ß-Artemether Plus
( ß-Artemether/ Artemisinin / Artusenate)
 
Timed-Release Blend of Fat & Alcohol & Water Soluable Fractions
( Same material used in the original U. of WA Study )
 
Dihydroartemisinin Article/Elsevir
Artemesinin & derivatives
The use of artemisinin-based technologies as oncology therapeutics was pioneered at the University of Washington ("UW") in Seattle by Dr Henry Lai and Dr Narendra Singh (Department of Bioengineering) and Dr Tomikazu Sasaki (Department of Chemistry). They're consultants to a new company developed specifically to research the promising therapeutic effects and applications of these artemesinin compounds, called Artemesia BioMedical, Inc. (see link below).
 
ß-Artemether Plus™ is a pharmaceutical grade timed-release blend of both water soluable and fat soluable compounds (ß-Artemether, Artemesinin, Artusenate) from Dihydroartemesinin. it has been tested for bioactivity and found to have an 100% effective rate against cells with high iron content which was verified by the University of Washington, bioengineering department through the work of worldwide-known professor Dr. Narendra P. Singh, MD. 100% of the extract is absorbed through G-I tracts, acting directly on cells with high iron content via enhanced effect with administered Iron (FeSO4).***
 
ß-Artemether Plus™ is manufactured by the same pharmacist and was the original formula used for the study at U of WA.
 
It contains a mixture of biologically active extracts from Dihydro-Artemesisin: Artemesinin, ß-Artemether, and Artusenate proprietarly manufactured in a timed release formulation. (this gives the best levels of the active agent--dihydroartemisinin). After using clinically plain Artemesini, Artusenate or ß-Artemether, we have determined that this product is the most cost effective and clinically biologically effective. We had to mix each of the other extracts and dose them much more frequently, every 3-4 hours, 3 pills, one of each. This product requires only 2 caps per day in most cases. It seems expensive on the surface the but the technology used to combine them with enteric coating, etc. is what we believe makes it the best choice out there, of course except perhaps injectible, which the WHO is not permitting to be used currently as yet in research.
 
*** Iron (hallotransferrin) is usually very high in cancer cells. Lukemia cells can be as high as 1000x that found in a normal cell. Since cancer is iron-dependent usually, we hesitate to give extra iron to a cancer patient unless they're anemic. If the patient is anemic, natural sources of iron can be supplied from certified New Zealand calf liver, USP liver peptone powder (Dews Research), herbal and plant sources such as Spirulina, Yellow Dock Root,Beets or the use of transmuted mineral solutions such as those angstrom mineral waters from Eniva Corp. or Water Oz. Additionally, the use of Frozen Grapefruit Juice Concentrate (which includes peel, rind,seeds which has separate chemical properities that fresh grapefruit juice or bottled versions doesn't contain) will potentize the action of Artemether and Artemesinin as well as many other drugs and compounds and therefore dosing needs to be altered to compensate sometimes.
 
IMPORTANT NOTE from Europa Clinic Physicians to Cancer Patients... Cancer is a multifaceted illness with no single magic bullets. This product works via oxidation mechanisms (peroxide burst). If the patient has had radiation, or extensive chemo, we usually request that the patient be put on an high antioxidant i.v. or protocol for a few weeks to help repair the excess free radical damage prior to starting this product as a precaution against excessive oxidative damage. Our clinical protocol we utilize high dose slow drip (8hrs) IV-C, Lipoic Acid (European origin only), Quercetin, Reduced Lipisomal Glutathione, RALA, Modified Aloe Polysaccharide Est., or PolyMVA, given with IPT if possible.
 
We can't mix antioxidant therapies simultaneously with oxidant therapies, to avoid canceling each other out. In general, antioxidant therapies are Alkalyzing and Oxidant theraies are acidifying. Certain cancers die in alkaline and certain ones die in acid environments (we're talking about INTRACELLULAR pH, not EXTRACELLULAR). The patient is always put on cultured digestive enzymes, a reasonable but very high quality diet with raw vegs, fruits, soaked sprouted nuts, NO SOY...Quality Proteins (100% Grass Fed Organic Bison, Ostrich, New Zeland Organic Lamb, Organic Free Range Eggs and Raw Milk, Butter, Salmon, Organic Turkey, etc.) if EFA's (Cranberry seed Oil or Barleans Flaxoil, Cottage Cheesse protocol for electron donation), Neiper Mineral Therapy, Irididioil (DNA repair substance from ants ala the movie The Medicine Man with Sean Connery), Liver and Kidney herbal support formulas, Far Infrared Sauna Therapy & Laser Lymphatic Drainage Therapy to assist in detox if indicated, Shark Liver Oil antiangiogenics, Fibrinase enzymes to help unmask the cancer cells protein coat, lots of pure clustered water and other modalities. For those who aren't utilizing this product alongside an Integrative Medical Approach but with standard cook-book cancer therapies, the outcomes may not be as dramatic as what we've encountered. YOU SHOULD ALWAYS WORK WITH AN INTEGRATIVELY TRAINED PHYSICIAN WHILE TAKING THIS PRODUCT IF POSSIBLE. BE CAREFUL OF BECOMING ANEMIC FROM OVERUSE.
 
