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Study to Assess the Safety, Tolerability and Pharmacokinetics of Fimepinostat (CUDC-907) in Patients With Lymphoma

Phase 1
Completed
Conditions
Lymphoma
Relapsed Lymphoma
Refractory Lymphoma
Relapsed and/or Refractory Lymphoma
Relapsed Ddiffuse Large B-Cell Lymphoma (DLBCL)
Relapsed and/or Refractory Diffuse Large B-Cell Lymphoma (DLBCL)
Refractory Diffuse Large B-Cell Lymphoma (DLBCL)
Double-expressor Lymphoma (DEL)
High-grade B-cell Lymphoma (HGBL)
Double-hit Lymphoma (DHL)
Interventions
Registration Number
NCT01742988
Lead Sponsor
Curis, Inc.
Brief Summary

This is a phase 1, open-label, dose-escalation study of fimepinostat (CUDC-907) in patients with relapsed and/or refractory diffuse large B-cell lymphoma (DLBCL), or high-grade B-cell lymphoma (HGBL) with or without MYC and BCL2 alterations. Fimepinostat (CUDC-907) is a multi-targeted agent designed to inhibit phosphoinositide 3-kinase (PI3K)and histone deacetylase (HDAC). The study is designed to assess the safety, the maximum tolerated dose, the recommended phase 2 dose (RP2D), pharmacokinetics and the anti-cancer activity of oral fimepinostat in combination with 1 or more anti-cancer regimens.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
106
Inclusion Criteria
  • Patients ≥ 18 years of age with any of the following: Histopathologically confirmed DLBCL or HGBL (i.e., HGBL with MYC, BCL2, and/or BCL6 rearrangements, HGBL, not otherwise specified [NOS], or DLBCL, NOS) that is refractory to, or has relapsed after, treatment with at least 1 prior regimen. Eligible sub-types include DHL, THL, or DEL, as well as DLBCL or HGBL without MYC and/or BCL2 alterations. Criteria for DHL are concurrent MYC translocation+ and BCL2 translocation+ by fluorescence in situ hybridization (FISH) (same criteria for THL, which also includes BCL6 translocation+ by FISH); criteria for DEL are concurrent overexpression of MYC (≥ 40%) and BCL2 (> 50%) by immunohistochemistry (IHC).
  • Measurable disease by CT or PET/CT. MRI acceptable as per protocol.
  • Eastern Cooperative Oncology Group (ECOG) performance status of 0 to 1.
  • Recovery to Grade 1 or baseline of any toxicity due to prior systemic treatments (excluding alopecia).
  • Absolute neutrophil count ≥ 1,000/µL; platelets ≥ 75,000/µL for patients with no bone marrow involvement by malignancy; platelets ≥ 50,000/µL for patients with bone marrow involvement by malignancy.
  • Creatinine ≤ 1.5x upper limit of normal (ULN); total bilirubin ≤ 1.5x ULN; AST/ALT ≤ 2.5x ULN.
  • Life expectancy of at least 3 months.
Exclusion Criteria
  • Intention to undergo stem cell transplant (SCT) or treatment with chimeric antigen receptor (CAR) T-cell therapy.
  • SCT therapy within 100 days prior to starting study treatment.
  • Systemic anti-cancer therapy or investigational agent within 3 weeks of study entry, except for nitrosoureas or mitomycin C (6 weeks).
  • Other non-cytotoxic anti-cancer therapy or investigational agent within 5 half-lives or 21 days prior to study treatment, whichever is shorter, as long as any drug related toxicities have resolved to Grade 1 or less. Dexamethasone up to 12 mg/d is allowed as supportive therapy and does not exclude participation.
  • Contraindication to venetoclax or rituximab.
  • Progressive disease during treatment or within 3 months of stopping prior treatment with a BCL2 inhibitor, histone deacetylase (HDAC) inhibitor, or phosphoinositide-3 kinase (PI3k) inhibitor, or prior discontinuation of any of these therapies due to clinically significant toxicity.
  • Graft vs. host disease following prior allogeneic transplant within 3 months prior to study treatment.
  • Ongoing treatment with chronic immunosuppressants.
  • Active CNS lymphoma.
  • Known gastrointestinal condition that would interfere with swallowing or the oral absorption or tolerance of fimepinostat.
  • Serious infection requiring systemic antibiotic therapy within 14 days prior to study treatment.
  • Uncontrolled or severe cardiovascular disease
  • Unstable or clinically significant concurrent medical condition.
  • Second primary malignancy within 2 years of study entry other than what is specified in the protocol.
  • Known HIV positive, hepatitis B surface antigen-positive status, or known or suspected active hepatitis C infection.
  • Active CMV infection, presence of CMV antigenemia, or evidence of any invasive CMV end organ disease (e.g., CMV colitis).

