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A Study to Evaluate Lanraplenib (LANRA) in Combination With Gilteritinib in Participants With FLT3-mutated Relapsed or Refractory Acute Myeloid Leukemia (AML)

Phase 1
Terminated
Conditions
Acute Myeloid Leukemia
Relapsed Acute Myeloid Leukemia
Refractory Acute Myeloid Leukemia
Interventions
Registration Number
NCT05028751
Lead Sponsor
Kronos Bio
Brief Summary

The primary objective of this study is to evaluate the safety of lanraplenib (LANRA) in combination with the FMS-like tyrosine kinase 3 (FLT3) inhibitor gilteritinib, in participants with relapsed or refractory (R/R) FLT3-mutated acute myeloid leukemia (AML).

Detailed Description

Not available

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
24
Inclusion Criteria
  • Adults ≥18 years of age with acute myeloid leukemia (AML) and at least 1 prior line of therapy
  • FMS-like tyrosine kinase 3 (FLT3)-mutated disease documented in a local reference laboratory at the time of consideration for enrollment in the study
  • Have the ability to understand the requirements and procedures of the study and sign a written informed consent form
  • Eastern Cooperative Oncology Group (ECOG) performance status (PS) of 0, 1 or 2
  • Adequate hepatic and renal function
  • Prothrombin time (PT), activated partial thromboplastin time (aPTT) and international normalized ratio (INR) ≤1.5x upper limit of normal (ULN) unless receiving therapeutic anticoagulation
  • Negative serum ß-human chorionic gonadotropin (HCG) test in women of child-bearing potential (WOCBP)
  • Left ventricular ejection fraction ≥50% confirmed by echocardiogram (ECHO) or multi-gated acquisition (MUGA) scan
Exclusion Criteria
  • Known central nervous system (CNS) involvement with leukemia
  • Clinical signs/symptoms of leukostasis that have failed therapy including hydroxyurea and/or leukapheresis of at least 3 days duration
  • Pregnant or breastfeeding women
  • Active infection with hepatitis B, C or human immunodeficiency virus (HIV) infection
  • Disseminated intravascular coagulation with active bleeding or signs of thrombosis
  • Known active coronavirus disease 2019 (COVID-19)
  • Administration of a live attenuated virus vaccine within 35 days before Cycle 1 Day 1 (C1D1)
  • History of non-myeloid malignancy except for the following: adequately treated localized basal cell, or squamous cell carcinoma of the skin, or localized melanoma (with TNM stage either Tis [melanoma in-situ] or T1aN0M0) with complete resection; cervical carcinoma in situ; superficial bladder cancer; asymptomatic prostate cancer without known metastatic disease, with no requirement for therapy or requiring only hormonal therapy and with normal prostate specific antigen for > 1 year prior to start of study therapy; or any other cancer that has been in complete remission without treatment for ≥3 years prior to enrollment
  • Clinically significant heart disease
  • Prolongation of the long measure between Q wave and T wave in the electrocardiogram (QT) interval at baseline
  • Evidence of ongoing uncontrolled systemic bacterial, fungal, or viral infection at the time of study treatment initiation
  • Current (within 30 days of study enrollment) drug-induced liver injury, chronic active hepatitis, alcoholic liver disease, nonalcoholic steatohepatitis, primary biliary cholangitis with inadequate response to ursodeoxycholic acid or other health authority approved therapy, extrahepatic obstruction caused by cholelithiasis, cirrhosis of the liver, or portal hypertension
  • Ongoing (within 6 weeks of study enrollment) hepatic encephalopathy
  • Ongoing immunosuppressive therapy, including systemic chemotherapy for treatment of leukemia

