Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ether doai
Reexamination Certificate
2000-07-21
2001-06-12
Henley, III, Raymond (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ether doai
Reexamination Certificate
active
06245819
ABSTRACT:
FIELD OF THE INVENTION
This invention relates to a method for the treatment of vaginal dryness or sexual dysfunction in women during or after menopause.
BACKGROUND OF THE INVENTION
The publications and other materials used herein to illuminate the background of the invention, and in particular, cases to provide additional details respecting the practice, are incorporated by reference.
During and after menopause, elderly women commonly develop symptoms which are due to estrogen deficiency. These symptoms include hot flashes, sweating, insomnia, depression, vaginal dryness, urinary incontinence, nausea, pain, osteoporosis, coronary heart disease, breast tenderness, oedema, fatigue, decreased sexual activity, as well as subsequent psychosocial problems (Payer, 1990; Rekers, 1990). In addition, estrogens are suggested to have neuroprotective effects. Thus, declining estrogen concentrations may negatively affect the mental activities of aging women (Schneider & Finch, 1997; Wickelgren, 1997). Estradiol is known to be excellent in the treatment of climacteric symptoms, and its use in the treatment of these symptoms is rapidly increasing. However, estrogens cause an increased risk of endometrial and breast cancers. It is possible to decrease the carcinogenicity of endometrial cancer by sequential progestin administration, but the risk of breast cancer is not diminished by progestins. The carcinogenicity risk limits the length of estrogen replacement therapy, although it would be very useful to continue the therapy long term, due to the protective effects of estrogens in the bone, in the cardiovascular system, in the central nervous system, and for urinary symptoms.
Antiestrogens, now often referred to as “SERM”s (selective estrogen receptor modulators), have both estrogen-like and antiestrogenic properties (Kauffman & Bryant, 1995). The effects may be tissue-specific as in the case of tamoxifen and toremifene which have estrogen-like effects in the bone, partial estrogen-like effect in the uterus and liver, and pure antiestrogenic effect in breast cancer. Raloxifene and droloxifen are similar to tamoxifen and toremifene, except that their antiestrogenic properties dominate. Based on the published information, all SERMs are more likely to cause menopausal symptoms than to prevent them. They have, however, other important benefits in elderly women: they decrease total and LDL cholesterol, thus deminishing the risk of cardiovascular diseases, and they may prevent osteoporosis and inhibit breast cancer growth in postmenopausal women. There are also almost pure antiestrogens under development. They are mainly aimed at the treatment of breast cancer (Wakeling & Bowler, 1988).
The compound (deaminohydroxy)toremifene, which also is known under the code FC-1271 a, has relatively weak estrogenic and antiestrogenic effects in the classical hormonal tests (Kangas, 1990). It has antiosteoporosis actions and it decreases total and LDL cholesterol levels in both experimental models and in human volunteers (International patent publications WO 96/07402 and WO 97/32574). It also has antitumor activity in an early stage of breast cancer development in an animal breast cancer model. The effect of antiestrogens on climacteric symptoms has not been studied earlier. FC-1271 a is the first SERM which has been shown to have beneficial effects in age-related syndromes in healthy women.
SUMMARY OF THE INVENTION
The invention concerns a method for the treatment of vaginal dryness or sexual dysfunction in women during or after the menopause, said method comprising administering to the woman an effective amount of the compound (deaminohydroxy)toremifene or a pharmaceutically acceptable salt or ester thereof, or a metabolite thereof.
REFERENCES:
patent: 5750576 (1998-05-01), DeGregorio et al.
patent: 5912273 (1999-06-01), Degregorio et al.
patent: 6037379 (2000-03-01), Harkonen et al.
Baynes, K.C.R. and Compston, J.E. (1998). “Selective oestrogen receptor modulators: a new paradigm for HRT.”Curr. Opin. Obstetrics Gynecology10:189-192.
DeGregorio, M.W. and Taras, T.L. (1998). “Hormone replacement therapy and breast cancer: revisiting the issues.”J. Am. Pharm. Assoc.38:738-746.
Kangas, L. (1990). Biochemical and pharmacological effects of toremifene metabolites.:Cancer Chemother. Pharmacol.27:8-12.
Kennedy, M.M. et al. (1999). “Tamoxifen and the endometrium: review of 102 cases and comparison with HRT-related and non-HRT-related endometrial pathology.”Int'l. J. Gynecological Patholoy18:130-137.
Whitehead, M. (1996). “Treatments for menopausal and post-menopausal problems: present and future.”Bailliere's Clin. Obstetrics Gynaecology10:515-530.
DeGregorio Michael W.
Halonen Kaija
Kangas Lauri
Henley III Raymond
Hormos Medical Oy Ltd.
Rothwell Figg Ernst & Manbeck p.c.
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