Open Label Clinical Study #2

A Non-Randomized Uncontrolled Follow Up Clinical Study to Determine the Efficacy of HairGenesis™, a new hair loss treatment for androgenetic alopecia (AGA), also known as pattern hairloss.

Introduction

Androgenic Alopecia, or pattern hair loss, is an autosomally mediated chronbiologic phenomenon, affecting over 40 million American men and 20 million American women. To date, there has been no safe, efficacious method of treating and/or reversing the progression of this disorder without the potential for negative side effect.

There have been numerous proposed treatments for baldness, but only a few have provided effective treatment over a wide range of patients, and none so far have been based on naturally occurring substances. AGA which describes pattern alopecia, is considered to be a genetically based disorder  and is commonly characterized by thinning and loss of hair in affected individuals within a given pattern on the scalp.

This disorder progresses by causing the affected hair follicles to become smaller and correspondingly finer. Eventually, the fine hairs may be lost and, thus, baldness results in the affected area. Hair has been classified as being of at least two distinct types, terminal and vellus.

A vellus hair is short, fine, thin, and non-pigmented, with the bulb of the hair follicle seated superficially in the dermis of the scalp.  Terminal hairs are long, coarse and pigmented, with the bulb of the follicle seated deep in the dermis. During the thinning stage of AGA, the hairs in the affected area are observed to transform from terminal to vellus. It is this transformation to vellus hairs that is equated to baldness. The core of the phenomenon is associated with structural miniaturization.

Background

Androgenic Alopecia (AGA) as well as Benign Prostatic Hyperplasia (BPH) are believed to result from a genetic sensitivity to the steroid hormone 5alpha dihydrotestosterone, which is a highly bio-active metabolite of the androgenic hormone testosterone.  Although these disorders are vastly different in physiology and presentation, the etiology of each stems from this specific hormonal metabolism.  It has therefore been desireable to create treatments which may safely block this metabolic pathway.   In developing such treatments, various hormones such as estrogen and other anti androgens have been tested and found unsuitable due to undesirable side effects, such as feminization of male subjects.

Therefore, it would be useful to establish a treatment for AGA that minimizes the use of bio-effecting drugs. It would be expected that natural ingredients will be biologically more friendly to the user and suitable for long term use with minimal side effects.

Mechanism of Action

This study contemplates the benefit of a naturally derived composition for AGA in order to reduce or arrest the onset of hair loss associated with the disorder. The preferred formulation employs Beta-Sitosterol, saw palmetto berry extract, lecithin, inositol, phosphatidyl choline, niacin, and biotin in orally administered dosages. The method of treatment is administering a dosage of the stated ingredients. In one embodiment, the dosages may be combined in a single soft gel capsule. The preferred quantities of each is as shown in the following preferred dosage.

According to the capsule formulation of Table 1, a gel capsule containing 200 mg of standardized saw palmetto extract is taken twice per day such as each morning and each evening. According to another aspect, the invention provides a means for emulsifying Beta Sitosterol and saw palmetto extract, or an emulsifier system component that aids the other components in penetrating the stomach lining.

A suitable emulsifier is lecithin, inositol, or preferably a mixture of both.. The preferred dosage of Table I is stated with respect to lecithin consisting of 61-64% phosphatides, for which the dosage is 50 mg each twelve hours. The preferred dosage of inositol is 100 mg each twelve hours. These emulsifier system components can be varied in dosage by a large factor without harm or toxicity.

As means of protecting follicles from degeneration due to oxidation, free radicals and metabolic by-products, the treatment provides and antioxidant component such as phosphatidyl choline. An orally administered dosage of 25 mg per twelve hours provides a general antioxidant prophylactic effect throughout the body.

A vasodilator component is also provided, wherein preferred elements are niacin, biotin, and preferably both. Niacin, or vitamin B3, generally promotes circulation and is beneficial in maintaining and promoting circulation to the follicles. D-Biotin, or vitamin H, compliments the effects of niacin. These dosages are approximate and may be varied by a large factor such as 50% or more.

The shell of a gel capsule may be formed of gelatin, glycerin, water, titanium dioxide, and such other pigments as may be desired. The preferred dosage of Table I provides a suitable quantity of each ingredient for treatment at twelve hour intervals.

In the dosages and treatments, Beta Sitosterol and saw palmetto berry extract are considered the active ingredients. Their disclosed dosage is suitable for achieving effective treatment with intermittent administration approximately at twelve hour intervals. The remaining components are administered in a mixture with the active ingredients for internal administration and may be considered supplemental to enhance the action of the active ingredients.

