Wednesday, November 18, 2015

Potential New Natural Cancer Treatments - Artesunate

Artesunate, Artemisinin & Artemether

Are you looking for a cancer treatment that attacks, and kills cancer cells with little harm to healthy cells? Now add, it should have zero to minimal side effects when administered properly, cost less than $3.00 per day for treatment, and obtain excellent results. The answer may be closer than you think.

One of the most promising new cancer treatment possibilities is Artesunate, a standardized pharmaceutical grade derivative of Artemisinin from the Artemisia annua plant, also known as Sweet Wormwood or Sweet Annie. Artemisia annua has been used in traditional Chinese medicine for thousands of years. In fact, records of its use were unearthed in an ancient Han Tomb at Mawangdui outlining treatment for malaria with Artemisia. Also discovered, was a small region in Viet Nam that has been quietly relying on the Artemisia Anna plant for its malaria healing powers.

As a result of these discoveries, in the 1960’s the Chinese began using this plant to treat malaria. In the 1970’s the World Health Organization began investigating Artemisia annua as a malaria cure when Quinine became less effective. And in 1972, Artemisinin was isolated from the plant by Dr. Tu Youyou of China as one of its principal active ingredients. For this discovery and his work with Artemisinin, Dr Tu received a Nobel Prize in 2015.

Since then, Artemisinin, and its two most common derivatives, Artesunate and Artemether, have been used around the world to treat malaria. Artemisinin works because malaria parasites consume large quantities of red blood cells containing iron. They become loaded with iron. Adding Artemisinin causes a reaction with this iron releasing reactive oxygen species that destroy the parasite.

In the U.S., the FDA has also approved a drug made from this research for malaria treatment. In addition, because of Artemisinin’s extended use, there are excellent records for dosage, effectiveness, and side effects regarding the Artemisia annua plant, Artemisinin, Artesunate, and Artemether. So what does this have to do with cancer? The answer revolves around malaria and cancer’s need for iron to survive.

Now fast forward to present time. Due to recent research, some provided by the University of Washington, scientists are looking at the Artemesia family of compounds as a treatment for cancer. In fact, preliminary research has progressed so well that one company in the Pacific Northwest, working to improve Artemisinin’s effectiveness, is ready to initiate phase one trials in relation to breast and prostate cancer, as soon as they are able to fund the project. So you’re probably asking yourself, how does it work? To answer, it’s important first to understand one of the principal processes of cancer cells. This is, cancer’s critical need for iron.

Iron is essential for each cancer cell’s metabolism, cell division, and survival. It plays a part in DNA synthesis, cellular respiration, and macromolecule biosynthesis. It is vital for cell growth and proliferation. In fact, it is so necessary for cancer cells that without it they die. Now we all need a certain level of iron for proper bodily functions. Too little iron, you become sick and anemic. Too much iron and you could experience chronic fatigue, joint and abdominal pain, even liver and heart failure. And an over-abundance of iron is also believed to fuel cancer’s growth like pouring gasoline on a fire.

Normal cells in your body need minimal iron, but cancer cells need more. It’s their key for cellular division. To gather the iron cancer needs, prostate and breast cancer cells have many more transferrin iron-receptors on their surface than healthy cells, as many as 15 times more! Leukemia cancer cells require the highest concentration of iron. Their iron storage can reach 1,000 times more than healthy cells. All this iron comes from the food we eat.

When we consume foods with iron, the iron is absorbed by the small intestine. It’s then carried to the cells by a plasma protein called transferrin. Our cells have transferrin receptors on their surface. Sort of like a receptacle or dock waiting for its mate or ship to arrive.  As the iron carrying transferrin joins with each cell’s transferrin receptors, it’s transported into the cell by a kind of vesicle, essentially a sac. The transferrin is then released into the cell and the empty receptor is transported back to the cell surface to gather more transferrin. This is a process of continuous repetition, though much more abundant for cancer cells due to their greater quantity of transferrin receptors. In addition to cells collecting iron, much iron is transported to the bone marrow where it’s used to make hemoglobin and red blood cells. These then circulate throughout the body supplying oxygen to tissues and organs. Iron in the blood is an important factor when considering Artemisinin treatment, and it also presents an excellent way of monitoring for side effects. More on this later. 

