WO2007106264A3 - Extended cycle multiphasic oral contraceptive method - Google Patents

Extended cycle multiphasic oral contraceptive method Download PDF

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Publication number
WO2007106264A3
WO2007106264A3 PCT/US2007/003508 US2007003508W WO2007106264A3 WO 2007106264 A3 WO2007106264 A3 WO 2007106264A3 US 2007003508 W US2007003508 W US 2007003508W WO 2007106264 A3 WO2007106264 A3 WO 2007106264A3
Authority
WO
WIPO (PCT)
Prior art keywords
estrogen
ethinyl estradiol
amount equivalent
phase
equivalent
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.)
Ceased
Application number
PCT/US2007/003508
Other languages
French (fr)
Other versions
WO2007106264A2 (en
Inventor
Herman Ellman
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Warner Chilcott Co LLC
Original Assignee
Warner Chilcott Co LLC
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Warner Chilcott Co LLC filed Critical Warner Chilcott Co LLC
Priority to MX2008011074A priority Critical patent/MX2008011074A/en
Priority to CA2640520A priority patent/CA2640520C/en
Priority to EP07750352.2A priority patent/EP1993531B1/en
Priority to ES07750352.2T priority patent/ES2558030T3/en
Publication of WO2007106264A2 publication Critical patent/WO2007106264A2/en
Publication of WO2007106264A3 publication Critical patent/WO2007106264A3/en
Priority to IL193013A priority patent/IL193013A/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K31/28—Compounds containing heavy metals
    • A61K31/285—Arsenic compounds
    • 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
    • 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
    • A61K31/565—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
    • A61K31/567—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 substituted in position 17 alpha, e.g. mestranol, norethandrolone
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Reproductive Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

A multiphasic method of contraception comprising the steps of sequentially administering to a female of child bearing age a Phase I composition containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg norethiiidrpne acetate and an estrogen in an amount equivalent to about 5 to aboμt 15 mcg of ethinyl estradiol for about 7 to about 14 days; a Phase II composition containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg of norethindrone acetate and an estrogen in an amount equivalent to about 10 to about 25 meg of ethinyl estradiol for about 14 to about 22 days; a Phase m composition containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg of norethindrone acetate and an estrogen in an amount equivalent to about 15 to about 35 meg of ethinyl estradiol for about 20 to about 31 days; and an optional Phase IV composition containing (i) an estrogen in an amount equivalent to about 5 to about 20 meg of ethinyl estradiol, or (ii) a placebo or a non-steroidal component, or (iii) a combination of (i) and (ii), for about 2 to about 8 days. The ethinyl estradiol equivalent amount of estrogen in each of the successive Phases II and III is at least 5 meg greater than the ethinyl estradiol equivalent amount of estrogen in the immediately-preceding phase.
PCT/US2007/003508 2006-03-02 2007-02-09 Extended cycle multiphasic oral contraceptive method Ceased WO2007106264A2 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
MX2008011074A MX2008011074A (en) 2006-03-02 2007-02-09 Extended cycle multiphasic oral contraceptive method.
CA2640520A CA2640520C (en) 2006-03-02 2007-02-09 Extended cycle multiphasic oral contraceptive method
EP07750352.2A EP1993531B1 (en) 2006-03-02 2007-02-09 Extended cycle multiphasic oral contraceptive method
ES07750352.2T ES2558030T3 (en) 2006-03-02 2007-02-09 Long-cycle multiphase oral contraceptive method
IL193013A IL193013A (en) 2006-03-02 2008-07-24 Multiphasic method of contraception and kit associated therewith

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US77806706P 2006-03-02 2006-03-02
US60/778,067 2006-03-02
US79265306P 2006-04-18 2006-04-18
US60/792,653 2006-04-18

Publications (2)

Publication Number Publication Date
WO2007106264A2 WO2007106264A2 (en) 2007-09-20
WO2007106264A3 true WO2007106264A3 (en) 2008-05-02

Family

ID=38229300

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2007/003508 Ceased WO2007106264A2 (en) 2006-03-02 2007-02-09 Extended cycle multiphasic oral contraceptive method

Country Status (8)

