US4775660A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Treatment of breast cancer by combination therapy
Assignee: Individual
•
Filing: 1984-08-02
•
Granted: 1988-10-04
•
Expires: 2004-08-02
Abstract
Abstract A method of treatment of breast cancer in susceptible animals whose ovarian hormonal secretions were previously blocked by surgical or chemical means, e.g., by use of an LH-RH agonist, e.g., [D-Trp 6 , des-Gly-NH 2 10 ]LH-RH ethylamide with a combination therapy comprising administering an antiandrogen, e.g., flutamide and an antiestrogen, e.g., Tamoxifen, pharmaceutical compositions useful for such treatment and two and three component pharmaceutical kits containing such compositions are disclosed.
Inventors
- 👤 Fernand Labrie
- 👤 Alain Belanger
- 👤 Andre Dupont
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 10:42
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K31/445; A61K31/495; A61K38/00; A61K38/04; A61P; A61P35/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/13
Claims Analysis
Total Claims: 46
Claim 1
Independent Claim
48 words
A method of treating breast cancer in a warm-blooded animal in need of such treatment which comprises blocking the ovarian hormonal secretions of said animal by surgical or chemical means and administering to said animal therapeutically effective amounts of an antiandrogen and an antiestrogen, or pharmaceutical compositions thereof.
Claim 2
Independent Claim
48 words
A method of treating breast cancer in a warm-blooded animal in need of such treatment which comprises blocking the ovarian hormonal secretions of said animal by surgical or chemical means and administering to said animal therapeutically effective amounts of an antiandrogen and an antiestrogen, or pharmaceutical compositions thereof.
Claim 3
Dependent Claim
11 words
The method of claim 1 wherein the ovaries are surgically removed.
Claim 4
Dependent Claim
35 words
The method of claim 1 wherein the ovarian hormonal secretions are blocked by administering an amount of a LH-RH agonist or a LH-RH antagonist or a pharmaceutical composition thereof effective to block said hormonal secretions.
Claim 5
Dependent Claim
20 words
The method according to claim 1 wherein the LH-RH agonist is administered parenterally together with a pharmaceutically acceptable parenteral carrier.
Claim 6
Dependent Claim
22 words
The method of claim 1 wherein the antiandrogen and the antiestrogen are each administered orally, together with a pharmaceutically acceptable oral carrier.
Claim 7
Dependent Claim
61 words
The method of claim 1 wherein the LH-RH agonist is a nonapeptide or a decapeptide represented by the formula: L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-X-Y-L-arginyl-L-prolyl-Z, wherein X is D-tryptophyl, D-leucyl, D-alanyl, 3-(2-naphthyl)-D-alanyl, O-tert-butyl-D-seryl, D-tyrosyl, D-lysyl, D-phenylalanyl or N-methyl-D-alanyl and wherein Y is L-leucyl or D-leucyl or D-alanyl and wherein Z is glycyl-NHR 1 or NHR 1 wherein R 1 is H, lower alkyl or lower haloalkyl.
Claim 8
Dependent Claim
10 words
The method of claim 1 wherein the antiestrogen is (Z)-2-[4-(1,2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethanamine.
Claim 9
Dependent Claim
16 words
The method of claim 1 which further comprises administering aminoglutethimide or ketoconasole or pharmaceutical compositions thereof.
Claim 10
Dependent Claim
10 words
The method of claim 1 wherein the antiandrogen is 1-(3'-trifluoromethyl-4'-nitrophenyl)-4,4-dimethylimidazoline-2,5-dione.
Claim 11
Dependent Claim
10 words
The method of claim 1 wherein the antiandrogen is 4'-nitro-3'-trifluoromethylisobutyranilide.
Claim 12
Independent Claim
45 words
A method of treating breast cancer in a warm-blooded animal having breast cancer whose ovarian hormonal secretions have been previously blocked by surgical or chemical means, which comprises administering to said animal therapeutically effective amounts of an antiandrogen and an antiestrogen, or pharmaceutical compositions thereof.
