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Acute Myelogenous Leukemia (AML)Phase 1NCT01451437

Study of MK-8242 Alone and in Combination With Cytarabine in Participants With Acute Myelogenous Leukemia (P07649)

A Phase 1 study testing MK-8242 in people with Acute Myelogenous Leukemia (AML), run by Merck Sharp & Dohme LLC.

Terminated

Stopped early. The study ended before it was planned to and will not resume.

Official record
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Trial summary

This is a study of MK-8242 alone and in combination with cytarabine in adult participants with refractory or recurrent acute myelogenous leukemia (AML). The study will have 2 Arms. Arm A is for participants with refractory or recurrent AML who are considered ineligible for standard chemotherapy. Read more about this study

Who is it for?
Ages 18 years and older
Conditions the study is for
Acute Myelogenous Leukemia (AML)
What is being tested?
MK-8242
Type of treatment
Pill or oral medicine
Could I receive a placebo?
No, everyone receives an active treatment
How many people
26 participants
Where
No sites listed yet
Study dates
18 Nov 2011to 5 Sep 2014
Phase
Phase 1
Are there results?
Yes, posted in the registrySummary in the doctors' view

Key requirements

Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.

  • Ages 18 years and older
  • All sexes
  • No healthy volunteers
  • Adult, Older adult

Who may be able to join

  • For Arm A Part 1 (monotherapy/dose escalation): refractory or recurrent AML, not an appropriate candidate for standard therapy
  • For Arm A Part 2 (monotherapy/dose confirmation/cohort expansion): refractory or recurrent AML, not an appropriate candidate for standard therapy, and have wild type p53 gene mutation analysis
  • For Arm B Part 1 (combination therapy/dose escalation): recurrent AML having achieved an initial CR or CRi of 6-12 months duration and age ≥18 years old and <70 years old
  • For Arm B Part 2 (combination therapy/dose confirmation/cohort expansion): recurrent AML having achieved an initial CR or CRi of 6-12 months duration, age ≥18 years old and <70 years old, and have wild type P53 gene mutation analysis
  • Eastern Cooperative Oncology Group (ECOG) performance status of 0, 1, or 2 for all Arm A, or 0 or 1 for all Arm B
  • Negative pregnancy test within 72 hours of the first dose of study medication
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  • Female participants and male participants and their partners who are of childbearing potential must agree to abstain from sexual intercourse or to use an acceptable method of contraception during the study and for 90 days following the last dose of study therapy
  • Adequate organ function
  • Recovered from the effects of any prior surgery, radiotherapy or anti-neoplastic treatment, with the exception of alopecia
  • Must be able to swallow, retain, and absorb oral medications and oral nutrition
  • Must follow the appropriate washout period for prohibited treatments

Who cannot join

  • Active malignancy other than AML
  • Leptomeningeal leukemia requiring intrathecal therapy
  • For Arm A and B, Part 1 only: history of myelodysplastic syndrome (MDS)
  • For Arm A and B, Part 2: AML in the background of MDS may be included
  • Isolated extramedullary leukemia without also meeting bone marrow criteria for acute leukemia
  • AML blast crisis of chronic myelogenous leukemia (CML)
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  • Bone marrow transplant with active graft-versus host disease (GVHD) or who receives immunosuppressive therapy
  • Uncontrolled active infection that requires systemic treatment
  • Clinically significant hepatitis at Screening, or hepatitis C antibody positive, hepatitis B surface antigen positive, or human immunodeficiency virus (HIV) seropositive
  • Persistent, unresolved, drug-related toxicity
  • Breast-feeding, pregnant, intends to become pregnant or intends to breast feed during the study or has a positive pregnancy test at Screening
  • A person participating in any other clinical study with a potentially therapeutic agent or who has received another investigational product within 5 half-lives (if the half-life is known) or 28 days (if the half-life is unknown) prior to Day 1 of cycle 1
  • A participant who, within the past 6 months, has had any of the following: myocardial infarction, coronary/peripheral artery bypass graft, cerebrovascular accident, transient ischemic attack, or uncontrolled seizure disorder (i.e., seizures within the past 6 months)
  • A participant who, at the time of Screening, presents with: unstable or uncontrolled angina, New York Heart Association (NYHA) class III or IV congestive heart failure, uncontrolled hypertension, clinically significant cardiac dysrhythmia or clinically significant electrocardiogram (ECG) abnormality
  • Known bleeding disorder, e.g. hemophilia or disseminated intravascular coagulopathy or on anti-coagulation therapy
  • For Arm B only: Known hypersensitivity to cytarabine

