Actively Recruiting

Phase 1
Age: 12Years - 120Years
All Genders
ID04222413

First-in-Human Phase I Trial to Investigate the Safety, Tolerability, Pharmacokinetics, Biological and Clinical Activity of Metarrestin (ML-246) in Subjects With Metastatic Solid Tumors

Led by National Cancer Institute (NCI) · Updated on 2026-06-08

116

Participants Needed

2

Research Sites

52 weeks

Total Duration

On this page

AI-Summary

What this Trial Is About

Researchers are studying metarrestin, a new drug designed to target metastatic solid tumors, including pancreatic, breast, colorectal cancers, and certain pediatric solid tumors. Metastasis, the spread of cancer to other organs, causes most cancer deaths, and there are currently no treatments specifically to prevent or reduce it. This Phase I trial aims to find a safe dose of metarrestin and evaluate its ability to shrink tumors in patients whose cancers have not responded to standard treatments. Participants will receive metarrestin by mouth in cycles lasting about 28 days. The dosing involves an initial loading dose followed by regular doses three times a week. Adults and pediatric patients will be treated at doses determined to be safe in earlier parts of the study. Treatment continues until the cancer progresses or side effects become unacceptable. There are two phases: Phase IA focuses on finding the maximum tolerated dose, while Phase IB assesses the drug's effects at that dose. During the study, participants will undergo physical exams, blood tests, imaging scans like CT or MRI, cognitive tests, and brain activity monitoring. Adults may have tumor biopsies. They will keep a medicine diary and visit the clinic regularly, including two brief hospital stays in the first month and frequent visits afterward. After treatment ends, there is a follow-up visit after 30 days and then check-ins every six months for the rest of their life or until the study concludes. The main outcomes measured are the maximum tolerated dose and how well tumors respond to treatment.

CONDITIONS

Brief Title

Metarrestin (ML-246) in Subjects With Metastatic Solid Tumors

Who Can Participate

Age: 12Years - 120Years
All Genders

Eligibility Criteria

Eligible

You may qualify if you...

  • Adults aged 18 years or older with histologically or cytologically confirmed solid tumors (Phase IA).
  • Adults with pancreatic, colorectal, or breast cancer (Phase IB).
  • Pediatric subjects aged 12 to under 18 years with confirmed solid tumors other than rhabdomyosarcoma (Phase IB).
  • Disease not suitable for curative surgery, spread to at least one other organ, measurable by RECIST 1.1.
  • Disease progressed after at least one line of standard chemotherapy or no standard therapy option (depending on cohort).
  • Recovery from any prior treatment toxicity to grade 1 or less.
  • Karnofsky or Lansky performance status of 70% or higher.
  • Adequate blood, liver, kidney, and coagulation function per specified lab values.
  • Use of effective contraception for individuals of childbearing potential during and 120 days after treatment.
  • Willingness to discontinue nursing at treatment start.
  • Weight of at least 35 kg.
  • Ability to understand and sign informed consent.
  • Lesions accessible for biopsy and willingness to undergo biopsy (Cohort IB1).
  • Ability to swallow oral capsules.
Not Eligible

You will not qualify if you...

  • Recent anticancer treatments or surgeries within specified timeframes before starting treatment.
  • Use of medications strongly affecting CYP3A4 that cannot be safely stopped.
  • Cardiomyopathy or significant heart conditions diagnosed within 6 months.
  • Positive for HIV, HCV, or HBV and on antiviral drugs.
  • History of other cancers within 3 years, except certain non-invasive types.
  • Rapidly progressing disease that may prevent study participation.
  • Central nervous system metastases or disorders increasing neurotoxicity risk.
  • Active infections including tuberculosis with symptoms.
  • History of seizures or increased seizure risk based on EEG.
  • Clinically relevant uncontrolled medical conditions.
  • Previous gastric bypass, feeding tubes, or malabsorption conditions.
  • Pregnant individuals.

AI-Screening

AI-Powered Screening

Complete this quick 3-step screening to check your eligibility

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Your Study Journey

Screening

Duration - 2 to 4 weeks

Participants are screened for eligibility to participate in the trial.

1 visit (in-person)

Treatment

Duration - Repeated 28-day cycles until disease progression or discontinuation

Participants receive metarrestin orally in 28-day cycles with dosing schedules that vary by dose level during Phase IA and at the maximum tolerated dose during Phase IB until disease progression or unacceptable toxicity.

Visits on Mondays, Wednesdays, and Fridays of each cycle after initial loading dose days

Follow-up

Duration - 28 days after treatment ends

Participants are monitored for safety and tolerability up to 28 days after treatment discontinuation.

Approximately 1 to 2 visits

Trial Site Locations

Total: 2 locations

1

University of Kansas

Fairway, Kansas, United States, 66205

Actively Recruiting

2

National Institutes of Health Clinical Center

Bethesda, Maryland, United States, 20892

Actively Recruiting

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Research Team

M

Murielle Hogu

U

Udo Rudloff, M.D.

How is the study designed?

Study Type

INTERVENTIONAL

Masking

NONE

Allocation

NON_RANDOMIZED

Model

SEQUENTIAL

Primary Purpose

TREATMENT

Number of Arms

2

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