Low-dose naltrexone (LDN) is a fascinating drug and it is finally coming out of obscurity as more and more doctors discover its amazing benefits for treating cancer and other diseases. I had never heard of this drug until a naturopathic doctor (ND) recommended it to me early on in my cancer journey. Since then, I have used this medication on and off and I know others who use it. LDN is a first line treatment recommended by many NDs for cancer and you need to know about it. In fact, some NDs take it themselves for all the health benefits it has.
LDN can be a powerful adjunct in your cancer regimen and I would advise you discuss this with your primary care physician or better yet, your ND if you have one. I don’t know of any oncologists who use this drug or even know about its benefits so you might not get far there. They may even discourage you from using it saying it isn’t proven, but the science is there and it isn’t hard to find. If you do an online search with LDN in the phrase, you will find more than half a million results! Remember, you have to be your own advocate in this journey and stick up for yourself.
WHAT IS LOW-DOSE NALTREXONE?
Naltrexone was discovered by accident. In the 1960s scientists were looking for morphine derivatives to help wounded soldiers. Instead, they discovered naltrexone, which has the opposite effects of morphine.
Naltrexone is a drug that binds to and blocks opioid receptors in the brain. This means it also blocks the effects of opioids like heroin, morphine and other painkillers. In the 1980s, it was developed and approved for use by the FDA (Food and Drug Administration) as a drug for the treatment of heroin and opioid addiction and alcohol dependence. Naltrexone dosages for drug addiction are typically 50-100mg per day.
In the mid-1980s, Dr. Bernard Bihari was using naltrexone to treat heroin addicts. He was also a researcher and in studying the drug further, he discovered that it boosted endorphin levels and the immune system. He started experimenting with lower doses (1-5mg) to see what was the lowest dose that would produce those effects in particular. This was the beginning of low-dose naltrexone.
At the time, the AIDS epidemic was in full swing. Dr. Bihari tested AIDS patients and found their endorphin levels were much lower than normal and with that their immune systems were also suppressed. Endorphins are necessary for a strong immune system. He started doing clinical trials using low doses of naltrexone for the treatment of AIDS patients. The patients taking LDN had less deaths, less infections and less drops in their T-helper cells than patients not taking LDN and they felt better.
By the mid-1990s he noticed that some of his patients with cancer, including pancreatic cancer, lymphoma and Kaposi’s sarcoma also benefited from LDN, in some cases dramatically. Dr. Bihari found that cancer patients also had very low endorphin levels and suppressed immune systems. He had so much success with the drug that he and his wife took it for over 10 years to prevent cancer, with no side effects.
Dr. Bihari and others came up against many roadblocks to getting funding for research into this potentially life-saving drug. He funded most of his research himself. As with many off-label drugs that are low-cost, safe, non-toxic and already approved for use, pharmaceutical companies, big corporations and the FDA are not interested. LDN is off-patent and these big industries want to develop new, patented drugs where they can make a lot of money. Not only that, but they don’t want to see a very inexpensive drug like LDN start to compete with their extremely expensive drugs, which it very well could! Cancer is a multi-billion dollar industry, do you think they really want to find a cure? But, I digress.
Starting in 2007, renewed interest in this drug by clinicians has boosted studies on LDN for many diseases including cancer. Many NDs and primary care doctors are now prescribing it for their cancer patients and especially those who have advanced disease, have exhausted all options and are without hope. They are seeing very good to excellent results.
So how does a drug used to treat drug addiction help cancer patients? Continue reading to learn all about the amazing powers of LDN and how this could be a game-changer for you.
HOW DOES LOW-DOSE NALTREXONE WORK
Naltrexone is a bit of a mystery as to how it does so many things, but at low doses it definitely works differently than at high doses. Here are some of the things they have discovered in researching LDN.
SUPPRESSING CANCER GROWTH THROUGH THE OGF-OGFr AXIS
LDN temporarily blocks a very important receptor called the opioid growth factor receptor (OGFr). When LDN blocks OGFr, there is a compensatory increase in opioid growth factor (OGF) also called [met 5]-enkephalin and the OGF receptors on cells.
The OGF-OGFr axis is very important when it comes to cancer. When activated it inhibits DNA synthesis and cell proliferation by arresting the cell cycle. By increasing OGF and OGFr, LDN has the ability to suppress the proliferation of cancer cells and slow or stop tumor growth. This has been shown in studies involving both ovarian and cervical cancer cell lines and mouse models.