SUPPLEMENT FACTS
INGREDIENTS: Timed-release formula of DihydroArtemesinin 50 mg., Artusenate 50 mg., ß-Artemeter 40mg.
NO. SERVINGS: 30 capsules /140 mg. (Pharmaceutical grade, bioactivity 100% tested by Dr. Narendra P. Singh's lab)
THIS IS THE EXACT PRODUCT USED IN THE UWA STUDY. The mix seems to have a slight advantage over any of the individual isolates below and results seem to be faster and more profound. This product combines the fat soluable timed-release fraction with the water soluable fractions.
DIRECTIONS: Advanced Agressive Cancers Take one capsule 2x/ daily or as directed by your physician. Chronic Cancer which is not active or agressive may use 1 per day. We recommend the use of Grapefruit Juice Frozen Concentrate to potentize the effect also (see articles below). However if on heart or other medication, use caution. USE OF ANY ARTEMESININ PRODUCT CAN CAUSE IRON-ANEMIA. WE SUGGEST SUPPLEMENT WITH NATURAL IRON LIKE NEW ZEALAND CALF LIVER, SPIRULINA, YELLOW DOCK AND ALFALFA, ETC. **
 
** This product has not been evaluated by the FDA. It is not intended to diagnose, treat, cure or prevent any disease. Store in cool dry place. Avoid sunlight. KEEP OUT OF REACH OF CHILDREN.
 
NOTE: This is a special order. We don't stock a lot of this in our Calif. Office. Since it is non-refundable by our pharmacist, all sales on this item are final.
Beware of Fake Artemesinin Products! Artemesinin Herbal Extracts are NOT THE SAME
 
Artemisia BioMedical, Inc
http://www.artbiomedical.com/aboutus.html


March 2005 - Issue
 

 

 

 

 

http://www.washington.edu/alumni/columns/index.html5
 
Old Medicine, New Cure?
 
As funding for cellphone-related research has become increasingly scarce in this country, University of Washington Bioengineer Henry Lai has pursued other areas of interest. Chief among them is a foray into the ancient arts of Chinese folk medicine to find a promising potential treatment for cancer.
 
Lai and colleague Narendra Singh have exploited the chemical properties of a wormwood derivative called artemisinin to target cancer cells, with surprisingly effective results. Last fall, the UW TechTransfer Office signed a licensing agreement with a Chinese pharmaceutical company to develop a group of artemisinin-based compounds for possible use in humans.
 
The compounds are promising, officials say, but medical applications are still years away. Lai says he became interested in artemisinin about 10 years ago. The chemical isn't new-wormwood was apparently used by the Chinese thousands of years ago to combat malaria.
The treatment became lost, but was rediscovered in the 1970s in an ancient record listing medical remedies. It's now widely used to fight malaria in Asia and Africa.
The chemical helps control malaria because it reacts with the high iron concentrations found in the single-cell malaria parasite. When artemisinin comes into contact with iron, a chemical reaction ensues, spawning charged atoms that chemists call "free radicals." The free radicals attack cell membranes and other molecules, breaking them apart and killing the single-cell parasite.
 
Lai began to wonder if the process might work with cancer, too. "Cancer cells need a lot of iron to replicate DNA when they divide," Lai explains. "As a result, cancer cells have much higher iron concentrations than normal cells."
 
Most recently, Lai and Singh looked at a method that involves the use of the protein transferrin, to which the researchers bound artemisinin at the molecular level. Transferrin is an iron-carrying protein found in blood, and it is transported into cells via transferrin receptors on the cell's surface.
 