About this study

Official title: A Phase I Study to Evaluate the Safety and Tolerability and Pharmacokinetic/Pharmacodynamics of MK-8242 Administered Alone and in Combination With Chemotherapy in Subjects With Refractory or Recurrent Acute Myelogenous Leukemia (Protocol No. P07649 (005))

This is a study of MK-8242 alone and in combination with cytarabine in adult participants with refractory or recurrent acute myelogenous leukemia (AML). The study will have 2 Arms. Arm A is for participants with refractory or recurrent AML who are considered ineligible for standard chemotherapy. In Part 1 of Arm A, participants will receive MK-8242 monotherapy in escalating doses to determine the recommended phase 2 dose [RP2D]. In Part 2, participants will receive monotherapy with MK-8242 to confirm the RP2D and assess preliminary efficacy. Arm B is for participants with recurrent AML following an initial complete remission (CR) or CR with incomplete marrow recovery (CRi) of 6 to 12 months duration. In Part 1 of Arm B, participants will receive MK-8242 in escalating doses + cytarabine to determine the RP2D in combination with cytarabine. In Part 2, participants will receive MK-8242 + cytarabine to confirm the RP2D and assess preliminary efficacy. The pharmacokinetics of MK-8242 will be studied in both arms. With Amendment 4 (22 August 2013) a 21-day dosing cycle is added, with MK-8242 being given on Days 1-7 of each 21-day cycle in both the monotherapy and combination therapy arms; data from Arm A will be used to determine whether a participant receives 21-day or 28-day therapy in Arm B.

Being tested
MK-8242
Medical subject headings
Leukemia, Myeloid, Acute

What participants receive

What participants receive. In a randomised study each person is assigned to one group by chance.

  • MK-8242Drug

    Also called SCH 900242

    MK-8242 capsules, orally, once per day on Days 1-7 and Days 15-21 of each 28-day cycle (except Cycle 1 Day 7) up to a maximum of 12 cycles. Starting dose will be 30 mg and will be escalated in successive cohorts until maximum tolerated dose (MTD) is established. Beginning at a dose level of ≥120 mg total daily dose (TDD), the dosing regimen will switch to twice daily (BID). Amendment 4 added a 21-day dosing cycle in which MK-8242 would be given BID on Days 1-7 of each cycle, at the assigned dose level.

Study groups in NCT01451437
Study groupRoleWhat they receive
Pt 1 Arm A: MK-8242 30 mg QDExperimentalParticipants received MK-8242 30 mg once daily (QD) monotherapy on Days 1-7 and Days 15-21 of a 28-day cycle up to a maximum of 12 cycles in Part 1 Arm A.
Receives: Drug: MK-8242
Pt 1 Arm A: MK-8242 60 mg QDExperimentalParticipants received MK-8242 60 mg QD monotherapy on Days 1-7 and Days 15-21 of a 28-day cycle up to a maximum of 12 cycles in Part 1 Arm A.
Receives: Drug: MK-8242
Pt 1 Arm A: MK-8242 120 mg QDExperimentalParticipants received MK-8242 120 mg QD monotherapy on Days 1-7 and Days 15-21 of a 28-day cycle up to a maximum of 12 cycles in Part 1 Arm A.
Receives: Drug: MK-8242
Pt 1 Arm A: MK-8242 250 mg QDExperimentalParticipants received MK-8242 250 mg QD monotherapy on Days 1-7 and Days 15-21 of a 28-day cycle up to a maximum of 12 cycles in Part 1 Arm A.
Receives: Drug: MK-8242
Pt 1 Arm A: MK-8242 120 mg BIDExperimentalParticipants received MK-8242 120 mg twice daily (BID) monotherapy on Days 1-7 and Days 15-21 of a 28-day cycle up to a maximum of 12 cycles (except Cycle 1 Day 7 on which MK-8242 120 mg was administered QD in the morning) in Part 1 Arm A.
Receives: Drug: MK-8242
Pt 1 Arm A: MK-8242 170 mg BIDExperimentalParticipants received MK-8242 170 mg BID monotherapy on Days 1-7 and Days 15-21 of a 28-day cycle up to a maximum of 12 cycles (except Cycle 1 Day 7 on which MK-8242 170 mg was administered QD in the morning) in Part 1 Arm A.
Receives: Drug: MK-8242
Pt 1 Arm A: MK-8242 210 mg BIDExperimentalParticipants received MK-8242 210 mg BID monotherapy on Days 1-7 of a 21-day cycle up to a maximum of 12 cycles (except Cycle 1 Day 7 on which MK-8242 210 mg was administered QD in the morning) in Part 1 Arm A.
Receives: Drug: MK-8242
Pt 1 Arm A: MK-8242 250 mg BIDExperimentalParticipants received MK-8242 250 mg BID monotherapy on Days 1-7 and Days 15-21 of a 28-day cycle up to a maximum of 12 cycles (except Cycle 1 Day 7 on which MK-8242 250 mg was administered QD in the morning) in Part 1 Arm A.
Receives: Drug: MK-8242
Pt 1 Arm A: MK-8242 300 mg BIDExperimentalParticipants received MK-8242 300 mg BID monotherapy on Days 1-7 of a 21-day cycle up to a maximum of 12 cycles (except Cycle 1 Day 7 on which MK-8242 300 mg was administered QD in the morning) in Part 1 Arm A.
Receives: Drug: MK-8242

