Mepacrine

Mepacrine, also known as quinacrine, is a medication that has been studied in clinical trials for its potential effectiveness in treating various conditions. This article explores the use of mepacrine in clinical trials for diseases such as prion diseases, non-small cell lung cancer, colorectal cancer, and prostate cancer. We’ll discuss the key findings, potential benefits, and ongoing research efforts to better understand mepacrine’s role in medical treatments.

Table of Contents

What is Mepacrine?

Mepacrine, also known as quinacrine, is a medication with a long history of use in various medical conditions. It’s important to note that this drug is known by several names, including:[1][2]

  • Quinacrine
  • Atabrine
  • CBLB102
  • SN 390
These different names all refer to the same medication, which has been used for various purposes over the years.

Conditions Treated with Mepacrine

Mepacrine is being studied for its potential effectiveness in treating several serious conditions:[1][2][3][4][5]

  • Androgen-Independent Prostate Cancer: This is a type of prostate cancer that no longer responds to hormone therapy.
  • Prion Diseases: These are rare, fatal brain disorders caused by abnormally folded proteins. Creutzfeldt-Jakob Disease (CJD) is an example of a prion disease.
  • Renal Cell Carcinoma: This is a type of kidney cancer.
  • Non-Small Cell Lung Cancer: A common type of lung cancer.
  • Colorectal Adenocarcinoma: A type of colon or rectal cancer.
It’s important to note that while mepacrine is being studied for these conditions, it may not be approved for all of these uses yet. Clinical trials are ongoing to determine its effectiveness and safety for these various conditions.

How Mepacrine Works

Mepacrine works in several ways to potentially fight diseases:[1]

  • Activating p53: p53 is often called the “guardian of the genome” because it helps prevent cancer by stopping cells with damaged DNA from dividing.
  • Inhibiting NF-kB: NF-kB is a protein complex that controls cell survival. By inhibiting it, mepacrine may help reduce cancer cell survival.
  • Clearing abnormal prion proteins: In prion diseases, mepacrine has shown the ability to clear abnormal proteins from cells in laboratory studies.
These mechanisms suggest that mepacrine could potentially be effective against various types of cancer and prion diseases. However, more research is needed to fully understand how it works in the human body.

Dosage and Administration

The dosage and administration of mepacrine can vary depending on the condition being treated and the specific clinical trial. Here are some examples from current studies:[3][4][5]

  • For prostate cancer and renal cell carcinoma: 100 mg daily.
  • For non-small cell lung cancer: Various dosing schedules are being tested, including:
    • A loading dose of 50-200 mg three times daily for 7 days
    • Followed by a maintenance dose of 50-400 mg daily or every other day
  • For Creutzfeldt-Jakob Disease: 100 mg three times a day.
It’s crucial to understand that these dosages are part of clinical trials and should only be taken under strict medical supervision. Never attempt to self-medicate with mepacrine.

Current Clinical Trials

Mepacrine is currently being studied in several clinical trials for different conditions:[1][2][3][4][5]

  • A Phase II trial for androgen-independent prostate cancer
  • The PRION-1 trial for human prion diseases
  • A study on advanced renal cell carcinoma
  • A Phase I/II trial combining mepacrine with erlotinib for non-small cell lung cancer
  • A study combining mepacrine with capecitabine for colorectal cancer
  • A randomized, double-blinded, placebo-controlled study for sporadic Creutzfeldt-Jakob Disease
These trials aim to determine the safety, effectiveness, and optimal dosing of mepacrine for these various conditions. Participation in clinical trials is crucial for advancing medical knowledge and potentially finding new treatments for serious diseases.

Potential Side Effects

As with any medication, mepacrine can potentially cause side effects. The full range of side effects is still being studied in clinical trials. Some known side effects from its historical use include:[2]

  • Yellowing of the skin (not related to liver problems)
  • Gastrointestinal issues (nausea, vomiting, diarrhea)
  • Headaches
  • Dizziness
It’s important to note that the side effects can vary depending on the dosage and the condition being treated. In clinical trials, patients are closely monitored for any adverse reactions. Always discuss potential side effects with your healthcare provider before starting any new medication.

Disease Study Type Mepacrine Dosage Key Outcomes Measured
Prion Disease (Creutzfeldt-Jakob Disease) Phase I/II 100 mg three times daily Survival, cognitive function, activities of daily living
Non-small Cell Lung Cancer Phase I Varied (50-200 mg daily or three times daily) Maximum tolerated dose, progression-free survival, overall survival
Colorectal Adenocarcinoma Phase I/II 100-200 mg twice daily Tolerability, safety, response rate, time to progression
Androgen-Independent Prostate Cancer Phase II 100 mg daily PSA response, time to progression
Renal Cell Carcinoma Phase II 100 mg daily Time to tumor progression

Ongoing Clinical Trials on Mepacrine

  • Study Comparing Mepacrine and Metronidazole for Treating Resistant Giardiasis in Children Aged 1 to 18 Years

    Not yet recruiting

    1 1 1 1
    Investigated diseases:
    Investigated drugs:
    Spain

Glossary

  • Mepacrine: Also known as quinacrine, it's a medication originally used as an antimalarial drug but now being studied for its potential in treating various diseases.
  • Prion disease: A rare, fatal brain disorder caused by abnormally folded proteins called prions. Creutzfeldt-Jakob disease is an example of a prion disease.
  • Non-small cell lung cancer (NSCLC): A type of lung cancer that is the most common form of the disease, accounting for about 80-85% of all lung cancers.
  • Renal cell carcinoma: The most common type of kidney cancer in adults, which begins in the lining of the small tubes in the kidney that filter blood and remove waste products.
  • Androgen-independent prostate cancer: A form of prostate cancer that continues to grow even when the level of testosterone is reduced to very low levels in the body.
  • Maximum Tolerated Dose (MTD): The highest dose of a drug or treatment that does not cause unacceptable side effects in patients.
  • Progression-Free Survival (PFS): The length of time during and after treatment that a patient lives with the disease but it does not get worse.
  • Overall Survival (OS): The length of time from either the date of diagnosis or the start of treatment for a disease that patients are still alive.
  • Response Evaluation Criteria in Solid Tumors (RECIST): A set of rules used to measure how well a cancer patient responds to treatment, based on whether tumors shrink, stay the same, or get bigger.
  • Pharmacokinetics: The study of how a drug is absorbed, distributed, metabolized, and eliminated by the body.

References

  1. https://clinicaltrials.gov/study/NCT00417274
  2. https://clinicaltrials.gov/study/NCT00104663
  3. https://clinicaltrials.gov/study/NCT00574483
  4. https://clinicaltrials.gov/study/NCT01839955
  5. https://clinicaltrials.gov/study/NCT01844076