ENDORPHINS AND IMMUNE SYSTEM REGULATION
LDN temporarily blocks the mu and delta opioid receptors in the brain and throughout the body. This gives the body a false message that the body doesn’t have enough endorphins so it makes more. The two main endorphins that are up-regulated include, beta-endorphins and enkephalins. Endorphins are essential hormones that are necessary to boost and regulate immune function. In fact, when endorphins are low, the number of CD8+ cytotoxic T-cells and natural killer cells are also low.
Studies have shown that AIDS and cancer patients have <30% of the normal endorphin levels of healthy people so is it any wonder our immune systems are suppressed and dysfunctional. By up-regulating the production of beta-endorphins and enkephalins, LDN helps boost immune response and immune cell growth. Endorphins increase the number of natural killer cells and their activity. They also activate cytotoxic CD8+ and CD4+ T cells and macrophages. These immune cells are responsible for detecting and killing cancer cells.
In over 300 studies, Dr. Zagon and his colleagues, confirmed that the endorphin-receptor system is involved in every biological system that regulates the immune response. He showed that by blocking the opioid receptors briefly with LDN, it caused an up-regulation in the production of endorphins, which ultimately acted to correct the immune system dysfunction. They also demonstrated that LDN was able to retard tumor growth in animal models.
Cancer cells have an increased number of endorphin receptors compared to normal cells. Endorphins have been shown to be directly toxic to cancer cells and cause apoptosis. In one study a researcher added a small amount of metenkephalin to petri dishes with rapidly growing pancreatic and colon cancer cells. The metenkephalin directly killed the cancer cells through apoptosis while the cells were dividing.
LDN also promotes the function of T-regulatory cells (TREGs). These cells play a critical role in maintaining immune homeostasis by suppressing excessive immune responses, preventing autoimmunity and dampening overall inflammation.
OTHER ACTIONS OF LDN
Studies have shown that endorphins made in the body, specifically act on rapidly dividing cancer cells similar to chemotherapy drugs, but without the toxic side effects.
Researchers found that priming cancer cells with LDN before chemotherapy, significantly boosted the efficacy and cytotoxicity of standard chemo drugs.
In several case reports, the use of LDN with intravenous alpha-lipoic acid provided excellent results and prolonged survival for pancreatic cancer patients.
LDN up-regulates pro-apoptotic genes including BAK1 and BAX leading to cancer cell death.
PI3K/AKT/mTOR signaling pathways contribute to tumor growth, angiogenesis, metastasis and drug resistance in many cancers. In one study, LDN indirectly reduced the expressions of PI3K, pAKT and mTOR in vitro and in vivo. Commonly used chemo drugs that do this include everolimus and sirolimus, which have many undesirable side effects. LDN might be a better alternative or act to increase the efficacy of these drugs.
STOPS INFLAMMATION
LDN can block toll-like receptors (TLRs). Activation of TLRs leads to the production of pro-inflammatory cytokines that are often involved in cancer oncogene stimulation and activation of signaling pathways leading to tumor growth. For instance, LDN specifically blocks TLR 9. TLR 9 activation is associated with chronic inflammatory conditions, which are well-known precursors to cancer. TLR 9 stimulation leads to production of IL-6, the cytokine most closely associated with cancer progression.
TLR 4 is associated with microglial cell activation. Microglial cells play a key role in nerve inflammation by producing pro-inflammatory cytokines, free radicals and nitric oxide. These have all been linked to neuropathic pain, fatigue, feeling rundown and like you are coming down with something. By blocking TLR 4, LDN stops this activation. This is one way it helps treat neuropathic pain in particular.
OTHER BENEFITS OF LDN
LDN has shown significant benefits for a variety of other conditions, including autoimmune diseases (lupus, rheumatoid arthritis, crohn’s disease, thyroid conditions, etc.), neurodegenerative diseases like multiple sclerosis, chronic pain conditions, irritable bowel syndrome, late stage Lyme disease and certain viral infections.
LDN can be a remarkable treatment for neuropathic pain, which is a common side effect from chemotherapy for uterine cancer. It can also help ease symptoms of myalgia (muscle pain) secondary to aromatase inhibitors and other cancer treatments.
With the boost in endorphins (feel good hormones) that LDN creates, it is helpful in treating depression and anxiety and significantly improving the quality of life for a lot of people.
POSSIBLE SIDE EFFECTS
LDN is extremely safe and non-toxic. Side effects are very rare (1-8% of patients), but they include the following.
