Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
1992-11-10
2002-01-29
Goldberg, Jerome D. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
active
06342491
ABSTRACT:
BACKGROUND OF THE INVENTION
Estrogens have been shown to play an important role in the modulation of estrogen receptor positive breast carcinoma. Binding of endogenous estrogens, in particular 17&bgr;-estradiol (E
2
), to the estrogen receptor has been linked to proliferation of the carcinoma cells, by causing the carcinoma cells to shift from the G
1
phase of the cell cycle to the S phase of the cell cycle. The G
1
stage of interphase is characterized by the cell being in a resting state, whereas it is during the S phase that the DNA synthesis necessary for cell survival and proliferation occurs.
Current trends in the treatment of estrogen receptor positive breast carcinoma are focused on the use of anti-estrogenic agents that prevent the binding of E
2
to the estrogen receptor. It has been postulated that an anti-estrogen may inhibit E
2
binding through competitive inhibition at the estrogen receptor or alternatively by binding to another site such as the anti-estrogen or calmodulin receptor, thereby preventing the binding of E
2
to the estrogen receptor. [V. C. Jordan, Pharmacol Rev 36: 245 (1984)]. In one study, approximately 60% of patients with estrogen receptor positive breast cancer (>10 femtomol/mg cytosol protein) responded to anti-estrogen therapy, whereas less than 10% of patients with estrogen receptor negative tumors (<10 femtomol/mg cytosol protein) responded. [J. L. Borgna, Biochem Pharmacol 31: 3187 (1982)]. Treatment of the estrogen receptor positive MCF-7 human breast cancer cells with tamoxifen [Z-1-(4&bgr;-dimethylaminoethoxyphenyl) 1,2-diphenylbut-1-ene citrate], a non-steroidal anti-estrogen, has been shown to inhibit cell E
2
stimulated cell growth by virtue of its ability to prevent the MCF-7 cells from entering the S phase of the cell cycle. [N. Brunner, Cancer Res 49: 1515 (1989)]. Chronic administration of tamoxifen (200 &mgr;g/day for 3 weeks) to mature female rats with dimethylbenzanthracene (DMBA) induced tumors prevents the accumulation of administered [
3
H]-E
2
in uterine, vaginal, and mammary tumor tissue. [V. C. Jordan, J Endocr 68: 297 (1976)]. Presently, the treatment of choice for postmenopausal estrogen receptor positive breast carcinoma is tamoxifen. [V. C. Jordan, Pharmacol Rev 36: 245 (1984); A. U. Buzdar, Cancer 62: 2098, (1988); V. Hug, Br J Cancer 59: 421, (1989)].
Positive results with tamoxifen have been reported in several estrogen receptor positive ovarian carcinoma cell lines. [S. P. Langdon, J Endocrin 127(Supp): 119 (1990); G. dePalo, Acta Oncol 28: 163 (1989); K. R. Geisinger, Cancer 65: 1055 (1990); S. P. Langdon, Br J Cancer 62: 213 (1990)]. In addition, tamoxifen produced positive results in inhibiting the growth of several other estrogen receptor positive carcinomas including, DMBA-induced uterine adenocarcinoma in rats [S. Sekiya, J Obstet Gynaec Br Commonw 83: 183 (1976)]; Dunning R3327 rat prostrate adenocarcinoma [M. M. Ip, Cancer Res 40: 2188 (1980)]; and diethylstilbesterol induced renal tumors in hamsters [A. H. Dodge, Eur J Cancer Clin Oncol 13: 1377 (1977)].
In humans, tamoxifen has been used with varying degrees of success to treat a variety of estrogen receptor positive carcinomas such as breast cancer, endometrial carcinoma, prostate carcinoma, ovarian carcinoma, renal carcinoma, melanoma, colorectal tumors, desmoid tumors, pancreatic carcinoma, and pituitary tumors. [B. J. Furr, Pharmac Ther 25: 127 (1984)].
REFERENCES:
Escher et al., “Current Views on the Management of Metastatic Mammary Carcinoma,”M. Clin., North America 45:613-626 (1961).
Segaloff and Ochsner, “Results of Studies of the Cooperative Breast Cancer Group—1961-631.2,”Cancer Chemotherapy Reports, 41:1-24 (1964).
Segaloff and Ochsner, “Progress Report: Results of Studies of the Cooperative Breast Cancer Group—1956-601.2,”Cancer Chemotherapy Reports, 11:109-141 (1961).
“Current Status of Hormone Therapy of Advanced Mammary Cancer,”Journal of American Medical Assoc.146(5):471-477 (Jun. 1951).
Lewison et al., “Tracer Studies of Radioactive Sodium Estrone Sulfate (S35) in Cases of Advanced Breast Cancer,”Cancer. 537-548 (May 1951).
McCormick, “Benign and Malignant Diseases of the Breast,”Journal of American Medical Association146(5):461-464 (Jun. 1951).
