JP2012522055A5 - - Google Patents
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- JP2012522055A5 JP2012522055A5 JP2012503526A JP2012503526A JP2012522055A5 JP 2012522055 A5 JP2012522055 A5 JP 2012522055A5 JP 2012503526 A JP2012503526 A JP 2012503526A JP 2012503526 A JP2012503526 A JP 2012503526A JP 2012522055 A5 JP2012522055 A5 JP 2012522055A5
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- 239000002245 particle Substances 0.000 claims description 329
- 229920001600 hydrophobic polymer Polymers 0.000 claims description 221
- 239000003814 drug Substances 0.000 claims description 189
- 229940079593 drug Drugs 0.000 claims description 169
- 229960003668 docetaxel Drugs 0.000 claims description 111
- 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 claims description 104
- 229920000642 polymer Polymers 0.000 claims description 97
- 230000002209 hydrophobic effect Effects 0.000 claims description 93
- 239000000562 conjugate Substances 0.000 claims description 83
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims description 76
- 239000003795 chemical substances by application Substances 0.000 claims description 46
- 239000000580 polymer-drug conjugate Substances 0.000 claims description 46
- 239000000178 monomer Substances 0.000 claims description 37
- 239000000203 mixture Substances 0.000 claims description 35
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 34
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims description 24
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims description 22
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 22
- 239000004615 ingredient Substances 0.000 claims description 21
- 239000004094 surface-active agent Substances 0.000 claims description 20
- 229940124597 therapeutic agent Drugs 0.000 claims description 17
- 229920001519 homopolymer Polymers 0.000 claims description 15
- 239000000243 solution Substances 0.000 claims description 14
- 229940123237 Taxane Drugs 0.000 claims description 13
- 239000002246 antineoplastic agent Substances 0.000 claims description 13
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 claims description 13
- 125000002252 acyl group Chemical group 0.000 claims description 12
- 229910052697 platinum Inorganic materials 0.000 claims description 12
- 235000014655 lactic acid Nutrition 0.000 claims description 11
- 239000004310 lactic acid Substances 0.000 claims description 11
- 229940045799 anthracyclines and related substance Drugs 0.000 claims description 7
- 239000007864 aqueous solution Substances 0.000 claims description 7
- 238000004519 manufacturing process Methods 0.000 claims description 7
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims description 6
- 229940041181 antineoplastic drug Drugs 0.000 claims description 6
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 5
- 239000002577 cryoprotective agent Substances 0.000 claims description 4
- 229930012538 Paclitaxel Natural products 0.000 claims description 3
- 229940122803 Vinca alkaloid Drugs 0.000 claims description 3
- 239000004037 angiogenesis inhibitor Substances 0.000 claims description 3
- 230000002491 angiogenic effect Effects 0.000 claims description 3
- 239000002256 antimetabolite Substances 0.000 claims description 3
- 229960001573 cabazitaxel Drugs 0.000 claims description 3
- BMQGVNUXMIRLCK-OAGWZNDDSA-N cabazitaxel Chemical compound O([C@H]1[C@@H]2[C@]3(OC(C)=O)CO[C@@H]3C[C@@H]([C@]2(C(=O)[C@H](OC)C2=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=3C=CC=CC=3)C[C@]1(O)C2(C)C)C)OC)C(=O)C1=CC=CC=C1 BMQGVNUXMIRLCK-OAGWZNDDSA-N 0.000 claims description 3
- 239000003534 dna topoisomerase inhibitor Substances 0.000 claims description 3
- 229960004679 doxorubicin Drugs 0.000 claims description 3
- 229950005692 larotaxel Drugs 0.000 claims description 3
- SEFGUGYLLVNFIJ-QDRLFVHASA-N larotaxel dihydrate Chemical compound O.O.O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@@]23[C@H]1[C@@]1(CO[C@@H]1C[C@@H]2C3)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 SEFGUGYLLVNFIJ-QDRLFVHASA-N 0.000 claims description 3
- 229960001592 paclitaxel Drugs 0.000 claims description 3
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims description 3
- 229940044693 topoisomerase inhibitor Drugs 0.000 claims description 3
- 229940100198 alkylating agent Drugs 0.000 claims description 2
- 239000002168 alkylating agent Substances 0.000 claims description 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 2
- 229960004562 carboplatin Drugs 0.000 claims description 2
- 190000008236 carboplatin Chemical compound 0.000 claims description 2
- 229960004316 cisplatin Drugs 0.000 claims description 2
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 2
- 239000000032 diagnostic agent Substances 0.000 claims description 2
- 229940039227 diagnostic agent Drugs 0.000 claims description 2
- 229960005277 gemcitabine Drugs 0.000 claims description 2
