MedPath

CA-4948-101: Open-Label, Dose Escalation and Expansion Trial of Emavusertib (CA-4948) in Relapsed or Refractory Primary Central Nervous System Lymphoma (R/R PCNSL)

Phase 1
Recruiting
Conditions
Relapsed Primary Central Nervous System Lymphoma
Relapsed Hematologic Malignancy
Refractory Primary Central Nervous System Lymphoma
Refractory Hematologic Malignancy
Interventions
Registration Number
NCT03328078
Lead Sponsor
Curis, Inc.
Brief Summary

This is a multi-center, open-label study to evaluate the safety, pharmacokinetics (PK), and anti-cancer activity of oral administration of emavusertib alone or in combination with ibrutinib in adult participants with relapsed or refractory (R/R) hematologic malignancies.

This trial will be completed in four parts. In Part A1, emavusertib will be evaluated first in a dose escalating monotherapy setting to establish the safety and tolerability (complete). In Part A2, emavusertib will be evaluated in combination with ibrutinib at 560 milligrams (mg) once daily (QD) or 420 mg QD as indicated by disease (Part A2 complete).

Part B will comprise 2 cohorts to assess safety and efficacy of emavusertib in combination with ibrutinib in participants with R/R primary central nervous system lymphoma (PCNSL) who have directly progressed on a bruton tyrosine kinase inhibitor (BTKi). In this part of the study, emavusertib will be dosed at 100 mg or 200 mg twice daily (BID) in combination with ibrutinib in 28-day treatment cycles.

Part C will comprise 3 treatment arms in the second-line setting to assess the efficacy and safety of emavusertib monotherapy, ibrutinib monotherapy, and emavusertib in combination with ibrutinib in participants with R/R PCNSL who are naïve to BTKi treatment. In this part of the study, eligible second-line participants with R/R PCNSL who are naïve to BTKi treatment will be randomized 1:1:1 to 1 of 3 treatment arms: (1) emavusertib 200 mg BID, (2) ibrutinib 560 mg QD, or (3) emavusertib 200 mg BID in combination with ibrutinib 560 mg QD.

Detailed Description

Not available

Recruitment & Eligibility

Status
RECRUITING
Sex
All
Target Recruitment
152
Inclusion Criteria
  1. Males and females greater than or equal to 18 years of age

  2. Life expectancy of at least 3 months

  3. Eastern Cooperative Oncology Group (ECOG) Performance Status of 0, 1 or 2

  4. Histopathologically confirmed diagnosis of PCNSL (medical record is acceptable). Cerebral biopsies are not required if imaging reveals typical images of PCNSL.

    1. Participants with parenchymal lesions must have unequivocal evidence of disease progression (e.g., presence of at least 1 measurable target lesion [≥ 10 millimeters (mm) and ≤ 40 mm in the longest diameter on brain magnetic resonance imaging [MRI] or head computed tomography [CT] on imaging within 28 days prior to Cycle 1 Day 1]). In cases where the tumor size is smaller but still measurable and located at a critical central nervous system (CNS) location, disabling the participant and/or causing symptoms, this participant may be eligible following a discussion with the Sponsor Medical Monitor.
    2. For participants limited to leptomeningeal involvement, cerebrospinal fluid (CSF) analysis (cytology and/or flow cytometry) with or without additional imaging (MRI) of the spine as clinically indicated is required to document abnormal cells within 28 days prior to Cycle 1 Day 1.

Exclusion Criteria for Part B and Part C

  1. Participants with only intraocular PCNSL without brain lesion or CSF involvement, T-cell lymphoma, systemic presence of lymphoma, or non-CNS lymphoma metastatic to the CNS

  2. Evidence of systemic lymphoma. This must be demonstrated by a positron emission tomography (PET) scan (or CT scan with contrast if applicable) of the chest, abdomen, and pelvis at Screening (testicular ultrasound may be considered to exclude a testicular lymphoma disseminated to the brain).

  3. Prior history of malignancies other than lymphoma (except for basal cell or squamous cell carcinoma of the skin or carcinoma in situ of the cervix or breast) or prior history of systemic lymphoma, unless the participant has been free of the disease for ≥ 3 years.

  4. Active malignancy other than PCNSL requiring systemic therapy

  5. Previous BTKi treatment (Part C only).

  6. History of Grade ≥ 3 rhabdomyolysis without complete recovery

  7. Requirement for urgent therapy due to uncontrolled tumor mass/edema effects.

  8. Received external beam radiation therapy to the CNS within 28 days prior to Cycle 1 Day 1.

  9. Received prior investigational drugs (including treatment in clinical research, unapproved combination products, and new dosage forms) within 28 days or 5 half-lives, whichever is shorter, prior to Cycle 1 Day 1; allogeneic hematopoietic stem cell transplant (HSCT) within 60 days prior to Cycle 1 Day 1; or had clinically significant graft-versus-host disease (GVHD) requiring ongoing up-titration of immunosuppressive medications prior to Screening (with the exception of a BTKi for Part B only).