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Fimepinostat - Continuous Once DailyfimepinostatFimepinostat 30-60 mg/day
Fimepinostat - 5x/weekfimepinostatFimepinostat 60-180 mg/day
Fimepinostat - Expansion 5x/weekfimepinostatFimepinostat 60 mg on the 5 days on/2 days off
Fimepinostat 60 mg - Combination w/ rituximabRituximabFimepinostat 60 mg 5 days on.2 days off plus rituximab
Fimepinostat 120 mg - Combination w/ rituximabfimepinostatFimepinostat 120 mg 3x/week plus rituximab
Fimepinostat 120 mg - Combination w/ rituximabRituximabFimepinostat 120 mg 3x/week plus rituximab
Fimepinostat 60 mg - Combination w/ rituximabfimepinostatFimepinostat 60 mg 5 days on.2 days off plus rituximab
Fimepinostat - Biocomparability ArmfimepinostatBiocomparability Arm
Fimepinostat 30 mg - Combination w/ venetoclaxfimepinostatFimepinostat 30 mg 5 days on/2 days off plus venetoclax. Different combinations of dose levels for venetoclax will be explored
Fimepinostat 30 mg - Combination w/ venetoclaxvenetoclaxFimepinostat 30 mg 5 days on/2 days off plus venetoclax. Different combinations of dose levels for venetoclax will be explored
Fimepinostat - Combination w/ venetoclax and rituximabfimepinostatFimepinostat and venetoclax dosed at dose levels determined for that combination. Rituximab dosed at 375 mg/m2 IV on Day 1 of each 21 day cycle
Fimepinostat - Combination w/ venetoclax and rituximabRituximabFimepinostat and venetoclax dosed at dose levels determined for that combination. Rituximab dosed at 375 mg/m2 IV on Day 1 of each 21 day cycle
Fimepinostat - 2x/weekfimepinostatFimepinostat 60-240 mg/day
Fimepinostat - 4x/weekfimepinostatFimepinosta 60-180 mg/day
Fimepinostat - 3x/weekfimepinostatFimepinostat 60-180 mg/day
Fimepinostat - Expansion 3x/weekfimepinostatFimepinostat 120 mg 3 days on/4 days off
Fimepinostat 60 mg - Combination w/ venetoclaxfimepinostatFimepinostat 60 mg 5 days on/2 days off plus venetoclax. Different combinations of dose levels for venetoclax will be explored
Fimepinostat 60 mg - Combination w/ venetoclaxvenetoclaxFimepinostat 60 mg 5 days on/2 days off plus venetoclax. Different combinations of dose levels for venetoclax will be explored
Primary Outcome Measures
NameTimeMethod
To determine the maximum tolerated dose (MTD) and recommended Phase 2 dose (RP2D) of oral fimepinostat (CUDC-907) in combination with venetoclax and rituximabAt the end of cycle 1 or 2 (each cycle is 21 days)

To be evaluated in patients with relapsed and/or refractory (R/R) diffuse large B-cell lymphoma (DLBCL) or high-grade B-cell lymphoma (HGBL). Within any given study arm, the highest dose level studied at which fewer than 2 out of 6 subjects (\< 33%) experience a dose limiting toxicity (DLT).

To assess the safety and tolerability of fimepinostat in combination with anti-cancer regimens by evaluating the number of participants with adverse events assessed using the NCI Common Terminology Criteria for Adverse Events (CTCAE, v4.0).18 months

Number of participants with adverse events assessed using the NCI Common Terminology Criteria for Adverse Events (CTCAE, v4.0).

To evaluate the efficacy of fimepinostat in combination with anti-cancer regimens by evaluating ORR24 months

ORR assessments as measured using Lugano criteria.

To evaluate the efficacy of fimepinostat in combination with anti-cancer regimens by evaluating DOR24 months

DOR assessments as measured using Lugano criteria.

