MedPath

Study of Oral MRT-2359 in Selected Cancer Patients

Phase 1
Recruiting
Conditions
NSCLC
Prostate Cancer
HR-positive, HER2-negative Breast Cancer
DLBCL
L-MYC and N-MYC Amplified Solid Tumors
SCLC
High Grade Neuroendocrine Cancer
NSCLC With High or Low L-MYC or N-MYC Expression
Interventions
Registration Number
NCT05546268
Lead Sponsor
Monte Rosa Therapeutics, Inc
Brief Summary

This Phase 1/2, open-label, multicenter study is conducted in patients with previously treated selected solid tumors, including non-small cell lung cancer (NSCLC), small cell lung cancer (SCLC), high-grade neuroendocrine cancer of any primary site, diffuse large B-cell lymphoma (DLBCL), and tumors with L-MYC or N-MYC amplification. Patients receive escalating doses of a GSPT1 molecular glue degrader MRT-2359 to determine safety, tolerability, maximum tolerated dose (MTD) and/or recommended Phase 2 dose (RP2D) of MRT-2359. Once the MTD and/or RP2D is identified, additional patients enroll to Phase 2 study, which includes molecular biomarkers stratification or selection, namely expression or amplification of L-MYC and N-MYC genes, hormone receptor positive (HR)-positive, human epidermal growth factor 2 (HER2)-negative breast cancer and prostate cancer.

Detailed Description

This Phase 1/2, open-label, multicenter, dose escalation and expansion study to assess the safety, tolerability, pharmacokinetic (PK), pharmacodynamic (PD), and preliminary clinical activity of MRT-2359 in patients with previously treated selected solid tumors, including lung cancer (NSCLC and SCLC), high-grade neuroendocrine cancer of any primary site, and DLBCL.

* The primary aim of Phase 1 part is safety, tolerability, MTD and/or RP2D of MRT-2359.

* The primary aim of Phase 2 part is assessment of preliminary anti-tumor activity of MRT-2359.

Recruitment & Eligibility

Status
RECRUITING
Sex
All
Target Recruitment
174
Inclusion Criteria
  • Have a selected advanced solid tumor or DLBCL (listed above) for which there are no further standard therapeutic options available
  • Be age ≥ 18 years and willing to voluntarily complete the informed consent process
  • A predicted life expectancy of ≥ 3 months and an ECOG performance status ≤ 2
  • Have measurable disease by RECIST 1.1 (Eisenhauer et al., 2009) in case of solid tumors or Revised Response Criteria for Malignant Lymphoma (Phase 1 only) (Cheson et al., 2014) in case of DLBCL
  • Have adequate organ function defined by the selected laboratory parameters
  • If female of childbearing potential, avoid becoming pregnant and agree to use acceptable methods of contraception after informed consent, throughout the study, and for 90 days after the last dose of MRT-2359
  • Male of reproductive potential must use an approved methods of contraception from informed consent until 90 days after study discharge
Read More
Exclusion Criteria
  • Have received prior chemotherapy, definitive radiation, biological cancer therapy or any investigational agent within 21 days before the first dose of study treatment, or have any AEs that have failed to recover to baseline. In patients with prostate cancer, continuance of systemic therapies to maintain castration levels of testosterone is allowed. Pre-menopausal patients with hormone-dependent breast cancer can continue on therapies used for suppression of ovarian function.
  • Have received bisphosphonates or denosumab within 14 days before the first administration of the study drug unless they were given for acute hypercalcemia
  • Inability to swallow oral medication
  • Have received prior therapy with a GSPT1 degrader that was discontinued due to an AE
  • Have received prior auto-HCT and not fully recovered from effects of the last transplant
  • Have received prior allogeneic hematopoietic stem cell transplantation within past 6 months and/or have symptoms of graft-versus-host disease. Patients requiring minimal intervention such as topical steroids are eligible
  • Have received a live vaccine within 90 days before the first dose of study treatment
  • COVID-19 immunization within 14 days of receiving the first dose of MRT-2359
  • Current use of chronic systemic steroid therapy in excess of replacement doses (prednisone ≤ 10 mg/day is acceptable)
  • Have clinically significant active malabsorption syndrome or other condition likely to affect gastrointestinal absorption of the study drug
  • Have a history of a second malignancy, unless controlled not requiring therapy
  • Have clinically active central nervous system involvement and/or carcinomatous meningitis. Patients with treated and stable brain metastases (not progressing for at least 4 weeks prior to enrollment) not requiring steroids are eligible
  • Have a confirmed history of (non-infectious) pneumonitis that required steroids
  • Have known human immunodeficiency virus (HIV) unless the patient is on antiviral therapy with undetectable HIV RNA levels
  • Have known hepatitis B or C infection(s) unless treated with undetectable hepatitis B DNA or hepatitis C RNA levels
  • Clinically significant cardiac disease
  • Be pregnant or breastfeeding
Read More

