There are two serious problems with current cancer therapies. The first is severe side effects and toxicity. The second is very limited efficacy. Consequently, cancer patients are still dying of the disease.
The majority of current therapeutic agents, in both cytotoxic and noncytotoxic category, are chemicals foreign to the human body. As a result, the body tries extremely hard to get rid of them using whatever metabolic ways available. Since our body does not have a natural and safe way of metabolizing those foreign chemicals, some nonspecific oxidation reactions then are used as major means of metabolism. The consequence is that the elimination process unavoidably generates a lot of chemically active intermediates or radicals, which will assault also normal cellular substances in the body including nucleic acids and proteins, leading to serious side effects including even the induction of new types of cancer. Since these agents are designed by humans but not the nature, they have very high chance to bind to and interact with other molecules (including proteins and receptors) than their expected targets in the body. These “off-target” bindings and interactions account for significant opportunities for side effects. The two scenarios are also true for most of the other therapies including that for obesity.
The second is the effectiveness of those therapeutic agents currently in marketplace. The effectiveness of cytotoxic agents is mainly limited by their indiscriminate toxicity to normal cells and tissues so that they cannot be administered too frequently or for too long. The dosing level of those agents cannot be raised further to effectively fight cancers as one may wish due to their toxicity to normal tissues. The efficacy of noncytotoxic agents, which target specific functions important for the survival of cancers, is limited by their single mechanism based strategy. An important hallmark for cancers is their constant genetic change or mutation. Once a cancer changes into a state that it is no longer dependent on a specific function a therapeutic agent targets for survival, the efficacy of the agent will be lost immediately. The situation thus calls for the emergence of a novel therapeutic agent that can assault cancer with multiple combat strategies for sustained potency (making cancer eradication a possibility) and can be safely metabolized for low side effect(s).
We have recently discovered a new natural hormone named ITE, short for 2-(1’H-indole-3’-carbonyl)-thiazole-4-carboxylic acid methyl ester, which is a physiological ligand for a receptor called Ah (aryl hydrocarbon) receptor. We then have demonstrated that ITE is very potent in inhibiting the generation of new blood vessels from existing ones, a process termed angiogenesis, in a mouse corneal grafting model. Cancers cannot grow further beyond 1 to 2 mm in diameter without newly generated blood vessels to supply nutrients with oxygen and remove wastes. Thus, ITE will be very effective in combating cancers by choking them off the blood supply, a technique called anti-angiogenesis. However, the hormone does not simply stop here.
ITE may possess other capabilities of cancer combating. For example, ITE may inhibit cell division. Since cancer is resulted from uncontrolled cell division, ITE then may be able to stop the progression of cancers. ITE may also promote programmed cell death (apoptosis) of cancer cells. Finally, ITE may have the ability to induce cell differentiation. When cancer cells differentiate, they stop being cancer cells and therefore stop reproducing but may start dying. Additionally, ITE may be able to block actions of estrogen and androgen. Certain breast and prostate cancers are dependent on estrogen and androgen, respectively, for their sustained advancement. This capability of ITE can thus further enhance the therapy for the estrogen dependent breast cancer and androgen dependent prostate cancer
The multiple strategy backed cancer combating capability makes the ITE therapy truly unique and outstanding. The multiplicity of combating strategy is crucial in maintaining its high therapeutic potency over cancers in constant genetic change. That means we can hold cancer under control for much longer time than any other available therapies. When we can hold cancer under control for longer enough time while keep assaulting it and sending death signals to it at the same time, the cancer may eventually die off. Therefore, the multiplicity of the assaulting strategy makes therapeutic potency of ITE sustainable. The sustainability of the potency then makes the eradication of cancers finally a possibility.
2-4. The natural hormone may offer therapeutic specificity
Another important issue in cancer therapy is that it is highly desirable for a therapeutic agent specifically working on cancer cells instead of normal cells. This type of specificity can be achieved if there are more target molecules the agent binds in cancer cells than in normal cells. The target molecule for ITE hormone is a cellular protein named Ah (aryl hydrocarbon) receptor (AhR). In the literature, the Ah receptor was reportedly to be highly concentrated in pancreatic cancer tissues from 14 out of 15 patients but very diluted in all normal pancreatic tissues examined. Similarly, the concentrated Ah receptor is also documented with prostate cancer. This means that the therapeutic specificity of ITE could be achieved at least in those reported types of cancer.
Contrary to those chemicals (used in current therapies) foreign to human body, ITE is a natural hormone produced by the human body, so the nature has designed and implemented a natural and safe way for its metabolism. Its metabolic process thus will cause less or even no problem to the body. This means that it will be very low in side effect(s). Another important reason for possible low side effect is that the binding of the natural hormone to its receptor (the Ah receptor) is very specific and precise since it is designed and manufactured by the nature. The hormone ITE, other than those human designed chemicals, will then have low chance of binding to other proteins or molecules to provoke “off-target” problems. Low side effect(s) of ITE therapy, in turn, can be interpreted as a possibility of further raising its dosing levels to further enhance its potency. It can also be translated into a possibility of more frequent and prolonged administration, paving the way for eventual cancer eradication, an extra goal of ours.
The hormone ITE is a small organic compound with a molecular weight of only 286 Dalton. It can be easily not only synthesized chemically but also formulated for oral administration, the most convenient route for our patients.
3. THE SCIENTIFIC FOUNDATION
Please review the science behind the proposed therapeutic capabilities of this new natural hormone by clicking the Scientific Foundation.
4. FURTHER RESEARCH AND DEVELOPMENT
We are actively preparing for the initial study of xenograft mouse models for human cancers. We will report to you as soon as data are collected. Briefly, human cancer tissues or cell lines will be inoculated into those immune compromised mice (so that they will not reject human cancer tissues or cell lines) to establish human cancers on animals. The hormone ITE dissolved in a selected vehicle system will be injected for a month or so. The tumor sizes will be continuously monitored and compared with the ones on those mice injected with the vehicle system alone.
If you would like to have a general information sheet about ITE science and further development, please click here to download a PDF file for that. |
