JP2015521615A - 抗体コンジュゲートの調製のための新規方法及び新規抗体コンジュゲート - Google Patents

抗体コンジュゲートの調製のための新規方法及び新規抗体コンジュゲート Download PDF

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JP2015521615A
JP2015521615A JP2015517843A JP2015517843A JP2015521615A JP 2015521615 A JP2015521615 A JP 2015521615A JP 2015517843 A JP2015517843 A JP 2015517843A JP 2015517843 A JP2015517843 A JP 2015517843A JP 2015521615 A JP2015521615 A JP 2015521615A
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antibody
conjugate
cysteine
group
heavy chain
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Japanese (ja)
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ジョン・バート
アントニー・ゴドウィン
ジョージ・バデスク
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ポリセリックス・リミテッド
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Priority claimed from GBGB1210838.7A external-priority patent/GB201210838D0/en
Priority claimed from GB201306706A external-priority patent/GB201306706D0/en
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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
    • A61K47/50—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
    • A61K47/50—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • 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
    • A61K47/68031—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
    • 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
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • 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
    • A61K47/6871—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 an enzyme
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2863—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for growth factors, growth regulators
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07K16/32—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/52—Constant or Fc region; Isotype
    • C07K2317/53—Hinge

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Oncology (AREA)
  • Cell Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2015517843A 2012-06-19 2013-06-19 抗体コンジュゲートの調製のための新規方法及び新規抗体コンジュゲート Pending JP2015521615A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GBGB1210838.7A GB201210838D0 (en) 2012-06-19 2012-06-19 Novel process for preparation of antibody conjugates and novel antibody conjugates
GB1210838.7 2012-06-19
GB1306706.1 2013-04-12
GB201306706A GB201306706D0 (en) 2013-04-12 2013-04-12 Novel process for preparation of antibody conjugates and novel antibody conjugates
PCT/GB2013/051593 WO2013190292A2 (en) 2012-06-19 2013-06-19 Novel process for preparation of antibody conjugates and novel antibody conjugates

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JP2015521615A true JP2015521615A (ja) 2015-07-30

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US (1) US20150125473A1 (cg-RX-API-DMAC7.html)
EP (1) EP2861261A2 (cg-RX-API-DMAC7.html)
JP (1) JP2015521615A (cg-RX-API-DMAC7.html)
KR (1) KR20150023027A (cg-RX-API-DMAC7.html)
CN (1) CN104379178A (cg-RX-API-DMAC7.html)
AU (1) AU2013279099A1 (cg-RX-API-DMAC7.html)
BR (1) BR112014031613A2 (cg-RX-API-DMAC7.html)
CA (1) CA2876365A1 (cg-RX-API-DMAC7.html)
HK (1) HK1204924A1 (cg-RX-API-DMAC7.html)
IL (1) IL235646A0 (cg-RX-API-DMAC7.html)
IN (1) IN2014DN10428A (cg-RX-API-DMAC7.html)
MX (1) MX2014015682A (cg-RX-API-DMAC7.html)
RU (1) RU2015101333A (cg-RX-API-DMAC7.html)
SG (1) SG11201407600UA (cg-RX-API-DMAC7.html)
WO (1) WO2013190292A2 (cg-RX-API-DMAC7.html)
ZA (1) ZA201408916B (cg-RX-API-DMAC7.html)

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JP2015533847A (ja) * 2012-10-24 2015-11-26 ポリセリックス・リミテッド 新規薬物−タンパク質コンジュゲート
JP2019532663A (ja) * 2016-11-07 2019-11-14 シアトル ジェネティックス， インコーポレイテッド 工学的に操作されたシステインキャップの分配
JP2021515793A (ja) * 2018-03-13 2021-06-24 ザイムワークス，インコーポレイテッド 抗ｈｅｒ２バイパラトピック抗体−薬物コンジュゲート及び使用方法
JP2022516032A (ja) * 2018-12-20 2022-02-24 スパイリーア リミテッド 抗体－薬物複合体

