CA2623024C - Use of estradiol valerate or estradiol combined with dienogest for the oral therapy of dysfunctional uterine bleeding in the form of oral contraceptives - Google Patents
Use of estradiol valerate or estradiol combined with dienogest for the oral therapy of dysfunctional uterine bleeding in the form of oral contraceptives Download PDFInfo
- Publication number
- CA2623024C CA2623024C CA2623024A CA2623024A CA2623024C CA 2623024 C CA2623024 C CA 2623024C CA 2623024 A CA2623024 A CA 2623024A CA 2623024 A CA2623024 A CA 2623024A CA 2623024 C CA2623024 C CA 2623024C
- Authority
- CA
- Canada
- Prior art keywords
- daily doses
- stage
- dienogest
- combination
- estradiol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- RSEPBGGWRJCQGY-RBRWEJTLSA-N Estradiol valerate Chemical compound C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCC)[C@@]1(C)CC2 RSEPBGGWRJCQGY-RBRWEJTLSA-N 0.000 title claims abstract description 50
- 229960003309 dienogest Drugs 0.000 title claims abstract description 32
- AZFLJNIPTRTECV-FUMNGEBKSA-N dienogest Chemical compound C1CC(=O)C=C2CC[C@@H]([C@H]3[C@@](C)([C@](CC3)(O)CC#N)CC3)C3=C21 AZFLJNIPTRTECV-FUMNGEBKSA-N 0.000 title claims abstract description 31
- 206010027514 Metrorrhagia Diseases 0.000 title claims abstract description 27
- 206010013908 Dysfunctional uterine bleeding Diseases 0.000 title claims abstract description 26
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 title abstract description 18
- 229930182833 estradiol Natural products 0.000 title abstract description 18
- 229960005309 estradiol Drugs 0.000 title abstract description 8
- 229960004766 estradiol valerate Drugs 0.000 title abstract description 8
- 229940127234 oral contraceptive Drugs 0.000 title abstract description 4
- 239000003539 oral contraceptive agent Substances 0.000 title abstract description 4
- 238000002560 therapeutic procedure Methods 0.000 title abstract description 3
- 239000000902 placebo Substances 0.000 claims abstract description 18
- 229940068196 placebo Drugs 0.000 claims abstract description 18
- 208000032843 Hemorrhage Diseases 0.000 claims description 19
- 230000000740 bleeding effect Effects 0.000 claims description 19
- 238000011282 treatment Methods 0.000 claims description 16
- 230000002175 menstrual effect Effects 0.000 claims description 11
- 239000008280 blood Substances 0.000 claims description 7
- 210000004369 blood Anatomy 0.000 claims description 7
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 230000001419 dependent effect Effects 0.000 abstract 1
- 230000005906 menstruation Effects 0.000 abstract 1
- 208000034158 bleeding Diseases 0.000 description 16
- 239000000583 progesterone congener Substances 0.000 description 5
- BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SLHNCBLASA-N 0.000 description 4
- 229960002568 ethinylestradiol Drugs 0.000 description 4
- 208000024891 symptom Diseases 0.000 description 4
- 210000004696 endometrium Anatomy 0.000 description 3
- 239000000262 estrogen Substances 0.000 description 3
- 230000003821 menstrual periods Effects 0.000 description 3
- 229960000417 norgestimate Drugs 0.000 description 3
- KIQQMECNKUGGKA-NMYWJIRASA-N norgestimate Chemical compound O/N=C/1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(OC(C)=O)C#C)[C@@H]4[C@@H]3CCC2=C\1 KIQQMECNKUGGKA-NMYWJIRASA-N 0.000 description 3
- 201000005670 Anovulation Diseases 0.000 description 2
- 206010002659 Anovulatory cycle Diseases 0.000 description 2
- 206010030295 Oligomenorrhoea Diseases 0.000 description 2
- 206010046788 Uterine haemorrhage Diseases 0.000 description 2
- 231100000552 anovulation Toxicity 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 239000000890 drug combination Substances 0.000 description 2
- 201000006828 endometrial hyperplasia Diseases 0.000 description 2
- 229940088597 hormone Drugs 0.000 description 2
- 239000005556 hormone Substances 0.000 description 2
- 230000001788 irregular Effects 0.000 description 2
- 230000002045 lasting effect Effects 0.000 description 2
- 230000027758 ovulation cycle Effects 0.000 description 2
