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Binimetinib

Binimetinib is an innovative drug being studied in clinical trials for treating several types of cancer. This article summarizes key information about ongoing research into binimetinib’s potential as a cancer therapy, including its mechanisms, target cancers, and early results from clinical studies.

Table of Contents

What is Binimetinib?

Binimetinib is a medication used in the treatment of various types of cancer. It’s also known by several other names, including MEK162, ARRY-438162, and Mektovi[1]. This drug belongs to a class of medications called MEK inhibitors, which work by targeting specific proteins in cancer cells to slow down or stop their growth[2].

How Binimetinib Works

Binimetinib works by blocking proteins called MEK1 and MEK2. These proteins are part of a pathway in cells that helps control cell growth. In some cancers, this pathway is overactive, leading to uncontrolled cell growth. By blocking MEK1 and MEK2, binimetinib can help slow down or stop the growth of cancer cells[1].

Conditions Treated with Binimetinib

Binimetinib is being studied for the treatment of several types of cancer, including:

  • Melanoma: A type of skin cancer[3]
  • Colorectal cancer: Cancer of the colon or rectum[4]
  • Gastrointestinal stromal tumors (GIST): A rare type of cancer that occurs in the digestive tract[5]
  • Hairy cell leukemia: A rare type of blood cancer[6]
  • Plexiform neurofibromas: Tumors that grow on nerves, associated with a condition called neurofibromatosis type 1[7]

Combination Therapies

Binimetinib is often used in combination with other cancer drugs to enhance its effectiveness. Some common combinations include:

  • Binimetinib + Encorafenib: This combination is used to treat melanoma with a specific genetic mutation called BRAF V600[8]
  • Binimetinib + Encorafenib + Cetuximab: This triple combination is being studied for colorectal cancer[4]
  • Binimetinib + Avelumab: This combination is being studied for various solid tumors[2]
  • Binimetinib + Pexidartinib: This combination is being studied for gastrointestinal stromal tumors[5]

Current Clinical Trials

Binimetinib is currently being studied in several clinical trials for different types of cancer. These trials are investigating its effectiveness, safety, and optimal dosing. Some notable trials include:

  • A study comparing binimetinib combined with encorafenib and pembrolizumab to standard immunotherapy for advanced melanoma[9]
  • A trial testing binimetinib for cancers with specific genetic changes (NRAS mutations)[1]
  • A study of binimetinib in children and adults with plexiform neurofibromas[7]

Potential Side Effects

Like all medications, binimetinib can cause side effects. Common side effects may include:

  • Fatigue
  • Nausea
  • Diarrhea
  • Vomiting
  • Skin rashes
  • Vision changes

More serious side effects can occur, which is why patients are closely monitored during treatment[7].

How Binimetinib is Administered

Binimetinib is typically taken orally (by mouth) in the form of tablets. The usual dose is 45mg twice daily, but this can vary depending on the specific treatment plan and any other medications being taken[6]. It’s important to take binimetinib exactly as prescribed by your doctor.

Cancer Type Trial Phase Combination Key Findings/Objectives
Various advanced cancers with NRAS mutations Phase II Binimetinib alone Evaluating objective response rate and progression-free survival
Gastrointestinal stromal tumor (GIST) Phase I Binimetinib + Pexidartinib Assessing safety, tolerability, and recommended Phase 2 dose
Hairy cell leukemia (BRAF wild-type) Phase II Binimetinib alone Determining overall response rate in relapsed/refractory patients
Neurofibromatosis type 1 (NF1) plexiform neurofibromas Phase II Binimetinib alone Evaluating tumor volume reduction and safety in children and adults
Melanoma with BRAF V600 mutation and hepatic impairment Phase I Binimetinib + Encorafenib Assessing pharmacokinetics and safety in patients with liver dysfunction
Colorectal cancer with BRAF V600E mutation Phase II Binimetinib + Encorafenib + Cetuximab Evaluating neoadjuvant treatment efficacy and tumor regression
Advanced cancers with non-V600 BRAF mutations Phase I/II Binimetinib + Encorafenib Determining safety and efficacy of combination therapy
KIT-mutant melanoma (Stage III-IV) Phase II Binimetinib + Imatinib Assessing overall response rate and safety of combination
Pediatric adamantinomatous craniopharyngioma Phase II Binimetinib alone Evaluating sustained objective response rate in recurrent/progressive disease

