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April 4, 2002

FLURIDIL,
A NOVEL DERMO-COSMETIC AGENT FOR TOPICAL APPLICATION IN ANDROGENIC HAIR LOSS, i.e. EFFLUVIUM AND ALOPECIA

In an effort to develop a more powerful inhibitor of the androgen receptor, the biomedical laboratories Biophysica in California, in collaboration with the research laboratories of a Czech biotech pharma company, Interpharma Praha, developed a new class of substances which proved to render the androgen receptor inactive in a novel way. A large number of new molecules were synthesized and tested. Some were not resorbed when given orally or topically. The most promising molecule was structurally modified so that minor amounts of water would cause the molecule's decomposition, thus rendering it pharmacologically inactive and incapable to act inside the body. To prove that this substance, now called Fluridil, once resorbed into the skin would not enter into the body, a number of experimental studies were conducted using rats and rabbits, who are capable of taking up substances through their skin 6 to 10 times more than humans. We applied large quantities of Fluridil, far surpassing the highest conceivable dose in humans. Using sophisticated equipment of high sensitivity no trace of Fluridil or its fragments were ever found in the blood.

Many studies were conducted to ascertain the systemic and topical toxicity in animals and finally in human volunteers at the specialized Experimental Dermatology Institute of the University of California in San Francisco, under the leadership of Professor Howard Maibach. The result of this study was remarkable in that no irritation whatsoever was observed, thus confirming the data we previously gleened from experimental animals.

By then, news had spread and several of our colleagues of ours on their own started applying the compound to their scalp, soon to report the unusual efficacy of the alcoholic solution of Fluridil. We have thereafter optimized the composition of the solution, conducted all required safety tests and after having presented our findings to the authorities, gained marketing approval in the Czech Republic.

In a study with human volunteers, not even trace levels of Fluridil were detected in the serum; therefore, it cannot be expected to have systemic effects. This was also confirmed by the clinical study conducted presently at the Medical School dermatology department (Chairman: J. Bucek, M.D., Palacky University, Olomouc, Czech Republic): in most subjects, increase in anagens (growing hair) and decrease in telogens (dying hair) after 3 months of daily application of 2 ml Fluridil was substantial; there were no changes in the hematological and hormonal profiles and there were no adverse effects.


From what has been said above, it is obvious that the mechanism of Fluridil as a dermo-cosmetic device is sufficiently clear to judge Fluridil's prospective usefulness. Surely, when hair has been missing from the scalp for a long time and the hair follicles were obliterated by the ingrowth of connective tissue, there is very little chance for growing new hair. Here only transplants can reasonably work. Fluridil is therefore useful only when the hair follicles are still active and their androgen receptors are still intact.

So far, the most successful findings were reported by volunteers who started using Fluridil at the time when the first loss of hair was encountered. With men, this can start any time after 30 years of age; with women very often the hair effluvium sometimes dramatically and suddenly appears concurrently with menopause. In these clients we find that the hair loss ceases after a few weeks of once-a-day application.

Perhaps, unfortunately, but understandably based on what had been said above, in order to keep the androgen receptor in check it is necessary to continue applying Fluridil daily. In a number of volunteers we found that after some 3 to 4 months of use, new hair growth, "peach fuzz" - the appearance of baby hair - was induced in the scalp, unless it had been hairless for many years. With time and patience which the hair growth cycle requires - and which may be as long as one year - we often observe a gradual transformation of the "baby hair" into hair of normal appearance.

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