RU2012101999A - РЕКОМБИНАНТНЫЕ УЧАСТКИ Fc ДЛЯ САЙТ-СПЕЦИФИЧЕСКОЙ КОНЪЮГАЦИИ - Google Patents
РЕКОМБИНАНТНЫЕ УЧАСТКИ Fc ДЛЯ САЙТ-СПЕЦИФИЧЕСКОЙ КОНЪЮГАЦИИ Download PDFInfo
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- RJFAYQIBOAGBLC-BYPYZUCNSA-N Selenium-L-methionine Chemical compound C[Se]CC[C@H](N)C(O)=O RJFAYQIBOAGBLC-BYPYZUCNSA-N 0.000 claims abstract 2
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- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 claims abstract 2
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- ZKZBPNGNEQAJSX-UHFFFAOYSA-N selenocysteine Natural products [SeH]CC(N)C(O)=O ZKZBPNGNEQAJSX-UHFFFAOYSA-N 0.000 claims abstract 2
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- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
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- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
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- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
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- A61P37/00—Drugs for immunological or allergic disorders
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- G—PHYSICS
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- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
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- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
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Abstract
1. Участок Fc антитела, где участок Fc содержит замещение одной или более аминокислот, выбранных из положений 239, 282, 289, 297, 312, 324, 330, 335, 337, 339, 356, 359, 361, 383, 384, 398, 400, 440, 422 и 442.2. Участок Fc по п.1, где участок Fc содержит одну или более из следующих пар замещений:a) 289 и 440;б) 330 и 440;в) 339 и 440;г) 359 и 440;д) 289 и 359;е) 330 и 359;ж) 339 и 359;з) 289 и 339;и) 330 и 339;к) 289 и 330; ил) 339 и 442.3. Участок Fc по п.1, где участок Fc содержит одну или более из следующих групп замещений:a) 289, 339 и 442;б) 289, 330 и 339;в) 330, 339 и 442; иг) 289, 330 и 442.4. Участок Fc по п.1, где участок Fc выбран из изотипа IgG1, IgG2, IgG3 или IgG4.5. Участок Fc по п.1, в котором замещение содержит аминокислоты аминокислотой, выбираемой из цистеина, лизина, тирозина, гистидина, селеноцистеина и селенометионина.6. Участок Fc по п.5, в котором замещение содержит цистеин.7. Участок Fc по п.6, в котором цистеин содержит тиоловую группу.8. Участок Fc по п.7, в котором тиоловая группа способна к химической конъюгации.9. Участок Fc по п.8, в котором участок Fc конъюгирован с одним или более из цитотоксического агента, химиотерапевтического агента, токсина, радионуклида, ДНК, РНК, миРНК, микро-РНК, пептидной нуклеиновой кислоты, не встречающейся в природе нуклеиновой кислоты, пептида, фермента, флуоресцентной метки и биотина.10. Антитело или его антигенсвязывающий фрагмент, содержащие участок Fc по п.1.11. Антитело или его антигенсвязывающий фрагмент по п.10, где указанное антитело является моноклональным, химерным, гуманизированным, полностью человеческим, биспецифическим, мультиспецифическим антителом или антителоподобной молекулой.12. Антитело или его антигенсвязывающий фрагмент по п.10, где антитело дополнительно содержит замещение одной или нескольких амино�
Claims (20)
1. Участок Fc антитела, где участок Fc содержит замещение одной или более аминокислот, выбранных из положений 239, 282, 289, 297, 312, 324, 330, 335, 337, 339, 356, 359, 361, 383, 384, 398, 400, 440, 422 и 442.
2. Участок Fc по п.1, где участок Fc содержит одну или более из следующих пар замещений:
a) 289 и 440;
б) 330 и 440;
в) 339 и 440;
г) 359 и 440;
д) 289 и 359;
е) 330 и 359;
ж) 339 и 359;
з) 289 и 339;
и) 330 и 339;
к) 289 и 330; и
л) 339 и 442.
3. Участок Fc по п.1, где участок Fc содержит одну или более из следующих групп замещений:
a) 289, 339 и 442;
б) 289, 330 и 339;
в) 330, 339 и 442; и
г) 289, 330 и 442.
4. Участок Fc по п.1, где участок Fc выбран из изотипа IgG1, IgG2, IgG3 или IgG4.
5. Участок Fc по п.1, в котором замещение содержит аминокислоты аминокислотой, выбираемой из цистеина, лизина, тирозина, гистидина, селеноцистеина и селенометионина.
6. Участок Fc по п.5, в котором замещение содержит цистеин.
7. Участок Fc по п.6, в котором цистеин содержит тиоловую группу.
8. Участок Fc по п.7, в котором тиоловая группа способна к химической конъюгации.
