RU2016132635A - Конъюгаты антитело-лекарственное средство (adc) с дуокармицином, применяемые для лечения рака эндометрия - Google Patents
Конъюгаты антитело-лекарственное средство (adc) с дуокармицином, применяемые для лечения рака эндометрия Download PDFInfo
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- 206010028980 Neoplasm Diseases 0.000 title claims 3
- 201000011510 cancer Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 9
- 206010014733 Endometrial cancer Diseases 0.000 claims 4
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 4
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 4
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 4
- 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 2
- 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 229940127089 cytotoxic agent Drugs 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000007787 solid Substances 0.000 claims 2
- 206010046766 uterine cancer Diseases 0.000 claims 2
- 208000012991 uterine carcinoma Diseases 0.000 claims 2
- 229940123237 Taxane Drugs 0.000 claims 1
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000008176 lyophilized powder Substances 0.000 claims 1
- 229940125645 monoclonal antibody drug Drugs 0.000 claims 1
- 229960002087 pertuzumab Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 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 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims 1
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 claims 1
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Claims (32)
1. Соединение формулы (I)
где
анти-HER2 Ab представляет собой анти-HER2 антитело или фрагмент антитела,
n составляет от 0 до 3,
m представляет собой среднее значение DAR от 1 до 4,
R1 выбирают из
y составляет от 1 до 16, и
R2 выбирают из
для применения в лечении солидных опухолей человека, экспрессирующих HER2, где солидная опухоль человека, экспрессирующая HER2, представляет собой рак эндометрия.
2. Соединение для применения по п.1, где
анти-HER2 Ab представляет собой анти-HER2 антитело или фрагмент антитела,
n составляет от 0 до 1,
m представляет собой среднее значение DAR от 1 до 4,
R1 выбирают из
y составляет от 1 до 16, и
R2 выбирают из
3. Соединение для применения по п. 1 или 2 формулы (II)
4. Соединение для применения по п. 3 формулы (II), имеющее среднее значение DAR от 2,6 до 2,9.
5. Соединение для применения по любому из пп. 1-4 для лечения серозной карциномы матки.
6. Соединение для применения по любому из пп. 1-5, где рак эндометрия является HER2 IHC 2+ или 1+.
7. Соединение для применения по любому из пп. 1-6, где рак эндометрия является HER2 FISH-негативным.
8. Комбинация соединения для применения по любому из пп. 1-7 с лекарственным препаратом на основе моноклонального антитела и/или химиотерапевтическим средством для применения в лечении рака эндометрия.
9. Комбинация для применения по п.8, для применения в лечении серозной карциномы матки.
10. Комбинация для применения по п. 8 или 9, где лекарственное средство на основе моноклонального антитела представляет собой пертузумаб, а химиотерапевтическое средство представляет собой таксан, антрациклин или ингибитор тирозинкиназ.
11. Фармацевтическая композиция, включающая соединение для применения по любому из пп. 1-7 или комбинацию для применения по любому из пп. 8-10, а также один или более фармацевтически приемлемых эксципиентов.
12. Фармацевтическая композиция по п. 11 в форме лиофилизированного порошка или замороженного раствора.
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PCT/EP2015/050332 WO2015104373A2 (en) | 2014-01-10 | 2015-01-09 | Duocarmycin adcs for use in treatment of endometrial cancer |
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JP6224268B2 (ja) | 2017-11-01 |
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SG11201605597VA (en) | 2016-08-30 |
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CL2016001743A1 (es) | 2017-01-06 |
ES2578831T3 (es) | 2016-08-01 |
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RU2686085C2 (ru) | 2019-04-24 |
MX368234B (es) | 2019-09-25 |
KR20220045075A (ko) | 2022-04-12 |
HUE029672T2 (en) | 2017-03-28 |
MX2016009069A (es) | 2017-02-06 |
WO2015104373A2 (en) | 2015-07-16 |
CA2935430A1 (en) | 2015-07-16 |
PT2948183T (pt) | 2016-07-13 |
CN105899237B (zh) | 2019-09-03 |
MY189713A (en) | 2022-02-28 |
AU2015205588B2 (en) | 2019-08-08 |
CN105899237A (zh) | 2016-08-24 |
RU2016132635A3 (ru) | 2018-08-13 |
DK2948183T3 (en) | 2016-06-27 |
JP2017502086A (ja) | 2017-01-19 |
AU2015205588A1 (en) | 2016-07-28 |
CA2935430C (en) | 2018-09-18 |
US9427480B2 (en) | 2016-08-30 |
US10092659B2 (en) | 2018-10-09 |
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