JP2015527411A5 - - Google Patents
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- JP2015527411A5 JP2015527411A5 JP2015531335A JP2015531335A JP2015527411A5 JP 2015527411 A5 JP2015527411 A5 JP 2015527411A5 JP 2015531335 A JP2015531335 A JP 2015531335A JP 2015531335 A JP2015531335 A JP 2015531335A JP 2015527411 A5 JP2015527411 A5 JP 2015527411A5
- Authority
- JP
- Japan
- Prior art keywords
- polymer
- enzalutamide
- weight
- pharmaceutical composition
- solid dispersion
- 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.)
- Granted
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- 229920000642 polymer Polymers 0.000 claims 14
- 229960004671 enzalutamide Drugs 0.000 claims 12
- WXCXUHSOUPDCQV-UHFFFAOYSA-N enzalutamide Chemical compound C1=C(F)C(C(=O)NC)=CC=C1N1C(C)(C)C(=O)N(C=2C=C(C(C#N)=CC=2)C(F)(F)F)C1=S WXCXUHSOUPDCQV-UHFFFAOYSA-N 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 239000007962 solid dispersion Substances 0.000 claims 7
- 239000000203 mixture Substances 0.000 claims 5
- 206010060862 Prostate cancer Diseases 0.000 claims 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 230000003463 hyperproliferative effect Effects 0.000 claims 3
- 229920002307 Dextran Polymers 0.000 claims 2
- 229920002678 cellulose Polymers 0.000 claims 2
- 239000001913 cellulose Substances 0.000 claims 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 2
- 238000002156 mixing Methods 0.000 claims 2
- -1 polyoxyethylene Polymers 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- ARCGXLSVLAOJQL-UHFFFAOYSA-N trimellitic acid Chemical compound OC(=O)C1=CC=C(C(O)=O)C(C(O)=O)=C1 ARCGXLSVLAOJQL-UHFFFAOYSA-N 0.000 claims 2
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims 1
- XBBVURRQGJPTHH-UHFFFAOYSA-N 2-hydroxyacetic acid;2-hydroxypropanoic acid Chemical compound OCC(O)=O.CC(O)C(O)=O XBBVURRQGJPTHH-UHFFFAOYSA-N 0.000 claims 1
- SQDAZGGFXASXDW-UHFFFAOYSA-N 5-bromo-2-(trifluoromethoxy)pyridine Chemical compound FC(F)(F)OC1=CC=C(Br)C=N1 SQDAZGGFXASXDW-UHFFFAOYSA-N 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 229920000623 Cellulose acetate phthalate Polymers 0.000 claims 1
- 229920001287 Chondroitin sulfate Polymers 0.000 claims 1
- 239000001856 Ethyl cellulose Substances 0.000 claims 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 claims 1
- 229920000855 Fucoidan Polymers 0.000 claims 1
- HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 claims 1
- 206010062904 Hormone-refractory prostate cancer Diseases 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- 229920002774 Maltodextrin Polymers 0.000 claims 1
- 239000005913 Maltodextrin Substances 0.000 claims 1
- 229920002292 Nylon 6 Polymers 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 229920000954 Polyglycolide Polymers 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 229920001218 Pullulan Polymers 0.000 claims 1
- 239000004373 Pullulan Substances 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 150000005215 alkyl ethers Chemical class 0.000 claims 1
- 239000004359 castor oil Substances 0.000 claims 1
- 235000019438 castor oil Nutrition 0.000 claims 1
- 229920002301 cellulose acetate Polymers 0.000 claims 1
- 229920006217 cellulose acetate butyrate Polymers 0.000 claims 1
- 229940081734 cellulose acetate phthalate Drugs 0.000 claims 1
- 229920001727 cellulose butyrate Polymers 0.000 claims 1
- 229940059329 chondroitin sulfate Drugs 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 229960002086 dextran Drugs 0.000 claims 1
- 229920001249 ethyl cellulose Polymers 0.000 claims 1
