1. How was phenoxodiol discovered?
2. What is phenoxodiol and how is it made?
3. What effect does phenoxodiol have on cancer cells?
4. How does phenoxodiol work?
5. How specific is phenoxodiol?
6. How is phenoxodiol given?
7. What cancers may phenoxodiol be useful for?
8. Is phenoxodiol strong enough to work on its own?
1. How was phenoxodiol discovered?
Phenoxodiol was created as an analogue (derivative) of genistein, a naturally occurring plant isoflavone. Genistein was discovered in the 1980s to have modest anti-cancer activity. The genistein structure was altered to change and to increase the anti-cancer activity.
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2. What is phenoxodiol and how is it made?
Phenoxodiol belongs to the chemical class known as isoflavenes.
It is manufactured by standard synthetic chemistry.
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3. What effect does phenoxodiol have on cancer cells?
Cancer cells display signs of distress within several hours of exposure to phenoxodiol. The cancer cell stops dividing almost immediately, and then dies by the process of apoptosis within 24-48 hours.
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4. How does phenoxodiol work?
The primary target of phenoxodiol is a protein receptor known as ECTO-NOX (external NADH oxidase). This receptor plays an important role in helping to maintain high levels of anti-apoptotic proteins in the cancer cell. By binding to the ECTO-NOX receptor and blocking its function, phenoxodiol eventually switches off the production of the anti-apoptotic proteins. This in turn leads to activation of proteolytic enzymes within the cancer cell known as caspases. These digest the cancer cell when activated, leading to the self-destructive form of cell death known as apoptosis.
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5. How specific is phenoxodiol?
Phenoxodiol is highly specific for cancer cells. This is because the primary target of phenoxodiol, ECTO-NOX, is preferentially expressed on abnormally rapidly dividing cells such as cancer cells.
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6. How is phenoxodiol given?
Phenoxodiol is formulated both in oral dosage form and intravenous dosage form.
An oral dosage form is being used in all current clinical applications.
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7. What cancers may phenoxodiol be useful for?
In the test tube, phenoxodiol kills virtually all types of cancer cells to which it has been exposed. This includes breast, prostate, ovarian, lung, colorectal and head & neck carcinomas, mesotheliomas, leukemias, rhabdomyosarcoma and neuroglioma.
The metabolism of phenoxodiol within the body suggests that it would not be suitable for colorectal cancer and hematological cancers (leukemia). A derivative drug of phenoxodiol has been identified as being suitable for these forms of cancer and is undergoing development.
With the exception of colorectal and hematological cancers, phenoxodiol is considered appropriate in the treatment of all other solid cancers.
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8. Is phenoxodiol strong enough to work on its own?
In some cancers, phenoxodiol appears to be strong enough to work on its own (as a monotherapy).
However, one of the major benefits of phenoxodiol is its ability to condition cancer cells to the toxic effects of standard anti-cancer drugs. This is known as synergy.
This works in two ways:
- in cancer cells that are susceptible to the effects of standard anti-cancer drugs, phenoxodiol substantially increases their sensitivity to those drugs (known as synergy). Exposing cancer cells to phenoxodiol first, increases the subsequent killing capacity of a second drug by as much as 100,000 fold according to test tube experiments.
- in cancer cells that have become resistant to the effects of standard anti-cancer drugs, phenoxodiol restores chemo-sensitivity. By exposing chemo-resistant cancer cells to phenoxodiol first, long-standing drug-resistance is removed, making cancer cells susceptible once again to standard anti-cancer drugs such as cisplatin, carboplatin, taxanes and gemcitabine.
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