What is being measured

The primary outcome is the main question the study is designed to answer.

  1. Number of Participants With Dose Limiting Toxicities (DLTs)

    DLTs were identified using Common Terminology Criteria for Adverse Events (CTCAE) v. 4.0 for toxicities attributable to the study drug. Hematologic DLTs were defined in the absence of morphological evidence of acute leukemia in the marrow if 1) bone marrow: aplastic marrow with <5% cellularity without erythroid, myeloid, or megakaryocytic precursors and 2) peripheral blood: absolute neutrophil count (ANC) <100/µL, platelet count <10,000/µL, and transfusion-dependent anemia. Non-hematologic DLTs were defined as any ≥Grade 3 toxicity with the following exceptions/clarifications: 1) infection, fatigue, anorexia, or alopecia are not included in determination of the DLT 2) Grade 3 nausea, vomiting, diarrhea, or dehydration occurring in a setting of inadequate treatment 3) any abnormal non-hematological laboratory value ≥Grade 3 will be considered a DLT after 72 hours of appropriate medical intervention if not related to an underlying disease or not attributable to another event.

    Measured: Up to 28 days (Cycle 1) for non-hematologic toxicities and 42 days (Cycle 1) for hematologic toxicities

  2. Number of Participants With Complete Remission (CR) at RP2D

    Clinical activity of MK-8242 given as monotherapy in participants with refractory or recurrent AML measured as participants who achieved CR according to Cheson (2003) criteria at the RP2D. The outcome analysis was not performed since the RP2D for MK-8242 monotherapy could not be established due to early termination of the study.

    Measured: End of Treatment (up to 198 days)

  3. Number of Participants With Complete Remission With Incomplete Marrow Recovery (CRi) at RP2D

    Clinical activity of MK-8242 given as monotherapy in participants with refractory or recurrent AML measured as participants who achieved CRi according to Cheson (2003) criteria at the RP2D. The outcome analysis was not performed since the RP2D for MK-8242 monotherapy could not be established due to early termination of the study.

    Measured: End of Treatment (up to 198 days)

Secondary outcomes (10)
  1. Number of Participants With CR at Dose Levels Other Than RP2D

    Clinical activity of MK-8242 given as monotherapy in participants with refractory or recurrent AML measured as participants who achieved CR according to Cheson (2003) criteria at dose levels other than RP2D. CR is defined as a morphologic leukemia-free state with a neutrophil count ≥1,000/µL, a platelet count ≥100,000/µL, no extramedullary disease, and RBC transfusion independence. Presented outcome values are not stratified for dose levels other than RP2D; the RP2D for MK-8242 monotherapy could not be established due to early termination of the study.