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
LANRA 90 mg QD + Gilteritinib 120 mg QDLanraplenibParticipants received LANRA 90 mg QD as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 1. Participants also received gilteritinib 120 mg QD as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 2. Participants received treatment until progression/relapse or lack of at least a PR after 6 months of study treatment, intolerance, or withdrawal from treatment by the participant or study investigator.
LANRA 90 mg QD + Gilteritinib 120 mg QDGilteritinibParticipants received LANRA 90 mg QD as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 1. Participants also received gilteritinib 120 mg QD as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 2. Participants received treatment until progression/relapse or lack of at least a PR after 6 months of study treatment, intolerance, or withdrawal from treatment by the participant or study investigator.
LANRA 20 mg QD + Gilteritinib 120 mg QDGilteritinibParticipants received LANRA 20 mg once daily (QD) as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 1. Participants also received gilteritinib 120 mg QD as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 2. Participants received treatment until progression/relapse or lack of at least a partial remission (PR) after 6 months of study treatment, intolerance, or withdrawal from treatment by the participant or study investigator.
LANRA 40 mg QD + Gilteritinib 120 mg QDGilteritinibParticipants received LANRA 40 mg QD as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 1. Participants also received gilteritinib 120 mg QD as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 2. Participants received treatment until progression/relapse or lack of at least a PR after 6 months of study treatment, intolerance, or withdrawal from treatment by the participant or study investigator.
LANRA 60 mg QD + Gilteritinib 120 mg QDGilteritinibParticipants received LANRA 60 mg QD as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 1. Participants also received gilteritinib 120 mg QD as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 2. Participants received treatment until progression/relapse or lack of at least a PR after 6 months of study treatment, intolerance, or withdrawal from treatment by the participant or study investigator.
LANRA 20 mg QD + Gilteritinib 120 mg QDLanraplenibParticipants received LANRA 20 mg once daily (QD) as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 1. Participants also received gilteritinib 120 mg QD as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 2. Participants received treatment until progression/relapse or lack of at least a partial remission (PR) after 6 months of study treatment, intolerance, or withdrawal from treatment by the participant or study investigator.
LANRA 40 mg QD + Gilteritinib 120 mg QDLanraplenibParticipants received LANRA 40 mg QD as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 1. Participants also received gilteritinib 120 mg QD as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 2. Participants received treatment until progression/relapse or lack of at least a PR after 6 months of study treatment, intolerance, or withdrawal from treatment by the participant or study investigator.
LANRA 60 mg QD + Gilteritinib 120 mg QDLanraplenibParticipants received LANRA 60 mg QD as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 1. Participants also received gilteritinib 120 mg QD as oral tablets in consecutive 28-day cycles starting from Cycle 1 Day 2. Participants received treatment until progression/relapse or lack of at least a PR after 6 months of study treatment, intolerance, or withdrawal from treatment by the participant or study investigator.
Primary Outcome Measures
NameTimeMethod
Maximally Tolerated Dose (MTD)/Recommended Phase 2 Dose (RP2D) of LANRA in Combination With Standard Doses of GilteritinibCycle 1 Day 1 to pre-dose Cycle 2 Day 1 (each cycle was 28 days)

The MTD/RP2D was defined as the highest dose with either 0 of 3 or no more than 1 of 6 patients with LANRA-related DLTs. All decisions regarding dose escalation including declaration of the MTD/RP2D were made by the dose-escalation committee (DEC).

Number of Participants Who Experienced a Treatment-emergent Adverse Event (TEAE)Cycle 1 Day 1 (each cycle was 28 days) to 30 days after last dose of either LANRA or gilteritinib or initiation of non-protocol antileukemic therapy, whichever was earlier (maximum duration of treatment was 183 days)

A TEAE was any unfavorable or unintended sign, symptom, laboratory abnormality or disease (new or exacerbated) temporally associated with the use of a study drug, whether considered causally related to the study drug or not that started after the first dose of the earliest study drug through the lesser of non-protocol anti-leukemic therapy initiation or end of treatment visit.

A serious TEAE was defined as any TEAE that:

* Resulted in death.

* Was life-threatening.

* Required or prolonged a pre-existing hospitalization.

* Resulted in disability/incapacity.

* Was a congenital anomaly/birth defect.

* Was considered a significant medical event by the investigator.

TEAEs were graded for severity based on the National Cancer Institute-Common Terminology Criteria for Adverse Events (NCI-CTCAE) version 5.0 as follows:

* Grade 1 - Mild.

