RU2017131430A - Способ лечения рака, ассоциированного с мутацией ras - Google Patents
Способ лечения рака, ассоциированного с мутацией ras Download PDFInfo
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- 238000000034 method Methods 0.000 title claims 35
- 230000035772 mutation Effects 0.000 title claims 12
- 206010028980 Neoplasm Diseases 0.000 title claims 10
- 201000011510 cancer Diseases 0.000 title claims 10
- 102100030708 GTPase KRas Human genes 0.000 claims 11
- 101000584612 Homo sapiens GTPase KRas Proteins 0.000 claims 11
- 125000003275 alpha amino acid group Chemical group 0.000 claims 10
- UNRCMCRRFYFGFX-TYPNBTCFSA-N plinabulin Chemical compound N1C=NC(\C=C/2C(NC(=C\C=3C=CC=CC=3)/C(=O)N\2)=O)=C1C(C)(C)C UNRCMCRRFYFGFX-TYPNBTCFSA-N 0.000 claims 7
- 229950011498 plinabulin Drugs 0.000 claims 7
- 102000016914 ras Proteins Human genes 0.000 claims 7
- 102100039788 GTPase NRas Human genes 0.000 claims 6
- 101000744505 Homo sapiens GTPase NRas Proteins 0.000 claims 6
- 238000006467 substitution reaction Methods 0.000 claims 6
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- 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 1
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- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims 1
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Classifications
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- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- 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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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Claims (34)
1. Способ лечения рака, характеризующегося экспрессией мутантной формы белка RAS, включающий введение плинабулина субъекту, нуждающемуся в этом.
2. Способ по п. 1, в котором указанный белок RAS представляет собой белок KRAS, NRAS или HRAS.
3. Способ по п. 2, в котором указанная мутантная форма белка RAS представляет собой мутантную форму белка K-RAS.
4. Способ по любому из пп. 1-3, в котором указанный рак выбран из колоректального рака, рака поджелудочной железы, рака почек, рака легких, рака печени, рака груди, рака предстательной железы, рака желудочно-кишечного тракта, перитонеального рака, меланомы, рака эндометрия, рака яичников, рака шейки матки, карциномы матки, рака мочевого пузыря, глиобластомы, метастазов в головной мозг, карциномы слюнных желез, рака щитовидной железы, рака мозга, лимфомы, миеломы и рака головы и шеи.
5. Способ по любому из пп. 1-4, в котором указанный рак выбран из плоскоклеточного рака, мелкоклеточного рака легких, немелкоклеточного рака легких, аденокарциномы легких, плоскоклеточной карциномы легких, гепатоцеллюлярной карциномы, рака толстой кишки, карциномы эндометрия и гепатоцеллюлярной карциномы.
6. Способ по любому из пп. 1-5, в котором указанный рак выбран из колоректального рака, рака предстательной железы, рака груди, рака легких, рака эндометрия, множественной миеломы, рака поджелудочной железы, рака почек и глиобластомы.
7. Способ по п. 6, в котором указанный рак выбран из немелкоклеточного рака легких, рака поджелудочной железы и глиобластомы.
8. Способ по п. 7, в котором указанный рак представляет собой немелкоклеточный рак легких.
9. Способ по любому из пп. 3-8, в котором указанный белок KRAS содержит мутацию в одном или более положениях, выбранных из кодонов 12, 13, 59, 61 и 146.
10. Способ по любому из пп. 3-8, в котором указанная мутантная форма белка KRAS содержит мутацию в одном или более положениях аминокислот, выбранных из G12, G13, S17, Р34, A59 и Q61.
11. Способ по п. 10, в котором указанная мутантная форма белка KRAS содержит одну или более аминокислотных замен, выбранных из группы, состоящей из G12C, G12S, G12R, G12F, G12L, G12N, G12A, G12D, G12V, G13C, G13S, G13D, G13V, G13P, S17G, P34S, А59Е, A59G, А59Т, Q61K, Q61L, Q61R и Q61H.
12. Способ по любому из пп. 3-8, в котором указанная мутантная форма белка KRAS содержит мутацию в одном или более положениях аминокислот, выбранных из G12, G13, А59, Q61, K117 и A146.