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims description 2
- 229960001756 oxaliplatin Drugs 0.000 claims description 2
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 1
- 150000003230 pyrimidines Chemical class 0.000 claims 1
- 238000000034 method Methods 0.000 description 102
- 206010028980 Neoplasm Diseases 0.000 description 63
- 201000011510 cancer Diseases 0.000 description 63
- 208000035475 disorder Diseases 0.000 description 33
- 206010006187 Breast cancer Diseases 0.000 description 28
- 208000026310 Breast neoplasm Diseases 0.000 description 21
- 230000001394 metastastic effect Effects 0.000 description 21
- 206010061289 metastatic neoplasm Diseases 0.000 description 21
- 206010060862 Prostate cancer Diseases 0.000 description 7
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 7
- 229940044683 chemotherapy drug Drugs 0.000 description 7
- 239000005556 hormone Substances 0.000 description 7
- 229940088597 hormone Drugs 0.000 description 7
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 7
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 7
- 208000016691 refractory malignant neoplasm Diseases 0.000 description 6
- 238000002560 therapeutic procedure Methods 0.000 description 5
- 125000006239 protecting group Chemical group 0.000 description 4
- 229920000858 Cyclodextrin Polymers 0.000 description 3
- 206010070308 Refractory cancer Diseases 0.000 description 3
- 150000001720 carbohydrates Chemical group 0.000 description 3
- 239000003085 diluting agent Substances 0.000 description 3
- 229910052739 hydrogen Inorganic materials 0.000 description 3
- 239000001257 hydrogen Substances 0.000 description 3
- 208000027866 inflammatory disease Diseases 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 3
- 230000035755 proliferation Effects 0.000 description 3
- 230000005855 radiation Effects 0.000 description 3
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical group O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 3
- ODLHGICHYURWBS-LKONHMLTSA-N trappsol cyclo Chemical group CC(O)COC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)COCC(O)C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1COCC(C)O ODLHGICHYURWBS-LKONHMLTSA-N 0.000 description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- 206010038111 Recurrent cancer Diseases 0.000 description 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 2
- 230000000973 chemotherapeutic effect Effects 0.000 description 2
- 125000001424 substituent group Chemical group 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 241000283080 Proboscidea <mammal> Species 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 230000002152 alkylating effect Effects 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 150000004676 glycans Chemical class 0.000 description 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 238000012544 monitoring process Methods 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 230000000306 recurrent effect Effects 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
Applications Claiming Priority (17)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16473409P | 2009-03-30 | 2009-03-30 | |
| US16472009P | 2009-03-30 | 2009-03-30 | |
| US16472209P | 2009-03-30 | 2009-03-30 | |
| US16473109P | 2009-03-30 | 2009-03-30 | |
| US16472509P | 2009-03-30 | 2009-03-30 | |
| US16472809P | 2009-03-30 | 2009-03-30 | |
| US61/164,720 | 2009-03-30 | ||
| US61/164,725 | 2009-03-30 | ||
| US61/164,722 | 2009-03-30 | ||
| US61/164,734 | 2009-03-30 | ||
| US61/164,731 | 2009-03-30 | ||
| US61/164,728 | 2009-03-30 | ||
| US26299409P | 2009-11-20 | 2009-11-20 | |
| US26299309P | 2009-11-20 | 2009-11-20 | |
| US61/262,993 | 2009-11-20 | ||
| US61/262,994 | 2009-11-20 | ||
| PCT/US2010/028770 WO2010117668A1 (en) | 2009-03-30 | 2010-03-26 | Polymer-agent conjugates, particles, compositions, and related methods of use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015051314A Division JP2015117250A (ja) | 2009-03-30 | 2015-03-13 | ポリマー‐薬剤抱合体、粒子、組成物、および関連する使用方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012522055A JP2012522055A (ja) | 2012-09-20 |
| JP2012522055A5 true JP2012522055A5 (enExample) | 2013-04-25 |
Family
ID=42936493
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012503526A Pending JP2012522055A (ja) | 2009-03-30 | 2010-03-26 | ポリマー‐薬剤抱合体、粒子、組成物、および関連する使用方法 |
| JP2015051314A Pending JP2015117250A (ja) | 2009-03-30 | 2015-03-13 | ポリマー‐薬剤抱合体、粒子、組成物、および関連する使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015051314A Pending JP2015117250A (ja) | 2009-03-30 | 2015-03-13 | ポリマー‐薬剤抱合体、粒子、組成物、および関連する使用方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (7) | US20100247668A1 (enExample) |
| EP (1) | EP2413901A4 (enExample) |
| JP (2) | JP2012522055A (enExample) |
| CN (2) | CN102378626B (enExample) |
| AU (1) | AU2010234916A1 (enExample) |
