NPM1-m) AML.

In Sub-study 1, the effects of co-administration of ziftomenib on the pharmacokinetics (PK) of midazolam will be studied in patients with R/R AML with certain genetic mutations.

In Sub-study 2, the effects of co-administration of itraconazole on the PK of ziftomenib will be studied in patients with R/R AML with certain genetic mutations.

In Sub-study 3, the safety, tolerability, and MBED/RP2D of ziftomenib will be studied in patients with R/R KMT2A-rearranged (KMT2A-r) ALL (Phase 1a dose escalation). These parameters will be investigated further for the RP2D in a Phase 1b dose-validation/cohort expansion part of the sub-study.

In Sub-study 4, the clinical activity of ziftomenib will be studied in patients with R/R AML with certain genetic mutations.

Conditions

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Advanced Malignant Neoplasm Acute Myeloid Leukemia Mixed Lineage Leukemia Mixed Lineage Acute Leukemia Acute Leukemia of Ambiguous Lineage Mixed Phenotype Acute Leukemia Acute Lymphoblastic Leukemia

Keywords

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AML Hematological malignancy KMT2A NPM1 Menin Leukemia Acute Leukemia ALL MLL Acute Lymphoblastic Leukemia Acute Myeloid Leukemia MEIS1

Study Design

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Allocation Method

RANDOMIZED

Intervention Model

PARALLEL

Primary Study Purpose

TREATMENT

Blinding Strategy

NONE

Study Groups

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Phase 2

NPM1-m R/R AML patients will receive the recommended phase 2 ziftomenib dose

Group Type EXPERIMENTAL

Ziftomenib

Intervention Type DRUG

Oral administration

Sub-study 1

R/R AML patients with mutations associated with MEIS1 overexpression will receive ziftomenib + midazolam

Group Type EXPERIMENTAL

Ziftomenib

Intervention Type DRUG

Oral administration

Midazolam

Intervention Type DRUG

Oral administration

Sub-study 2

R/R AML patients with mutations associated with MEIS1 overexpression will receive ziftomenib + itraconazole

Group Type EXPERIMENTAL

Ziftomenib

Intervention Type DRUG

Oral administration

Itraconazole

Intervention Type DRUG

Oral administration

Sub-study 3

Part 1a: KMT2A-r R/R ALL patients will receive multiple ziftomenib doses

Part 1b: KMT2A-r R/R ALL patients will receive ziftomenib

Group Type EXPERIMENTAL

Ziftomenib

Intervention Type DRUG

Oral administration

Sub-study 4

R/R AML patients with mutations associated with MEIS1 overexpression will receive ziftomenib

Group Type EXPERIMENTAL

Ziftomenib

Intervention Type DRUG

Oral administration

Phase 1a - Dose Escalation

AML patients will receive multiple doses of ziftomenib

Group Type EXPERIMENTAL

Ziftomenib

Intervention Type DRUG

Oral administration

Phase 1b - Dose-Validation Expansion

Cohort 1: KMT2A-r / NPM1-m R/R AML patients will receive ziftomenib

Cohort 2: KMT2A-r / NPM1-m R/R AML patients will receive ziftomenib

Group Type EXPERIMENTAL

Ziftomenib

Intervention Type DRUG

Oral administration

Interventions

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Ziftomenib

Oral administration

Intervention Type DRUG

Midazolam

Oral administration

Intervention Type DRUG

Itraconazole

Oral administration

Intervention Type DRUG

Other Intervention Names

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KO-539 Seizalam Hypnovel Dormicum Sporanox Onmel Tolsura

Eligibility Criteria

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Inclusion Criteria

Patients with refractory or relapsed AML defined as the reappearance of ≥ 5% blasts in the bone marrow and who have also failed or are ineligible for any approved standard of care therapies, including HSCT.

1. Phase 1b:

* Patients with a documented lysine\[K\]-specific methyltransferase 2-rearrangement (KMT2A-r), or
* Patients with a documented nucleophosmin 1 mutation (NPM1-m)
2. Phase 2:

* Patients with a documented nucleophosmin 1 mutation (NPM1-m)
3. Sub-studies:

* Sub-studies 1 and 2: Patients with R/R AML with NPM1-m or other mutations associated with MEIS1 overexpression.
* Sub-study 3: Patients with R/R Acute Lymphoblastic Leukemia (ALL) with KMT2A-r.
* Sub-study 4: Patients with R/R AML with mutations associated with MEIS1 overexpression.
4. ≥ 18 years of age.
5. Eastern Cooperative Oncology Group (ECOG) performance status of 0 to 2, and a life expectancy of at least 2 months.
6. Adequate liver and kidney function according to protocol requirements.
7. Peripheral white blood cell (WBC) counts ≤ 30,000/μL. Patients may receive hydroxyurea to control and maintain white blood cell count prior to enrollment.
8. Women of childbearing potential must be willing to use a highly effective method of contraception throughout the study and for at least 187 days after the last dose of study treatment.
9. Males with female partners of childbearing potential must agree to use a highly effective method of contraception throughout the study and for at least 97 days after the last dose of study treatment.