Now comes the important cancer termination part. The Artemisinin family of compounds contains two oxygen atoms hooked together in an endoperoxide linkage. When put together with iron this bond breaks, thus forming free radicals that destroy the cancer cell from within.

Technically Artesunate, which is readily hydrolyzed back to a DHA metabolite, is activated by iron in the cancer cells. This combination produces highly alkylating carbon-centered radicals and reactive oxygen species (ROS). Because tumor cells are already damaged, they have lower expression of antioxidant compounds and other factors necessary to repair the damage caused by the flood of alkylating carbon-centered radicals and ROS. Thus the cancer cell ceases to function.

Healthy cells require much less iron. They also are better equipped to repair oxidative damage. Because of this, Artemisinin effectively targets cancer cells while leaving healthy cells in tact.

Though few official studies have been completed, reported results from cancer patients taking Artemisinin Compounds are remarkable.

• A 47-year-old male with an egg-sized head lymphoma who took Artemisinin for two weeks experienced complete healing four weeks later. The tumor was gone with no mass remaining.

• A woman with stage-4 breast cancer after receiving Artemisinin derivatives reported renewed wellness, feeling like before she was diagnosed with cancer. Her CT Scan confirmed remission.

• A 40-year-old woman with breast cancer and spine metastases after four months of supplementation with oral Artemisinin derivatives showed no remaining cancer on her spine using a PET scan.

• A woman with metastasized breast cancer was able to stop her drug use of zoledronic acid and Tamoxifen with her oncologist’s understanding because her cancer markers had so improved after taking a course of Artesunate.

• A male, with larynx cancer treated with Artesunate injections for two months was able to shrink his tumor by 70 %.

• A Belgium man with a PSA of 12 reported his PSA dropped to 0.38 with Artemisinin derivative treatment.

• Others with prostate cancer have been able to drop their PSA significantly with Artemisinin and derivative treatment, from 4 to 2, from 7.8 to 1.9, and from 3 to 0.45 respectively, all within 3 to 6 weeks.

Then, there is the recent Colorectal Cancer Study from St George’s University of London combining Artesunate followed by curative resection. This was a 14-day, randomized, double blind, placebo-controlled pilot study. Follow-up revealed, of the 11 patients on placebo, six experienced a cancer recurrence within 3.5 years, three of these died. Whereas, only one of the nine patients on Artesunate experienced a recurrence, and none died. Given the very short time on Artesunate, these are fascinating results. 

In all, at least 55 cancer cell lines appear to experience some level of cancer cell death and remission with Artemisinin derivatives… with leukemia, colon, melanoma, breast, renal, CNS, and prostate cancer showing the best results.
Additional research papers on the Artemisinin and its derivatives may be found through the University of Washington.

This is exciting information. But do NOT rush out to your local health food store, or onto to purchase Artemisinin. It may not work. Testing on readily available Artemisinin products has revealed capsules containing wide ranges of potency, some with only 5% to 10% active Artemisinin levels. Using these products is most likely a waste of time, money, and your health. There is too little Artemisinin to be effective. This is due to processing, and that different subspecies of Artemesia annua contain different concentrations of Artemisinin. The species with the best yield and quality is found in southwestern China and Vietnam.

Then too, Artemisinin and its derivatives are light sensitive, loosing potency when exposed to light so packaging and storage are very important. And since successful treatment, and side effects are dose-dependent, it is critical to know exactly the amount you’re taking. Therefore, the only Artemisinin family product to consume must be of ‘pharmaceutical grade’ quality. There are several pharmaceutical grade sources for Artemisinin family products, but which form of Artemisinin should be used?

Several derivatives of Artemisinin have been developed since it’s recent discovery in an attempt to improve absorption and stability while reducing toxic effects. Currently, doctors principally use three product forms. Let’s start by looking at each of these.

            Artemisinin – This is the initial product derived directly from the Artemesia annua plant. It is Not Water-Soluble and has poorer absorption than some other forms. When taken, it reaches its peak concentration in the blood in about 40 minutes. The liver quickly breaks it down, and by four hours it has reached the end of its effectiveness.

            Artesunate – This is a semi-synthetic form of Artemisinin. Many sources believe it is the most effective form to use for killing cancer because of its DHA conversion in the body. Artesunate is partially water-soluble. It is available in pill, injection, and IV forms. It has a higher absorption rate, around 61%, but also the shortest activity period.

