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Entinostat

Entinostat, a histone deacetylase (HDAC) inhibitor, is being extensively studied in clinical trials for its potential in treating various types of cancer. This article explores the ongoing research on entinostat, its mechanisms of action, and its potential benefits in cancer therapy. We’ll examine its use in different cancer types, its combination with other drugs, and the current findings from clinical trials.

Table of Contents

What is Entinostat?

Entinostat is an investigational drug being studied for the treatment of various types of cancer. It is also known by several other names, including SNDX-275, MS-275, and KHK2375[1][2]. Entinostat belongs to a class of drugs called histone deacetylase (HDAC) inhibitors, which work by affecting how genes are expressed in cancer cells[3].

How Entinostat Works

Entinostat works by inhibiting certain enzymes called histone deacetylases. These enzymes play a role in regulating gene expression. By inhibiting these enzymes, entinostat can potentially:

  • Slow down or stop the growth of cancer cells
  • Cause cancer cells to die
  • Make cancer cells more sensitive to other treatments
  • Enhance the body’s immune response against cancer
Research has shown that entinostat may also affect certain immune cells, potentially making cancer treatments that boost the immune system (immunotherapies) more effective[4].

Conditions Treated with Entinostat

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

  • Breast cancer: Particularly advanced or recurrent hormone receptor-positive breast cancer[2][5]
  • Lung cancer: Including non-small cell lung cancer[3]
  • Hodgkin’s lymphoma: A type of blood cancer that affects the lymphatic system[6]
  • Cholangiocarcinoma: A type of bile duct cancer[7]
  • Pancreatic cancer[7]
  • Prostate cancer: Specifically, castration-resistant prostate cancer[8]
It’s important to note that entinostat is still considered an investigational drug, which means it has not yet been approved by regulatory agencies like the FDA for widespread use in treating these conditions.

How Entinostat is Administered

Entinostat is typically administered orally in tablet form. The dosage and frequency can vary depending on the specific study or condition being treated. Some common dosing schedules include:

  • 5 mg taken once weekly[9]
  • 5 mg taken on days 1, 8, 15, and 22 of a 28-day cycle[2]
It’s important to note that entinostat should be taken on an empty stomach, usually at least 1 hour before or 2 hours after a meal. This is because food can affect how the drug is absorbed by the body[8].

Ongoing Clinical Trials

Entinostat is currently being studied in various clinical trials to determine its effectiveness and safety for different types of cancer. Some of these trials are:

  • Combining entinostat with other cancer drugs, such as exemestane for breast cancer or nivolumab for cholangiocarcinoma and pancreatic cancer[2][7]
  • Studying the effects of entinostat on the immune system and its potential to enhance immunotherapy[4]
  • Investigating the safety and effectiveness of entinostat in specific populations, such as Chinese postmenopausal women with breast cancer[5]
These trials help researchers understand how well entinostat works, what side effects it may cause, and which patients might benefit most from this treatment.

Potential Side Effects

As with any medication, entinostat can cause side effects. Some of the potential side effects being monitored in clinical trials include:

  • Changes in heart rate and other heart-related parameters[3]
  • Changes in blood cell counts
  • Fatigue
  • Nausea
  • Changes in appetite
It’s important to note that the full range of potential side effects is still being studied, and the severity and frequency of these effects can vary from person to person. In clinical trials, patients are closely monitored for any adverse events to ensure their safety[7].

Aspect Details
Drug Name Entinostat (also known as SNDX-275, MS-275, KHK2375)
Drug Class Histone Deacetylase (HDAC) Inhibitor
Administration Oral tablet, typically taken on an empty stomach
Cancer Types Studied Breast cancer, Hodgkin’s lymphoma, cholangiocarcinoma, pancreatic cancer, prostate cancer, solid tumors
Key Combinations Exemestane, Nivolumab, Enzalutamide
Primary Outcomes Progression-Free Survival (PFS), Overall Survival (OS), Objective Response Rate (ORR)
Safety Assessments Adverse events, changes in vital signs, ECG parameters, laboratory values
Pharmacokinetics Studies on absorption, distribution, metabolism, and elimination
Current Status Investigational, undergoing various phase clinical trials

FAQ

  • What is Entinostat? Entinostat is a histone deacetylase (HDAC) inhibitor being studied for its potential in treating various types of cancer. It works by modifying gene expression and potentially enhancing the effectiveness of other cancer treatments.
  • What types of cancer is Entinostat being studied for? Entinostat is being investigated for several cancer types, including breast cancer, Hodgkin's lymphoma, cholangiocarcinoma, pancreatic cancer, prostate cancer, and solid tumors.
  • How is Entinostat administered? Entinostat is typically administered orally in tablet form. The dosage and frequency can vary depending on the specific clinical trial and cancer type being studied.
  • Are there any known side effects of Entinostat? While side effects can vary, clinical trials are monitoring for adverse events. Common areas of focus include changes in blood cell counts, liver function, and potential cardiac effects. Specific side effects are being evaluated in ongoing studies.
  • Is Entinostat approved for use in cancer treatment? As of now, Entinostat is still investigational and has not yet been approved by the FDA for cancer treatment. It is being studied in various clinical trials to determine its efficacy and safety.

Ongoing Clinical Trials on Entinostat

  • Study of Nivolumab and Entinostat for Children and Adolescents with High-Risk Refractory or Relapsed Malignant Disease

    Recruiting

    1 1 1 1
    Investigated diseases:
    Investigated drugs:
    Austria France Germany The Netherlands Sweden

Glossary

  • Histone Deacetylase (HDAC) Inhibitor: A class of drugs that work by blocking enzymes involved in removing acetyl groups from histone proteins, potentially affecting gene expression and cell function.
  • Pharmacokinetics: The study of how a drug is absorbed, distributed, metabolized, and eliminated by the body.
  • Progression-Free Survival (PFS): The length of time during and after treatment that a patient lives with cancer without the disease worsening.
  • Overall Survival (OS): The length of time from either the date of diagnosis or start of treatment that patients diagnosed with the disease are still alive.
  • Objective Response Rate (ORR): The proportion of patients who experience a tumor size reduction from the time of initial response to tumor progression.
  • RECIST: Response Evaluation Criteria in Solid Tumors, a set of rules used to evaluate changes in tumor size during cancer treatment.
  • Neuroendocrine Tumors (NETs): Rare tumors that develop from cells of the endocrine (hormonal) and nervous systems.
  • Triple Negative Breast Cancer (TNBC): A type of breast cancer that lacks estrogen receptors, progesterone receptors, and HER2 protein.
  • Castration-Resistant Prostate Cancer: Prostate cancer that continues to grow even when the amount of testosterone in the body is reduced to very low levels.
  • Adverse Event (AE): Any unfavorable and unintended sign, symptom, or disease temporarily associated with the use of a medical treatment or procedure.

References

  1. https://clinicaltrials.gov/study/NCT02922946
  2. https://clinicaltrials.gov/study/NCT03291886
  3. https://clinicaltrials.gov/study/NCT02897778
  4. https://clinicaltrials.gov/study/NCT03192111
  5. https://clinicaltrials.gov/study/NCT02833155
  6. https://clinicaltrials.gov/study/NCT00866333
  7. https://clinicaltrials.gov/study/NCT03250273
  8. https://clinicaltrials.gov/study/NCT03829930
  9. https://clinicaltrials.gov/study/NCT03211988