Exclusion Criteria

1. Diagnosis of acute promyelocytic leukemia.
2. Diagnosis of chronic myelogenous leukemia in blast crisis.
3. Donor lymphocyte infusion \< 30 days prior to study entry.
4. Clinically active central nervous system (CNS) leukemia.
5. Undergone HSCT and have not had adequate hematologic recovery.
6. Receiving immunosuppressive therapy post HSCT within 2 weeks of Cycle 1 Day 1.
7. Grade ≥ 2 active graft-versus-host disease (GVHD), moderate or severe limited chronic GVHD, or extensive chronic GVHD of any severity.
8. Received chemotherapy immunotherapy, radiotherapy, or any ancillary therapy that is considered to be investigational (i.e., used for non-approved indications(s) and in the context of a research investigation) \< 14 days prior to the first dose of ziftomenib or within 5 drug half-lives prior to the first dose of study drug.
9. Not recovered to \< Grade 2 (National Cancer Institute Common Terminology Criteria for Adverse Events v5.0) from all acute toxicities or deemed back to a stable baseline.
10. Treatment with concomitant drugs that are strong inhibitors or inducers of cytochrome P450-isozyme 3A4 (CYP3A4), as follows:

* Phase 1a, 1b, 2, and sub-studies 3 and 4: with the exception of antibiotics, antifungals, and antivirals that are used as standard of care or to prevent or treat infections and other such drugs that are considered absolutely essential for the care of the patient.
* Sub-studies 1 and 2: No exceptions will be allowed except for the use of moderate CYP3A4 antifungal prophylaxis such as fluconazole or isavuconazole which is at steady state on Cycle 1 Day 1 and will continue through the completion of PKs on Cycle 1 Day 15 (for sub-study 1) or Cycle 1 Day 18 (for sub-study 2).
11. Detectable viral load for human immunodeficiency virus, hepatitis C, or hepatitis B surface antigen indicative of active infection. Patients with controlled disease will not be excluded from study enrollment.
12. Pre-existing disorder predisposing the patient to a serious or life-threatening infection (e.g. cystic fibrosis, congenital or acquired immunodeficiency, bleeding disorder, or cytopenias not related to AML).
13. Active uncontrolled acute or chronic systemic fungal, bacterial, viral, or other infection.
14. Significant cardiovascular disease including unstable angina pectoris, uncontrolled hypertension or arrhythmia, history of cerebrovascular accident including transient ischemic attack within the past 6 months, congestive heart failure (NYHA Class III or IV) related to primary cardiac disease, ischemic or severe valvular heart disease, or a myocardial infarction within 6 months prior to the first dose of study treatment.
15. Mean QTcF \>480 ms on triplicate ECG.
16. Major surgery within 4 weeks prior to the first dose of study treatment.
17. Women who are pregnant or lactating. All female patients with reproductive potential must have a negative serum pregnancy test within 72 hours prior to starting treatment.
18. For sub-studies 1 and 2: Any intake of grapefruit, grapefruit juice, Seville oranges, Seville orange marmalade, or other products containing grapefruit or Seville oranges within 7 days of the first administration of ziftomenib until the end of Cycle 1.
19. For sub-studies 1 and 2: Moderate (Child-Pugh class B) or severe (Child-Pugh class C) hepatic impairment.
Minimum Eligible Age

18 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

No

Sponsors

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Kura Oncology, Inc.

INDUSTRY

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Locations

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Banner MD Anderson Cancer Center