Claim 13
Independent Claim
45 words
A method of treating breast cancer in a warm-blooded animal having breast cancer whose ovarian hormonal secretions have been previously blocked by surgical or chemical means, which comprises administering to said animal therapeutically effective amounts of an antiandrogen and an antiestrogen, or pharmaceutical compositions thereof.
Claim 14
Dependent Claim
11 words
The method of claim 11 wherein the ovaries are surgically removed.
Claim 15
Dependent Claim
35 words
The method of claim 11 wherein the ovarian hormonal secretions are blocked by administering an amount of a LH-RH agonist or a LH-RH antagonist or a pharmaceutical composition thereof effective to block said hormonal secretions.
Claim 16
Dependent Claim
20 words
The method according to claim 11 wherein the LH-RH agonist is administered parenterally together with a pharmaceutically acceptable parenteral carrier.
Claim 17
Dependent Claim
22 words
The method of claim 11 wherein the antiandrogen and the antiestrogen are each administered orally, together with a pharmaceutically acceptable oral carrier.
Claim 18
Dependent Claim
61 words
The method of claim 11 wherein the LH-RH agonist is a nonapeptide or a decapeptide represented by the formula: L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-X-Y-L-arginyl-L-prolyl-Z, wherein X is D-tryptophyl, D-leucyl, D-alanyl, 3-(2-naphthyl)-D-alanyl, O-tert-butyl-D-seryl, D-tyrosyl, D-lysyl, D-phenylalanyl or N-methyl-D-alanyl and wherein Y is L-leucyl or D-leucyl or D-alanyl and wherein Z is glycyl-NHR 1 or NHR 1 wherein R 1 is H, lower alkyl or lower haloalkyl.
Claim 19
Dependent Claim
10 words
The method of claim 11 wherein the anti-estrogen is (Z)-2-[4-(1,2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethanamine.
Claim 20
Dependent Claim
16 words
The method of claim 11 which further comprises administering aminoglutethimide or ketoconazole or pharmaceutical compositions thereof.
Claim 21
Dependent Claim
10 words
The method of claim 11 wherein the antiandrogen is 1-(3'-trifluoromethyl-4'-nitrophenyl)-4,4-dimethylimidazoline-2,5-dione.
Claim 22
Dependent Claim
10 words
The method of claim 11 wherein the antiandrogen is 4'-nitro-3'-trifluoromethylisobutyranilide.
Claim 23
Independent Claim
39 words
A method of treating breast cancer in a warm-blooded animal having breast cancer which comprises administering to said animal therapeutically effective amounts of a LH-RH agonist or a LH-RH antagonist, an antiandrogen and an antiestrogen, or pharmaceutical compositions thereof.
Claim 24
Independent Claim
39 words
A method of treating breast cancer in a warm-blooded animal having breast cancer which comprises administering to said animal therapeutically effective amounts of a LH-RH agonist or a LH-RH antagonist, an antiandrogen and an antiestrogen, or pharmaceutical compositions thereof.
Claim 25
Dependent Claim
19 words
The method of claim 21 wherein the LH-RH agonist is administered parenterally together with a pharmaceutically acceptable parenteral carrier.
Claim 26
Dependent Claim
21 words
The method of claim 18 wherein the antiestrogen and the antiandrogen are each administered orally, together with pharmaceutically acceptable oral carrier.
Claim 27
Dependent Claim
22 words
The method of claim 14 wherein the LH-RH agonist is administered at a daily parenteral dose of between 250 and 500 μg.
Claim 28
Dependent Claim
39 words
The method of claim 15 wherein the antiandrogen is administered at a daily oral dose of between about 0.20 and 20 mg and the antiestrogen is administered at a daily oral dose of between about 0.10 and 10 mg.
Claim 29
Dependent Claim
32 words
A kit comprising in separate containers pharmaceutical compositions for combined use in treating breast cancer which comprises (1) a pharmaceutical composition comprising an antiandrogen and (2) a pharmaceutical composition comprising an antiestrogen.
Claim 30
Dependent Claim
32 words
A kit comprising in separate containers pharmaceutical compositions for combined use in treating breast cancer which comprises (1) a pharmaceutical composition comprising an antiandrogen and (2) a pharmaceutical composition comprising an antiestrogen.