* Grade 2 - Moderate.

* Grade 3 - Severe.

* Grade 4 - Life-threatening.

* Grade 5 - Death related to adverse event (AE).

Number of Participants Who Experienced a Dose-limiting Toxicity (DLT) for LANRACycle 1 Day 1 to pre-dose Cycle 2 Day 1 (each cycle was 28 days)

A DLT was defined as any of the following occurring within the DLT assessment period:

* A nonhematologic toxicity of Grade ≥ 3 that was at least possibly related to LANRA (with noted exceptions).

* Any toxicity that resulted in administration of \< 80% of the cumulative, Cycle 1 dose for either LANRA or gilteritinib.

* Grade 4 neutropenia or thrombocytopenia lasting \> 28 days after treatment onset that was not attributed to active acute myeloid leukemia (AML) and was at least possibly related to LANRA.

* Any toxicity that resulted in reduction in the dose of LANRA in Cycle 1.

DLTs were graded for severity based on the NCI-CTCAE version 5.0 as follows:

* Grade 3 - Severe.

* Grade 4 - Life-threatening.

Secondary Outcome Measures
NameTimeMethod
Tmax of GilteritinibCycle 1 Day 15: Pre-dose and 0.5, 1, 2, 3, 4, 6, 8 and 24 hours post-dose.

Tmax was derived from plasma concentrations of gilteritinib using standard non-compartmental methods and actual sample times.

Composite Complete Remission (cCR) Rate Per European LeukemiaNet (ELN) 2017 CriteriaCycle 1 Day 1 until occurrence of documented CR or CRh (maximum duration of follow-up was 16.1 months).

Percentage of participants with cCR included CR and CR with partial hematologic recovery (CRh).

CR required all of the following, per ELN 2017 criteria:

* Bone marrow blasts \< 5 %.

* Absence of circulating blasts and blasts with Auer rods.

* Absence of extramedullary disease (ie, leukemia outside of bone marrow confirmed by biopsy).

* Absolute neutrophil count \> 1.0 x 10\^9/L (1,000/μL).

* Platelet count \>100 x 10\^9/L (100,000/μL).

CRh required all aforementioned CR criteria except for the below:

* Absolute neutrophil count \> 0.5 x 10\^9/L (500/μL) and/or;

* Platelet count \> 50 x 10\^9/L (50,000/μL).

Duration of Response (DOR)From first qualifying response (CR/CRh) until relapse or death from any cause (maximum duration of follow-up was 16.1 months).

DOR was defined as the time from first qualifying response (CR/CRh) until relapse or death from any cause, as assessed by study investigators.

CR required all of the following:

* Bone marrow blasts \< 5 %.

* Absence of circulating blasts and blasts with Auer rods.

* Absence of extramedullary disease (ie, leukemia outside of bone marrow confirmed by biopsy).

* Absolute neutrophil count \> 1.0 x 10\^9/L (1,000/μL).

* Platelet count \>100 x 10\^9/L (100,000/μL).

CRh required all aforementioned CR criteria except for the below:

* Absolute neutrophil count \> 0.5 x 10\^9/L (500/μL) and/or;

* Platelet count \> 50 x 10\^9/L (50,000/μL).

Relapse was defined as the reappearance of circulating blasts or ≥ 5% blasts in the bone marrow not attributable to any other cause or reappearance of cytologically or biopsy documented extramedullary disease.

Maximal Plasma Concentration (Cmax) of LANRACycle 1 Day 1 and Cycle 1 Day 15: Pre-dose and 0.5, 1, 2, 3, 4, 6, 8 and 24 hours post-dose.

Cmax was derived from plasma concentrations of LANRA using standard non-compartmental methods and actual sample times.

Time to Cmax (Tmax) of LANRACycle 1 Day 1 and Cycle 1 Day 15: Pre-dose and 0.5, 1, 2, 3, 4, 6, 8 and 24 hours post-dose.

