About HYG-440
HYG-440
HYG-440 is Hygeia’s lead topical antiandrogenic compound under preclinical
development. HYG-440 is the first anti-androgenic drug candidate engineered
to be rapidly deactivated by hydrolytic enzymes at or near the site of
application.
In preclinical in vitro models, HYG-440 has strong androgen-receptor affinity
and can inhibit androgenic effects of co administered androgens in rat cells
transfected with human androgen receptors. The expected major metabolite
had no detectable androgen-receptor affinity or ability to interfere with the
androgenic effects of endogenous androgens.
HYG-440 is a synthetic non-steroidal compound and represents one of four
structural classes of antiandrogenic compounds in Hygeia's portfolio.
Rationale for a Topical Antiandrogen to Treat Acne
Excess testosterone-like hormones in the skin can lead to the overproduction
of sebum which can block the pore and lead to localized infection. An anti-
androgen applied to skin can block the actions of testosterone-like hormones
in the skin. To limit the effects to the skin, HYG-440 was designed to be
deactivated by enzymes at or near the site of application.
Rationale for a Topical Antiandrogen to Treat Hirsutism
Paradoxically, excess androgens (testosterone-like hormones) in facial and
body skin can lead to unwanted localized hair growth in women (Hirsutism). An
antiandrogen applied to skin areas of unwanted body hair can reduce or
minimize excess body hair growth caused by excess androgens in the skin.
Rationale for a Topical Antiandrogen to Treat Androgenic Alopecia
Androgenic alopecia (hair loss due to excess androgens in the scalp) is the
most common cause of hair loss and affects both men and women. An anti-
androgen applied to the scalp can block the actions of testosterone-like
hormones. Hygeia's biodegradable topical antiandrogen HYG-440 was
specifically designed to avoid the risks associated with currently available oral
antiandrogen products.
The combination of an antiandrogen (HYG-440) and a biodegradable estrogen
(HYG-102) could be more effective than an antiandrogen alone in treating hair
loss due to excess androgens in the scalp.
References
1. Thiboutot D. et al., New Insights into the Treatment of Acne: an Update from
the Global Alliance to Improve Outcomes in Acne Group. Journal of the
American Academy of Dermatology 2009: 60(5 Suppl): S1-50.
2. Lee DL, Van Dyke GS and Kim J. Update on the Pathogenesis and Treatment
of Acne. Current Opinion in Pediatrics 2003: 15(4): 405-410.
3. Poulin Y. Practical Approach to the Hormonal Treatment of Acne. Journal of
Cutaneous Medicine and Surgery 2005: 8(4 Suppl) 16-21.
4. Paus R, Cotsarelis G. The Biology of Hair Follicles. The New England Medical
Journal 1999: 341(7): 491-497.
5. Randall VA, Hibberts NA, Thornton MJ, Hamada K, et al., The Hair Follicle: A
Paraxical Androgen Target Organ. Hormone Research 2000: 54(5-6): 243-250.
6. Hibberts NA, Howell AE, and Randall VA. Balding Hair Follicle Dermal Papilla
Cells Contain Higher Levels of Androgen Receptors than those from Non-
balding Scalp. Journal of Endocrinology 1998: 156(1): 59-65.
7. Harrison S and Bergfeld W. Diffuse Hair Loss: Its Triggers and Management.
Cleveland Clinic Journal of Medicine 2009: 76(6): 361-367.
8. Shapiro J. Hair Loss in Women. The New England Journal of Medicine 2007: 357
(16): 1620-30.
9. Sinclair R. Wewerinke M., and Jolley D. Treatment of Female Pattern Hair Loss
with Oral Antiandrogens. British Journal of Dermatology 2005: 152(3): 466-473.
HYG-440 is Hygeia’s lead topical antiandrogenic compound under preclinical
development. HYG-440 is the first anti-androgenic drug candidate engineered
to be rapidly deactivated by hydrolytic enzymes at or near the site of
application.
In preclinical in vitro models, HYG-440 has strong androgen-receptor affinity
and can inhibit androgenic effects of co administered androgens in rat cells
transfected with human androgen receptors. The expected major metabolite
had no detectable androgen-receptor affinity or ability to interfere with the
androgenic effects of endogenous androgens.
HYG-440 is a synthetic non-steroidal compound and represents one of four
structural classes of antiandrogenic compounds in Hygeia's portfolio.
Rationale for a Topical Antiandrogen to Treat Acne
Excess testosterone-like hormones in the skin can lead to the overproduction
of sebum which can block the pore and lead to localized infection. An anti-
androgen applied to skin can block the actions of testosterone-like hormones
in the skin. To limit the effects to the skin, HYG-440 was designed to be
deactivated by enzymes at or near the site of application.
Rationale for a Topical Antiandrogen to Treat Hirsutism
Paradoxically, excess androgens (testosterone-like hormones) in facial and
body skin can lead to unwanted localized hair growth in women (Hirsutism). An
antiandrogen applied to skin areas of unwanted body hair can reduce or
minimize excess body hair growth caused by excess androgens in the skin.
Rationale for a Topical Antiandrogen to Treat Androgenic Alopecia
Androgenic alopecia (hair loss due to excess androgens in the scalp) is the
most common cause of hair loss and affects both men and women. An anti-
androgen applied to the scalp can block the actions of testosterone-like
hormones. Hygeia's biodegradable topical antiandrogen HYG-440 was
specifically designed to avoid the risks associated with currently available oral
antiandrogen products.
The combination of an antiandrogen (HYG-440) and a biodegradable estrogen
(HYG-102) could be more effective than an antiandrogen alone in treating hair
loss due to excess androgens in the scalp.
References
1. Thiboutot D. et al., New Insights into the Treatment of Acne: an Update from
the Global Alliance to Improve Outcomes in Acne Group. Journal of the
American Academy of Dermatology 2009: 60(5 Suppl): S1-50.
2. Lee DL, Van Dyke GS and Kim J. Update on the Pathogenesis and Treatment
of Acne. Current Opinion in Pediatrics 2003: 15(4): 405-410.
3. Poulin Y. Practical Approach to the Hormonal Treatment of Acne. Journal of
Cutaneous Medicine and Surgery 2005: 8(4 Suppl) 16-21.
4. Paus R, Cotsarelis G. The Biology of Hair Follicles. The New England Medical
Journal 1999: 341(7): 491-497.
5. Randall VA, Hibberts NA, Thornton MJ, Hamada K, et al., The Hair Follicle: A
Paraxical Androgen Target Organ. Hormone Research 2000: 54(5-6): 243-250.
6. Hibberts NA, Howell AE, and Randall VA. Balding Hair Follicle Dermal Papilla
Cells Contain Higher Levels of Androgen Receptors than those from Non-
balding Scalp. Journal of Endocrinology 1998: 156(1): 59-65.
7. Harrison S and Bergfeld W. Diffuse Hair Loss: Its Triggers and Management.
Cleveland Clinic Journal of Medicine 2009: 76(6): 361-367.
8. Shapiro J. Hair Loss in Women. The New England Journal of Medicine 2007: 357
(16): 1620-30.
9. Sinclair R. Wewerinke M., and Jolley D. Treatment of Female Pattern Hair Loss
with Oral Antiandrogens. British Journal of Dermatology 2005: 152(3): 466-473.
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| Copyright © 2009 Hygeia Therapeutics, Inc. All Rights Reserved. |
