JP2015504869A - 複合体安定性を改善するためのn−ヒドロキシスクシンイミドの使用 - Google Patents

複合体安定性を改善するためのn−ヒドロキシスクシンイミドの使用 Download PDF

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Publication number
JP2015504869A
JP2015504869A JP2014547433A JP2014547433A JP2015504869A JP 2015504869 A JP2015504869 A JP 2015504869A JP 2014547433 A JP2014547433 A JP 2014547433A JP 2014547433 A JP2014547433 A JP 2014547433A JP 2015504869 A JP2015504869 A JP 2015504869A
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Prior art keywords
cell binding
binding agent
mixture
cytotoxic agent
agent
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Japanese (ja)
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JP2015504869A5 (enExample
Inventor
リウ,ファング
アンフレット,ゴッドフレー・ダブリュー
メシュラム,デボラ・エイチ
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イミュノジェン・インコーポレーテッド
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Publication of JP2015504869A5 publication Critical patent/JP2015504869A5/ja
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    • 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
    • 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
    • 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
    • A61K47/68033—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
    • 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

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Cell Biology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2014547433A 2011-12-13 2012-12-13 複合体安定性を改善するためのn−ヒドロキシスクシンイミドの使用 Pending JP2015504869A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161570139P 2011-12-13 2011-12-13
US61/570,139 2011-12-13
PCT/US2012/069527 WO2013090590A1 (en) 2011-12-13 2012-12-13 Use of n-hydroxysuccinimide to improve conjugate stability

Publications (2)

Publication Number Publication Date
JP2015504869A true JP2015504869A (ja) 2015-02-16
JP2015504869A5 JP2015504869A5 (enExample) 2016-01-28

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JP2014547433A Pending JP2015504869A (ja) 2011-12-13 2012-12-13 複合体安定性を改善するためのn−ヒドロキシスクシンイミドの使用

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Country Link
US (1) US20140350228A1 (enExample)
EP (1) EP2790724A4 (enExample)
JP (1) JP2015504869A (enExample)
KR (1) KR20140107418A (enExample)
CN (1) CN104093425A (enExample)
AU (1) AU2012352210A1 (enExample)
BR (1) BR112014014464A8 (enExample)
CA (1) CA2859444A1 (enExample)
EA (1) EA201491173A1 (enExample)
HK (1) HK1203364A1 (enExample)
IL (1) IL233086A0 (enExample)
MX (1) MX2014007125A (enExample)
SG (2) SG11201403179QA (enExample)
WO (1) WO2013090590A1 (enExample)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7811572B2 (en) 2005-08-24 2010-10-12 Immunogen, Inc. Process for preparing purified drug conjugates
JP5784592B2 (ja) 2009-06-03 2015-09-24 イミュノジェン・インコーポレーテッド 抱合方法
EA033468B1 (ru) 2011-03-29 2019-10-31 Immunogen Inc Способы получения конъюгата "антитело-майтансиноид"
EP2904089A4 (en) 2012-10-04 2016-05-25 Immunogen Inc USE OF A PVDF MEMBRANE FOR PURIFYING CELL BINDING AGENT-CYTOTOXIC AGENT CONJUGATES
KR20160042871A (ko) * 2013-06-21 2016-04-20 이나뜨 파르마, 에스.아. 폴리펩티드의 효소적 콘쥬게이션
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
CN109152845B (zh) 2016-04-14 2022-07-12 宝力泰锐克斯有限公司 含有在环内包含至少两个(-ch2-ch2-o-)单元的接头的缀合物和缀合试剂
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
WO2025151380A1 (en) * 2024-01-08 2025-07-17 Azvlz, Inc. Functionalized conjugation crosslinkers and uses thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009506032A (ja) * 2005-08-24 2009-02-12 イムノゲン インコーポレーティッド メイタンシノイド(maytansinoid)抗体複合体の調製方法
WO2010141566A1 (en) * 2009-06-03 2010-12-09 Immunogen, Inc. Conjugation methods

Family Cites Families (5)

* 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
WO2007059195A1 (en) * 2005-11-14 2007-05-24 University Of Southern California Integrin-binding small molecules
PT2019104E (pt) * 2007-07-19 2013-12-03 Sanofi Sa Agentes citotóxicos compreendendo novos derivados de tomaimicina e sua utilização terapêutica
CA3014224C (en) * 2009-02-05 2022-05-24 Immunogen, Inc. Condensed benzodiazepine-indoline derivatives and processes to prepare said derivatives

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009506032A (ja) * 2005-08-24 2009-02-12 イムノゲン インコーポレーティッド メイタンシノイド(maytansinoid)抗体複合体の調製方法
WO2010141566A1 (en) * 2009-06-03 2010-12-09 Immunogen, Inc. Conjugation methods

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ANALYTICAL BIOCHEMISTRY, vol. 218, JPN7016002466, 1994, pages 87 - 91, ISSN: 0003384705 *

Also Published As

Publication number Publication date
AU2012352210A1 (en) 2014-07-24
BR112014014464A2 (pt) 2017-06-13
SG11201403179QA (en) 2014-07-30
BR112014014464A8 (pt) 2017-06-13
EA201491173A1 (ru) 2014-11-28
KR20140107418A (ko) 2014-09-04
MX2014007125A (es) 2015-04-16
WO2013090590A1 (en) 2013-06-20
EP2790724A1 (en) 2014-10-22
CA2859444A1 (en) 2013-06-20
IL233086A0 (en) 2014-07-31
HK1203364A1 (en) 2015-10-30
CN104093425A (zh) 2014-10-08
SG10201604747WA (en) 2016-08-30
EP2790724A4 (en) 2015-08-05
US20140350228A1 (en) 2014-11-27

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