CA2966753A1 - Onapristone extended-release compositions and methods - Google Patents
Onapristone extended-release compositions and methods Download PDFInfo
- Publication number
- CA2966753A1 CA2966753A1 CA2966753A CA2966753A CA2966753A1 CA 2966753 A1 CA2966753 A1 CA 2966753A1 CA 2966753 A CA2966753 A CA 2966753A CA 2966753 A CA2966753 A CA 2966753A CA 2966753 A1 CA2966753 A1 CA 2966753A1
- Authority
- CA
- Canada
- Prior art keywords
- onapristone
- extended release
- pharmaceutical composition
- per day
- extended
- 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.)
- Pending
Links
- IEXUMDBQLIVNHZ-YOUGDJEHSA-N (8s,11r,13r,14s,17s)-11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(3-hydroxypropyl)-13-methyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one Chemical compound C1=CC(N(C)C)=CC=C1[C@@H]1C2=C3CCC(=O)C=C3CC[C@H]2[C@H](CC[C@]2(O)CCCO)[C@@]2(C)C1 IEXUMDBQLIVNHZ-YOUGDJEHSA-N 0.000 title claims abstract description 172
- 229950011093 onapristone Drugs 0.000 title claims abstract description 172
- 239000000203 mixture Substances 0.000 title claims abstract description 84
- 238000013265 extended release Methods 0.000 title claims abstract description 53
- 238000000034 method Methods 0.000 title claims abstract description 25
- 238000009472 formulation Methods 0.000 claims abstract description 73
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 30
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 8
- 239000002775 capsule Substances 0.000 claims abstract description 4
- 239000002552 dosage form Substances 0.000 claims abstract description 4
- 102000003998 progesterone receptors Human genes 0.000 claims description 33
- 108090000468 progesterone receptors Proteins 0.000 claims description 33
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- 239000012729 immediate-release (IR) formulation Substances 0.000 abstract description 26
- 239000004480 active ingredient Substances 0.000 abstract description 10
- 230000000694 effects Effects 0.000 abstract description 5
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- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 description 4
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- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
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- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 3
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- 239000003433 contraceptive agent Substances 0.000 description 2
- 230000002254 contraceptive effect Effects 0.000 description 2
- DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 0.000 description 2
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- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
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- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 239000000044 progesterone antagonist Substances 0.000 description 2
- 239000000583 progesterone congener Substances 0.000 description 2
- 208000037821 progressive disease Diseases 0.000 description 2
- 150000003431 steroids Chemical class 0.000 description 2
- 230000001629 suppression Effects 0.000 description 2
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- 239000001856 Ethyl cellulose Substances 0.000 description 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 1
- -1 Hydroxypropyl Chemical group 0.000 description 1
- 102000009151 Luteinizing Hormone Human genes 0.000 description 1
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- 206010027452 Metastases to bone Diseases 0.000 description 1
- 206010059282 Metastases to central nervous system Diseases 0.000 description 1
- 206010027457 Metastases to liver Diseases 0.000 description 1
- 108020005497 Nuclear hormone receptor Proteins 0.000 description 1
- 206010033128 Ovarian cancer Diseases 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- XUIMIQQOPSSXEZ-UHFFFAOYSA-N Silicon Chemical compound [Si] XUIMIQQOPSSXEZ-UHFFFAOYSA-N 0.000 description 1
- 102220497176 Small vasohibin-binding protein_T47D_mutation Human genes 0.000 description 1
- 238000008050 Total Bilirubin Reagent Methods 0.000 description 1
- 238000010811 Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry Methods 0.000 description 1
- 208000002495 Uterine Neoplasms Diseases 0.000 description 1
- 206010046798 Uterine leiomyoma Diseases 0.000 description 1
- 239000012190 activator Substances 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 229940041181 antineoplastic drug Drugs 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
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- 229940075614 colloidal silicon dioxide Drugs 0.000 description 1
- 238000010276 construction Methods 0.000 description 1