| BR (1) | BRPI1014854A2 (enExample) |
| CA (1) | CA2756072A1 (enExample) |
| EA (1) | EA201171195A8 (enExample) |
| IL (1) | IL215123A0 (enExample) |
| MX (1) | MX2011010390A (enExample) |
| WO (1) | WO2010117668A1 (enExample) |
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| KR101476067B1 (ko) | 2002-09-06 | 2014-12-23 | 인설트 테라페틱스, 인코퍼레이티드 | 공유결합된 치료제 전달을 위한 사이클로덱스트린-기초 중합체 |
| US20080176958A1 (en) | 2007-01-24 | 2008-07-24 | Insert Therapeutics, Inc. | Cyclodextrin-based polymers for therapeutics delivery |
| WO2010005726A2 (en) | 2008-06-16 | 2010-01-14 | Bind Biosciences Inc. | Therapeutic polymeric nanoparticles with mtor inhibitors and methods of making and using same |
| EA020753B1 (ru) | 2008-06-16 | 2015-01-30 | Бинд Терапьютикс, Инк. | Терапевтические полимерные наночастицы, содержащие алкалоиды vinca, и их применение |
| ES2765240T3 (es) | 2008-06-16 | 2020-06-08 | Pfizer | Nanopartículas poliméricas cargadas de fármaco y procedimientos de fabricación y uso de las mismas |
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| ES2776126T3 (es) | 2008-12-15 | 2020-07-29 | Pfizer | Nanopartículas de circulación prolongada para la liberación sostenida de agentes terapéuticos |
| EA201171195A8 (ru) * | 2009-03-30 | 2014-08-29 | Серулин Фарма Инк. | Конъюгаты, частицы, композиции "полимер-агент" и способы их применения |
| WO2010114770A1 (en) * | 2009-03-30 | 2010-10-07 | Cerulean Pharma Inc. | Polymer-agent conjugates, particles, compositions, and related methods of use |
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| KR101712231B1 (ko) | 2009-10-29 | 2017-03-03 | 아벤티스 파마 소시에떼아노님 | 카바지탁셀의 신규한 항종양 용도 |
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| WO2011084513A2 (en) | 2009-12-15 | 2011-07-14 | Bind Biosciences, Inc. | Therapeutic polymeric nanoparticle compositions with high glass transition temperature or high molecular weight copolymers |
| JP5898627B2 (ja) * | 2009-12-15 | 2016-04-06 | バインド セラピューティックス インコーポレイテッド | エポチロンを含む治療用ポリマーナノ粒子ならびにそれを製造および使用する方法 |
| WO2011119995A2 (en) * | 2010-03-26 | 2011-09-29 | Cerulean Pharma Inc. | Formulations and methods of use |
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| WO2012097049A2 (en) * | 2011-01-11 | 2012-07-19 | The University Of North Carolina At Chapel Hill | Dna repair enzyme inhibitor nanoparticles and uses thereof |
| ES2712779T3 (es) * | 2011-01-24 | 2019-05-14 | Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd | Nanopartículas para la administración dérmica y sistémica de fármacos |
| CN102617517B (zh) * | 2011-01-27 | 2015-11-18 | 李勤耕 | 一类新的7,10-o,o-二甲多西紫杉醇衍生物及其应用 |
| US20180326081A1 (en) * | 2011-06-06 | 2018-11-15 | Starpharma Pty Ltd | Macromolecules |
| AU2012294326A1 (en) * | 2011-08-10 | 2013-03-21 | Merrimack Pharmaceuticals, Inc. | Treatment of advanced solid tumors using combination of anti-ErbB3 immunotherapy and selected chemotherapy |
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| US11596599B2 (en) | 2012-05-03 | 2023-03-07 | The Johns Hopkins University | Compositions and methods for ophthalmic and/or other applications |
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| TWI726291B (zh) * | 2013-01-07 | 2021-05-01 | 英屬維爾京群島商遠東超級實驗室有限公司 | 通過干擾素的經皮和/或經粘膜給藥治療骨癌、皮膚癌、皮下癌、粘膜癌和/或粘膜下癌的方法和組合物 |
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2010
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- 2010-03-26 EP EP10762122.9A patent/EP2413901A4/en not_active Withdrawn
- 2010-03-26 WO PCT/US2010/028770 patent/WO2010117668A1/en not_active Ceased
- 2010-03-26 JP JP2012503526A patent/JP2012522055A/ja active Pending
- 2010-03-26 AU AU2010234916A patent/AU2010234916A1/en not_active Abandoned
- 2010-03-26 CN CN201080014516.1A patent/CN102378626B/zh not_active Expired - Fee Related
- 2010-03-26 CA CA2756072A patent/CA2756072A1/en not_active Abandoned
- 2010-03-26 MX MX2011010390A patent/MX2011010390A/es not_active Application Discontinuation
- 2010-03-26 CN CN201410161936.2A patent/CN103932972A/zh active Pending
- 2010-03-29 US US12/748,637 patent/US20100247668A1/en not_active Abandoned
- 2010-09-29 US US12/894,040 patent/US20110189092A1/en not_active Abandoned
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2011
- 2011-01-11 US US13/004,838 patent/US20110268658A1/en not_active Abandoned
- 2011-09-13 IL IL215123A patent/IL215123A0/en unknown
-
2012
- 2012-07-12 US US13/548,143 patent/US20120282306A1/en not_active Abandoned
- 2012-07-12 US US13/548,108 patent/US20130011445A1/en not_active Abandoned
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2013
- 2013-03-19 US US13/847,391 patent/US20140099263A1/en not_active Abandoned
- 2013-10-08 US US14/048,537 patent/US20140286873A1/en not_active Abandoned
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2015
- 2015-03-13 JP JP2015051314A patent/JP2015117250A/ja active Pending
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