3-Bromopyruvate (3-BP): An effective metabolic inhibitor

Is 3-Bromopyruvate (3-BP) more beneficial than other metabolic inhibitors?

First, 3-BP is less toxic and more effective than DCA and 2DOG due to its preferential entry into cancer cells and its capacity to target simultaneously the two major energy production pathways (glycolysis and mitochondrial oxidative phosphorylation).  DCA and 2DOG are more cytotoxic because they enter both normal healthy and cancerous cells. Their chemical structures do not provide specificity to cancer cells. In fact, they enter more normal cells than cancer cells and harm normal cellular functions.

Secondly, DCA and 2DOG are less effective than 3BP in killing cancer cells because each agent targets primarily only one of a cell’s two energy production pathways, thus allowing such cells to rely on the other pathway for survival. For example, 2DOG will slow down only the glycolytic pathway but not mitochondrial function.

Consequently, cancer cells will thrive utilizing mitochondrial functions. DCA improves mitochondrial function but not the glycolytic energy production pathway. Unlike 2DOG and DCA, 3-BP while leaving normal cells unharmed will destroy both energy production pathways of cancer cells upon its preferential entry via monocarboxylate transporters (MCTs). That is why 3-BP is more effective than DCA and 2DOG while exhibiting little to no toxicity.

Chemotherapy warning as hundreds die from cancer-fighting drugs

Patients should be warned about the dangers of chemotherapy after research showed that cancer drugs are killing up to 50 percent of patients in some hospitals.  For the first time, researchers looked at the numbers of cancer patients who died within 30 days of starting chemotherapy, which indicates that the medication is the cause of death, rather than cancer.” There are serious effects from chemotherapy as seen in this article by Sarah Knapton, science editor of The Telegraph.

Dayspring Cancer Clinic is one of only a few cancer clinics in the United States currently making available 3-Bromopyruvate (3-BP) to patients with all types of cancer, not just liver cancer. Dayspring has an IRB accepted proposal to make this compound available to patients.

In 1931 a German physician/scientist, Dr. Otto Warburg, Ph.D., received a Nobel prize for proving that all cancer cells use anaerobic metabolism (burn sugar without using oxygen) to produce energy.  The problem is that this mechanism is 18 times less efficient than the aerobic (oxygen utilizing) metabolism that normal cells will use.  Therefore a cancer cell needs 18 times more sugar than a normal cell to grow and remain metabolically active. The resultant metabolic drain on the host is significant.

In cancer, 3-BP surpasses targeted therapies as targeted therapies are quickly made obsolete by intra-tumoral heterogeneities (too genetically varied for a sustained effect). But 3-BP works on all PET scan positive cancer cells. These cancer cells have a cellular metabolism that can be attacked by a small molecule such as 3-BP. Dr. Peter Pedersen’s lab at Johns Hopkins in Baltimore Maryland has thoroughly investigated 3-BP and then a formulation for 3-BP has been worked out to increase efficacy, decrease toxicity and nuance the delivery to cancer cells.

Patients, scientists, and many others are frequently interested in knowing whether 3-BP is more effective and less toxic to cancer patients than currently approved chemotherapy drugs.1   Certainly, this is the case for experimental animals. In fact, 3-BP is one of the most effective anti-cancer drugs, and in some cases, perhaps the most effective.2  3-BP targets the essential energy production machinery of cancer cells while leaving the same machinery in normal cells preserved. This discovery has been instrumental in propelling a new direction in cancer research focused on selectively targeting the cancer cells’ energy production factories. In fact, Dr. Peter Pedersen’s lab of Johns Hopkins is the pioneer in conceptualizing/inventing this new strategy.

There is two energy (ATP) production factories inside the cell, i.e., glycolysis and mitochondrial oxidative phosphorylation. In normal cells, about 5 percent of the total cellular energy (ATP) production is derived from glycolysis and about 95 percent from mitochondria.3 In cancer cells, the energy production by glycolysis is significantly increased (up to 60 percent).4  This dramatic increase in glycolysis in cancer cells results in a significant increase in lactic acid production.