- 235000019325 ethyl cellulose Nutrition 0.000 claims 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims 1
- 239000008187 granular material Substances 0.000 claims 1
- 229920000669 heparin Polymers 0.000 claims 1
- 229960002897 heparin Drugs 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 229920002674 hyaluronan Polymers 0.000 claims 1
- 229960003160 hyaluronic acid Drugs 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 229920000639 hydroxypropylmethylcellulose acetate succinate Polymers 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 229940035034 maltodextrin Drugs 0.000 claims 1
- 229940043138 pentosan polysulfate Drugs 0.000 claims 1
- 229920000747 poly(lactic acid) Polymers 0.000 claims 1
- 229940074982 poly(vinylpyrrolidone-co-vinyl-acetate) Drugs 0.000 claims 1
- 239000004633 polyglycolic acid Substances 0.000 claims 1
- 239000004626 polylactic acid Substances 0.000 claims 1
- 229920000193 polymethacrylate Polymers 0.000 claims 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- 235000019423 pullulan Nutrition 0.000 claims 1
- 238000001694 spray drying Methods 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261699351P | 2012-09-11 | 2012-09-11 | |
| US61/699,351 | 2012-09-11 | ||
| PCT/US2013/059223 WO2014043208A1 (en) | 2012-09-11 | 2013-09-11 | Formulations of enzalutamide |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016176557A Division JP2016204392A (ja) | 2012-09-11 | 2016-09-09 | エンザルタミドの製剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015527411A JP2015527411A (ja) | 2015-09-17 |
| JP2015527411A5 true JP2015527411A5 (enExample) | 2016-11-04 |
| JP6404217B2 JP6404217B2 (ja) | 2018-10-10 |
Family
ID=49231627
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015531335A Active JP6404217B2 (ja) | 2012-09-11 | 2013-09-11 | エンザルタミドの製剤 |
| JP2016176557A Pending JP2016204392A (ja) | 2012-09-11 | 2016-09-09 | エンザルタミドの製剤 |
| JP2018011759A Pending JP2018087206A (ja) | 2012-09-11 | 2018-01-26 | エンザルタミドの製剤 |
| JP2019146714A Active JP6932746B2 (ja) | 2012-09-11 | 2019-08-08 | エンザルタミドの製剤 |
| JP2021132868A Pending JP2021178871A (ja) | 2012-09-11 | 2021-08-17 | エンザルタミドの製剤 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016176557A Pending JP2016204392A (ja) | 2012-09-11 | 2016-09-09 | エンザルタミドの製剤 |
| JP2018011759A Pending JP2018087206A (ja) | 2012-09-11 | 2018-01-26 | エンザルタミドの製剤 |
| JP2019146714A Active JP6932746B2 (ja) | 2012-09-11 | 2019-08-08 | エンザルタミドの製剤 |
| JP2021132868A Pending JP2021178871A (ja) | 2012-09-11 | 2021-08-17 | エンザルタミドの製剤 |
Country Status (29)
| Country | Link |
|---|---|
| US (10) | US20140179749A1 (enExample) |
| EP (6) | EP4450130A3 (enExample) |
| JP (5) | JP6404217B2 (enExample) |
| KR (1) | KR102225416B1 (enExample) |
| CN (2) | CN105358535B (enExample) |
| AU (2) | AU2013315619B2 (enExample) |
| BR (1) | BR112015005432B1 (enExample) |
| CA (1) | CA2884795C (enExample) |
| CY (1) | CY1124729T1 (enExample) |
| DK (1) | DK3725778T3 (enExample) |
| EA (2) | EA201991484A1 (enExample) |
| ES (1) | ES2892029T3 (enExample) |
| HK (1) | HK1212701A1 (enExample) |
| HR (1) | HRP20211423T1 (enExample) |
| HU (1) | HUE057701T2 (enExample) |
| IL (1) | IL237604B (enExample) |
| IN (1) | IN2015DN02875A (enExample) |
| LT (1) | LT3725778T (enExample) |
| MX (3) | MX363974B (enExample) |
| PH (1) | PH12015500525A1 (enExample) |
| PL (1) | PL3725778T3 (enExample) |
| PT (1) | PT3725778T (enExample) |
| RS (1) | RS62676B1 (enExample) |
| SI (1) | SI3725778T1 (enExample) |
| SM (1) | SMT202100550T1 (enExample) |
| TW (1) | TWI673051B (enExample) |
| UA (1) | UA117353C2 (enExample) |
| WO (1) | WO2014043208A1 (enExample) |