Secondary Outcome Measures
NameTimeMethod
To assess PK of venetoclax when administered in combination with fimepinostat as measured by half-life (T1/2).Pre-dose to 21 - 28 days post dose

Pharmacokinetic parameters will include half-life (T1/2).

To assess PK of venetoclax when administered in combination with fimepinostat as measured by clearance (Cl).Pre-dose to 21 - 28 days post dose

Pharmacokinetic parameters will include clearance (Cl).

To assess PK of venetoclax when administered in combination with fimepinostat as measured by volume of distribution (Vd).Pre-dose to 21 - 28 days post dose

Pharmacokinetic parameters will include volume of distribution (Vd).

To assess pharmacokinetics (PK) of fimepinostat when administered in combination with anti-cancer regimens as measured by area under the concentration-time curve (AUC).Pre-dose to 21 - 28 days post dose

Pharmacokinetic parameters will include area under the concentration-time curve (AUC).

To assess pharmacokinetics (PK) of fimepinostat when administered in combination with anti-cancer regimens as measured by maximum plasma concentration (Cmax).Pre-dose to 21 - 28 days post dose

Pharmacokinetic parameters will include maximum plasma concentration (Cmax).

To assess pharmacokinetics (PK) of fimepinostat when administered in combination with anti-cancer regimens as measured by half-life (T1/2).Pre-dose to 21 - 28 days post dose

Pharmacokinetic parameters will include half-life (T1/2).

To assess pharmacokinetics (PK) of fimepinostat when administered in combination with anti-cancer regimens as measured by clearance (Cl).Pre-dose to 21 - 28 days post dose

Pharmacokinetic parameters will include clearance (Cl).

To assess pharmacokinetics (PK) of fimepinostat when administered in combination with anti-cancer regimens as measured by volume of distribution (Vd).Pre-dose to 21 - 28 days post dose

Pharmacokinetic parameters will include volume of distribution (Vd).

To assess PK of venetoclax when administered in combination with fimepinostat as measured by area under the concentration-time curve (AUC).Pre-dose to 21 - 28 days post dose

Pharmacokinetic parameters will include area under the concentration-time curve (AUC).

To assess PK of venetoclax when administered in combination with fimepinostat as measured by maximum plasma concentration (Cmax).Pre-dose to 21 - 28 days post dose

Pharmacokinetic parameters will include maximum plasma concentration (Cmax).

To evaluate the efficacy of fimepinostat in combination with anti-cancer regimens as measured by OS.24 months

OS measured using RECIL 2017 criteria and revised RECIST 1.1.

To evaluate the efficacy of fimepinostat in combination with anti-cancer regimens as measured by PFS.24 months

PFS measured using RECIL 2017 criteria and revised RECIST 1.1.

To evaluate the efficacy of fimepinostat in combination with anti-cancer regimens as measured by ORR.24 months

ORR measured using RECIL 2017 criteria and revised RECIST 1.1.

To evaluate the efficacy of fimepinostat in combination with anti-cancer regimens as measured by DOR.24 months

DOR measured using RECIL 2017 criteria and revised RECIST 1.1.

To evaluate biomarkers of fimepinostat activity24 months

Exploratory biological markers of fimepinostat activity will be assessed in PBMCs, plasma, and tumor and samples to explore biomarkers that correlate with safety and/or efficacy, such as CREBBP/EP300.

Trial Locations

Locations (11)

Winship Cancer Institute, Emory University

🇺🇸

Atlanta, Georgia, United States

Florida Cancer Specialists

🇺🇸

Sarasota, Florida, United States

University of Chicago Medicine

🇺🇸

Chicago, Illinois, United States

Hospital of the University of Pennsylvania

🇺🇸

Philadelphia, Pennsylvania, United States

Sarah Cannon Research Institute

🇺🇸

Nashville, Tennessee, United States

MD Anderson Cancer Center

🇺🇸

Houston, Texas, United States

USC/Norris Comprehensive Cancer Center

🇺🇸

Los Angeles, California, United States

Memorial Sloan-Kettering Cancer Center

🇺🇸

New York, New York, United States

Stephenson Cancer Center, University of Oklahoma Health Sciences Center

🇺🇸

Oklahoma City, Oklahoma, United States

Swedish Cancer Institute

🇺🇸

Seattle, Washington, United States

University of Michigan

🇺🇸

Ann Arbor, Michigan, United States

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