- 229940109239 creatinine Drugs 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
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- 238000011161 development Methods 0.000 description 1
- 238000002405 diagnostic procedure Methods 0.000 description 1
- 230000000447 dimerizing effect Effects 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 238000009261 endocrine therapy Methods 0.000 description 1
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- 230000014509 gene expression Effects 0.000 description 1
- 238000011223 gene expression profiling Methods 0.000 description 1
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- 238000002657 hormone replacement therapy Methods 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 208000019016 inability to swallow Diseases 0.000 description 1
- 239000000411 inducer Substances 0.000 description 1
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- 239000003112 inhibitor Substances 0.000 description 1
- 230000003907 kidney function Effects 0.000 description 1
- 201000010260 leiomyoma Diseases 0.000 description 1
- 230000003908 liver function Effects 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 229940040129 luteinizing hormone Drugs 0.000 description 1
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- 239000013563 matrix tablet Substances 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
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- 102000006255 nuclear receptors Human genes 0.000 description 1
- 108020004017 nuclear receptors Proteins 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 230000001766 physiological effect Effects 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920000193 polymethacrylate Polymers 0.000 description 1
- 101150038105 pr gene Proteins 0.000 description 1
- 239000000186 progesterone Substances 0.000 description 1
- 229960003387 progesterone Drugs 0.000 description 1
- 239000002379 progesterone receptor modulator Substances 0.000 description 1
- 150000003146 progesterones Chemical class 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
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- 229940095745 sex hormone and modulator of the genital system progesterone receptor modulator Drugs 0.000 description 1
- 229910052710 silicon Inorganic materials 0.000 description 1
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- 230000004083 survival effect Effects 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
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- 238000004885 tandem mass spectrometry Methods 0.000 description 1
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- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- 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
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462080868P | 2014-11-17 | 2014-11-17 | |
| US62/080,868 | 2014-11-17 | ||
| PCT/US2015/060940 WO2016081383A1 (en) | 2014-11-17 | 2015-11-16 | Onapristone extended-release compositions and methods |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2966753A1 true CA2966753A1 (en) | 2016-05-26 |
Family
ID=56014429
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2966753A Pending CA2966753A1 (en) | 2014-11-17 | 2015-11-16 | Onapristone extended-release compositions and methods |
Country Status (11)
| Country | Link |
|---|---|
| US (3) | US10786461B2 (enExample) |
| EP (1) | EP3247362A4 (enExample) |
| JP (1) | JP6655075B2 (enExample) |
| KR (1) | KR20170084086A (enExample) |
| CN (2) | CN113559075A (enExample) |
| AU (2) | AU2015350241B2 (enExample) |
| CA (1) | CA2966753A1 (enExample) |
| HK (1) | HK1246653A1 (enExample) |
| MX (1) | MX391191B (enExample) |
| RU (1) | RU2017112748A (enExample) |
| WO (1) | WO2016081383A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX391191B (es) | 2014-11-17 | 2025-03-21 | Context Biopharma Inc | Composiciones de liberación extendida de onapristona y métodos. |
| CA2998924A1 (en) | 2015-09-25 | 2017-03-30 | Context Biopharma Inc. | Methods of making onapristone intermediates |
| US10548905B2 (en) | 2015-12-15 | 2020-02-04 | Context Biopharma Inc. | Amorphous onapristone compositions and methods of making the same |
| US20180148471A1 (en) | 2016-11-30 | 2018-05-31 | Arno Therapeutics, Inc. | Methods for onapristone synthesis dehydration and deprotection |
Family Cites Families (80)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4780461A (en) | 1983-06-15 | 1988-10-25 | Schering Aktiengesellschaft | 13α-alkyl-gonanes, their production, and pharmaceutical preparations containing same |
| ES533260A0 (es) | 1983-06-15 | 1985-02-01 | Schering Ag | Procedimiento para la preparacion de 13a-alquilgonanos |
| DE3321826A1 (de) | 1983-06-15 | 1984-12-20 | Schering AG, 1000 Berlin und 4709 Bergkamen | 13(alpha)-alkylgonane, deren herstellung und diese enthaltende pharmazeutische praeparate |