    Measured: End of Treatment (up to 198 days)

  2. Number of Participants With CRi at Dose Levels Other Than RP2D

    Clinical activity of MK-8242 given as monotherapy in participants with refractory or recurrent AML measured as participants who achieved CRi according to Cheson (2003) criteria at dose levels other than RP2D. CRi is defined as fulfillment of all CR criteria with exceptions for residual neutropenia (<1,000/µL), thrombocytopenia (<100,000/µL), and RBC transfusion dependence. Presented outcome values are not stratified for dose levels other than RP2D; the RP2D for MK-8242 monotherapy could not be established due to early termination of the study.

    Measured: End of Treatment (up to 198 days)

  3. Area Under the Concentration-time Curve From Time 0 to 24 Hours (AUC0-24hr) for MK-8242 Alone and in Combination With Cytarabine

    AUC(0-24hr) defined as AUC from time zero to 24 hours was determined for Cycle 1 Days 1 and 7 of MK-8242 QD and BID dosing using the trapezoidal up/log trapezoidal down method. For the BID arms, a projection beyond the last sampled time was made if a linear terminal elimination phase half-life was identified with three time-points after Tmax. Analysis for the combination therapy was not performed due to early termination of the study (Study Arm B was not performed).

    Measured: Cycle 1, Day 1 and Day 7 (QD arms: predose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 10, and 24 hrs postdose; BID arms: predose and 0.5, 1, 2, 4, 6, 8, 12 [optional], and 24 [Day 7 only] hrs postdose)

  4. Area Under the Concentration-time Curve From Time 0 to Last (AUC0-last) for MK-8242 Alone and in Combination With Cytarabine

    AUC(0-last) defined as AUC from time zero to the time of last quantifiable sample was determined for Cycle 1 Days 1 and 7 of MK-8242 QD and BID dosing using the trapezoidal up/log trapezoidal down method. Analysis for the combination therapy was not performed due to early termination of the study (Study Arm B was not performed).

    Measured: Cycle 1, Day 1 and Day 7 (QD arms: predose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 10, 24, and 48 [Day 7 only] hrs postdose; BID arms: predose and 0.5, 1, 2, 4, 6, 8, 12 [optional], 24 [Day 7 only], 48 [Day 7 only] hrs postdose)

  5. Area Under the Concentration-time Curve From Time 0 to Infinity (AUC0-∞) for MK-8242 Alone and in Combination With Cytarabine

    AUC0-∞ defined as AUC from time zero to infinity was determined for Cycle 1 Day 7 of MK-8242 QD and BID dosing using the trapezoidal up/log trapezoidal down method. Projection beyond the last sampled time was made if a linear terminal elimination phase half-life was identified with three time-points after Tmax (condition not met for 60 QD and 120 BID dose groups). Analysis for the combination therapy was not performed due to early termination of the study (Study Arm B was not performed).

    Measured: Cycle 1 Day 7 (QD arms: predose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 10, 24, and 48 hrs postdose; BID arms: predose and 0.5, 1, 2, 4, 6, 8, 12 [optional], 24, 48 hrs postdose)

  6. Maximum Plasma Concentration (Cmax) of MK-8242 Alone and in Combination With Cytarabine

    Cmax was determined for Cycle 1 Days 1 and 7 of MK-8226 QD and BID dosing. Analysis for the combination therapy was not performed due to early termination of the study (Study Arm B was not performed).

    Measured: Cycle 1, Day 1 and Day 7 (QD arms: predose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 10, 24, and 48 [Day 7 only] hrs postdose; BID arms: predose and 0.5, 1, 2, 4, 6, 8, 12 [optional], 24 [Day 7 only], 48 [Day 7 only] hrs postdose)

  7. Time to Maximum Concentration (Tmax) of MK-8242 Alone and in Combination With Cytarabine

    Tmax was determined for Cycle 1 Days 1 and 7 of MK-8226 QD and BID dosing. Analysis for the combination therapy was not performed due to early termination of the study (Study Arm B was not performed).

    Measured: Cycle 1, Day 1 and Day 7 (QD arms: predose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 10, 24, and 48 [Day 7 only] hrs postdose; BID arms: predose and 0.5, 1, 2, 4, 6, 8, 12 [optional], 24 [Day 7 only], 48 [Day 7 only] hrs postdose)

  8. Apparent Terminal Half-life (t1/2) for MK-8242 Alone and in Combination With Cytarabine

    Elimination phase t1/2 was determined for Cycle 1 Day 7 of MK-8242 QD and BID dosing. Analysis for the combination therapy was not performed due to early termination of the study (Study Arm B was not performed).