9. Участок Fc по п.8, в котором участок Fc конъюгирован с одним или более из цитотоксического агента, химиотерапевтического агента, токсина, радионуклида, ДНК, РНК, миРНК, микро-РНК, пептидной нуклеиновой кислоты, не встречающейся в природе нуклеиновой кислоты, пептида, фермента, флуоресцентной метки и биотина.
10. Антитело или его антигенсвязывающий фрагмент, содержащие участок Fc по п.1.
11. Антитело или его антигенсвязывающий фрагмент по п.10, где указанное антитело является моноклональным, химерным, гуманизированным, полностью человеческим, биспецифическим, мультиспецифическим антителом или антителоподобной молекулой.
12. Антитело или его антигенсвязывающий фрагмент по п.10, где антитело дополнительно содержит замещение одной или нескольких аминокислот, выбранных из положений 131, 132, 133, 134, 135, 136, 137, 138 и 139 домена СН1 антитела.
13. Фармацевтическая композиция, содержащая антитело или его антигенсвязывающий фрагмент по п.10.
14. Способ определения рака, аутоиммунных, воспалительных или инфекционных заболеваний или расстройств у нуждающегося в этом индивидуума, где способ включает введение указанному индивидууму антитела или его антигенсвязывающего фрагмента, при этом рекомбинантное антитело или его антигенсвязывающий фрагмент содержит замещение одной или более аминокислот в положениях тяжелой цепи, выбранных из положений 239, 282, 289, 297, 312, 324, 330, 335, 337, 339, 356, 359, 361, 383, 384, 398, 400, 440, 422 и 442.
15. Способ лечения рака, аутоиммунных, воспалительных или инфекционных заболеваний или расстройств у нуждающегося в этом индивидуума, где способ включает введение указанному индивидууму терапевтически эффективного количества антитела или его антигенсвязывающего фрагмента, при этом антитело или его антигенсвязывающий фрагмент содержит замещение одной или более аминокислот в положениях тяжелой цепи, выбранных из положений 239, 282, 289, 297, 312, 324, 330, 335, 337, 339, 356, 359, 361, 383, 384, 398, 400, 440, 422 и 442.
16. Нуклеиновая кислота, кодирующая участок Fc по п.1.
17. Нуклеиновая кислота по п.16, где нуклеиновая кислота содержит последовательность, кодирующую аминокислотную последовательность, выбранную из последовательностей SEQ ID NO:1-24.
18. Клетка-хозяин, содержащая нуклеиновую кислоту по п.17.
19. Клетка-хозяин по п.18, где клетка представлена клеткой млекопитающего.
20. Способ получения антитела или его антигенсвязывающего фрагмента, включающий инкубирование клетки-хозяина по п.19 в соответствующих условиях для экспрессии антитела или антигенсвязывающего фрагмента, и выделение антитела или антигенсвязывающего фрагмента.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21922509P | 2009-06-22 | 2009-06-22 | |
| US61/219,225 | 2009-06-22 | ||
| PCT/US2010/039351 WO2011005481A1 (en) | 2009-06-22 | 2010-06-21 | ENGINEERED Fc REGIONS FOR SITE-SPECIFIC CONJUGATION |
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| Publication Number | Publication Date |
|---|---|
| RU2012101999A true RU2012101999A (ru) | 2013-07-27 |
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| RU2012101999/15A RU2012101999A (ru) | 2009-06-22 | 2010-06-21 | РЕКОМБИНАНТНЫЕ УЧАСТКИ Fc ДЛЯ САЙТ-СПЕЦИФИЧЕСКОЙ КОНЪЮГАЦИИ |
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| Country | Link |
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| US (2) | US20120213705A1 (ru) |
| EP (2) | EP2711018A1 (ru) |
| JP (2) | JP5918129B2 (ru) |
| CN (1) | CN102802661B (ru) |
| AU (1) | AU2010270979B2 (ru) |
| BR (1) | BRPI1015234A2 (ru) |
| CA (1) | CA2766405A1 (ru) |
| MX (1) | MX2012000121A (ru) |
| RU (1) | RU2012101999A (ru) |
| WO (1) | WO2011005481A1 (ru) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US8981061B2 (en) | 2001-03-20 | 2015-03-17 | Novo Nordisk A/S | Receptor TREM (triggering receptor expressed on myeloid cells) and uses thereof |
