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EFFICACY AND SAFETY OF ASPACYTARABINE (BST-236) AS A FIRST-LINE MONOTHERAPY FOR PATIENTS WITH ACUTE MYELOID LEUKEMIA UNFIT FOR STANDARD CHEMOTHERAPY
Author(s): ,
Jessica K. Altman
Affiliations:
Robert H. Lurie Comprehensive Cancer Center Northwestern University,Chicago,United States
,
Jamie Koprivnikar
Affiliations:
John Theurer Cancer Center Hackensack University Medical Center,Hackensack,United States
,
James McCloskey
Affiliations:
John Theurer Cancer Center Hackensack University Medical Center,Hackensack,United States
,
Vamsi Kota
Affiliations:
Georgia Cancer Center Augusta University,Augusta,United States
,
Olga Frankfurt
Affiliations:
Robert H. Lurie Comprehensive Cancer Center Northwestern University,Chicago,United States
,
Ashkan Emadi
Affiliations:
University of Maryland School of Medicine,University of Maryland,Baltimore,United States
,
Dale Bixby
Affiliations:
University of Michigan Comprehensive Cancer Center,Ann Arbor,United States
,
Micah Burch
Affiliations:
Baylor Scott & White Research Institute,Dallas,United States
,
Moshe Levy
Affiliations:
Baylor Scott & White Research Institute,Dallas,United States
,
Selina Luger
Affiliations:
Abramson Cancer Center, University of Pennsylvania,Philadelphia,United States
,
Tsila Zuckerman
Affiliations:
Rambam Health Care Campus,Haifa,Israel
,
Bhavana Bhatnagar
Affiliations:
Arthur G James Cancer Hospital Comprehensive Cancer Center, Ohio State University,Ohio,United States
,
Ofir Wolach
Affiliations:
Rabin Medical Center,Petach Tikva,Israel
,
Chezi Ganzel
Affiliations:
Shaare Zedek Medical Center,Jerusalem,Israel
,
Itai Levi
Affiliations:
Soroka University Medical Center,Beer Sheva,Israel
,
Anna Gourevitch
Affiliations:
Soroka University Medical Center,Beer Sheva,Israel
,
Liat Flaishon
Affiliations:
BioSight Ltd.,Lod,Israel
,
Shoshi Tessler
Affiliations:
BioSight Ltd.,Lod,Israel
,
Chen Blomberg
Affiliations:
BioSight Ltd.,Lod,Israel
,
Stela Gengrinovitch
Affiliations:
BioSight Ltd.,Lod,Israel
,
Ruth Ben Yakar
Affiliations:
BioSight Ltd.,Lod,Israel
Jacob Rowe
Affiliations:
Shaare Zedek Medical Center,Jerusalem,Israel
EHA Library. K. Altman J. 06/09/21; 325222; EP462
Jessica K. Altman
Jessica K. Altman
Contributions
Abstract
Presentation during EHA2021: All e-poster presentations will be made available as of Friday, June 11, 2021 (09:00 CEST) and will be accessible for on-demand viewing until August 15, 2021 on the Virtual Congress platform.

Abstract: EP462

Type: E-Poster Presentation

Session title: Acute myeloid leukemia - Clinical

Background

Cytarabine, the backbone of acute myeloid leukemia (AML) standard of care chemotherapy, is associated with a toxicity which precludes its administration to older patients and those with comorbidities. Aspacytarabine (BST-236) is a prodrug of cytarabine. Its pharmacokinetics and metabolism lead to gradual release of cytarabine with shorter duration at peak toxic levels compared to direct cytarabine administration, resulting in relative sparing of normal tissues and enabling delivery of high cytarabine doses to patients otherwise unfit to receive it.

Aims

To evaluate the efficacy and safety of aspacytarabine as a first-line, single-agent therapy in newly-diagnosed AML patients unfit for standard induction therapy.

Methods
Aspacytarabine is administrated at a dose of 4.5 g/m2/d (equimolar of 3 g/m2/d cytarabine). Therapy is time-limited, with only 1-2 induction courses and 1-3 consolidation courses, each consists of 6 daily 1-hour intravenous infusions. Newly-diagnosed AML patients unfit for standard chemotherapy, including those with secondary AML, previously treated with HMA, and patients with therapy-related AML, are eligible. 

Results

To date, 71 AML patients were treated with aspacytarabine; 47 newly-diagnosed AML patients unfit for standard chemotherapy (median age 75 years) completed 1-4 courses of 4.5 g/m2/d aspacytarabine in an ongoing phase 2b study, including 30 patients (64%) with de novo AML and 17 (36%) with secondary AML. Six patients (13%) were previously treated with HMA (median 12 courses), and 21 (45%) patients had ECOG Performance Status 2. The median baseline bone marrow blast percentage was 45 (range 13-94), and 54% and 29% of patients had adverse or intermediate ELN score, respectively.


Aspacytarabine is safe and well-tolerated in repeated-course administration. Grade >2 drug-related adverse events include mainly hematological events and infections. The 30-day mortality rate is 11%.