13. Способ по п. 12, в котором указанная мутантная форма белка KRAS содержит одну или более аминокислотных замен, выбранных из группы, состоящей из G12C, G12R, G12S, G12A, G12D, G12V, G13C, G13R, G13S, G13A, G13D, G13V, А59Е, A59G, А59Т, Q61K, Q61L, Q61R, Q61H, K117N, А146Р, А146Т и A146V.
14. Способ по любому из пп. 3-8, в котором указанная мутантная форма белка KRAS содержит мутацию в одном или более положениях аминокислот, выбранных из G12, G13 А59 и Q61.
15. Способ по п. 14, в котором указанная мутантная форма белка KRAS содержит одну или более аминокислотных замен, выбранных из группы, состоящей из G12C, G12R, G12S, G12A, G12D, G12V, G13C, G13R, G13S, G13A, G13D, А59Е, A59G, А59Т, Q61K, Q61L, Q61R и Q61H.
16. Способ по любому из пп. 3-8, в котором указанная мутантная форма белка KRAS содержит мутацию в одном или более положениях аминокислот, выбранных из G12, G13 и D153.
17. Способ по п. 16, в котором указанная мутантная форма белка KRAS содержит одну или более аминокислотных замен, выбранных из группы, состоящей из G12A, G12C, G12D, G12V, G12S, G13D и D153V.
18. Способ по п. 17, в котором указанная мутантная форма белка KRAS содержит одну или более аминокислотных замен, выбранных из G12C, G12S и D153V.
19. Способ по любому из пп. 1-18, включающий определение того, имеет ли субъект мутацию KRAS.
20. Способ по п. 2, в котором указанная мутантная форма белка RAS представляет собой мутантную форму белка NRAS.
21. Способ по п. 20, в котором указанный белок NRAS содержит мутацию в одном или более положениях, выбранных из кодонов 12, 13, 59, 61 и 146.
22. Способ по п. 21, в котором указанная мутантная форма белка NRAS содержит мутацию в Q61 или А146.
23. Способ по п. 22, в котором указанная мутантная форма белка NRAS содержит одну или более аминокислотных замен, выбранных из Q61K, Q61H, Q61R, Q61L, Q61N, Q61E, Q61P, А146Т, А146Р и A146V.
24. Способ по любому из пп. 20-23, включающий определение того, имеет ли субъект мутацию NRAS.
25. Способ по любому из пп. 20-23, включающий определение того, имеет ли субъект мутацию HRAS.
26. Способ по любому из пп. 1-25, включающий совместное введение плинабулина с дополнительным активным агентом.
27. Способ по п. 26, в котором указанный дополнительный активный агент является дополнительным терапевтическим агентом.
28. Способ по п. 27, в котором указанным дополнительным терапевтическим агентом является доцетаксел, иа рак представляет собой немелкоклеточный рак легких человека.
29. Способ по п. 27, в котором указанным дополнительным терапевтическим агентом является иринотекан, и рак представляет собой рак толстой кишки человека.
30. Способ ингибирования пролиферации клетки с мутацией RAS, включающий приведение указанной клетки в контакт с плинабулином.
31. Способ по п. 30, в котором приведение в контакт включает введение плинабулина субъекту, имеющему указанную клетку.
32. Способ индуцирования апоптоза в клетке, содержащей мутацию RAS, включающий приведение указанной клетки в контакт с плинабулином.
33. Способ по п. 32, в котором приведение в контакт включает введение плинабулина субъекту, нуждающемуся в этом.
34. Способ ингибирования прогрессирования рака, характеризующегося экспрессией мутантной формы белка RAS, у субъекта, включающий введение плинабулина субъекту, нуждающемуся в этом.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562129654P | 2015-03-06 | 2015-03-06 | |
| US62/129,654 | 2015-03-06 | ||
| US201562249788P | 2015-11-02 | 2015-11-02 | |
| US62/249,788 | 2015-11-02 | ||
| PCT/US2016/020390 WO2016144635A1 (en) | 2015-03-06 | 2016-03-02 | Method of treating cancer associated with a ras mutation |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2017131430A true RU2017131430A (ru) | 2019-04-09 |
| RU2017131430A3 RU2017131430A3 (ru) | 2019-08-28 |
| RU2736045C2 RU2736045C2 (ru) | 2020-11-11 |
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| Application Number | Title | Priority Date | Filing Date |
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| RU2017131430A RU2736045C2 (ru) | 2015-03-06 | 2016-03-02 | Способ лечения рака, ассоциированного с мутацией ras |
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| Country | Link |
|---|---|
| US (4) | US10238650B2 (ru) |
| EP (1) | EP3265090A4 (ru) |
| JP (1) | JP6769982B2 (ru) |
| KR (1) | KR102626155B1 (ru) |
| CN (1) | CN107530341B (ru) |
| AU (2) | AU2016229294B2 (ru) |
| BR (1) | BR112017018954A2 (ru) |
| CA (1) | CA2978567A1 (ru) |
| CL (1) | CL2017002241A1 (ru) |
| HK (2) | HK1250008A1 (ru) |
| IL (1) | IL254256A0 (ru) |
| MX (1) | MX2017011374A (ru) |
| MY (1) | MY190034A (ru) |
| RU (1) | RU2736045C2 (ru) |
| SG (2) | SG11201707127VA (ru) |
| WO (1) | WO2016144635A1 (ru) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016144635A1 (en) * | 2015-03-06 | 2016-09-15 | Beyondspring Pharmaceuticals, Inc. | Method of treating cancer associated with a ras mutation |
| US10076518B2 (en) | 2015-03-06 | 2018-09-18 | Beyondspring Pharmaceuticals, Inc. | Method of treating a brain tumor |
| MY181892A (en) | 2015-07-13 | 2021-01-12 | Beyondspring Pharmaceuticals Inc | Plinabulin compositions |
| SG11201806583XA (en) | 2016-02-08 | 2018-09-27 | Beyondspring Pharmaceuticals Inc | Compositions containing tucaresol or its analogs |
| AU2017278245B2 (en) | 2016-06-06 | 2022-09-15 | Beyondspring Pharmaceuticals, Inc. | Composition and method for reducing neutropenia |
| US11633393B2 (en) | 2017-01-06 | 2023-04-25 | Beyondspring Pharmaceuticals, Inc. | Tubulin binding compounds and therapeutic use thereof |
| MY201811A (en) | 2017-02-01 | 2024-03-19 | Beyondspring Pharmaceuticals Inc | Method of reducing neutropenia |
| JP2019019094A (ja) * | 2017-07-19 | 2019-02-07 | 学校法人福岡大学 | 変異ｋｒａｓ関連シグナル阻害用組成物 |
| CN109498627B (zh) * | 2017-09-15 | 2021-06-04 | 深圳华大海洋科技有限公司 | 一种治疗肿瘤的药物组合物及其应用 |
| SG11202006985TA (en) | 2018-01-24 | 2020-08-28 | Beyondspring Pharmaceuticals Inc | Composition and method for reducing thrombocytopenia via the administration of plinabulin |
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| SG10202008673WA (en) | 2020-10-29 |
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| CA2978567A1 (en) | 2016-09-15 |
| RU2017131430A3 (ru) | 2019-08-28 |
| HK1249052A1 (zh) | 2018-10-26 |
| US20200289503A1 (en) | 2020-09-17 |
| US11918574B2 (en) | 2024-03-05 |
| JP2018507249A (ja) | 2018-03-15 |
| US20180036304A1 (en) | 2018-02-08 |
| EP3265090A1 (en) | 2018-01-10 |
| AU2016229294B2 (en) | 2021-11-04 |
| SG11201707127VA (en) | 2017-09-28 |
| CL2017002241A1 (es) | 2018-04-02 |
| AU2016229294A1 (en) | 2017-09-28 |
| KR102626155B1 (ko) | 2024-01-17 |
| MX2017011374A (es) | 2018-01-23 |
| EP3265090A4 (en) | 2018-08-01 |
| AU2021290270A1 (en) | 2022-01-27 |
| CN107530341B (zh) | 2021-10-01 |
| JP6769982B2 (ja) | 2020-10-14 |
| US20210275524A1 (en) | 2021-09-09 |
| MY190034A (en) | 2022-03-22 |
| RU2736045C2 (ru) | 2020-11-11 |
| HK1250008A1 (zh) | 2018-11-23 |
| IL254256A0 (en) | 2017-10-31 |
| US10238650B2 (en) | 2019-03-26 |
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