Hygeia Therpaeutics, Inc.

 

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 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. HYG-440 was designed to be metabolically "soft" so as 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 antiandrogen 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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