| GB0426146D0 (en) | 2004-11-29 | 2004-12-29 | Bioxell Spa | Therapeutic peptides and method |
| US20120213705A1 (en) * | 2009-06-22 | 2012-08-23 | Medimmune, Llc | ENGINEERED Fc REGIONS FOR SITE-SPECIFIC CONJUGATION |
| US8765432B2 (en) | 2009-12-18 | 2014-07-01 | Oligasis, Llc | Targeted drug phosphorylcholine polymer conjugates |
| EP3590966B1 (en) | 2010-02-23 | 2025-03-05 | Sanofi | Anti-alpha2 integrin antibodies and their uses |
| JP2013534520A (ja) | 2010-06-08 | 2013-09-05 | ジェネンテック， インコーポレイテッド | システイン操作抗体及びコンジュゲート |
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| CA2552788C (en) | 2004-01-12 | 2013-09-24 | Applied Molecular Evolution, Inc. | Fc region variants |
| EP2053062A1 (en) | 2004-03-24 | 2009-04-29 | Xencor, Inc. | Immunoglobin variants outside the Fc region |
| BRPI0514068B8 (pt) | 2004-08-04 | 2021-05-25 | Applied Molecular Evolution Inc | anticorpo anti-cd20, e, composição farmacêutica |
| ES2579805T3 (es) | 2004-09-23 | 2016-08-16 | Genentech, Inc. | Anticuerpos y conjugados modificados por ingeniería genética con cisteína |
| US20070135620A1 (en) | 2004-11-12 | 2007-06-14 | Xencor, Inc. | Fc variants with altered binding to FcRn |
| WO2007005786A2 (en) | 2005-06-30 | 2007-01-11 | Centocor, Inc. | Methods and compositions with enhanced therapeutic activity |
| EP3456351A1 (en) | 2006-04-05 | 2019-03-20 | The Rockefeller University | Polypeptides with enhanced anti-inflammatory and decreased cytotoxic properties and relating methods |
| US20080112961A1 (en) * | 2006-10-09 | 2008-05-15 | Macrogenics, Inc. | Identification and Engineering of Antibodies with Variant Fc Regions and Methods of Using Same |
| ES2523915T5 (es) * | 2006-12-01 | 2022-05-26 | Seagen Inc | Agentes de unión a la diana variantes y usos de los mismos |
| US20120213705A1 (en) * | 2009-06-22 | 2012-08-23 | Medimmune, Llc | ENGINEERED Fc REGIONS FOR SITE-SPECIFIC CONJUGATION |
| US11392902B2 (en) | 2017-06-06 | 2022-07-19 | United Parcel Service Of America, Inc. | Systems, methods, apparatuses and computer program products for providing notification of items for pickup and delivery |
-
2010
- 2010-06-21 US US13/379,207 patent/US20120213705A1/en not_active Abandoned
- 2010-06-21 BR BRPI1015234A patent/BRPI1015234A2/pt not_active IP Right Cessation
- 2010-06-21 RU RU2012101999/15A patent/RU2012101999A/ru unknown
- 2010-06-21 CN CN201080027743.8A patent/CN102802661B/zh not_active Expired - Fee Related
- 2010-06-21 JP JP2012517629A patent/JP5918129B2/ja not_active Expired - Fee Related
- 2010-06-21 EP EP13182099.5A patent/EP2711018A1/en not_active Ceased
- 2010-06-21 MX MX2012000121A patent/MX2012000121A/es not_active Application Discontinuation
- 2010-06-21 CA CA2766405A patent/CA2766405A1/en not_active Abandoned
- 2010-06-21 WO PCT/US2010/039351 patent/WO2011005481A1/en not_active Ceased
- 2010-06-21 EP EP10797547A patent/EP2445520A4/en not_active Withdrawn
- 2010-06-21 AU AU2010270979A patent/AU2010270979B2/en not_active Ceased
-
2015
- 2015-06-22 US US14/745,882 patent/US20160017023A1/en not_active Abandoned
-
2016
- 2016-04-07 JP JP2016076919A patent/JP2016183155A/ja not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| JP2012530514A (ja) | 2012-12-06 |
| CN102802661B (zh) | 2016-01-13 |
| MX2012000121A (es) | 2012-03-07 |
| AU2010270979A1 (en) | 2012-01-12 |
| EP2711018A1 (en) | 2014-03-26 |
| US20160017023A1 (en) | 2016-01-21 |
| JP2016183155A (ja) | 2016-10-20 |
| US20120213705A1 (en) | 2012-08-23 |
| EP2445520A1 (en) | 2012-05-02 |
| WO2011005481A1 (en) | 2011-01-13 |
| AU2010270979B2 (en) | 2015-04-23 |
| JP5918129B2 (ja) | 2016-05-18 |
| BRPI1015234A2 (pt) | 2018-02-20 |
| CN102802661A (zh) | 2012-11-28 |
| EP2445520A4 (en) | 2013-03-06 |
| CA2766405A1 (en) | 2011-01-13 |
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