Taylor et al., “Hormones in Breast Metastasis Therapy,”M. Clin. North America, 35:51-61 (1951).
Griboff, “The Rationale and Clinical Use of Steroid Hormones in Cancer,”A.M.A. Archives of Internal Medicine, 89: 635-685 (Apr. 1952).
Woodward, et al., “Changes in the Blood Chemistry of Patients with Disseminated Carcinoma of the Breast During Endocrine Therapy,”Cancer7(4):744-757 (Jul. 1954).
“Questions & Answers,”GP7(1):82-84 (Jan. 1954).
Taylor, “Hormonal Modification in the Treatment of Disseminated Cancer of the Breast,”American Journal of Medicine21:688-696 (Nov. 1956).
Kennedy et al., “Surgery as an Adjunct to Hormone Therapy of Breast Cancer,”Cancer10(5):1055-1075 (Sep.-Oct. 1957).
Mustacchi et al., Frequency of Cancer in Estrogen-Treated Osteoporotic Women, in Segaloff, A.:Breast Cancer, The Second Biennial Louisiana Cancer Conference, New Orleans, Jan. 22-23, 1958, St. Louis, The C.V. Mosby Company, pp 163-169 (1958).
Block, “Endocrine Treatment of Advanced Mammary Cancer,”GP20(4), 85-96 (Oct. 1959).
Lemon, “Prednisone Therapy of Advanced Mammary Cancer,”Cancer12(1) 93-107 (Jan.-Feb. 1959).
Baker et al., “Hormonal Treatment of Metastic Carcinoma of the Breast,”American Journal of Surgery99: 538-543 (Apr. 1960).
Council on Drugs: “Androgens and Estrogens in the Treatment of Disseminated Mammary Carcinoma,”Journal of American Medical Association, 172 (12):1271-1283 (1960).
Kelley, “Medical Aspects of the Hormonal Treatment of Cancer,”Modern Medicine28:117-126 (Apr. 1960).
Whitney, “The Endocrine Palliation of the Breast Cancer Patient,”The Journal of the Maine Medical Association, 51: 433-438 (Dec. 1960).
Kennedy, “Massive Estrogen Administration in Premonopausal Women with Advanced Breast Cancer,”Cancer Chemotherapy Reports, 16:283-284 (Feb. 1962).
Kennedy, “Massive Estrogen Administration in Premonopausal Women with Advanced Breast Cancer,”Cancer15(3): 641-648 (May-Jun. 1962).
Wilson, “The Roles of Estrogen and Progesterone in Breast and Genital Cancer,”Journal of American Medical Association, 182 (4): 327-331 (Oct. 1962).
Hertz et al., “Administration of Massive Dosage of Estrogen to Breast and Prostatic Cancer Patients; Blood Levels Attained,” Ciba Foundation Colloquia,Endocrinology, 1:157-169 (1952).
Rukes and Galante, “Palliative Treatment of Metastatic Cancer of the Breast,”GP, 10(4), 83-93 (Oct. 1954).
Adair et al., “The Use of Estrogens and Androgens in Advanced Mammary Cancer,”The Journal of American Medical Association, 140(15), 1193-1200 (Aug. 1949).
Garland et al., “Roentgen and Steroid Hormone Therapy in Mammary Cancer Metastatic to Bone.”Journal of American Medical Association, 144(12):997-1004 (Nov. 1950).
Kennedy and Nathanson, “Effects on Intensive Sex Steroid Hormone Therapy in Advanced Breast Cancer,”Journal of American Medical Association, 152(12):1135-1141 (Jul. 1953).
Segaloff et al., “Hormonal Therapy in Cancer of the Breast,”Cancer, 7(4):758-763 (Jul. 1954).
Kennedy et al., “Massive Estrogen Administration in Premenopausal Women with Advanced Breast Cancer,”Abstract of Proceedings of American Association of Cancer Research3:239 (#146) (1961).
Kaufman and Goodwin, “Cancer of the Prostate: Diagnosis and Treatment,”The Journal of American Geriatrics Society, 4:296-305 (Mar. 1956).
Beck, “Hormonal Therapy of Carcinoma of the Breast,”Canadian Services Medical Journal, 13:607-613 (Oct. 1957).
Stearns and Gordon, “Changes in Microscopic Pathology of Prostatic Carcinoma Following Estrogen Therapy and Surgery,”The Journal of Urology, 79(2): 333-338(Feb. 1958).
Treves, “The Treatment of Cancer, Especially Inoperable Cancer, of the Male Breast by Ablative Surgery (Orchiectomy, Adrenalectomy, and Hypophysectomy) and Hormone Therapy (Estrogens a
Bex Frederick J.
Corbin Alan
Dey Michael S.
American Home Products Corporation
Finnegan Henderson Farabow Garrett & Dunner L.L.P.
Goldberg Jerome D.
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