More than 90 percent of cancers exhibit this common metabolic phenotype. This is called the “Warburg Effect”, i.e., a significant increase in glycolysis in cancer cells even in the presence of oxygen. The most frequently used cancer detection method clinically, i.e., Positron Emission Tomography (PET), is based on this metabolic phenotype, i.e., the “Warburg effect”.

Cancer cells that exhibit the “Warburg effect” pump out the produced lactic acid via a monocarboxylate transporter (MCT).  The number of these transporters (considered as doors or gates) in cancer cells is much greater than in normal cells.

3-BP, a lactic acid analog, is a small chemical and mimics the lactic acid chemical structure. Therefore, 3-BP mimicking lactic acid can enter as a Trojan horse through the MCT’s into cancer cells.  It has little effect on normal cells as these contain very few MCT’s under normal physiological conditions.

Because of 3-BP’s highly reactive nature, it then neutralizes the two cancer energy production factories. Cellular energy (ATP) is depleted very rapidly as 3-BP attacks the two factories at the same time causing the cancer cells to die (by cell membrane rupturing). So when cancer cells are treated with 3-BP the cancer cells rupture and cellular death occur. Normal metabolic cells are unaffected.

Comparing 3-BP with complementary therapies to the cost, effectiveness of conventional immunotherapy drugs

Many healthcare systems rely on a mechanistic view of health and how to cure disease. This view developed in the late 19th century with the discoveries of Louis Pasteur. He experimented with pasteurization to prevent spoilage in beer and milk.

Pasteur is one of the fathers of germ theory and was involved in the development of the first vaccines. The germ theory has success in treating or preventing pneumonia, syphilis, malaria, polio, etc.

In spite of its success, the conventional model of medicine has its limitations. Its strengths have evolved into some major weaknesses. Both medical care professionals and patients have become used to the idea that we can take a drug to get a quick.

But this does not identify the root causes of disease. For example, why change my diet, eliminate sugar, and get more exercise to control my Type 2 diabetes? I can take a pill or inject insulin!

Yet, more dysfunctional is the current range of treatment options for cancer. The Emperor of All Maladies by Dr. Siddhartha Mukherjee details the evolution of cancer treatment. The book also addresses research on treatments including genetic and immunotherapy therapy.

“The same old ideas, and it's all crap”

But it is interesting to note what Dr. James Watson, who worked on the double helix (DNA) discovery, said about cancer genetic research:

“The depressing thing about the ‘cancer moonshot' is that it's the same old people getting together, forming committees, and the same old ideas, and it's all crap …” [1]

Genetic research will not develop meaningful treatments other than a few specific areas. This is because the paradigm of cancer being a genetic cause has not changed. But there is an up-and-coming idea that cancer is a metabolic disease.

The traditional treatments for most cancers continue to be surgery, chemotherapy, and radiation. There are other treatments for certain types of cancer — hormone therapy, bone marrow replacement, etc.

All treatments have some side effects, but the most common treatment is chemotherapy. It has severe side effects because chemo damages healthy cells and the immune system — both key to long-term health.

Analysis of the data claims the effectiveness of chemo for Stage IV cancers is around 2 percent. (It is higher for certain types of cancer, like childhood leukemia or testicular cancer.) Chemo side effects also may cause permanent damage or death. Additionally, it is expensive.

Limitations of cancer treatments are obvious. Now, cancer researchers have branched out into other possible treatments.

Still, drug companies, hospitals, and doctors make a lot of money with chemotherapy.

Immunotherapy is one of the hottest areas of research. It is somewhat more effective, has fewer side effects, but is expensive. This makes it attractive to the drugs companies. Several immunotherapy drugs were released in the past few years.

Drug companies are not motivated to develop drugs or treatment protocols that are not patentable, like the 3-BP that Daysprings uses. They want to continue to sell expensive drugs that maintain profit margins.