FAQ

  • What is binimetinib and how does it work? Binimetinib is an oral medication that blocks proteins called MEK1 and MEK2, which are involved in cancer cell growth. It works by inhibiting the MAPK/ERK pathway that is often overactive in cancer cells.
  • What types of cancer is binimetinib being studied for? Clinical trials are investigating binimetinib for various cancers including melanoma, colorectal cancer, gastrointestinal stromal tumors (GIST), hairy cell leukemia, and certain brain tumors like craniopharyngioma.
  • Is binimetinib used alone or combined with other drugs? Binimetinib is being studied both as a single agent and in combination with other targeted therapies like encorafenib, imatinib, and cetuximab, depending on the type of cancer.
  • What are some potential side effects of binimetinib? Common side effects may include skin rashes, eye problems, gastrointestinal issues, and fatigue. Patients are closely monitored for adverse events during clinical trials.
  • How is binimetinib administered? Binimetinib is taken orally, usually twice daily. The exact dosage and schedule varies between trials and may be adjusted based on how well it is tolerated.

Ongoing Clinical Trials on Binimetinib

  • Study on Binimetinib, Encorafenib, and Pembrolizumab for Patients with BRAF V600 Mutation-Positive Melanoma and Brain Metastasis

    Not recruiting

    1 1 1
    Investigated drugs:
    France

  • Study of Encorafenib, Binimetinib, and Pembrolizumab for Patients with Advanced Melanoma with BRAF V600E/K Mutation

    Not recruiting

    1 1 1
    Investigated drugs:
    Belgium Bulgaria Czechia Finland Germany Greece +5

  • Study of Encorafenib, Binimetinib, and Pembrolizumab for Patients with BRAF V600E/K Mutation-Positive Melanoma After Anti-PD-1 Therapy

    Not recruiting

    1 1 1
    Investigated diseases:
    Investigated drugs:
    Germany Italy Poland Slovakia Spain

  • Study on Melanoma Treatment: Comparing Encorafenib and Binimetinib with Ipilimumab and Nivolumab for Patients with BRAF V600 Mutation

    Not recruiting

    1 1 1
    Investigated drugs:
    France Germany Italy The Netherlands Poland Spain

Glossary

  • MEK1 and MEK2: Proteins involved in cell signaling pathways that regulate cell growth and survival. They are often overactive in cancer cells.
  • MAPK/ERK pathway: A chain of proteins in cells that communicates signals from receptors on the cell surface to the DNA in the cell nucleus. This pathway is often overactive in cancer.
  • BRAF mutation: A specific change in the BRAF gene that can lead to increased cell growth and cancer. It is common in certain types of cancer like melanoma.
  • Plexiform neurofibroma: A type of nerve tumor that occurs in people with neurofibromatosis type 1 (NF1).
  • Adamantinomatous craniopharyngioma: A rare, usually benign brain tumor that develops near the pituitary gland, often affecting children.
  • Objective response rate (ORR): The proportion of patients whose cancer shrinks or disappears after treatment.
  • Progression-free survival (PFS): The length of time during and after treatment that a patient lives with cancer without it worsening.
  • Overall survival (OS): The length of time from the start of treatment that patients are still alive.

References

  1. https://clinicaltrials.eu/trial/study-on-the-safety-of-encorafenib-binimetinib-and-ribociclib-for-patients-with-solid-tumors/
  2. https://clinicaltrials.gov/study/NCT03637491
  3. https://clinicaltrials.eu/trial/study-of-encorafenib-binimetinib-and-pembrolizumab-for-patients-with-advanced-melanoma-with-braf-v600e-k-mutation/
  4. https://clinicaltrials.gov/study/NCT03803553
  5. https://clinicaltrials.gov/study/NCT03158103
  6. https://clinicaltrials.gov/study/NCT04322383
  7. https://clinicaltrials.gov/study/NCT03231306
  8. https://clinicaltrials.gov/study/NCT04759846
  9. https://clinicaltrials.gov/study/NCT05926960