    Measured: Cycle 1 Day 7 (QD arms: predose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 10, 24, and 48 hrs postdose; BID arms: predose and 0.5, 1, 2, 4, 6, 8, 12 [optional], 24, 48 hrs postdose)

  9. Accumulation Ratio (R) of MK-8242 Alone and in Combination With Cytarabine

    The accumulation ratio (R) at steady state (based on dosing interval and apparent terminal half-life (t1/2)) for MK-8242 alone was not determined due to confounding of results by significant concentrations of a drug metabolite (M16). Analysis for the combination therapy was not performed due to early termination of the study (Study Arm B was not performed).

    Measured: Cycle 1 Day 7 (QD arms: predose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 10, 24, and 48 hrs postdose; BID arms: predose and 0.5, 1, 2, 4, 6, 8, 12 [optional], 24 [Day 7 only], 48 [Day 7 only] hrs postdose)

  10. Urine Concentration of MK-8242 (Part 2 Arm A Only)

    The urine concentration of MK-8242 assessed as a measure of drug bioavailability was not determined due to early termination of the study (Study Part 2 was not performed).

    Measured: Day 1 (predose and postdose) and Day 7 (postdose)

Timeline

From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.

  1. First posted13 Oct 2011 (estimated)
  2. Study start18 Nov 2011
  3. Primary completion5 Sep 2014
  4. Study completion5 Sep 2014

Why it stopped: The study was terminated early due to business reasons.

Resources

More details

For doctors and researchers: how the study is designed, who runs it, and its registry IDs.

Study design
Study type
Interventional
Phase
Phase 1
Primary purpose
Treatment
Allocation
Non-randomised
Intervention model
Parallel groups
Masking
None (open label)
Enrolment
26 participants (actual)
IDs, dates and publications
ClinicalTrials.gov ID
NCT01451437
Sponsor's protocol ID
P07649
Other IDs
2011-000709-31, MK-8242-005
Status last verified
Jul 2018
First submitted
11 Oct 2011
Last updated
27 Aug 2018
Data monitoring committee
No
Individual data sharing
Yes: https://www.merck.com/clinical-trials/pdf/ProcedureAccessClinicalTrialData.pdf

Publications

  • Ravandi F, Gojo I, Patnaik MM, Minden MD, Kantarjian H, Johnson-Levonas AO, Fancourt C, Lam R, Jones MB, Knox CD, Rose S, Patel PS, Tibes R. A phase I trial of the human double minute 2 inhibitor (MK-8242) in patients with refractory/recurrent acute myelogenous leukemia (AML). Leuk Res. 2016 Sep;48:92-100. doi: 10.1016/j.leukres.2016.07.004. Epub 2016 Jul 25.

    PubMed 27544076

Questions about this trial

What is this clinical trial studying?

A Phase 1 study testing MK-8242 in people with Acute Myelogenous Leukemia (AML), run by Merck Sharp & Dohme LLC.

The full registered description is in the About this study section and the official record.

Who may be eligible to take part?

The sponsor lists 11 inclusion and 16 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.

Is this clinical trial currently recruiting?

The record says: stopped early, as of the sponsor's last update on 27 Aug 2018. Status can change between updates, so confirm with the study contact before making plans.

What are the possible benefits and risks?

They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.

What does this phase mean?

Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.

Not every study follows the same path, and some studies (observational studies, device studies) have no phase.

Are results available for this study?

Yes. Results are posted in the registry (first posted 4 Mar 2016). A summary is in the For doctors view, and the full results are on ClinicalTrials.gov.

How can a doctor refer a patient or contact the research team?

The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.

What does the primary outcome measure?

Number of Participants With Dose Limiting Toxicities (DLTs) (time frame: Up to 28 days (Cycle 1) for non-hematologic toxicities and 42 days (Cycle 1) for hematologic toxicities). The study lists 3 primary outcomes in all. It is what the study was designed to measure, not a finding.

Where can I read the original study information?

On the ClinicalTrials.gov record for NCT01451437, which also lists 1 linked publication.

Does a listing mean the treatment is approved or proven to work?

No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.

How often is this information updated?

AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 27 Aug 2018.

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