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Clinical Trials/NCT00387465
NCT00387465
Completed
Phase 1

A Phase I/II Study of Entinostat in Combination With 5-Azacytidine in Patients With Recurrent Advanced Non-Small Cell Lung Cancer

National Cancer Institute (NCI)5 sites in 1 country94 target enrollmentAugust 2006

Overview

Phase
Phase 1
Intervention
Azacitidine 30mg/m2
Conditions
Recurrent Non-Small Cell Lung Carcinoma
Sponsor
National Cancer Institute (NCI)
Enrollment
94
Locations
5
Primary Endpoint
(Phase I) Maximum Tolerated Dose (MTD) of Azacitidine When Given Together With Entinostat as Determined by Number of Participants Experiencing Dose-limiting Toxicity (DLT)
Status
Completed
Last Updated
6 years ago

Overview

Brief Summary

This phase I/II trial is studying the side effects and best dose of azacitidine when given together with entinostat and to see how well they work in treating patients with recurrent advanced non-small cell lung cancer. Azacitidine and entinostat may stop the growth of tumor cells by blocking some of the enzymes needed for cell growth. Giving azacitidine together with entinostat may kill more tumor cells.

Detailed Description

PRIMARY OBJECTIVES: I. To assess safety, characterize toxicities, and determine the maximum tolerated dose of 5-AZA (azacitidine) with a fixed-dose of entinostat in patients with recurrent advanced non-small cell lung cancer (NSCLC). (Phase I) II. To determine the objective response rate of 5-AZA and entinostat in patients with recurrent NSCLC. (Phase II) SECONDARY OBJECTIVES: I. To determine the pharmacokinetic profile of 5-AZA and entinostat in patients with recurrent NSCLC. II. To assess the pharmacodynamic effects of 5-AZA and entinostat on deoxyribonucleic acid (DNA) methylation, histone acetylation, and gene re-expression in patients with recurrent NSCLC through analysis of blood, sputum and tissue biopsies. III. To explore the effect of 5-AZA and entinostat on progression-free and overall survival in patients with recurrent advanced non-small cell lung cancer. IV. To explore the differing response rates and progression-free survivals of two schedules of 5-AZA and entinostat in patients with recurrent advanced non-small cell lung cancer. OUTLINE: This is a multicenter, phase I, dose-escalation study of azacitidine followed by an open-label, phase II study. Patients receive azacitidine subcutaneously (SC) on days 1-6 and 8-10 and entinostat orally (PO) on days 3 and 10. Treatment repeats every 28 days in the absence of disease progression or unacceptable toxicity. After completion of study treatment, patients are followed up every 3 months.

Registry
clinicaltrials.gov
Start Date
August 2006
End Date
November 2014
Last Updated
6 years ago
Study Type
Interventional
Study Design
Single Group
Sex
All

Investigators

Responsible Party
Sponsor

Eligibility Criteria

Inclusion Criteria

  • Patients must have histologically or cytologically confirmed metastatic or unresectable NSCLC
  • Patient must have failed at least one previous chemotherapy regimen
  • Patients must have measurable disease, defined as at least one lesion that can be accurately measured in at least one dimension (longest diameter to be recorded) as \>= 20 mm with conventional techniques or as \>= 10 mm with spiral computed tomography (CT) scan
  • Life expectancy of greater than 12 weeks
  • Eastern Cooperative Oncology Group (ECOG) performance status (PS) =\< 2 (Karnofsky \>= 60%)
  • Leukocytes \>= 3,000/mcL
  • Absolute neutrophil count \>= 1,500/mcL
  • Platelet count \>= 100,000/mcL
  • Total bilirubin within normal institutional limits
  • Aspartate aminotransferase (AST) (serum glutamic oxaloacetic transaminase \[SGOT\] and alanine aminotransferase (ALT) (serum glutamic pyruvate transaminase \[SGPT\]) =\< 2.5 x upper limit of normal