Of the 43 phase 2b patients evaluable for efficacy analysis to date, 15 patients (35%) reached a complete remission (CR) following 1 (13 patients) or 2 (2 patients) aspacytarabine induction courses. All responders reached a complete hematological recovery (median 27.5 days, range 22-39 days). The CR rate excluding patients with prior HMA therapy is 41%, and 46% in de novo AML patients. The CR rate in patients at the age of ≥75 years and patients with adverse ELN score is 33%.


Of note, of the 11 patients evaluable to date for minimal residual disease (MRD) analysis, 8 (73%) are MRD negative.


While aspacytarabine treatment consists of a limited number of courses, median duration of response (DOR) and median overall survival (OS) for responders are not reached (NR) at end of follow up, 12 (95% CI 5-NR) and 24 (95% CI 6-NR) months, respectively. The median OS for all patients is 6.8 (95% CI 6-NR) months (Figure 1A). Median OS for de novo AML patients is NR (95% CI 6-NR) and 6.8 (95% CI 2.7-NR) for secondary AML patients (Figure 1B).


Follow-up is ongoing with additional patients enrolling on study; updated analysis will be presented at the meeting.

Conclusion
The cumulative clinical data suggest that aspacytarabine monotherapy is safe and efficacious as a first-line therapy for patients who are unfit for intensive chemotherapy, including patients with adverse cytogenetics and patients ≥75 year of age. The data may establish aspacytarabine, already granted Fast Track designation from the FDA, as a new intensive therapy backbone of AML and may, for the first time, allow older adults benefit from standard intensive therapy.

Keyword(s): Acute myeloid leukemia, Chemotherapy, Elderly, High dose therapy

Presentation during EHA2021: All e-poster presentations will be made available as of Friday, June 11, 2021 (09:00 CEST) and will be accessible for on-demand viewing until August 15, 2021 on the Virtual Congress platform.

Abstract: EP462

Type: E-Poster Presentation

Session title: Acute myeloid leukemia - Clinical

Background

Cytarabine, the backbone of acute myeloid leukemia (AML) standard of care chemotherapy, is associated with a toxicity which precludes its administration to older patients and those with comorbidities. Aspacytarabine (BST-236) is a prodrug of cytarabine. Its pharmacokinetics and metabolism lead to gradual release of cytarabine with shorter duration at peak toxic levels compared to direct cytarabine administration, resulting in relative sparing of normal tissues and enabling delivery of high cytarabine doses to patients otherwise unfit to receive it.

Aims

To evaluate the efficacy and safety of aspacytarabine as a first-line, single-agent therapy in newly-diagnosed AML patients unfit for standard induction therapy.

Methods
Aspacytarabine is administrated at a dose of 4.5 g/m2/d (equimolar of 3 g/m2/d cytarabine). Therapy is time-limited, with only 1-2 induction courses and 1-3 consolidation courses, each consists of 6 daily 1-hour intravenous infusions. Newly-diagnosed AML patients unfit for standard chemotherapy, including those with secondary AML, previously treated with HMA, and patients with therapy-related AML, are eligible. 

Results

To date, 71 AML patients were treated with aspacytarabine; 47 newly-diagnosed AML patients unfit for standard chemotherapy (median age 75 years) completed 1-4 courses of 4.5 g/m2/d aspacytarabine in an ongoing phase 2b study, including 30 patients (64%) with de novo AML and 17 (36%) with secondary AML. Six patients (13%) were previously treated with HMA (median 12 courses), and 21 (45%) patients had ECOG Performance Status 2. The median baseline bone marrow blast percentage was 45 (range 13-94), and 54% and 29% of patients had adverse or intermediate ELN score, respectively.


Aspacytarabine is safe and well-tolerated in repeated-course administration. Grade >2 drug-related adverse events include mainly hematological events and infections. The 30-day mortality rate is 11%.


Of the 43 phase 2b patients evaluable for efficacy analysis to date, 15 patients (35%) reached a complete remission (CR) following 1 (13 patients) or 2 (2 patients) aspacytarabine induction courses. All responders reached a complete hematological recovery (median 27.5 days, range 22-39 days). The CR rate excluding patients with prior HMA therapy is 41%, and 46% in de novo AML patients. The CR rate in patients at the age of ≥75 years and patients with adverse ELN score is 33%.


Of note, of the 11 patients evaluable to date for minimal residual disease (MRD) analysis, 8 (73%) are MRD negative.


While aspacytarabine treatment consists of a limited number of courses, median duration of response (DOR) and median overall survival (OS) for responders are not reached (NR) at end of follow up, 12 (95% CI 5-NR) and 24 (95% CI 6-NR) months, respectively. The median OS for all patients is 6.8 (95% CI 6-NR) months (Figure 1A). Median OS for de novo AML patients is NR (95% CI 6-NR) and 6.8 (95% CI 2.7-NR) for secondary AML patients (Figure 1B).


Follow-up is ongoing with additional patients enrolling on study; updated analysis will be presented at the meeting.

Conclusion
The cumulative clinical data suggest that aspacytarabine monotherapy is safe and efficacious as a first-line therapy for patients who are unfit for intensive chemotherapy, including patients with adverse cytogenetics and patients ≥75 year of age. The data may establish aspacytarabine, already granted Fast Track designation from the FDA, as a new intensive therapy backbone of AML and may, for the first time, allow older adults benefit from standard intensive therapy.

Keyword(s): Acute myeloid leukemia, Chemotherapy, Elderly, High dose therapy

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