EA201491173A1 - Применение n-гидроксисукцинимида для улучшения стабильности конъюгатов - Google Patents

Применение n-гидроксисукцинимида для улучшения стабильности конъюгатов

Info

Publication number
EA201491173A1
EA201491173A1 EA201491173A EA201491173A EA201491173A1 EA 201491173 A1 EA201491173 A1 EA 201491173A1 EA 201491173 A EA201491173 A EA 201491173A EA 201491173 A EA201491173 A EA 201491173A EA 201491173 A1 EA201491173 A1 EA 201491173A1
Authority
EA
Eurasian Patent Office
Prior art keywords
hydroxisuuccinimide
application
nhs
conjugate stability
improve conjugate
Prior art date
Application number
EA201491173A
Other languages
English (en)
Inventor
Фан Лю
Годфри В. Эмфлетт
Дебора Х. Мешулам
Original Assignee
Иммуноджен, Инк.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Иммуноджен, Инк. filed Critical Иммуноджен, Инк.
Publication of EA201491173A1 publication Critical patent/EA201491173A1/ru

Links

Classifications

    • A—HUMAN NECESSITIES
    • 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
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • A—HUMAN NECESSITIES
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39591—Stabilisation, fragmentation
    • A—HUMAN NECESSITIES
    • 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
    • A—HUMAN NECESSITIES
    • 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
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A—HUMAN NECESSITIES
    • 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
    • A61K47/6851—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 the antibody targeting a determinant of a tumour cell
    • A61K47/6857—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 the antibody targeting a determinant of a tumour cell the tumour determinant being from lung cancer cell
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Abstract

В изобретении представлены способы производства конъюгатов клеточно-связывающего агента - цитотоксического агента с улучшенной стабильностью в присутствии экзогенного NHS. В некоторых вариантах реализации способ изобретения включает добавление молярного соотношения экзогенного NHS в отношении количества NHS, образующегося во время реакции модификации в результате гидролиза/аминолиза бифункционального линкера.
EA201491173A 2011-12-13 2012-12-13 Применение n-гидроксисукцинимида для улучшения стабильности конъюгатов EA201491173A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161570139P 2011-12-13 2011-12-13
PCT/US2012/069527 WO2013090590A1 (en) 2011-12-13 2012-12-13 Use of n-hydroxysuccinimide to improve conjugate stability

Publications (1)

Publication Number Publication Date
EA201491173A1 true EA201491173A1 (ru) 2014-11-28

Family

ID=48613179

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201491173A EA201491173A1 (ru) 2011-12-13 2012-12-13 Применение n-гидроксисукцинимида для улучшения стабильности конъюгатов

Country Status (14)

Country Link
US (1) US20140350228A1 (ru)
EP (1) EP2790724A4 (ru)
JP (1) JP2015504869A (ru)
KR (1) KR20140107418A (ru)
CN (1) CN104093425A (ru)
AU (1) AU2012352210A1 (ru)
BR (1) BR112014014464A2 (ru)
CA (1) CA2859444A1 (ru)
EA (1) EA201491173A1 (ru)
HK (1) HK1203364A1 (ru)
IL (1) IL233086A0 (ru)
MX (1) MX2014007125A (ru)
SG (2) SG11201403179QA (ru)
WO (1) WO2013090590A1 (ru)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3000520C (en) 2005-08-24 2023-04-04 Immunogen, Inc. Process for preparing antibody maytansinoid conjugates
KR102560218B1 (ko) 2009-06-03 2023-07-26 이뮤노젠 아이엔씨 접합 방법
PL2691155T3 (pl) 2011-03-29 2019-06-28 Immunogen, Inc. Otrzymywanie koniugatu majtansynoidu przeciwciała jednoetapowym sposobem
MX359599B (es) 2012-10-04 2018-09-12 Immunogen Inc Uso de una membrana de pvdf para purificar conjugados de agentes de unión celular y agentes citotóxicos.
CN105517577A (zh) * 2013-06-21 2016-04-20 先天制药公司 多肽的酶促偶联
CN106267225B (zh) * 2015-05-29 2020-03-06 上海新理念生物医药科技有限公司 三马来酰亚胺型连接子及其应用
EP3442595A1 (en) 2016-04-14 2019-02-20 Polytherics Limited Conjugates and conjugating reagents comprising a linker that includes at least two (-ch2-ch2-0-) units in a ring
GB201615725D0 (en) 2016-09-15 2016-11-02 Polytherics Ltd Novel cytotoxic agents and conjugates thereof
CN113336823A (zh) * 2021-05-28 2021-09-03 联宁（苏州）生物制药有限公司 一种用于抗体偶联药物连接子lnd1067的合成方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2835829B1 (fr) * 2002-02-13 2007-09-14 Centre Nat Rech Scient Nouveau procede de preparation de biopuces a adn ou a proteines et leurs applications
DE10242076A1 (de) * 2002-09-11 2004-03-25 Fresenius Kabi Deutschland Gmbh HAS-Allergen-Konjugate
CA3000520C (en) * 2005-08-24 2023-04-04 Immunogen, Inc. Process for preparing antibody maytansinoid conjugates
WO2007059195A1 (en) * 2005-11-14 2007-05-24 University Of Southern California Integrin-binding small molecules
DK2019104T3 (da) * 2007-07-19 2013-12-16 Sanofi Sa Cytotoksiske midler, der omfatter nye tomaymycinderivater, og terapeutisk anvendelse deraf
JP5977522B2 (ja) * 2009-02-05 2016-08-24 イミュノジェン・インコーポレーテッド 新規ベンゾジアゼピン誘導体
KR102560218B1 (ko) * 2009-06-03 2023-07-26 이뮤노젠 아이엔씨 접합 방법