- 229940095055 progestogen systemic hormonal contraceptives Drugs 0.000 description 2
- 230000035755 proliferation Effects 0.000 description 2
- 208000037853 Abnormal uterine bleeding Diseases 0.000 description 1
- 206010061692 Benign muscle neoplasm Diseases 0.000 description 1
- 241000819038 Chichester Species 0.000 description 1
- 206010014759 Endometrial neoplasm Diseases 0.000 description 1
- 206010027295 Menometrorrhagia Diseases 0.000 description 1
- 201000004458 Myoma Diseases 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- IMONTRJLAWHYGT-ZCPXKWAGSA-N Norethindrone Acetate Chemical compound C1CC2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@](C#C)(OC(=O)C)[C@@]1(C)CC2 IMONTRJLAWHYGT-ZCPXKWAGSA-N 0.000 description 1
- 206010036086 Polymenorrhoea Diseases 0.000 description 1
- 208000037062 Polyps Diseases 0.000 description 1
- 206010047998 Withdrawal bleed Diseases 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 239000003433 contraceptive agent Substances 0.000 description 1
- 230000002254 contraceptive effect Effects 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 238000002405 diagnostic procedure Methods 0.000 description 1
- 230000003292 diminished effect Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000002357 endometrial effect Effects 0.000 description 1
- 230000001076 estrogenic effect Effects 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 208000000509 infertility Diseases 0.000 description 1
- 231100000535 infertility Toxicity 0.000 description 1
- 230000036512 infertility Effects 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 229960002985 medroxyprogesterone acetate Drugs 0.000 description 1
- PSGAAPLEWMOORI-PEINSRQWSA-N medroxyprogesterone acetate Chemical compound C([C@@]12C)CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2CC[C@]2(C)[C@@](OC(C)=O)(C(C)=O)CC[C@H]21 PSGAAPLEWMOORI-PEINSRQWSA-N 0.000 description 1
- 208000007106 menorrhagia Diseases 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 229940053934 norethindrone Drugs 0.000 description 1
- 229960001652 norethindrone acetate Drugs 0.000 description 1
- VIKNJXKGJWUCNN-XGXHKTLJSA-N norethisterone Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 VIKNJXKGJWUCNN-XGXHKTLJSA-N 0.000 description 1
- 229940096055 prax Drugs 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- GYDJEQRTZSCIOI-LJGSYFOKSA-N tranexamic acid Chemical compound NC[C@H]1CC[C@H](C(O)=O)CC1 GYDJEQRTZSCIOI-LJGSYFOKSA-N 0.000 description 1
- 229960000401 tranexamic acid Drugs 0.000 description 1
- 238000002604 ultrasonography Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/18—Feminine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05022324.7 | 2005-10-13 | ||
| EP05022324A EP1787649B1 (de) | 2005-10-13 | 2005-10-13 | Verwendung von Estradiolvalerat in Kombination mit Dienogest zur oralen Therapie der dysfunktionellen uterinen Blutung in Einheit mit einer oralen Kontrazeption |
| PCT/EP2006/009867 WO2007042296A1 (de) | 2005-10-13 | 2006-10-12 | Verwendung von estradiolvalerat oder estradiol in kombination mit dienogest zur oralen therapie der dysfunktionellen uterinen blutung in einheit mit einer oralen kontrazeption |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2623024A1 CA2623024A1 (en) | 2007-04-19 |
| CA2623024C true CA2623024C (en) | 2012-03-06 |
Family
ID=35811580
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2623024A Active CA2623024C (en) | 2005-10-13 | 2006-10-12 | Use of estradiol valerate or estradiol combined with dienogest for the oral therapy of dysfunctional uterine bleeding in the form of oral contraceptives |
Country Status (22)
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102004019743B4 (de) | 2004-04-20 | 2008-11-27 | Bayer Schering Pharma Aktiengesellschaft | Mehrphasenpräparat zur Kontrazeption auf der Basis eines natürlichen Estrogens |
| ME01056B (me) * | 2005-10-13 | 2012-10-20 | Bayer Ip Gmbh | Upotreba estradiolvalerata i dienogesta za oralno liječenje disfunkcionalnog uterinog krvarenja u kontracepcijskom metodu |