    Note: The use of a stable or tapering dose of immunosuppressive therapy post-HSCT and/or topical steroids for ongoing skin GVHD is permitted with Sponsor Medical Monitor approval

  10. Any prior systemic anti-cancer treatment such as chemotherapy, immunomodulatory drug therapy, etc., received within 14 days or 5 half-lives, whichever is shorter, prior to Cycle 1 Day 1 (with the exception of ibrutinib or other BTKi for Part B only, which may be continued until the day before Cycle 1 Day 1)

  11. Prior history of hypersensitivity or anaphylaxis to emavusertib, ibrutinib or any of their excipients.

Exclusion Criteria

Not provided

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Emavusertib (CA-4948) dose escalationEmavusertibPart A1: Dose-level cohorts with up to approximately 6 participants each will be used to define the Maximum Tolerated Dose (MTD) for emavusertib.
Emavusertib (CA-4948) and ibrutinib dose escalationEmavusertibPart A2: Evaluate escalating dose levels of oral emavusertib in combination with 560 mg QD or 420 mg QD of oral ibrutinib. The starting dose of emavusertib to be used in combination will be 200 mg BID. It is anticipated that 12 to 20 participants at a potential dose level will be required to establish optimal combination dosing.
Emavusertib (CA-4948) and ibrutinib dose escalationIbrutinibPart A2: Evaluate escalating dose levels of oral emavusertib in combination with 560 mg QD or 420 mg QD of oral ibrutinib. The starting dose of emavusertib to be used in combination will be 200 mg BID. It is anticipated that 12 to 20 participants at a potential dose level will be required to establish optimal combination dosing.
Emavusertib (CA-4948) and ibrutinib dose expansionEmavusertibIn two Expansion Cohorts (Part B), emavusertib in combination with ibrutinib will be administered in participants with R/R PCNSL who have progressed on a BTKi. In Cohort 1, emavusertib 100 mg BID will be administered with ibrutinib 560 mg QD consecutively in 28-day treatment cycles. In Cohort 2, emavusertib 200 mg BID will be administered with ibrutinib 560 mg QD consecutively in 28-day treatment cycles.
Emavusertib (CA-4948) and ibrutinib dose expansionIbrutinibIn two Expansion Cohorts (Part B), emavusertib in combination with ibrutinib will be administered in participants with R/R PCNSL who have progressed on a BTKi. In Cohort 1, emavusertib 100 mg BID will be administered with ibrutinib 560 mg QD consecutively in 28-day treatment cycles. In Cohort 2, emavusertib 200 mg BID will be administered with ibrutinib 560 mg QD consecutively in 28-day treatment cycles.
Emavusertib (CA-4948) and ibrutinibEmavusertibIn this part of the study (Part C), eligible second-line participants with R/R PCNSL who are naïve to BTKi treatment will receive 1 of 3 treatment arms: (1) emavusertib 200 mg BID, (2) ibrutinib 560 mg QD, or (3) emavusertib 200 mg BID in combination with ibrutinib 560 mg QD. Treatments will be administered continuously in 28-day treatment cycles.
Emavusertib (CA-4948) and ibrutinibIbrutinibIn this part of the study (Part C), eligible second-line participants with R/R PCNSL who are naïve to BTKi treatment will receive 1 of 3 treatment arms: (1) emavusertib 200 mg BID, (2) ibrutinib 560 mg QD, or (3) emavusertib 200 mg BID in combination with ibrutinib 560 mg QD. Treatments will be administered continuously in 28-day treatment cycles.
Primary Outcome Measures
NameTimeMethod
Part A: To determine the safety and tolerability of emavusertib as a monotherapy and in combination with ibrutinib: dose-limiting toxicity (DLT)12 months

The number of participants with a dose-limiting toxicity (DLT) in the first treatment cycle

Part A: Maximum tolerated dose (MTD) of emavusertib as a monotherapy and in combination with ibrutinib measured by dose-limiting toxicities (DLTs)12 months

MTD determined by the highest dose level studied at which fewer than 2 out of 6 subjects (\<33%) experience a dose limiting toxicity.

Part A: Recommended Phase 2 Dose (RP2D) of emavusertib as a monotherapy and in combination with ibrutinib based on overall tolerability data12 months

RP2D selected based on overall tolerability data from all participants treated at different dose levels and will not exceed the MTD.

Part B: Overall Response Rate (ORR) in participants with R/R PCNSL18 months
Part C: ORR in participants with R/R PCNSL18 months
Secondary Outcome Measures
NameTimeMethod
Parts A, B and C: Pharmacokinetic (PK) profile of emavusertib and ibrutinib measured by Cmax24- 66 months

Maximum plasma concentration (Cmax)

Parts A, B and C: Pharmacokinetic (PK) profile of emavusertib and ibrutinib measured by Cmin24- 66 months

Minimum plasma concentration (Cmin)

Parts A, B and C: Pharmacokinetic (PK) profile of emavusertib and ibrutinib measured by Tmax24- 66 months

Time to maximum plasma concentration (Tmax)

Parts A, B and C: Pharmacokinetic (PK) profile of emavusertib and ibrutinib measured by AUC24- 66 months

Area Under the concentration-time curve (AUC)