| ZA (1) | ZA201501847B (enExample) |
Families Citing this family (73)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2014043208A1 (en) | 2012-09-11 | 2014-03-20 | Medivation Prostate Therapeutics, Inc. | Formulations of enzalutamide |
| PT3305285T (pt) | 2012-09-26 | 2020-11-24 | Aragon Pharmaceuticals Inc | Antiandrogénios para o tratamento de cancro da próstata resistente à castração não metastático |
| BR112015026257B1 (pt) * | 2013-04-17 | 2022-12-20 | Signal Pharmaceuticals, Llc | Uso de um composto dihidropirazino-pirazina e enzalutamida, composição farmacêutica que os compreende, e kit |
| MX386859B (es) * | 2014-02-05 | 2025-03-19 | Lek Pharmaceuticals | Composiciones farmacéuticas sólidas de antagonistas de los receptores de andrógenos. |
| CN104356068A (zh) * | 2014-10-30 | 2015-02-18 | 杭州新博思生物医药有限公司 | 恩杂鲁胺新晶型及其制备方法 |
| BR112017011788A2 (pt) | 2014-12-05 | 2017-12-26 | Aragon Pharmaceuticals Inc | composições anticâncer |
| CA2969675C (en) | 2014-12-05 | 2023-06-06 | Aragon Pharmaceuticals, Inc. | Anticancer compositions |
| CR20170217A (es) * | 2014-12-05 | 2017-08-30 | Aragon Pharmaceuticals Inc | Composiciones anticancerígenas |
| CN104546714A (zh) * | 2015-02-11 | 2015-04-29 | 江苏慧博生物科技有限公司 | 一种恩杂鲁胺胶束制剂及其制备方法 |
| CA2976360A1 (en) * | 2015-02-11 | 2016-08-18 | Aptevo Research And Development Llc | Compositions and methods for combination therapy with prostate-specific membrane antigen binding proteins |
| CN104857517B (zh) * | 2015-05-14 | 2018-04-27 | 南京海纳医药科技股份有限公司 | 一种恩杂鲁胺软胶囊及其制备方法 |
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| EP3500310A1 (en) | 2016-08-20 | 2019-06-26 | FTF Pharma Private Limited | Pharmaceutical composition comprising an androgen receptor inhibitor |
| BR112019021324A2 (pt) * | 2017-04-13 | 2020-06-16 | Paul Remon Jean | Composições baseadas em xanthohumol |
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| WO2019016747A1 (en) * | 2017-07-20 | 2019-01-24 | Dr. Reddy's Laboratories Limited | AMORPHOUS SOLID DISPERSIONS OF APALUTAMIDE AND PROCESS FOR THEIR PREPARATION |
| WO2019030691A1 (en) * | 2017-08-08 | 2019-02-14 | Dr. Reddy’S Laboratories Limited | EXTRUDED COMPOSITIONS OF ENZALUTAMIDE |
| EP4438126A3 (en) | 2017-10-16 | 2025-01-01 | Aragon Pharmaceuticals, Inc. | Anti-androgens for the treatment of non-metastatic castration-resistant prostate cancer |
| US20200397756A1 (en) * | 2018-02-09 | 2020-12-24 | Kashiv Biosciences, Llc | A stable pharmaceutical composition of poorly soluble nonsteroidal antiandrogens |
| JP7244536B2 (ja) * | 2018-04-06 | 2023-03-22 | キャプシュゲル・ベルジウム・エヌ・ヴィ | メタクリル酸メチル－メタクリル酸コポリマーからなる低アスペクト比の粒子のための噴霧乾燥方法 |
| CZ2018234A3 (cs) | 2018-05-21 | 2019-12-04 | Zentiva Ks | Zvýšení rozpustnosti a biodostupnosti enzalutamidu |
| US12358870B2 (en) | 2018-10-30 | 2025-07-15 | Peloton Therapeutics, Inc. | Solid dispersions and pharmaceutical compositions comprising a substituted indane and methods for the preparation and use thereof |
| EA202191372A1 (ru) * | 2018-12-14 | 2021-09-16 | Фуджифилм Корпорэйшн | Таблетка и способ получения таблетки |
| CN109432016B (zh) * | 2018-12-26 | 2021-03-02 | 广州中医药大学(广州中医药研究院) | 一种恩杂鲁胺的三元固体制剂及其制备方法 |
| WO2020144646A1 (en) | 2019-01-10 | 2020-07-16 | Aragon Pharmaceuticals, Inc. | Apalutamide dispersed in applesauce for treating prostate cancer |
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| BR112021014657A2 (pt) | 2019-01-30 | 2021-09-21 | Janssen Pharmaceutica N.V. | Métodos para tratar câncer de próstata com base em subtipos moleculares |
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