            Artemether – Another semi-synthetic form of Artemisinin, Artemether lasts longest in the blood and is more fat-soluble. It also exhibits more side effects than the other two products.
Important Note: Because of its higher toxicity, it has been strongly recommended that Artemether dosage not exceed one milligram (mg) per kilogram (kg) of body weight per day (<1mg/kg/day).

Now knowing the different forms of Artemisinin, have a conversation with your health care provider to choose which approach may be best. From my own research and medical discussions, I tend to believe Artesunate to be most effective, though in some instances a blend of the three could be explored.

For all three of these forms, most doctors and researchers recommend they be taken on an empty stomach, away from food. If taken near food consumption, the Artemisinin may bind with iron in the food rendering it ineffective before reaching its cancer target. If taking these products twice a day the best times are just before bed at least three hours after eating, or in the morning an hour before food.

But if you are taking supplements, Vitamin-C, CoQ10, Fish Oil, etc., taking Artesunate or Artemisinin twice a day may be not practical. You see many supplements are strong antioxidants. The Artemisinin family works largely on the principal of oxidation. An antioxidant will counteract this oxidative process. Your supplements most likely stay in your body at least four to six hours. If taken too close to Artemisinin, your supplements will negate its use. Then too, one must consider your nutritional intake. You wouldn’t want to eat say a couple of oranges close to ingesting Artesunate because of the anti-oxidants. And, there are many foods with higher anti-oxidant activity. Some of these include red beans, blueberries, kidney beans, pinto beans, cranberries, artichoke, blackberries, prunes, raspberries, strawberries, apples, pecans, cherries, plumbs, potatoes, black beans, and the list goes on. Then there are all the exotic super food antioxidants. So what’s a person to do? You shouldn’t stop eating healthy. The answer is to simply separate the two. Enjoy your high antioxidant foods and supplements in the morning, and take Artesunate in one dose at night before bed.

With that said, there is another reason to take Artesunate before bed. Cancer cells grow faster at night. This is when protein receptor molecules on the cell’s surface are more active. The epidermal growth factor receptor (EGFR) facilitates cell growth, but is suppressed by another receptor during the day. All this cancer growth activity at night makes the cells more vulnerable, requiring more iron for cellular division. Bedtime then becomes the best time to slip in a little Artesunate, Artemisinin or Artemether.

Other points to consider are absorption, and absorption resistance. The Artemisinin family is mostly oil-soluble, not water-soluble. Artesunate’s increased absorption rate comes from its partial water solubility. For best absorption, some doctors are researchers suggest taking the dose with a little whole milk as it has fat to facilitate absorption with few antioxidants.

Then, when you ingest Artemisinin continuously your intestines quickly build up a resistance to absorbing the Artemisinin. In only a few days, amounts of Artemisinin absorbed can drop by over 30%. With continued use, this drop in absorption increases until the Artemisinin attained is far too little to be effective. The easy remedy for this issue is an intestinal reset. When one stops taking Artemisinin for a few days, absorption is believed to return to its necessary levels.

Before we continue with this discussion, I want to add an important warning. There can be serious side effects as a result of taking Artesunate, Artemisinin or Artemether in too large a dose without concurrent monitoring of hemoglobin and other appropriate tests. If you are considering using Artemisinin in any of its forms, it is vital you use it only under the supervision of a medical professional that understands the process, and can perform the safety and evaluation tests required.

With that said, let’s continue by focusing on dosage, and side effects. There are a few studies that provide a hint of dosage for Artesunate and Artemisinin as it relates for cancer treatment, though many studies exist for malaria. Doctors around the World have been using Artemisinin in its three principal forms for malaria treatment for decades. Therefore we do know something about dose tolerance.

Recent research, along with doctors and researchers I have chatted with regarding this subject, generally suggest the following Artesunate protocol for treatment:

            • Prior to use have your iron levels and hemoglobin tested
                        If low - these need to corrected before proceeding

            • Artesunate Dosage:
                        2.5mg to 3.5mg per kilogram of body weight per day

            • Take dose before bed,
                        away from food and antioxidants,
                        with a little milk

            • Take 5 days on then 2 days off for best absorption

            • After 14 days test Hemoglobin Levels –
                                                                                     This is critically important!
                        If no change in Hemoglobin on initial 14-day test–
                                    Talk with doctor about a small dosage increase
                        If Hemoglobin dropping –
                                    Reduce dosage and retest until stability reached

            • Continue for another 14 days – re-check Hemoglobin
                        Once Hemoglobin level is stable – re-check every 30 days

            • Check for liver function

            • Check cancer markers for results at 30 days, and as desired.

