Example :1 Effects of Topical PAI-1 inhibitor formulation on Hair Graying
[02431 A topical study oftopical PAI-1 inhibitor formulation after topical
administration ofa topical formulation ofPAI-1 inhibitor (e.g… see Table 1) in man is
performed. The study is designed to test whether the topical formulation of PAI-1 inhibitor
significantly reduces hair graying in man by measuring hair color change following topical treatment with a PAI-1 inhibitor.
[0244] The study includes two groups of 25 human subjects each. Both groups have subjects with varying levels ofhair follicle density and varying numbers and/or density of gray hairs. The scalp ofeach subject in the second group is treated twice a day for 6 months topically with a fixed volume of aPAI-1 inhibitor formulation that is at a fixed
concentration ofthe PAI-1 inhibitor. The concentration of the PAI-1 inhibitor in the formulation is 5% w/w. The administration of the topical preparation to the scalp takes about 5 minutes, after which the suspension is left on the site for about 8 to 12 hours. The scalps of the subjects in the first group are treated twice a day for 6 months topically with an empty formulation and is the control.
[0245| The expected effect of such a treatment is a reduction in the density of gray hairs at the site of the PAI-I inhibitor formulation treatment. The number of gray hairs at the treatment sites is measured by two methods: 1) A photograph of the treated area is taken to observe a change in the hair color; or 2) A gray hair density test, wherein the gray hair count in a small site on each subject’s scalp is measured. The small site on the scalp is selected prior to the commencement of the study.
[0246] A photograph and the gray hair density test method are employed at baseline prior to a PAI-1 inhibitor treatment. Following this photographs of the scalp of each subject is obtained every four weeks after start oftreatment and at the end of the 6-month study; the gray hair density test is also performed every four weeks after start of treatment and at the end of the 6-month study. The study finds that at Baseline, the average amount of gray hairs counted by either the gray hair density tests or as observed from the photographs is approximately equal across the control and treatment groups. Photographs of the scalps of the subjects of the treatment group on average show a visual reduction in the total number of gray hairs with every four weeks. The gray hair density test also on average shows a reduction in the number of gray hairs in the site selected on the scalp of each subject belonging to the treatment group with every four weeks. In contrast subjects in the control group showed no visual reduction in gray hairs in the treatment site, or reduction in the density ofgray hairs in the selected site on the scalp.
[02471 This study establishes that topical administration of the topical formulation of PAI-1 inhibitor reduces gray hair count and reverses hair graying in humans.
Example 2: Effects of Oral PAI-1 inhibitor formulation on Hair Graying
[0248] A study of oral administration of an oral formulation of PAI-1 inhibitor in man is performed. The study is designed to test whether the oral formulation of PAI-1 inhibitor significantly reduces hair graying in man by measuring hair color change following oral treatment with a PAI-1 inhibitor.
[02491
The study includes two groups of 25 human subjects each. Both groups have subjects with varying levels of hair follicle density and varying numbers and/or density of
gray hairs. Each subject in the second group is administered an oral preparation of PAl-1 inhibitor formulated as a 75 mg capsule thrice a day for 6 months. Each subject in the first group are administered an oral empty preparation formulated as a 75 mg capsule thrice a day for 6 months and serve as the control.
[02501
The expected effect of such a treatment is a reduction in the density of gray hairs due to the PAI-1 inhibitor formulation treatment. The number of gray hairs on the scalps of the subjects is measured by two methods: 1) A photograph of the scalp is taken to observe a change in the hair color, or 2) A gray hair density test, wherein the gray hair count in a small site on each subject’s scalp is measured. The small site on the scalp is is selected prior to the commencement of the study.
[02511 A photograph and the gray hair density test method are employed at baseline prior to a PAI-1 inhibitor treatment. Following this photographs ofthe scalp of each subject is obtained every four weeks after start of treatment and at the end ofthe 6-month study; the gray hair density test is also performed every four weeks after start of treatment and at the end of the 6-month study. The study finds that at baseline, the average amount of gray hairs counted by either the gray hairdensity tests or as observed from the photographs is approximately equal across the control and treatment groups. Photographs of the scalps of the subjects of the treatment group on average show a visual reduction in the total number of gray hairs with every four weeks. The gray hair density test also on average shows a reduction in the number ofgray hairs in the site selected on the scalp of each subject belonging to the treatment group with every four weeks. In contrast subjects in the control group showed no visual reduction in gray hairs in the treatment site, or reduction in the density of gray hairs in the selected site on the scalp.
[0252]
This study establishes that oral administration of the oral formulation of PAI- 1inhibitor reduces gray hair count and reverses hair graying in humans.