| US8153616B2 (en) | 2005-10-17 | 2012-04-10 | Bayer Pharma Aktiengesellschaft | Combination preparation for oral contraception and oral therapy of dysfunctional uterine bleeding containing estradiol valerate and dienogest and method of using same |
| EP1930010A1 (de) | 2006-10-20 | 2008-06-11 | Bayer Schering Pharma Aktiengesellschaft | Verwendung von Estradiolvalerat oder 17ß-Estradiol in Kombination mit Dienogest zur oralen Therapie für den Erhalt und/oder die Steigerung der weiblichen Libido |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4429374C1 (de) * | 1994-08-12 | 1996-02-01 | Jenapharm Gmbh | Pharmazeutische Präparate zur Kontrazeption/Hormonsubstitution mit biogener Estrogenkomponente |
| DE19540253C2 (de) * | 1995-10-28 | 1998-06-04 | Jenapharm Gmbh | Mehrphasenpräparat zur Kontrazeption auf der Basis natürlicher Estrogene |
| PT921804E (pt) * | 1996-07-26 | 2004-01-30 | Wyeth Corp | Metodo contraceptivo bifasico e conjunto ("kit") compreendendo uma combinacao de uma progestina e um estrogenio |
| US6251956B1 (en) | 1998-08-20 | 2001-06-26 | Ortho Pharmaceutical Corporation | Combination progestin oral contraceptive regimen |
| EP1462106A1 (en) * | 2003-03-28 | 2004-09-29 | Pantarhei Bioscience B.V. | Pharmaceutical compositions and kits comprising 17-beta-estradiol and a progesteron for the treatment of gynecological disorders |
| DE102004019743B4 (de) * | 2004-04-20 | 2008-11-27 | Bayer Schering Pharma Aktiengesellschaft | Mehrphasenpräparat zur Kontrazeption auf der Basis eines natürlichen Estrogens |
| ME01056B (me) * | 2005-10-13 | 2012-10-20 | Bayer Ip Gmbh | Upotreba estradiolvalerata i dienogesta za oralno liječenje disfunkcionalnog uterinog krvarenja u kontracepcijskom metodu |
-
2005
- 2005-10-13 ME MEP-2009-171A patent/ME01056B/me unknown
- 2005-10-13 EP EP05022324A patent/EP1787649B1/de not_active Revoked
- 2005-10-13 ES ES05022324T patent/ES2322479T3/es active Active
- 2005-10-13 PL PL05022324T patent/PL1787649T3/pl unknown
- 2005-10-13 AT AT05022324T patent/ATE424828T1/de active
- 2005-10-13 SI SI200530672T patent/SI1787649T1/sl unknown
- 2005-10-13 DK DK05022324T patent/DK1787649T3/da active
- 2005-10-13 DE DE502005006837T patent/DE502005006837D1/de active Active
- 2005-10-13 PT PT05022324T patent/PT1787649E/pt unknown
-
2006
- 2006-10-12 KR KR1020087011203A patent/KR20080065651A/ko not_active Ceased
- 2006-10-12 PE PE2009001256A patent/PE20100090A1/es not_active Application Discontinuation
- 2006-10-12 PE PE2006001241A patent/PE20070555A1/es not_active Application Discontinuation
- 2006-10-12 DE DE502006008853T patent/DE502006008853D1/de active Active
- 2006-10-12 PT PT06806225T patent/PT1933843E/pt unknown
- 2006-10-12 TW TW095137564A patent/TWI328453B/zh active
- 2006-10-12 PL PL06806225T patent/PL1933843T3/pl unknown
- 2006-10-12 KR KR1020107014574A patent/KR101218872B1/ko active Active
- 2006-10-12 CA CA2623024A patent/CA2623024C/en active Active
- 2006-10-12 EP EP06806225A patent/EP1933843B1/de active Active
- 2006-10-12 WO PCT/EP2006/009867 patent/WO2007042296A1/de active Application Filing
- 2006-10-12 JP JP2008534936A patent/JP5735200B2/ja active Active
- 2006-10-12 SI SI200630991T patent/SI1933843T1/sl unknown
- 2006-10-12 CN CNA2006800381810A patent/CN101312733A/zh active Pending
- 2006-10-12 DK DK06806225.6T patent/DK1933843T3/da active
- 2006-10-12 AT AT06806225T patent/ATE497387T1/de active
- 2006-10-12 ES ES06806225T patent/ES2360302T3/es active Active
- 2006-10-13 UY UY29861A patent/UY29861A1/es not_active Application Discontinuation
- 2006-10-13 AR ARP060104489A patent/AR056694A1/es not_active Application Discontinuation
- 2006-10-13 DO DO2006000221A patent/DOP2006000221A/es unknown
-
2007
- 2007-01-09 TW TW096100872A patent/TW200829255A/zh unknown
-
2009
- 2009-05-05 HR HR20090256T patent/HRP20090256T1/xx unknown
- 2009-06-11 CY CY20091100621T patent/CY1110321T1/el unknown
-
2011
- 2011-02-10 CL CL2011000283A patent/CL2011000283A1/es unknown
- 2011-05-02 CY CY20111100422T patent/CY1111406T1/el unknown
-
2012
- 2012-11-19 JP JP2012253067A patent/JP2013047269A/ja active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |