JP2018527335A5 - - Google Patents
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- Publication number
- JP2018527335A5 JP2018527335A5 JP2018506339A JP2018506339A JP2018527335A5 JP 2018527335 A5 JP2018527335 A5 JP 2018527335A5 JP 2018506339 A JP2018506339 A JP 2018506339A JP 2018506339 A JP2018506339 A JP 2018506339A JP 2018527335 A5 JP2018527335 A5 JP 2018527335A5
- Authority
- JP
- Japan
- Prior art keywords
- drug
- liposome
- phosphatidylcholine
- cholesterol
- stable
- 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
- 239000002502 liposome Substances 0.000 claims 22
- 229940079593 drug Drugs 0.000 claims 18
- 239000003814 drug Substances 0.000 claims 18
- 239000000203 mixture Substances 0.000 claims 13
- WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 claims 12
- 230000002209 hydrophobic effect Effects 0.000 claims 9
- 238000009472 formulation Methods 0.000 claims 8
- 238000000034 method Methods 0.000 claims 8
- 239000000725 suspension Substances 0.000 claims 8
- 229920001223 polyethylene glycol Polymers 0.000 claims 7
- CITHEXJVPOWHKC-UUWRZZSWSA-N 1,2-di-O-myristoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCC CITHEXJVPOWHKC-UUWRZZSWSA-N 0.000 claims 6
- SNKAWJBJQDLSFF-NVKMUCNASA-N 1,2-dioleoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/CCCCCCCC SNKAWJBJQDLSFF-NVKMUCNASA-N 0.000 claims 6
- 229960003724 dimyristoylphosphatidylcholine Drugs 0.000 claims 6
- YYSFXUWWPNHNAZ-PKJQJFMNSA-N umirolimus Chemical compound C1[C@@H](OC)[C@H](OCCOCC)CC[C@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 YYSFXUWWPNHNAZ-PKJQJFMNSA-N 0.000 claims 6
- 229950007775 umirolimus Drugs 0.000 claims 6
- 239000002202 Polyethylene glycol Substances 0.000 claims 5
- LVNGJLRDBYCPGB-UHFFFAOYSA-N 1,2-distearoylphosphatidylethanolamine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(COP([O-])(=O)OCC[NH3+])OC(=O)CCCCCCCCCCCCCCCCC LVNGJLRDBYCPGB-UHFFFAOYSA-N 0.000 claims 4
- 239000000232 Lipid Bilayer Substances 0.000 claims 4
- 238000002360 preparation method Methods 0.000 claims 4
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 3
- 229960005167 everolimus Drugs 0.000 claims 3
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 3
- 229960002930 sirolimus Drugs 0.000 claims 3
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 3
- 239000012062 aqueous buffer Substances 0.000 claims 2
- 239000007864 aqueous solution Substances 0.000 claims 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 2
- 150000002632 lipids Chemical class 0.000 claims 2
- 239000012528 membrane Substances 0.000 claims 2
- 150000003904 phospholipids Chemical class 0.000 claims 2
- 239000008137 solubility enhancer Substances 0.000 claims 2
- 238000003756 stirring Methods 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 238000001914 filtration Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000002356 single layer Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14/849,100 US20170065520A1 (en) | 2015-09-09 | 2015-09-09 | Stable liposomal formulations of rapamycin and rapamycin derivatives for treating cancer |
| US14/849,100 | 2015-09-09 | ||
| PCT/US2015/051206 WO2017044135A1 (en) | 2015-09-09 | 2015-09-21 | Stable liposomal formulations of rapamycin and rapamycin derivatives for treating cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018527335A JP2018527335A (ja) | 2018-09-20 |
| JP2018527335A5 true JP2018527335A5 (https=) | 2018-11-01 |
Family
ID=58189920
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018506339A Pending JP2018527335A (ja) | 2015-09-09 | 2015-09-21 | 癌の治療に対するラパマイシン及びラパマイシン誘導体の安定なリポソーム製剤 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20170065520A1 (https=) |
| EP (1) | EP3346989B1 (https=) |
| JP (1) | JP2018527335A (https=) |
| CN (1) | CN108024962A (https=) |
| ES (1) | ES2849730T3 (https=) |
| WO (1) | WO2017044135A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014144365A1 (en) * | 2013-03-15 | 2014-09-18 | University Of Maryland, College Park | Nano-liposomal formulations and methods of use |
| CN108926533B (zh) * | 2017-05-24 | 2022-03-25 | 江苏天士力帝益药业有限公司 | 一种替西罗莫司脂质体及其制备方法 |
| IT201900003887A1 (it) | 2019-03-18 | 2020-09-18 | Fidia Farm Spa | Sistemi di stabilizzazione e di rilascio controllato di farmaci instabili alla sterilizzazione |
| IT202000007228A1 (it) * | 2020-04-06 | 2021-10-06 | Diego Dolcetta | SOMMINISTRAZIONE DI INIBITORI DI mTOR NEL SISTEMA NERVOSO CENTRALE |
| JP2023163355A (ja) * | 2022-04-28 | 2023-11-10 | プレシエンス バイオテクノロジー インコーポレイテッド | ラパマイシンまたはその誘導体を含むリポソーム、およびそれらの治療における使用 |
| US12433874B2 (en) | 2022-04-28 | 2025-10-07 | Prescience Biotechnology Inc. | Liposome comprising rapamycin or a derivative thereof and use thereof in therapy |
| CN117159724B (zh) * | 2023-04-04 | 2024-07-05 | 上海交通大学医学院附属仁济医院 | 一种脂质体-dna水凝胶复合给药系统及其制备方法 |
| CN121752252A (zh) * | 2023-08-16 | 2026-03-27 | 吉纳制药公司 | 含有mTOR抑制剂和脂质的组合物 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL111004A (en) * | 1993-09-30 | 1998-06-15 | American Home Prod | Oral formulations of rapamycin |
| CA2269758C (en) * | 1996-10-22 | 2008-01-08 | Hermes Biosciences, Inc. | Liposome compositions comprising ionizable compounds in stable precipitated form and methods for their preparation |
| CN103860469A (zh) * | 2007-10-23 | 2014-06-18 | 英斯麦德公司 | 脂质体万古霉素制剂 |
| US20110244028A1 (en) * | 2008-09-26 | 2011-10-06 | Steve Leigh | Method of solubilizing biologically active compounds |
| WO2012118376A1 (en) * | 2011-03-01 | 2012-09-07 | To-Bbb Holding B.V. | Advanced active liposomal loading of poorly water-soluble substances |
| EP2638896A1 (en) * | 2012-03-14 | 2013-09-18 | Bioneer A/S | Cationic liposomal drug delivery system for specific targeting of human cd14+ monocytes in whole blood |
| US20150157610A1 (en) * | 2012-05-23 | 2015-06-11 | Osaka University | Pharmaceutical composition for treating inflammatory disease |
| US10172796B2 (en) * | 2012-12-03 | 2019-01-08 | Manli International Ltd. | Use of umirolimus and its derivatives for treating cancer |
| EP4309657A3 (en) * | 2013-02-01 | 2024-02-28 | Celator Pharmaceuticals, Inc. | Remote loading of sparingly water-soluble drugs into liposomes |
| MX364310B (es) * | 2013-11-05 | 2019-04-22 | Gustavo A Garcia Sanchez | Método para preparar una formulación inmunosupresora. |
-
2015
- 2015-09-09 US US14/849,100 patent/US20170065520A1/en not_active Abandoned
- 2015-09-21 WO PCT/US2015/051206 patent/WO2017044135A1/en not_active Ceased
- 2015-09-21 EP EP15903759.7A patent/EP3346989B1/en active Active
- 2015-09-21 JP JP2018506339A patent/JP2018527335A/ja active Pending
- 2015-09-21 ES ES15903759T patent/ES2849730T3/es active Active
- 2015-09-21 CN CN201580082921.XA patent/CN108024962A/zh active Pending
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