About HYG-102
HYG-102
HYG-102 is Hygeia’s lead estrogenic compound under preclinical
development. HYG-102 is the first estrogenic drug candidate engineered to
be rapidly deactivated to non-estrogenic metabolites by hydrolytic enzymes.
In animal models, HYG-102 has strong estrogenic properties at the site of
application but no effect on the most estrogen-sensitive systemic tissues even
at high multiples of the locally effective dose. The expected major metabolite
has no detectable estrogenic effects in vitro.
HYG-102 is one of ten estrogen-receptor agonists in Hygeia's portfolio.
Rationale for a Safer Estrogen for Topical Use
Estrogens are steroid hormones that support skin health by maintaining skin
thickness, moisture content, and elasticity. The profound effects of estrogens
on skin were known long before it was discovered that estrogen receptors are
present in all epithelial tissues but most abundant in facial skin and the uterus.
Decades after estrogens were first used over-the-counter (OTC) to restore and
maintain skin health, unwanted estrogenic side effects were linked to the use
of these products. Safety concerns finally led to the removal of all estrogens
and other hormone-containing OTC products in the US in 1994. Less than 10
years later, the use of estrogen-containing prescription products were
associated with an increased risk of cancer and cardiovascular disease. These
risks associated with estrogen use have made many doctors and patients
hesitant to use estrogens to manage aging skin and vaginal atrophy
associated with low estrogen.
Hygeia's biodegradable topical estrogens were specifically designed to avoid
the risks associated with currently available estrogen products.
References
1. Rossouw JE. Risks and benefits of estrogen plus progestin in healthy
postmenopausal women: Principal results from the women's health initiative
randomized controlled trial. JAMA 2002: 288(3): 321-333.
2. Cushman M. Estrogen plus progestin and risk of venous thrombosis. JAMA
2004: 202(13) 1573-1580.
3. Thornton, MJ. The biological actions of estrogen on the skin. Exp Derm 2002:
11: 487-502.
4. Heldring N. et al., Estrogen receptors: How do they signal and what are their
targets. Physiol Rev 2007: 87: 905-931.
5. Levin ER. Cellular functions of plasma membrane estrogen receptors.
Steroids 2002: 67: 471-475.
6. Labrie, F. et al., Effect of one-week treatment with vaginal estrogen
preparations on serum estrogen levels in postmenopausal women. Menopause
2009: 16(1): 30-36.
7. SOGC Clinical Practice Guidelines- The detection and management of
vaginal atrophy. International Journal of Gynecology & Obstetrics 2005: 88: 222-
228.
8. Wolff EF, Narayan D., and Taylor HS. Long-term effects of hormone therapy on
skin rigidity and wrinkles. Fertility and Sterility 2005: 84(2): 285-288.
9. Crosignani PG. Hormones and cardiovascular health in women. Human
Reproduction Update 2006: 12(5) 483-497.
10. Leclair DM and Anandarajah G. Effects of estrogen deprivation- vasomotor
symptoms, urogenital atrophy, and phychobiological effects. Clinics in Family
Practice 2002: 4(1): 27-39.
HYG-102 is Hygeia’s lead estrogenic compound under preclinical
development. HYG-102 is the first estrogenic drug candidate engineered to
be rapidly deactivated to non-estrogenic metabolites by hydrolytic enzymes.
In animal models, HYG-102 has strong estrogenic properties at the site of
application but no effect on the most estrogen-sensitive systemic tissues even
at high multiples of the locally effective dose. The expected major metabolite
has no detectable estrogenic effects in vitro.
HYG-102 is one of ten estrogen-receptor agonists in Hygeia's portfolio.
Rationale for a Safer Estrogen for Topical Use
Estrogens are steroid hormones that support skin health by maintaining skin
thickness, moisture content, and elasticity. The profound effects of estrogens
on skin were known long before it was discovered that estrogen receptors are
present in all epithelial tissues but most abundant in facial skin and the uterus.
Decades after estrogens were first used over-the-counter (OTC) to restore and
maintain skin health, unwanted estrogenic side effects were linked to the use
of these products. Safety concerns finally led to the removal of all estrogens
and other hormone-containing OTC products in the US in 1994. Less than 10
years later, the use of estrogen-containing prescription products were
associated with an increased risk of cancer and cardiovascular disease. These
risks associated with estrogen use have made many doctors and patients
hesitant to use estrogens to manage aging skin and vaginal atrophy
associated with low estrogen.
Hygeia's biodegradable topical estrogens were specifically designed to avoid
the risks associated with currently available estrogen products.
References
1. Rossouw JE. Risks and benefits of estrogen plus progestin in healthy
postmenopausal women: Principal results from the women's health initiative
randomized controlled trial. JAMA 2002: 288(3): 321-333.
2. Cushman M. Estrogen plus progestin and risk of venous thrombosis. JAMA
2004: 202(13) 1573-1580.
3. Thornton, MJ. The biological actions of estrogen on the skin. Exp Derm 2002:
11: 487-502.
4. Heldring N. et al., Estrogen receptors: How do they signal and what are their
targets. Physiol Rev 2007: 87: 905-931.
5. Levin ER. Cellular functions of plasma membrane estrogen receptors.
Steroids 2002: 67: 471-475.
6. Labrie, F. et al., Effect of one-week treatment with vaginal estrogen
preparations on serum estrogen levels in postmenopausal women. Menopause
2009: 16(1): 30-36.
7. SOGC Clinical Practice Guidelines- The detection and management of
vaginal atrophy. International Journal of Gynecology & Obstetrics 2005: 88: 222-
228.
8. Wolff EF, Narayan D., and Taylor HS. Long-term effects of hormone therapy on
skin rigidity and wrinkles. Fertility and Sterility 2005: 84(2): 285-288.
9. Crosignani PG. Hormones and cardiovascular health in women. Human
Reproduction Update 2006: 12(5) 483-497.
10. Leclair DM and Anandarajah G. Effects of estrogen deprivation- vasomotor
symptoms, urogenital atrophy, and phychobiological effects. Clinics in Family
Practice 2002: 4(1): 27-39.
 |
| |
 |
| |
 |
| |
 |
| |
 |
| |
 |
| |
 |
| |
 |
| Copyright © 2009 Hygeia Therapeutics, Inc. All Rights Reserved. |