Gilbert, Arizona, United States

Site Status RECRUITING

Mayo Clinic

Phoenix, Arizona, United States

Site Status WITHDRAWN

University of Southern California

Los Angeles, California, United States

Site Status WITHDRAWN

UCLA Ronald Reagan Medical Center

Los Angeles, California, United States

Site Status RECRUITING

Mayo Clinic

Jacksonville, Florida, United States

Site Status ACTIVE_NOT_RECRUITING

Robert H. Lurie Comprehensive Cancer Center of Northwestern University

Chicago, Illinois, United States

Site Status RECRUITING

Indiana University Melvin and Bren Simon Comprehensive Cancer Center

Indianapolis, Indiana, United States

Site Status WITHDRAWN

University of Maryland Greenebaum Comprehensive Cancer Center

Baltimore, Maryland, United States

Site Status RECRUITING

Massachusetts General Hospital

Boston, Massachusetts, United States

Site Status RECRUITING

University of Michigan Hospitals

Ann Arbor, Michigan, United States

Site Status RECRUITING

Karmanos Cancer Institute

Detroit, Michigan, United States

Site Status RECRUITING

Mayo Clinic

Rochester, Minnesota, United States

Site Status ACTIVE_NOT_RECRUITING

Hackensack University Medical Center - John Theurer Cancer Center

Hackensack, New Jersey, United States

Site Status RECRUITING

Roswell Park Comprehensive Cancer Center

Buffalo, New York, United States

Site Status RECRUITING

Weill Cornell Medical College - NY Presbyterian Hospital

New York, New York, United States

Site Status ACTIVE_NOT_RECRUITING

The Mount Sinai Hospital

New York, New York, United States

Site Status RECRUITING

Duke Cancer Institute

Durham, North Carolina, United States

Site Status ACTIVE_NOT_RECRUITING

Oklahoma University Health - Stephenson Cancer Center

Oklahoma City, Oklahoma, United States

Site Status RECRUITING

UPMC Hillman Cancer Center

Pittsburgh, Pennsylvania, United States

Site Status RECRUITING

Vanderbilt-Ingram Cancer Center

Nashville, Tennessee, United States

Site Status ACTIVE_NOT_RECRUITING

Harold C. Simmons Comprehensive Cancer Center - UT Southwestern Medical Center

Dallas, Texas, United States

Site Status RECRUITING

MD Anderson Cancer Center

Houston, Texas, United States

Site Status RECRUITING

Fred Hutchinson Cancer Research Center

Seattle, Washington, United States

Site Status RECRUITING

UZ Brussel

Jette, , Belgium

Site Status WITHDRAWN

AZ Delta - Campus Rumbeke

Roeselare, , Belgium

Site Status RECRUITING

CHU UCL Namur

Yvoir, , Belgium

Site Status RECRUITING

Queen Elizabeth II Health Sciences Centre

Halifax, Nova Scotia, Canada

Site Status ACTIVE_NOT_RECRUITING

McMaster University Juravinski Cancer Centre

Hamilton, Ontario, Canada

Site Status WITHDRAWN

Hopital Maisonneuve-Rosemont

Montreal, Quebec, Canada

Site Status ACTIVE_NOT_RECRUITING

Hopital de l'Enfant-Jesus - Centre Integre en Cancerologie du CHU de Quebec - Universite Laval

Québec, Quebec, Canada

Site Status ACTIVE_NOT_RECRUITING

Centre Hospitalier Universitaire de Lille

Lille, , France

Site Status RECRUITING

Centre Hospitalier Universitaire de Nantes

Nantes, , France

Site Status RECRUITING

Hopital Saint Louis

Paris, , France

Site Status RECRUITING

Magendie Hopital Haut-Leveque

Pessac, , France

Site Status RECRUITING

Centre Hospitalier Lyon Sud

Pierre-Bénite, , France

Site Status RECRUITING

Institut Gustave Roussy

Villejuif, , France

Site Status RECRUITING

Charitè-Campus Benjamin Franklin

Berlin, , Germany

Site Status WITHDRAWN

University Medicine Greifswald

Greifswald, , Germany

Site Status ACTIVE_NOT_RECRUITING

Medizinische Hochsschule Hannover

Hanover, , Germany

Site Status ACTIVE_NOT_RECRUITING

Johannes Gutenberg - University Mainz

Mainz, , Germany

Site Status WITHDRAWN

Institute of Hematology and Medical Oncology "L. and A. Seragnoli"

Bologna, , Italy

Site Status RECRUITING

IRCCS Istituto Romagnolo per lo Studio dei Tumori "Dino Amadori"