Exclusion Criteria

  • Patients who have had chemotherapy or radiotherapy within 4 weeks (6 weeks for nitrosoureas or mitomycin C) prior to entering the study or those who have not recovered from adverse events due to agents administered more than 4 weeks earlier
  • Patients may not be receiving any other investigational agents
  • Patients with uncontrolled brain metastases; patients with brain metastases must have stable neurologic status following local therapy (surgery or radiation) for at least 4 weeks, and must be without neurologic dysfunction that would confound the evaluation of neurologic and other adverse events
  • Patients with liver metastases that replace greater than 30% of the liver parenchyma
  • History of allergic reactions attributed to compounds of similar chemical or biologic composition to entinostat, 5-AZA, mannitol or other agents used in the study
  • Uncontrolled intercurrent illness including, but not limited to, ongoing or active infection, symptomatic congestive heart failure, unstable angina pectoris, cardiac arrhythmia, or psychiatric illness/social situations that would limit compliance with study requirements
  • Pregnant women are excluded from this study; breastfeeding should be discontinued if the mother is treated on this protocol
  • Human immunodeficiency virus (HIV)-positive patients on combination antiretroviral therapy are ineligible

Arms & Interventions

Phase I - 30mg/m2 Azacitidine

Patients receive Azacitidine 30mg/m2 SQ and entinostat 7mg PO on days 3 and 10 of each cycle.

Intervention: Azacitidine 30mg/m2

Phase I - 30mg/m2 Azacitidine

Patients receive Azacitidine 30mg/m2 SQ and entinostat 7mg PO on days 3 and 10 of each cycle.

Intervention: Entinostat

Phase I - 40mg/m2 Azacitidine

Patients receive azacitidine 40mg/m2 SQ and entinostat 7mg PO on days 3 and 10 of each cycle.

Intervention: Entinostat

Phase I - 40mg/m2 Azacitidine

Patients receive azacitidine 40mg/m2 SQ and entinostat 7mg PO on days 3 and 10 of each cycle.

Intervention: Azacitidine 40mg/m2

Phase II Arm

Patients receive azacitidine 40mg/m2 subcutaneously (SQ) on days 1-6 and 8-10 and entinostat 7mg PO on days 3 and 10. Treatment repeats every 28 days in the absence of disease progression or unacceptable toxicity.

Intervention: Entinostat

Phase II Arm

Patients receive azacitidine 40mg/m2 subcutaneously (SQ) on days 1-6 and 8-10 and entinostat 7mg PO on days 3 and 10. Treatment repeats every 28 days in the absence of disease progression or unacceptable toxicity.

Intervention: Azacitidine 40mg/m2

Outcomes

Primary Outcomes

(Phase I) Maximum Tolerated Dose (MTD) of Azacitidine When Given Together With Entinostat as Determined by Number of Participants Experiencing Dose-limiting Toxicity (DLT)

Time Frame: Up to 28 days

DLT is defined by the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) v3.0

(Phase II) Objective Response Rate After Treatment With Azacitidine and Entinostat as Assessed by Number of Participants With Response After at Least One Cycle of Therapy

Time Frame: Up to 8 years

Number of participants with progressive disease (PD), stable disease (SD), complete response (CR), or partial response (PR), as defined by Response Evaluation Criteria in Solid Tumors (RECIST 1.0), after completing at least one cycle of therapy. Per RECIST 1.0, progression is defined as a 20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions; PR is defined as \>=30% decrease in the sum of the longest diameter of target lesions, CR is defined as the disappearance of all target lesions.

Secondary Outcomes

  • Effect of Entinostat and Azacitidine on DNA Methylation and Response(Baseline and days 10 and 29)
  • Major Objective Response After Immediate Subsequent Therapy as Measured by Number of Participants With PR, SD, PD After at Least 1 Cycle of Subsequent Chemotherapy(Up to 8 years)
  • Overall Survival(Up to 1 year)
  • Pharmacokinetic Profile of Azacytidine as Measured by Tmax(Day 1)
  • Progression-free Survival(Up to 1 year)
  • Pharmacokinetic Profile of Azacitidine as Measured by Cmax(Day 1)
  • Pharmacokinetic Profile of Azacitidine as Measured by AUC (ng*hr/mL)(Day 1)
  • Average Steady State Trough Concentration (ng/mL) of Entinostat(Day 10 and 17)
  • Pharmacokinetic Profile of Azacitidine as Measured by Half-life(Day 1)

Study Sites (5)

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