Country Link
US (1) US8063030B2 (en)
EP (1) EP1993531B1 (en)
CA (1) CA2640520C (en)
ES (1) ES2558030T3 (en)
IL (1) IL193013A (en)
MX (1) MX2008011074A (en)
SG (1) SG172654A1 (en)
WO (1) WO2007106264A2 (en)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE602004017045D1 (en) * 2003-11-14 2008-11-20 Warner Chilcott Co Inc GRADUATED ESTROGEN CONTRAZEPTIVA
US20070111975A1 (en) * 2004-10-07 2007-05-17 Duramed Pharmaceuticals, Inc. Methods of Hormonal Treatment Utilizing Ascending-Dose Extended Cycle Regimens
EP2383279A1 (en) 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
US8633178B2 (en) 2011-11-23 2014-01-21 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US9301920B2 (en) 2012-06-18 2016-04-05 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
DE202012012822U1 (en) 2011-12-13 2014-02-03 Arstat, Inc. Contraception set for consecutive daily use
US10806740B2 (en) 2012-06-18 2020-10-20 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US20130338122A1 (en) 2012-06-18 2013-12-19 Therapeuticsmd, Inc. Transdermal hormone replacement therapies
US20150196640A1 (en) 2012-06-18 2015-07-16 Therapeuticsmd, Inc. Progesterone formulations having a desirable pk profile
US10806697B2 (en) 2012-12-21 2020-10-20 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10537581B2 (en) 2012-12-21 2020-01-21 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US11266661B2 (en) 2012-12-21 2022-03-08 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US9180091B2 (en) 2012-12-21 2015-11-10 Therapeuticsmd, Inc. Soluble estradiol capsule for vaginal insertion
US10471072B2 (en) 2012-12-21 2019-11-12 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US11246875B2 (en) 2012-12-21 2022-02-15 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10568891B2 (en) 2012-12-21 2020-02-25 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
EP3145489A1 (en) 2014-05-22 2017-03-29 TherapeuticsMD, Inc. Natural combination hormone replacement formulations and therapies
CR20180042A (en) 2015-06-18 2018-05-03 Mithra Pharmaceuticals S A ORODISPERSABLE DOSAGE UNIT CONTAINING A STETROL COMPONENT.
LT3310345T (en) 2015-06-18 2021-06-25 Estetra Sprl ORAL DISPERSIBLE TABLET CONTAINING ESTETROL
LT3310346T (en) 2015-06-18 2021-06-10 Estetra Sprl Orodispersible tablet containing estetrol
DK3701944T3 (en) 2015-06-18 2022-03-14 Estetra Srl ORO-DISPERGABLE DOSAGE UNIT CONTAINING AN ESTETROL COMPONENT
US10328087B2 (en) 2015-07-23 2019-06-25 Therapeuticsmd, Inc. Formulations for solubilizing hormones
WO2017173044A1 (en) 2016-04-01 2017-10-05 Therapeuticsmd Inc. Steroid hormone compositions in medium chain oils
WO2017173071A1 (en) 2016-04-01 2017-10-05 Therapeuticsmd, Inc. Steroid hormone pharmaceutical composition
KR102712911B1 (en) 2016-08-05 2024-10-04 에스테트라, 소시에떼 아 레스폰서빌리떼 리미떼 Method for the management of dysmenorrhea and menstrual pain
TWI801561B (en) 2018-04-19 2023-05-11 比利時商依思特拉私人有限責任公司 Compounds and their uses for alleviating menopause-associated symptoms
CN111989105B (en) 2018-04-19 2024-07-19 埃斯特拉私人有限责任公司 Compounds and their use in relieving menopausal-related symptoms
US11633405B2 (en) 2020-02-07 2023-04-25 Therapeuticsmd, Inc. Steroid hormone pharmaceutical formulations
TWI893101B (en) 2020-04-16 2025-08-11 比利時商埃斯特拉有限責任公司 Contraceptive compositions with reduced adverse effects

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4962098A (en) * 1987-06-15 1990-10-09 Warner-Lambert Company Graduated estrogen contraceptive
DE4313926A1 (en) * 1993-04-28 1994-11-03 Jenapharm Gmbh Multiphase pharmaceutical product for hormonal contraception
EP0770388A1 (en) * 1995-10-28 1997-05-02 JENAPHARM GmbH Multiphase contraceptive preparation based on natural estrogens
WO1998004268A1 (en) * 1996-07-26 1998-02-05 American Home Products Corporation Oral contraceptive
WO2005049142A2 (en) * 2003-11-14 2005-06-02 Warner Chilcott Company, Inc. Graduated estrogen contraceptive
WO2005092441A2 (en) * 2004-03-19 2005-10-06 Warner Chilcott Company, Inc. Extended cycle multiphasic oral contraceptive method
WO2005102247A2 (en) * 2004-04-20 2005-11-03 Schering Ag Multi-phase contraceptive preparation based on a natural estrogen
WO2007002910A1 (en) * 2005-06-29 2007-01-04 Warner Chilcott Company, Inc. Quadraphasic continuous graduated estrogen contraceptive

