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Dual BET and CBP/p300 Inhibitor in Patients With Targeted Advanced Solid Tumors

Phase 1
Recruiting
Conditions
Castrate Resistant Prostate Cancer
NUT Carcinoma
Chronic Myelomonocytic Leukemia
Myelofibrosis
Interventions
Registration Number
NCT05488548
Lead Sponsor
Epigenetix, Inc.
Brief Summary

A Phase 1, first-in-human study of EP31670, a dual BET and CBP/p300 inhibitor in patients with targeted advanced solid tumors.

Detailed Description

EP31670 (also known as NEO2734) is a first-in-class dual BET and CBP/p300 inhibitor which has demonstrated antitumor activity in in vitro and in vivo models of human cancer. This Phase I open-label, multi-center, dose-escalation study will assess the safety and determine the maximum tolerated dose of EP31670 administered orally in patients with castration-resistant prostate cancer, NUT midline carcinoma and other targeted advanced solid tumors.

Recruitment & Eligibility

Status
RECRUITING
Sex
All
Target Recruitment
50
Inclusion Criteria
  • Relapse or refractory castration-resistant prostate cancer (CRPC) following at least one anti-androgen regimen and a docetaxel-containing regimen OR
  • metastatic or unresectable NUT midline carcinoma for which standard curative or palliative measures do not exist; OR
  • patients who have other types of relapsed or refractory solid tumors with pathological and/or biological features suggesting a potential benefit from dual BET and CBP/p300 inhibition may be enrolled after discussion with and approval from medical monitor and sponsor
  • Eastern Cooperative Oncology Group (ECOG) performance status 0-1
  • Life expectancy ≥ 3 months
  • Evaluable disease
  • Adequate bone marrow function:

Hemoglobin ≥ 9.0 g/dL Absolute neutrophil count (ANC) ≥ 1,500/dL Platelet count ≥100,000/μL

  • Adequate renal function:

Creatinine clearance (CLcr) estimated by Cockcroft-Gault Equation to be ≥ 60 mL/min. Estimated glomeruli filtration rate (eGRF) ≥ 60 mL/min may be used if provided by the testing laboratory

  • Adequate liver function

    • Total bilirubin ≤ 1.5 x ULN except in patients diagnosed with Gilbert's disease for which direct bilirubin must be ≤ 1.5 x ULN
    • Alanine aminotransferase (ALT) or aspartate Aminotransferase (AST) ≤ 2.5 x ULN or ≤ 5 x ULN in patients with liver metastases
  • Internal normalized ratio for prothrombin time (INR) ≤ 1.2 in patients not receiving chronic anticoagulation

  • Four weeks from prior anti-cancer therapy including chemotherapy, immunotherapy, investigational anti-cancer therapy or 5 half-lives from targeted agents, radiation and have recovered from prior treatment toxicities to grade 1 or less. Prostate cancer patients may continue androgen-deprivation therapy by luteinizing hormone-releasing hormone (LHRH) agonists.

  • Four weeks from major surgery.

  • For fertile men and women, agreement to use effective contraceptive methods duration of study participation and 4 weeks after the last dose of study drug.

  • Ability to understand and willingness to sign the informed consent form.

Exclusion Criteria
  • New and progressive central nervous system (CNS) metastasis; patients with treated brain metastases are eligible if follow-up brain imaging at least 4 weeks after CNS-directed therapy shows no evidence of progression and the patient is neurologically stable
  • Corrected QT interval ≥470 msec
  • Uncontrolled concurrent illnesses including, but not limited to, ongoing active infection requiring intravenous antibiotics or antifungal agents, symptomatic congestive heart failure, unstable angina pectoris, cardiac arrhythmia or psychiatric illness/social situations that would affect compliance with study requirements; patients with a prior or concurrent malignancy whose natural history or treatment does not have the potential to interfere with the safety or efficacy assessment of EP31670 are eligible for this trial
  • Pregnant or lactating women
  • Known history of hepatitis B, hepatitis C requiring antiviral treatment
  • Human immunodeficiency virus (HIV)-infected patients on effective anti-retroviral therapy with undetectable viral load within 6 months are eligible for this trial

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Part 1EP31670Patients will be assigned escalated dose according to BOIN design. The starting dose is 5 mg orally once a day for 7 consecutive days followed by 14 days of rest.
Part 2EP31670Patients will be assigned escalated dose according to BOIN design. The starting dose is 20 mg orally once a day for 14 consecutive days followed by 14 days of rest.
Part 3EP31670Patients will be assigned escalated dose according to BOIN design. The starting dose is 10 mg orally once a day for 14 consecutive days in combination with ruxolitinib or momelotinib followed by 14 days of rest according to the traditional 3 + 3 design by the modified Fibonacci sequence
Primary Outcome Measures
NameTimeMethod
Maximum Tolerated Dose (MTD)Within 3 weeks (one cycle) of treatment

MTD is the highest dose level at which ≤30% of patients experienced DLTs during cycle 1.

Dose Limiting Toxicities (DLT)Within 3 weeks (one cycle) of treatment

DLT is any of the following adverse events (AEs) that occur during cycle 1.

Recommended Phase 2 Dose (RP2D)through study completion, an average of 1 year

RP2D will be the MTD

Secondary Outcome Measures
NameTimeMethod

Trial Locations

Locations (6)

Mayo Clinic Arizona

🇺🇸

Phoenix, Arizona, United States

Mayo Clinic Florida

🇺🇸

Jacksonville, Florida, United States

Dana Farber Cancer Institute

🇺🇸

Boston, Massachusetts, United States

Mayo Clinic Rochester

🇺🇸

Rochester, Minnesota, United States

The University of Texas MD Anderson Cancer Center

🇺🇸

Houston, Texas, United States

University of Washington/Fred Hutchinson Cancer Center

🇺🇸

Seattle, Washington, United States

Mayo Clinic Arizona
🇺🇸Phoenix, Arizona, United States
Clinical Trials Referral Office
Contact
855-776-0015
Jeanne Palmer, MD
Principal Investigator

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