The formulation is believed to function on a molecular level via competitive mechanical inhibition of the T1 and T2 5-alpha-DHT androgen receptor sites found within susceptible scalp hair follicles. Unbound 5-alpha-DHT is thus metabolized out of the body via primary excretion pathways without triggering the secondary and pathological cascade of events associated with pattern hair loss.

Study Overview

The goal of this follow up study is to evaluate and corroborate the safety and efficacy of a naturally derived oral formulation (HairGenesis™) containing known anti-androgenic components, in arresting and/or reversing onset of typical AGA.   A previous open label study established baseline statistical evidence for safety and efficacy.  Statistical analysis to be determined by gross clinical evaluation, patient reporting, and baseline, intra-study, and endpoint photographic evidence.

Treatment Period

Orally, one (1) HairGenesis™ softgel twice a day. Participants to be followed over the course of six months time. Participants to report to clinic one time per month during this period for follow up investigator evaluation.

Adverse Events

Any participant adverse event reported during this study to be fully documented per standard protocol parameters.

Inclusion Parameters

Males and females between the ages of 18 and 55 who are experiencing Androgenetic Alopecia (pattern hair loss in men or women) as determined by the Norwood Class Scale, in a clinical investigator evaluation.

Exclusion Parameters

• Participants with undetermined reason for hairloss
• Participants using other medications on the scalp
• Participants with no family history of hair loss
• Participants with red, inflamed, infected, irritated or painful scalp
• Participants who have been diagnosed with alopecia areata, lupus, erythematosus, or other non- male pattern alopecia / hairloss.

Evaluation Analysis

Incidence and degree of side effects, if any.  Incidence and degree of adverse events, if any.  Reduction in rate of hairloss, if any..   Aesthetically meaningful change in caliber of affected scalp hair, if any, as evidenced by clinical photography, patient reporting and investigator clinical impression.  Dramatic thickening reported.

Study Synopsis

This follow up research study over a six month period did not reveal any side effects, drug interactions or adverse events. Based on the data gathered, all participants (100%) in the study reported an arresting of symptomatology commonly associated with Androgenic Alopecia and 33% reported an aesthetically meaningful change in the caliber of affected scalp hair.  A further 7% observed dramatic thickening of their hair.

These findings were determined via investigator observation, baseline, intra study, and endpoint photographic evidence, as well as patient reporting. This study suggests a highly efficacious and safe treatment methodology. Based on these highly positive findings, further study is clearly indicated and presently underway.

Exhibit A: Clinical Study Statistics with HairGenesis

Exhibit B: Before Use and After Use Photos with HairGenesis

Exhibit C: Before Use and After Use Photos with HairGenesis

Exhibit D: Norwood HairLoss Chart

References

• The Bald Truth, Fischer, David, US News and World Report, v123n5, pp 44-50 August 4, 1997
• His Health: The Buzz on Baldness, Leaf, Clifton, American Health vl5, n9 November, 1996 pp 34-35
• HAIR! From personal Statement to Personal Problem, Pine, Devera, FDA Consumer, December 1991 25(10): pp 20-23
• Management of Alopecia, Source: UTMB Dept of Otolaryngology Grand Rounds Presentation, September 9, 1998. Facility: Karen Calhoun, MD Resident: Kyle Kennedy, MD
• Alopecia, (Baldness), Source: UTMB Dept of Otolaryngology Grand Rounds, April 30, 1997, Resident Physician: Chris Thompson, MD, Faculty: Karen Calhoun, MD, FACS, Series Editor: Francis B. Quinn, Jr., MD, FACS
• Management of Alopecia, Source: UTMB Dept of Otolaryngology Grand Rounds Presentation, September 9, 1998. Facility: Karen Calhoun, MD Resident: Kyle Kennedy, MD
• The Bald Truth, Fischer, David, US News and World Report, v123n5, pp 44-50 August 4, 1997
• Management of Alopecia, Source: UTMB Dept of Otolaryngology Grand Rounds Presentation, September 9, 1998. Facility: Karen Calhoun, MD Resident: Kyle Kennedy, MD
• Estrogen-induced gynecomastia following use of estrogen-containing local agents. Schmidt KU: Wagner G; Mensing H, Dtsch Med Wochenschr, 112: 23, 1987 Jun 5, 9268