Iron-hungry cancer cells take in the transferrin without detecting the attached artemisinin. "We call it a Trojan horse because a cancer cell recognizes transferrin as a natural, harmless protein and picks up the tagged compound without knowing that a bomb - artemisinin - is hidden inside," Lai says.
 
According to a study published in January in the journal Life Sciences, the compound is 34,000 times more effective in selecting and killing cancer cells than normal cells. Artemisinin alone is 100 times more effective.
"So we've greatly enhanced the selectivity," Lai said. -Rob Harrill

Grapefruit juice concentrate increases the bioavailability of artemether
Objective: To evaluate the effect of grapefruit juice on the pharmacokinetics of artemether in plasma and saliva after a single oral dose and to detect concentration-dependent electrocardiographic changes (bradycardia and QTc prolongation).
 
Methods: Six healthy male subjects were given a standard breakfast followed by two tablets of 50 mg artemether administered with water; 1 week later, the tablets were administered with 350 ml double-strength fresh frozen grapefruit juice. For 8 h, 17 blood and saliva samples were collected, and 17 electrocardiograms were recorded. Drug and metabolite concentrations were measured by means of high-performance liquid chromatography with electrochemical detection.
 
The pharmacokinetic parameters were determined using a one-compartment model. Results: Grapefruit juice significantly (P = 0.001) increased the mean peak concentration (Cmax) of artemether more then twofold from 42 (SD 17) ng/ml to 107 (28) ng/ml. The time to reach Cmax (tmax) with grapefruit juice was 2.1 (0.6) h compared with 3.6 (17) h with water (P = 0.02). The area under the concentration-time curve (AUC) almost doubled with grapefruit juice from 177 ng-h/ml to 336 ng-h/ml (P = 0.003). The elimination half-life remained unchanged (1.0 h vs 1.3 h). No major changes in the kinetics of the metabolite dihydroartemisinin were detected. Low artemether levels and zero dihydroartemisinin levels were found in saliva. No influences of artemether were observed on 17 electrocardiograms during the 8 h after drug intake - in particular there were no signs of bradycardia or QTc prolongation.
Conclusion: Grapefruit juice significantly increases the oral bioavailability of artemether without an effect on the elimination half-life. It suggests a role for intestinal CYP3A4 in the presystemic metabolism of artemether.
_________________________________
Key words: Artemisinin derivative, Artemether, Grapefruit juice
M. A. van Agtmael, V. Gupta, T. H. van der Wosten, J-P. B. Rutten, C. J. van Hoxtel
Eur J Clin Pharmacol 1999; 55: 405-10.

The effect of grapefruit juice on the time-dependent decline of artemether plasma levels in healthy subjects.
 
BACKGROUND: ß-Artemether and other Artemesinin derivitives are new and effective treatments for malaria, although relapse is a problem in monotherapy. These relapses could be related to a time-dependent decline in artemether plasma levels described in multiple-dose studies and probably caused by autoinduction. The aim of this study was to evaluate the effect of grapefruit juice on the decreasing bioavailability over time of artemether.

METHODS: In a randomized, two-phase crossover study, eight healthy male subjects took 100 mg oral artemether with 350 mL water or with 350 mL double-strength fresh frozen grapefruit juice once daily for 5 days. On day 1 and day 5, 17 blood samples were collected over a period of 8 hours.

RESULTS: The mean peak artemether plasma concentration (Cmax) and the mean area under the concentration-time curve (AUC) after the last dose at day 5 were about one third compared with day 1, without a change in the elimination half-life after intake with water (P = .006 for Cmax; P = .005 for AUC) and with grapefruit juice (P < .001 for Cmax and AUC). Grapefruit juice increased Cmax (P = .021) and AUC (P < .001) twofold on day 1 (P = .021) and day 5 (P = .05 for Cmax; P = .004 for AUC). Dihydroartemisinin, the active metabolite, showed a twofold increase in
Cmax (P = .006) and AUC (P = .001) with grapefruit juice, without time-dependent changes of pharmacokinetic parameters.

CONCLUSIONS: Grapefruit juice (frozen concentrate specifically) significantly increased the oral bioavailability of artemether but did not prevent the time-dependent reduction in bioavailability. It suggests that CYP3A4 in the gut wall is one of the metabolizing enzymes of artemether but seems to not be involved in the autoinduction process.

__________________________________
van Agtmael MA, Gupta V, van der Graaf CA, van Boxtel CJ.
Clin Pharmacol Ther 1999; 66:408-14.

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