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Phase 2 Expansion - NSCLCOral MRT-2359Patients with NSCLC with high or low L-MYC or N-MYC expression
Phase 2 Expansion - L-MYC or N-MYC amplified solid tumorsOral MRT-2359Patients with L-MYC or N-MYC amplified solid tumors
Phase 1 Dose EscalationOral MRT-2359Patients with NSCLC, SCLC, high-grade neuroendocrine cancer of any primary site, any solid tumors with L-MYC or N-MYC amplification, or DLBCL
Phase 2 Expansion - SCLCOral MRT-2359Patients with SCLC
Phase 2 Expansion - HR-positive, HER2-negative breast cancerOral MRT-2359Patients with HR-positive, HER2-negative breast cancer in combination with fulvestrant
Phase 2 Expansion - Prostate CancerOral MRT-2359Patients with prostate cancer in combination with enzalutamide
Primary Outcome Measures
NameTimeMethod
Phase 1 Evaluates safety and tolerability of MRT-2359 over a 28-day cycle by the occurrence and frequency of dose limiting toxicities (DLTs) for determination of the MTD and/or RP2D28 days
Phase 2 Evaluates preliminary anti-tumor activity of MRT-2359 by overall response rate (ORR) as determined by RECIST 1.156 days (up to approximately 24 months from screening to end of study participation
Secondary Outcome Measures
NameTimeMethod
Phase 1 safety and tolerability of MRT-2359 (orally over a 28-day cycle) by the nature, incidence, and severity of all treatment-emergent adverse events (TEAEs), including treatment-related TEAEs and serious adverse events (SAEs)18 months
Phase 1 Dose Escalation evaluates the effect of a high-fat meal on the relative bioavailability of MRT-2359 by standard primary PK parameters including, but not limited to, AUC and Cmax7 days
Phase 1 Dose Escalation characterizes the PK profile of MRT-2359 by standard primary PK parameters including, but not limited to, AUC, Cmax, tmax, and t1/228 days
Phase 2 Dose Expansion further characterizes the PK profile of MRT-2359 by evaluating MRT-2359 plasma concentration to establish PK parameters including, but not limited to, Cmax, tmax, AUC0-t, AUC0inf, mean residence time, accumulation ratio, etc.28 days
Phase 2 Dose Expansion evaluates the safety and tolerability of MRT-2359 administered orally over a 28-day cycle by the nature, incidence, and severity of all TEAEs, including treatment-related TEAEs and SAEs according to the NCI CTCAE, version 5.024 months
Phase 1 preliminary anti-tumor activity: ORR (RECIST 1.1/Revised Response Criteria for Malignant Lymphoma),duration of response for complete response(CR)/partial response(PR), disease control rate, progression-free survival, overall survival18 months
Phase 2 Dose Expansion evaluates additional measures of the preliminary anti-tumor activity of MRT-2359 such as DoR (in patients with the best overall response of CR or PR)24 months
Phase 2 Dose Expansion evaluates additional measures of the preliminary anti-tumor activity of MRT-2359 such as PFS24 months
Phase 2 Dose Expansion evaluates additional measures of the preliminary anti-tumor activity of MRT-2359 such as OS24 months
Phase 2 Dose Expansion evaluates additional measures of the preliminary anti-tumor activity of MRT-2359 such as PSA response24 months
Phase 2 Dose Expansion evaluates additional measures of the preliminary anti-tumor activity of MRT-2359 such as DCR24 months

Trial Locations

Locations (19)

Honor Health Research Institute

🇺🇸

Scottsdale, Arizona, United States

Hoag Memorial Hospital Presbyterian

🇺🇸

Newport Beach, California, United States

University of California San Diego

🇺🇸

San Diego, California, United States

Yale University

🇺🇸

New Haven, Connecticut, United States

Sarah Cannon Research Institute

🇺🇸

Nashville, Tennessee, United States

Indiana University

🇺🇸

Bloomington, Indiana, United States

University of Kansas Cancer Center

🇺🇸

Lawrence, Kansas, United States

Dana Farber Cancer Institute

🇺🇸

Boston, Massachusetts, United States

Henry Ford Cancer Institute

🇺🇸

Detroit, Michigan, United States

Washington University

🇺🇸

Saint Louis, Missouri, United States

Memorial Sloan Kettering Cancer Center

🇺🇸

New York, New York, United States

Columbia University Irving Medical Centre

🇺🇸

New York, New York, United States

Mary Crowley Cancer Research

🇺🇸

Dallas, Texas, United States

MD Anderson Cancer Center

🇺🇸

Houston, Texas, United States

South Texas Accelerated Research Therapeutics (START)

🇺🇸

San Antonio, Texas, United States

Virginia Cancer Specialists Research Institute

🇺🇸

Fairfax, Virginia, United States

Fred Hutchinson Cancer Center

🇺🇸

Seattle, Washington, United States

Cross Cancer Institute

🇨🇦

Edmonton, Alberta, Canada

Princess Margaret Hospital

🇨🇦

Toronto, Ontario, Canada

© Copyright 2025. All Rights Reserved by MedPath