Parts A, B and C: Pharmacokinetic (PK) profile of emavusertib and ibrutinib measured by plasma terminal half-life24- 66 months

Plasma terminal elimination half-life (T 1/2)

Part A: To assess efficacy of emavusertib as a monotherapy and in combination with ibrutinib measured by ORR24- 36 months

Assessed by ORR

Parts A, B and C: To assess efficacy of emavusertib as a monotherapy and in combination with ibrutinib and ibrutinib as monotherapy measured by duration of response (DOR)24- 66 months

Assessed by DOR

Part A: To assess efficacy of emavusertib as a monotherapy and in combination with ibrutinib measured by disease control rate (DCR)24- 36 months

Assessed by DCR

Parts A, B and C: To assess efficacy of emavusertib as a monotherapy and in combination with ibrutinib and ibrutinib as monotherapy measured by progression free survival (PFS)24- 66 months

Assessed by PFS

Parts A, B and C: To assess efficacy of emavusertib as a monotherapy, in combination with ibrutinib and ibrutinib as monotherapy measured by overall survival (OS)24 - 66 months

Assessed by OS

Parts B and C: To assess the safety and tolerability of emavusertib as monotherapy, ibrutinib as monotherapy and emavusertib in combination with ibrutinib in participants with R/R PCNSLup to 66 months

Measured by the number of participants with treatment-emergent adverse events (TEAEs) and treatment-related adverse events

Trial Locations

Locations (41)

St. Joseph's Hospital and Medical Center

🇺🇸

Phoenix, Arizona, United States

Mayo Clinic

🇺🇸

Rochester, Minnesota, United States

City of Hope

🇺🇸

Duarte, California, United States

Providence St. John's Health Center

🇺🇸

Santa Monica, California, United States

UCLA Department of Medicine - Hematology/Oncology

🇺🇸

Santa Monica, California, United States

Smilow Cancer Hospital at Yale-New Haven

🇺🇸

New Haven, Connecticut, United States

Northwestern Memorial Hospital

🇺🇸

Chicago, Illinois, United States

Dana Farber Cancer Institute

🇺🇸

Boston, Massachusetts, United States

Fred and Pamela Buffett Cancer Center

🇺🇸

Omaha, Nebraska, United States

Hackensack University Medical Center

🇺🇸

Hackensack, New Jersey, United States

Roswell Park Comprehensive Cancer Center

🇺🇸

Buffalo, New York, United States

Mt Sinai

🇺🇸

New York, New York, United States

Columbia University Irving Medical Center

🇺🇸

New York, New York, United States

Memorial Sloan Kettering Cancer Center

🇺🇸

New York, New York, United States

Duke University Medical Center, Duke Cancer Center

🇺🇸

Durham, North Carolina, United States

Cleveland Clinic

🇺🇸

Cleveland, Ohio, United States

Providence Neurological Specialties West

🇺🇸

Portland, Oregon, United States

Hospital of the University of Pennsylvania

🇺🇸

Philadelphia, Pennsylvania, United States

UPMC Hilman Cancer Center

🇺🇸

Pittsburgh, Pennsylvania, United States

University of Tennessee Medical Center

🇺🇸

Knoxville, Tennessee, United States

UT Southwestern Medical Center

🇺🇸

Dallas, Texas, United States

The University of Texas MD Anderson Cancer Center

🇺🇸

Houston, Texas, United States

Huntsman Cancer Institute, University of Utah

🇺🇸

Salt Lake City, Utah, United States

Swedish Cancer Institute

🇺🇸

Seattle, Washington, United States

University of Washington Medical Center

🇺🇸

Seattle, Washington, United States

Všeobecná fakultní nemocnice v Praze

🇨🇿

Prague, Czechia

Institut Bergonie

🇫🇷

Bordeaux, France

Hopital de la Timone

🇫🇷

Marseille, France

Hospital Pitie Salpetriere

🇫🇷

Paris, France

Institut Curie Hospital

🇫🇷

Paris, France

Hematology Department Soroka UMC / Heanatology Department

🇮🇱

Be'er Sheva, Israel

Hadassah Medical Center / Ein-Carem

🇮🇱

Jerusalem, Israel

Università di Torino Croce e Carle

🇮🇹

Cuneo, Italy

SODc Ematologia Azienda Ospedaliera Universitaria Careggi

🇮🇹

Firenze, Italy

IRST - Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori

🇮🇹

Meldola, Italy

IRCCS San Raffaele Scientific Institute

🇮🇹

Milano, Italy

Uniwersyteckie Centrum Kliniczne Osrodek Badan Klinicznych Wczesnych Faz

🇵🇱

Gdańsk, Poland

Oddzial Kliniczny Hematologii

🇵🇱

Kraków, Poland

NarodowyInstytutu Onkologii im. Marii Sklodowskiej-Curie-Panstwowy Instytutu Badawczy

🇵🇱

Warsaw, Poland

MD Anderson Cancer Center Madrid

🇪🇸

Madrid, Spain

Hospital Universitario Virgen del Rocio

🇪🇸

Sevilla, Spain

© Copyright 2025. All Rights Reserved by MedPath