Meldola, , Italy

Site Status RECRUITING

UO Ematologia Ospedale di Ravenna

Ravenna, , Italy

Site Status RECRUITING

Institution Fondazione Policlinico Tor Vergata

Roma, , Italy

Site Status ACTIVE_NOT_RECRUITING

Nasz Lekarz Przychodnie Medyczne

Torun, , Poland

Site Status WITHDRAWN

Hospital Universitari Vall d'Hebron

Barcelona, , Spain

Site Status RECRUITING

Universitat de Barcelona

Barcelona, , Spain

Site Status RECRUITING

MD Anderson Cancer Center

Madrid, , Spain

Site Status RECRUITING

Hospital Universitario HM Sanchinarro

Madrid, , Spain

Site Status RECRUITING

Hospital Universitario Central de Asturias

Oviedo, , Spain

Site Status RECRUITING

Hospital Universitario Virgen del Rocio

Seville, , Spain

Site Status RECRUITING

Hospital Universitari i Politecnic La Fe

Valencia, , Spain

Site Status RECRUITING

Cardiff and Vale University

Cardiff, , United Kingdom

Site Status WITHDRAWN

Beatson West of Scotland Cancer Centre

Glasgow, , United Kingdom

Site Status WITHDRAWN

Barts Health NHS Trust

London, , United Kingdom

Site Status WITHDRAWN

St. George's Hospital

London, , United Kingdom

Site Status WITHDRAWN

Countries

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United States Belgium Canada France Germany Italy Poland Spain United Kingdom

Central Contacts

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Kura Medical Information

Role: CONTACT

Phone: 844-KURAONC (844-587-2662)

Email: [email protected]

Facility Contacts

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Role: primary

Bruck Habtemariam

Role: primary

Role: primary

Larissa Sanglard, MD

Role: primary

Christine Connolly

Role: primary

Role: primary

Emily Tolksdorf

Role: primary

Celina Joco Melendez

Role: primary

Role: primary

Tina Czaplinska

Role: primary

Silas Day

Role: primary

Felicia Kass

Role: primary

Yasmeen Akhtar, MBBS,MS,CCRP

Role: primary

Rachel Abramowicz

Role: primary

Kaysey Orlowski

Role: primary

References

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Wang ES, Montesinos P, Foran J, Erba H, Rodriguez-Arboli E, Fedorov K, Heiblig M, Heidel FH, Altman JK, Baer MR, Ades L, Pettit K, Peterlin P, Papayannidis C, Berthon C, Walter RB, Shah MV, Balasubramanian S, Khawandanah M, Salamero Garcia O, Bergeron J, Madanat YF, Roboz GJ, Ulrickson M, Redner RL, McCloskey J, Pigneux A, de la Fuente Burguera A, Mitra A, Soifer HS, Tabachri M, Zhang Z, Riches M, Corum D, Leoni M, Issa GC, Fathi AT; KOMET-001. Ziftomenib in Relapsed or Refractory NPM1-Mutated AML. J Clin Oncol. 2025 Nov;43(31):3381-3390. doi: 10.1200/JCO-25-01694. Epub 2025 Sep 25.

Reference Type DERIVED
PMID: 40997296 (View on PubMed)

Wang ES, Issa GC, Erba HP, Altman JK, Montesinos P, DeBotton S, Walter RB, Pettit K, Savona MR, Shah MV, Kremyanskaya M, Baer MR, Foran JM, Schiller G, Ades L, Heiblig M, Berthon C, Peterlin P, Rodriguez-Arboli E, Salamero O, Patnaik MM, Papayannidis C, Grembecka J, Cierpicki T, Clegg B, Ray J, Linhares BM, Nie K, Mitra A, Ahsan JM, Tabachri M, Soifer HS, Corum D, Leoni M, Dale S, Fathi AT. Ziftomenib in relapsed or refractory acute myeloid leukaemia (KOMET-001): a multicentre, open-label, multi-cohort, phase 1 trial. Lancet Oncol. 2024 Oct;25(10):1310-1324. doi: 10.1016/S1470-2045(24)00386-3.

Reference Type DERIVED
PMID: 39362248 (View on PubMed)

Sasca D, Guezguez B, Kuhn MWM. Next generation epigenetic modulators to target myeloid neoplasms. Curr Opin Hematol. 2021 Sep 1;28(5):356-363. doi: 10.1097/MOH.0000000000000673.

Reference Type DERIVED
PMID: 34267079 (View on PubMed)

Jimenez JA, Apfelbaum AA, Hawkins AG, Svoboda LK, Kumar A, Ruiz RO, Garcia AX, Haarer E, Nwosu ZC, Bradin J, Purohit T, Chen D, Cierpicki T, Grembecka J, Lyssiotis CA, Lawlor ER. EWS-FLI1 and Menin Converge to Regulate ATF4 Activity in Ewing Sarcoma. Mol Cancer Res. 2021 Jul;19(7):1182-1195. doi: 10.1158/1541-7786.MCR-20-0679. Epub 2021 Mar 19.

Reference Type DERIVED
PMID: 33741715 (View on PubMed)

Other Identifiers

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KO-MEN-001

Identifier Type: -

Identifier Source: org_study_id