Also Published As

Publication number Publication date
AU2012352210A1 (en) 2014-07-24
SG10201604747WA (en) 2016-08-30
JP2015504869A (ja) 2015-02-16
WO2013090590A1 (en) 2013-06-20
US20140350228A1 (en) 2014-11-27
KR20140107418A (ko) 2014-09-04
EP2790724A1 (en) 2014-10-22
MX2014007125A (es) 2015-04-16
CN104093425A (zh) 2014-10-08
BR112014014464A2 (pt) 2017-06-13
EP2790724A4 (en) 2015-08-05
CA2859444A1 (en) 2013-06-20
SG11201403179QA (en) 2014-07-30
IL233086A0 (en) 2014-07-31
HK1203364A1 (en) 2015-10-30

Similar Documents

Publication Publication Date Title
EA201491173A1 (ru) Применение n-гидроксисукцинимида для улучшения стабильности конъюгатов
NZ741211A (en) Self-stabilizing linker conjugates
MX339927B (es) Preparacion de conjugados de maitansinoides y anticuerpos mediante un proceso de una etapa.
EA201792652A2 (ru) Новые производные майтанзиноида с пептидным линкером и их конъюгаты
MX343337B (es) Metodos de preparacion de conjugados.
MY171008A (en) Preparation of maytansinoid antibody conjugates by a one-step process
EP4253395A3 (en) Processes for the preparation of carbohydrate conjugated rna agents
MX2019005879A (es) Enlazadores que contienen peptido para conjugados anticuerpo-farmaco.
PH12014502826A1 (en) Immunoconjugates comprising anti-cd79b antibodies
EA201590173A1 (ru) Иммуноконъюгаты, содержащие антитела к cd22
PH12015500667A1 (en) Antibody-drug conjugate
MY170719A (en) Antibody-drug conjugates
IN2014CN04961A (ru)
MX2018013332A (es) Conjugados de pirrolobenzodiazepina diana.
MY178680A (en) Hydrogel prodrugs
NZ703581A (en) Anti-cd70 antibody drug conjugates
SG195196A1 (en) Dual targeting
WO2013033438A3 (en) Nanoparticle peg modification with h-phosphonates
MX2016008189A (es) Conjugados helicoidales-anticuerpo anti-helicoidal unidos covalentemente y usos de los mismos.
MX2015002482A (es) Composicion inmunogenica.
MX2012000575A (es) Conjugados de epsilon-polilisina y uso de los mismos.
MX2019001093A (es) Profarmacos de metilfenidato, procesos de elaboracion y uso de los mismos.
WO2013103301A3 (en) Method for preparing cell targeting conjugates, and the complexes obtained
GB201103836D0 (en) Conjugation process
WO2013067199A3 (en) Subcutaneous delivery of polymer conjugates of therapeutic agents