- Insomnia
- Nightmares (wild dreams)
- Nausea or vomiting
- Heartburn
- Abdominal pain
- Diarrhea
FACTORS THAT CAN AFFECT YOUR RESULTS WHEN USING LDN
Some clinicians have noticed that when a patient has side effects or things aren’t clearing up as well as they should with the use of LDN, there may be underlying factors affecting the body and the immune system. Some people may be very sensitive to LDN and it could be due to other issues that haven’t been addressed. Examples include.
- Underlying infections (Lyme, Epstein-barre virus, mold, long-covid)
- Low vitamin D levels
- Toxins the patient may be exposed to
- Hormonal imbalances in the thyroid
- Cortisol levels that are too high or too low
- Poor blood sugar regulation
Remember, there is no “silver-bullet” when it comes to cancer. While the use of LDN can ultimately help resolve many of these issues and even be an effective cancer treatment, it is very important to maintain a healthy diet and lifestyle and support your immune system while using LDN for the best results.
DOSAGE AND HOW TO USE
- Although benefits can be seen with ultra low doses of LDN, the most common target dose for cancer is 3mg – 4.5mg once a day. It is recommended to gradually ramp up the dose instead of starting at the max dose all at once.
- Ideally start with 1.5mg in the evening for one week, then increase to 3mg for the next 2 weeks. If there are no side effects, you may increase to 4.5mg and see how you do. Once you establish what dose works best for you without side effects, then you can continue on that dose. Do not take more than 4.5mg at any time.
- If you are taking opioid medications or have a dependence on opioids, do not take LDN without consulting with a doctor first.
- It is best to take LDN in the evening before bed.
90% of endorphins are made in the middle of the night, specifically between 2am-4am. When you take LDN at night, it boosts endorphin production by as much as 300%! The naltrexone is cleared from the body in 4-6 hours, but the endorphins remain elevated all the next day. In fact, the half-life of beta-endorphin (how long it takes for half of it to leave the body) is 20 hours.
- Do not take it more than once a day or use an extended release formula.
- If you have side effects, reduce the dose by 0.5mg increments.
- If you have nightmares or insomnia, take LDN in the morning instead of at bedtime for a period of time until your body adjusts to it. Then try taking it at night again and see how you do. You will still be getting the beneficial effects of LDN and taking it during the day is better than not taking it at all.
- Supplementing vitamin D and maintaining blood levels of 80-100mg/dl greatly improves the function of LDN.
- Talk to your naturopathic doctor about a dosing schedule. Some doctors recommend continuous treatment. Other doctors advise to take breaks, for example, one month on, one month off or 4 days on and 3 days off. Each of us is different, so this is where you need to work with a doctor to help you figure out what works best for you.
When you are using LDN, opioid pain-relievers will not work. These include morphine, oxycontin, vicodin, codeine, fentanyl, etc. Non-steroidal anti-inflammatories will work for pain relief and these include ibuprofen, acetaminophen and aspirin. If you have to have a painful procedure like surgery or dental work, stop the LDN at least 3 days before the procedure.
IN SUMMARY
According to Dr. Neil NcKinney, a leader in naturopathic integrative cancer care, LDN is particularly indicated for many different cancers including uterine and ovarian cancer. He said, good responses are seen in about 60% of patients and improvement may be seen within one month and remission within 6 months.
Dr. Dana Flavin, another leading authority in the naturopathic cancer field, said in an interview that she prescribes this medication for every single one of her cancer patients and that if she ever had cancer herself, it would be the first thing she would take.
Low-dose naltrexone is a powerful repurposed drug that has many benefits for cancer patients. Not only can it help you heal from cancer and prevent recurrence, it can treat autoimmune conditions, neuropathic pain, infections and work synergistically with other supplements and cancer treatments to make them more effective. This is an amazing adjunctive treatment and I encourage you to consider using LDN.
SCIENTIFIC REFERENCES AND LINKS
Naltrexone’s Impact on Cancer Progression and Mortality: A Systematic Review of Studies in Humans, Animal Models, and Cell Cultures Read More
Naltrexone at low doses (LDN) and its relevance to cancer therapy Read More
Low-Dose Naltrexone in Endometrial Intraepithelial Neoplasia Read More
The long-term survival of a patient with pancreatic cancer with metastases to the liver after treatment with the intravenous alpha-lipoic acid/low-dose naltrexone protocol Read More
Low-dose naltrexone plays antineoplastic role in cervical cancer progression through suppressing PI3K/AKT/mTOR pathway Read More
Low-Dose Naltrexone as an Adjuvant in Combined Anticancer Therapy Read More
The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain Read More
I will praise the Lord, who counsels me; even at night my heart instructs me.
~Psalm 16:7