Research suggests, if the Artesunate is administered properly, positive results in cancer markers should be seen after the first 28 days. I know cancer survivors who have taken Artesunate for months with desired result starting small, then building. Treatment is without side effects for the most part, though some have experienced issues.

Side Effects are often dose-dependent. When side effects show up they can present as stomach or digestive distress, though in rare instances flu-like symptoms of dizziness, fever, nausea, skin rashes, drowsiness, sweating, even vomiting has occurred. Some people with allergies to ragweed related plants also experience an allergic reaction. In one study with 500 patients, approximately 50% of the participants taking Artemisinin compounds experienced some form of minor side effect with no major side effects during treatment. These side effects though concerning, can be controlled with your doctor’s help. But woe to those who take Artemisinin compounds without counsel and medical supervision.

If taken without regard for proper dosage and monitoring, more serious dose-dependent side effects can exist. There have been rare instances of large doses of Artesunate and Artemisinin attacking bone marrow and red blood cells. Nearly 70% of the iron in your body is stored in red blood cell’s hemoglobin and muscle cells. Too much Artemisinin, Artesunate, or Artemether may begin to attack your hemoglobin, or the bone marrow where red blood cells are made. This can result in anemia or abnormal bone marrow. Too much Artemisinin may also effect to liver.

These situations are thought to be easily avoided by monitoring your hemoglobin level at specific times, then adjusting the dosage of Artesunate, Artemisinin or Artemether as required to a maintain proper hemoglobin level.

Contraindications for the use of Artesunate, Artemisinin or Artemether may include allergy, pregnancy, low weight, anemia, hearing or balance problems, liver disease, or adverse drug interactions. Though the Artemisinin family has been successfully tested to enhance 22 cancer drug therapies, in some drugs like doxorubicin, it makes the drug less effective. Again, be sure to cover drug interactions with your doctor.

Lastly, a warning! If you have recently experienced radiation therapy, do not use Artesunate, Artemisinin or Artemether for up to months. When healthy cells experience radiation they go into a repair mode. This requires extra iron. Adding Artemisinin compounds during the repair time could hinder this cellular repair, disrupting the healing. On the other hand, using Artesunate, Artemisinin or Artemether before radiation has been show to enhance the cancer killing effect of the radiation.

Now you know the most recent facts, where do you go from here?
There are two quality sources for Artesunate, Artemisinin or Artemether providing tested pharmaceutical grade products. The Artesunate suggested in the one treatment scenario above is labeled Hepasunate 50 and comes from a company called Hepalin. Another quality source of Artemisinin comes from a company named Holley Pharmaceuticals. Both of these companies are located in California.

Is Artesunate a treatment for your cancer? Limited research, medical opinions, and stories from cancer survivors indicate it, or a close form, could well be the treatment to put cancer into remission. One doctor indicated he has only witnessed improvement in his cancer patients using this process, and many of his patients have experienced profound healing. Are there some people where it has no effect? This may also be possible considering there are over 100 different types of prostate cancer with slightly different reactions. Each person’s cancer and body is unique though this oxidative process appears to bridge the gaps between many forms of cancer.  

People around the Globe have been taking Artemisinin and its derivatives for years with success for malaria, and now for cancer. New research is being accomplished, though unfocused and grindingly slow. Much research still needs to be done. You see no pharmaceutical wants to fund a cancer drug’s research without financial return. Artesunate, Artemisinin and Artemether are already commercially available at around $3.00 a pill, and new derivatives will not be that much more. So where’s the profit? And without financial research backing for human trials Artesunate, Artemisinin and Artemether will never see FDA approval. Does lack of FDA approval mean that it doesn’t work. Not in the least. It just means that this is one of those promising cures kept from official approval due to our system and lack of funds

This is the First of Five Promising Cancer Treatments. Over the weeks to come I will cover each treatment with the most updated information available. In each case these potential healing processes, due to lack of future financial return, have been excluded from proper research and trials thus eliminating them from FDA approval. At the end of these articles, I will propose several solutions to this problem and hopefully a process to increase cancer remissions and enhance the quality of our lives.

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