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US5010070A (en) * 1987-06-15 1991-04-23 Warner-Lambert Company Graduated estrogen contraceptive
DE4411585A1 (en) * 1994-03-30 1995-10-05 Schering Ag Combined pharmaceutical preparation for hormonal contraception
DE19525017A1 (en) 1995-06-28 1997-01-02 Schering Ag Pharmaceutical combination preparation, kit and method for hormonal contraception
DE19531936A1 (en) 1995-08-17 1997-02-20 Schering Ag Combination preparation for contraception, containing kits and a method using them
US5898032A (en) 1997-06-23 1999-04-27 Medical College Of Hampton Roads Ultra low dose oral contraceptives with less menstrual bleeding and sustained efficacy
US6251956B1 (en) 1998-08-20 2001-06-26 Ortho Pharmaceutical Corporation Combination progestin oral contraceptive regimen
DE19739916C2 (en) 1997-09-11 2001-09-13 Hesch Rolf Dieter Use of a combination of a progestogen and an estrogen for the continuous inhibition of ovulation and possibly simultaneous treatment and / or prophylaxis of tumors of the mammary glands
US20040202713A1 (en) 2001-05-23 2004-10-14 Van Beek Agatha Antonia Magdalena Means and method for hormonal contraception
CN100581550C (en) 2001-12-05 2010-01-20 杜拉美德药物有限公司 Oral contraceptive for preventing pregnancy and reducing premenstrual symptoms
AU2003213842A1 (en) 2002-03-11 2003-09-29 Janssen Pharmaceutica N.V. Sulfatase inhibiting continuous progestogen contraceptive regimens
US20040142914A1 (en) 2002-03-11 2004-07-22 Friedman Andrew Joseph Extended transdermal contraceptive regimens
US20030219471A1 (en) 2002-03-11 2003-11-27 Caubel Patrick Michel Extended cycle estrogen and sulfatase inhibiting progestogen contraceptive regimens
EP1624848A4 (en) 2003-05-02 2009-02-25 Duramed Pharmaceuticals Inc Methods of hormornal treatment utilizing extended cycle contraceptive regimens
CN101001631B (en) 2003-07-16 2014-08-06 特卫华妇女健康有限公司 Hormone therapy using a contraceptive regimen with continuous administration of estrogen
WO2005032558A1 (en) 2003-10-01 2005-04-14 Janssen Pharmaceutica N.V. Extended triphasic contraceptive regimens
US20050113350A1 (en) * 2003-11-26 2005-05-26 Bernd Duesterberg Extended use combination comprising estrogens and progestins
CA2564365A1 (en) * 2004-05-14 2005-12-01 Irm Llc Compounds and compositions as ppar modulators

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4962098A (en) * 1987-06-15 1990-10-09 Warner-Lambert Company Graduated estrogen contraceptive
DE4313926A1 (en) * 1993-04-28 1994-11-03 Jenapharm Gmbh Multiphase pharmaceutical product for hormonal contraception
EP0770388A1 (en) * 1995-10-28 1997-05-02 JENAPHARM GmbH Multiphase contraceptive preparation based on natural estrogens
WO1998004268A1 (en) * 1996-07-26 1998-02-05 American Home Products Corporation Oral contraceptive
WO2005049142A2 (en) * 2003-11-14 2005-06-02 Warner Chilcott Company, Inc. Graduated estrogen contraceptive
WO2005092441A2 (en) * 2004-03-19 2005-10-06 Warner Chilcott Company, Inc. Extended cycle multiphasic oral contraceptive method
WO2005102247A2 (en) * 2004-04-20 2005-11-03 Schering Ag Multi-phase contraceptive preparation based on a natural estrogen
WO2007002910A1 (en) * 2005-06-29 2007-01-04 Warner Chilcott Company, Inc. Quadraphasic continuous graduated estrogen contraceptive

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
EDWARDS L A: "An update on oral contraceptive options", FORMULARY, ADVANSTAR COMMUNICATIONS, CLEVELAND, OH, US, vol. 39, no. 2, February 2004 (2004-02-01), pages 104 - 121, XP008065761, ISSN: 1082-801X *

Also Published As

Publication number Publication date
MX2008011074A (en) 2008-09-10
EP1993531A2 (en) 2008-11-26
IL193013A (en) 2011-11-30
IL193013A0 (en) 2009-08-03
EP1993531B1 (en) 2015-10-14
ES2558030T3 (en) 2016-02-01
WO2007106264A2 (en) 2007-09-20
US8063030B2 (en) 2011-11-22
CA2640520C (en) 2014-04-22
US20070207945A1 (en) 2007-09-06
SG172654A1 (en) 2011-07-28
CA2640520A1 (en) 2007-09-20

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