| US4742000A (en) | 1986-05-02 | 1988-05-03 | University Of Chicago | Antibody to human progesterone receptor and diagnostic materials and methods |
| DE3630030A1 (de) | 1986-09-01 | 1988-03-03 | Schering Ag | 13(alpha)-alkylgonan-(delta)(pfeil hoch)9(pfeil hoch)(pfeil hoch)((pfeil hoch)(pfeil hoch)1(pfeil hoch)1(pfeil hoch))(pfeil hoch)-5,10-epoxide |
| US4774236A (en) | 1986-09-17 | 1988-09-27 | Research Triangle Institute | 17α-(substituted-methyl)-17β-hydroxy/esterified hydroxy steroids and pharmaceutical compositions containing them |
| IE60780B1 (en) | 1987-01-23 | 1994-08-10 | Akzo Nv | New 11-aryl steroid derivatives |
| DE3822770A1 (de) | 1988-07-01 | 1990-01-04 | Schering Ag | 13-alkyl-11ss-phenylgonane |
| US5283190A (en) | 1989-07-31 | 1994-02-01 | Traish Adbulmaged M | Specific monoclonal antibodies against a defined epitope of progesterone receptor and methods for their use |
| DE4008584A1 (de) | 1990-03-15 | 1991-09-26 | Schering Ag | Verfahren zur herstellung von zwischenprodukten fuer die antigestagensynthese (onapristonsynthese) |
| US5141961A (en) | 1991-06-27 | 1992-08-25 | Richrdson-Vicks Inc. | Process for solubilizing difficulty soluble pharmaceutical actives |
| MX9301121A (es) | 1992-03-02 | 1993-09-01 | Schering Ag | Metodo y equipo para la contracepcion oral y regulacion de la menstruacion con estrogeno/progestina/aniprogestina. |
| CN1053450C (zh) | 1992-11-19 | 2000-06-14 | 北京第三制药厂 | 17位取代11β－取代芳香基－4,9－雌甾二烯类化合物的全合成法 |
| DE4332283A1 (de) | 1993-09-20 | 1995-04-13 | Jenapharm Gmbh | Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| HU226566B1 (en) | 1994-10-24 | 2009-04-28 | Schering Ag | Use of competitive progesterone antagonists for producing pharmaceutical compositions for regulating female fertility as required |
| US5759577A (en) | 1995-01-17 | 1998-06-02 | American Home Products Corporation | Controlled release of steroids from sugar coatings |
| US6900193B1 (en) | 1996-05-01 | 2005-05-31 | The United States Of America As Represented By The Department Of Health And Human Services | Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents |
| IL122740A (en) | 1997-01-15 | 2003-09-17 | Akzo Nobel Nv | 16-hydroxy-11-(substituted phenyl)-estra-9,4-diene derivatives, their preparation and pharmaceutical compositions containing them |
| US5962444A (en) | 1998-05-29 | 1999-10-05 | Research Triangle Institute | 17β-nitro-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties |
| US6537584B1 (en) | 1999-11-12 | 2003-03-25 | Macromed, Inc. | Polymer blends that swell in an acidic environment and deswell in a basic environment |
| NZ522444A (en) | 2000-05-19 | 2004-09-24 | Genentech Inc | Gene detection assay for improving the likelihood of an effective response to an ErbB antagonist cancer therapy |
| US6750015B2 (en) | 2000-06-28 | 2004-06-15 | Kathryn B. Horwitz | Progesterone receptor-regulated gene expression and methods related thereto |
| UY26966A1 (es) | 2000-10-18 | 2002-06-20 | Schering Ag | Uso de antiprogestinas para la inducción de apoptosis en una célula |
| US7381976B2 (en) | 2001-03-13 | 2008-06-03 | Triton Thalassic Technologies, Inc. | Monochromatic fluid treatment systems |
| AUPR546801A0 (en) | 2001-06-05 | 2001-06-28 | Commonwealth Scientific And Industrial Research Organisation | Recombinant antibodies |
| US7105642B2 (en) | 2001-08-03 | 2006-09-12 | Cell Signalling Technology, Inc. | Monoclonal antibodies specific for phosphorylated estrogen receptor alpha (Ser118) and uses thereof |
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2015
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- 2015-11-16 AU AU2015350241A patent/AU2015350241B2/en not_active Ceased
- 2015-11-16 HK HK18106169.2A patent/HK1246653A1/zh unknown
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| AU2015350241B2 (en) | 2021-05-20 |
| US20230157960A1 (en) | 2023-05-25 |
| CN106999501A (zh) | 2017-08-01 |
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| US20210220279A1 (en) | 2021-07-22 |
| CN106999501B (zh) | 2021-08-13 |
| RU2017112748A (ru) | 2018-12-19 |
| AU2021218093A1 (en) | 2021-09-09 |
| WO2016081383A1 (en) | 2016-05-26 |
| AU2015350241A1 (en) | 2017-05-04 |
| EP3247362A4 (en) | 2018-10-10 |
| JP2017537883A (ja) | 2017-12-21 |
| RU2017112748A3 (enExample) | 2019-06-26 |
| US11672762B2 (en) | 2023-06-13 |
| JP6655075B2 (ja) | 2020-02-26 |
| US10786461B2 (en) | 2020-09-29 |
| KR20170084086A (ko) | 2017-07-19 |
| HK1246653A1 (zh) | 2018-09-14 |
| MX2017005163A (es) | 2018-01-18 |
| MX391191B (es) | 2025-03-21 |
| CN113559075A (zh) | 2021-10-29 |
| US20160166583A1 (en) | 2016-06-16 |
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