But desperate cancer patients will go bankrupt to save or extend their life. Yet, even with insurance, the cost of these immunotherapy drugs is unimaginable.

In his presentation at the 2015 American Society of Clinical Oncologists], Dr. Leonard Saltz showed the cost of immunotherapy drugs: [2, 3]

A cost 4,000 times more than gold!

Opdivo costs $29 per mg, whereas Yervoy costs $157 per mg. Yervoy costs 4,000 times more than gold!

In the latest trial, the cost of using Yervoy alone was $158,282 to get an extra 2.4 months. The cost of Opdivo alone was $103,220 for an extra 6.9 months.

Combined, that costs $295,566 for an extra 11.4 months.

For patients on Medicare, and those whose insurance requires a 20 percent co-pay, it will cost $60,000 out of pocket for one year of the treatment.

Pembrolizumab is an immunotherapy drug approved for melanoma. The brand name is Keytruda and it currently costs around $14,500 per month. It is being studied on 20 different types of cancer. It has shown anti-tumor activity in 13 tumor types like small cell lung cancer, esophageal cancer, and ovarian cancer.

But the latest clinical trials are using a dose five times higher than approved for melanoma. It also costs about $83,000 per month. Yes, per month. For a 165-pound patient, Keytruda at the higher dose will cost more than $1 million per patient per year. (26 doses per year at $51.79 per mg.)

The FDA-approved Opdivo to treat squamous non-small cell lung cancer. At ASCO 2015, researchers presented a study using Opdivo on non-squamous non-small-cell lung cancer. The late-stage study showed that patients receiving Opdivo had a median survival of 12.2 months. Compare that to 9.4 months for patients taking the chemo drug Docetaxel. Adverse effects also were less severe.

Again, we're talking about the median; half the patients lived more than 12 months, half of them did not. Comparing the two median patients, one got an extra 3 months of life from a $100,000 therapy.

For the 589,430 people dying each year from metastatic cancer, this will cost $174 billion dollars. That is per year for the drug treatment with no other costs included.

So, what is the take-home message? Patented immunotherapy drugs are outrageously expensive and not tremendously effective. And yet, profit-oriented pharmaceutical companies still push these drugs to doctors. And the companies tout their drugs on TV.

Our holistic approach is more beneficial

At Dayspring, our holistic approach is more beneficial to find the root cause of cancer. A metabolic treatment, 3-bromopyruvate, is the backbone of our protocol. Dr. Peter Pederson has researched 3-BP for almost 20 years at Johns Hopkins University. (JHU is one of the most prestigious cancer institutes in the world.)

3-BP is an off-the-shelf chemical and not patentable or profitable to drug companies. When administered properly, it is more effective than conventional chemotherapy. [4] 3-BP also has limited side effects. It attacks only cancer cells; untouched are normal cells and the immune system.

Dayspring adds complementary therapies to the 3-BP protocol. This helps to detoxify the body and enhance immune function. Together, this treatment helps the body re-establish long-term health. This is not a short-term extension of life.

The root causes of cancer are different for everybody. At Dayspring, we customize treatment for each patient. Call Dayspring at (800) 351-5913 for a cost-effective and productive cancer treatment plan.

References

1 BMC Research Notes 2013, 6:277 doi:10.1186/1756-0500-6-277
2 J Bioenerg Biomembr. 2012 Feb;44(1):1-6. doi: 10.1007/s10863-012-9425-4.
3 Annual Review of Cell and Developmental BiologyVol. 27: 441-464 (Volume publication date November 2011)
4 The Hexokinase 2 Dependent “Warburg effect” and Mitochondrial Oxidative Phosphorylation in Cancer: Targets for effective therapy with the powerful small molecule 3-bromopyruvate. Prepublication paper June 6, 2014 Paweł Lis, Young H. Ko, Peter L. Pedersen*, Andre Goffeau and Stanisław Ułaszewski.

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