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EP3038624B1 (en) 2013-08-26 2024-09-25 Regeneron Pharmaceuticals, Inc. Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses
US10406198B2 (en) 2014-05-23 2019-09-10 Novartis Ag Methods for making conjugates from disulfide-containing proteins
EP3148592A2 (en) 2014-06-02 2017-04-05 Regeneron Pharmaceuticals, Inc. Antibody-drug conjugates, their preparation and their therapeutic use
CN106536540A (zh) 2014-07-24 2017-03-22 基因泰克公司 将试剂缀合至含有至少一个三硫键的蛋白质中的巯基部分的方法
ES2885854T3 (es) 2014-10-14 2021-12-15 Polytherics Ltd Proceso para la conjugación de un péptido o proteína con un reactivo que comprende un grupo saliente que incluye una porción de PEG
US20170290925A1 (en) * 2014-10-24 2017-10-12 Polytherics Limited Conjugates And Conjugating Reagents
US10077287B2 (en) 2014-11-10 2018-09-18 Bristol-Myers Squibb Company Tubulysin analogs and methods of making and use
BR112017012042A2 (pt) * 2014-12-08 2018-01-16 Sorrento Therapeutics Inc composição de conjugado anticorpo-droga e método para tratar câncer de mama
CN107231804B (zh) 2015-01-14 2019-11-26 百时美施贵宝公司 亚杂芳基桥连苯并二氮杂*二聚体、其缀合物及制备和使用方法
HK1249528A1 (zh) * 2015-02-05 2018-11-02 Ablynx N.V. 通过c-末端合成半胱氨酸连接的纳米抗体二聚体
SG11201707148PA (en) 2015-03-27 2017-10-30 Regeneron Pharma Maytansinoid derivatives, conjugates thereof, and methods of use
US10509035B2 (en) 2015-08-07 2019-12-17 Gamamabs Pharma Sa Antibodies, antibody drug conjugates and methods of use
US10233212B2 (en) 2015-11-03 2019-03-19 Industrial Technology Research Institute Compounds, linker-drugs and ligand-drug conjugates
PH12018501589B1 (en) 2016-01-25 2022-08-10 Regeneron Pharma Maytansinoid derivatives, conjugates thereof, and methods of use
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
GB201614162D0 (en) * 2016-08-18 2016-10-05 Polytherics Ltd Antibodies, uses thereof and conjugates thereof
US11376317B2 (en) 2017-08-30 2022-07-05 University Of Maryland, College Park FcRn-targeted mucosal vaccination against RSV
US11591371B2 (en) 2018-04-02 2023-02-28 University Of Maryland, College Park FcRn-targeted mucosal vaccination against influenza infections
US12109273B2 (en) 2019-02-15 2024-10-08 Wuxi Xdc Singapore Private Limited Process for preparing antibody-drug conjugates with improved homogeneity
CN113423730B (zh) 2019-02-15 2024-01-05 上海药明合联生物技术有限公司 用于制备具有改善的同质性的抗体-药物缀合物的方法
BR112022009398A2 (pt) * 2019-11-18 2022-08-09 Kleo Pharmaceuticals Inc Tecnologias de conjugação direcionadas
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WO2021115497A2 (zh) * 2020-12-08 2021-06-17 和铂医药(上海)有限责任公司 蛋白-药物偶联物和定点偶联方法

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Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015533847A (ja) * 2012-10-24 2015-11-26 ポリセリックス・リミテッド 新規薬物−タンパク質コンジュゲート
JP2019532663A (ja) * 2016-11-07 2019-11-14 シアトル ジェネティックス， インコーポレイテッド 工学的に操作されたシステインキャップの分配
JP7073363B2 (ja) 2016-11-07 2022-05-23 シージェン インコーポレイテッド 工学的に操作されたシステインキャップの分配
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JP7547205B2 (ja) 2018-03-13 2024-09-09 ザイムワークス ビーシー インコーポレイテッド 抗ｈｅｒ２バイパラトピック抗体－薬物コンジュゲート及び使用方法
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AU2013279099A1 (en) 2014-12-18
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WO2013190292A2 (en) 2013-12-27
CN104379178A (zh) 2015-02-25
CA2876365A1 (en) 2013-12-27
MX2014015682A (es) 2015-07-23
IL235646A0 (en) 2015-01-29
US20150125473A1 (en) 2015-05-07
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RU2015101333A (ru) 2016-08-10
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