Claim 31
Dependent Claim
44 words
A kit comprising in separate containers pharmaceutical compositions for combined use in treating breast cancer which comprises (1) a pharmaceutical composition comprising a LH-RH agonist or a LH-RH antagonist (2) a pharmaceutical composition comprising an antiandrogen and (3) a pharmaceutical composition comprising an antiestrogen.
Claim 32
Dependent Claim
44 words
A kit comprising in separate containers pharmaceutical compositions for combined use in treating breast cancer which comprises (1) a pharmaceutical composition comprising a LH-RH agonist or a LH-RH antagonist (2) a pharmaceutical composition comprising an antiandrogen and (3) a pharmaceutical composition comprising an antiestrogen.
Claim 33
Dependent Claim
12 words
The kit of claim 27 wherein the pharmaceutical compositions are oral compositions.
Claim 34
Dependent Claim
27 words
The kit of claim 28 wherein the LH-RH agonist pharmaceutical composition comprises the LH-RH agonist in one container and a solvent for parenteral administration in another container.
Claim 35
Dependent Claim
19 words
The kit of claim 28 wherein the pharmaceutical compositions of the antiandrogen and the antiestrogen are each oral compositions
Claim 36
Independent Claim
50 words
The method of inhibiting the growth of breast tumors in a warm blood animal whose ovarian hormonal secretions have been previously blocked by surgical or chemical means which comprises administering to the warm-blooded animal having such tumors therapeutically effective amounts of an antiandrogen and an antiestrogen, or pharmaceutical compositions thereof.
Claim 37
Independent Claim
50 words
The method of inhibiting the growth of breast tumors in a warm blood animal whose ovarian hormonal secretions have been previously blocked by surgical or chemical means which comprises administering to the warm-blooded animal having such tumors therapeutically effective amounts of an antiandrogen and an antiestrogen, or pharmaceutical compositions thereof.
Claim 38
Dependent Claim
11 words
The method of claim 31 wherein the ovaries are surgically removed.
Claim 39
Dependent Claim
36 words
The method of claim 31 wherein the ovarian hrmonal secretions are blocked by administering and amount of a LH-RH agonist or a LH-RH antagonist or a pharmaceutical composition there of effective to block said hormonal secretions.
Claim 40
Dependent Claim
20 words
The method according to claim 31 wherein the LH-RH agonist is administered parenterally together with a pharmaceutically acceptable parenteral carrier
Claim 41
Dependent Claim
22 words
The method of claim 31 wherein the antiandrogen and the antiestrogen are each administered orally together with a pharmaceutically acceptable oral carrier.
Claim 42
Dependent Claim
61 words
The method of claim 31 wherein the LH-RH agonist is a nonapeptide or a decapeptide represented by the formula: L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-X-Y-L-arginyl-L-prolyl-Z, wherein X is D-tryptophyl, D-leucyl, D-alanyl, 3-(2-naphthyl)-D-alanyl, 0-tert-butyl-D-seryl, D-tyrosyl, D-lysyl, D-phenylalanyl or N-methyl-D-alanyl and wherein Y is L-leucyl or D-leucyl or D-alanyl and wherein Z is glycyl-NHR 1 or NHR 1 wherein R 1 is H, lower alkyl or lower haloalkyl.
Claim 43
Dependent Claim
10 words
The method of claim 31 wherein the antiestrogen is (Z)-2-[4-(1,2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethanamine.
Claim 44
Dependent Claim
16 words
The method of claim 31 which further comprises administering aminoglutethimide or ketoconasole or pharmaceutical compositions thereof.
Claim 45
Dependent Claim
10 words
The method of claim 31 wherein the antiandrogen is 1-(3'-trifluoromethyl-4'-nitrophenyl)-4,4-dimethylimidazoline-2,5-dione.
Claim 46
Dependent Claim
10 words
The method of claim 31 wherein the antiandrogen is 4'-nitro-3'-trifluoromethylisobutyranilide.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-10-04 | 1992-04-04 | 1992-10-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-10-04 | 1996-04-04 | 1996-10-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-10-04 | 2000-04-04 | 2000-10-04 | $7700.00 | Window Closed / Lapsed |