Tmax was derived from plasma concentrations of LANRA using standard non-compartmental methods and actual sample times.

Area of the Plasma Concentration x Time Curve From Hour 0 to the Last Measurable Time Point (AUC0-last) of LANRACycle 1 Day 1 and Cycle 1 Day 15: Pre-dose and 0.5, 1, 2, 3, 4, 6, 8 and 24 hours post-dose.

AUC0-last was derived from plasma concentrations of LANRA using standard non-compartmental methods and actual sample times.

Cmax of GilteritinibCycle 1 Day 15: Pre-dose and 0.5, 1, 2, 3, 4, 6, 8 and 24 hours post-dose.

Cmax was derived from plasma concentrations of gilteritinib using standard non-compartmental methods and actual sample times.

AUC0-last of GilteritinibCycle 1 Day 15: Pre-dose and 0.5, 1, 2, 3, 4, 6, 8 and 24 hours post-dose.

AUC0-last was derived from plasma concentrations of gilteritinib using standard non-compartmental methods and actual sample times.

Event-free Survival (EFS)Cycle 1 Day 1 to treatment failure (ie, failure to achieve CR or CRh, relapse from CR/CRh or death from any cause) (maximum duration of follow-up was 16.1 months).

EFS was defined as the time from treatment onset until treatment failure (ie, failure to achieve CR/CRh, relapse from CR/CRh, or death from any cause).

CR required all of the following:

* Bone marrow blasts \< 5 %.

* Absence of circulating blasts and blasts with Auer rods.

* Absence of extramedullary disease (ie, leukemia outside of bone marrow confirmed by biopsy).

* Absolute neutrophil count \> 1.0 x 10\^9/L (1,000/μL).

* Platelet count \>100 x 10\^9/L (100,000/μL).

CRh required all aforementioned CR criteria except for the below:

* Absolute neutrophil count \> 0.5 x 10\^9/L (500/μL) and/or;

* Platelet count \> 50 x 10\^9/L (50,000/μL).

Relapse was defined as the reappearance of circulating blasts or ≥ 5% blasts in the bone marrow not attributable to any other cause or reappearance of cytologically or biopsy documented extramedullary disease.

Overall SurvivalEnrollment until death from any cause (maximum duration of follow-up was 16.1 months).

Overall survival was defined as the time from enrollment until death from any cause. Overall survival was estimated using Kaplan-Meier methodology.

Trial Locations

Locations (17)

Institut Català d'Oncologia - Hospital Duran i Reynals (ICO L'Hospitalet)

🇪🇸

Barcelona, Spain

The Blood and Marrow Transplant Group of Georgia

🇺🇸

Atlanta, Georgia, United States

Memorial Sloan Kettering Cancer Center

🇺🇸

New York, New York, United States

Oregon Health and Science University

🇺🇸

Portland, Oregon, United States

University of Texas MD Anderson Cancer Center

🇺🇸

Houston, Texas, United States

University of California Los Angeles (UCLA)

🇺🇸

Los Angeles, California, United States

University of Chicago Medical Center

🇺🇸

Chicago, Illinois, United States

Texas Oncology - Baylor Charles A. Sammons Cancer Center

🇺🇸

Dallas, Texas, United States

Hospital Universitario 12 de Octubre

🇪🇸

Madrid, Avenida De Córdoba Sin Número, Spain

Froedtert Hospital

🇺🇸

Milwaukee, Wisconsin, United States

Hospital Universitari Vall d'Hebrón

🇪🇸

Barcelona, Spain

MD Anderson Cancer Center Madrid

🇪🇸

Madrid, Calle De Arturo Soria, Spain

Hospital Clínic de Barcelona

🇪🇸

Barcelona, Spain

Hospital San Pedro de Alcantara

🇪🇸

Cáceres, Spain

Hospital Universitari i Politècnic La Fe

🇪🇸

Valencia, Spain

Hospital Germans Trias i Pujol

🇪🇸

Barcelona, Badalona, Spain

Hospital Universitario Fundación Jiménez Díaz

🇪🇸

Madrid, Spain

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