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)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Cell Biology (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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
GB201306706A GB201306706D0 (en) 2013-04-12 2013-04-12 Novel process for preparation of antibody conjugates and novel antibody conjugates
GB1306706.1 2013-04-12
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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JP2015517843A Pending JP2015521615A (ja) 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

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

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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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NO2789793T3 (enExample) * 2012-10-24 2018-01-27
MY183572A (en) 2013-03-15 2021-02-26 Regeneron Pharma Biologically active molecules, conjugates thereof, and therapeutic uses
CN105530942B (zh) 2013-08-26 2019-10-11 瑞泽恩制药公司 一种包含大环内酯类非对映体的药物组合物、其制备方法和用途
EP3145552B1 (en) * 2014-05-23 2020-03-04 Novartis AG Methods for making conjugates from disulfide-containing proteins
HK1231367A1 (zh) 2014-06-02 2017-12-22 Regeneron Pharmaceuticals, Inc. 抗体药物偶联物、试剂和制备方法及其治疗用途
AU2015294389B2 (en) * 2014-07-24 2021-04-29 Genentech, Inc. Methods of conjugating an agent to a thiol moiety in a protein that contains at least one trisulfide bond
KR20230158134A (ko) 2014-10-14 2023-11-17 폴리테릭스 리미티드 Peg의 일부를 포함하는 이탈기를 포함하는 시약을 사용한, 펩티드 또는 단백질의 접합방법
JP6612860B2 (ja) * 2014-10-24 2019-11-27 ポリセリックス・リミテッド コンジュゲート及びコンジュゲート試薬
US10077287B2 (en) 2014-11-10 2018-09-18 Bristol-Myers Squibb Company Tubulysin analogs and methods of making and use
SG11201704458SA (en) * 2014-12-08 2017-06-29 Sorrento Therapeutics Inc C-met antibody drug conjugate
ES2747386T3 (es) 2015-01-14 2020-03-10 Bristol Myers Squibb Co Dímeros de benzodiacepina unidos por heteroarileno, conjugados de los mismos y métodos de preparación y uso
WO2016124781A1 (en) * 2015-02-05 2016-08-11 Ablynx N.V. Nanobody dimers linked via c-terminally engineered cysteins
MX386328B (es) 2015-03-27 2025-03-18 Regeneron Pharma Derivados de maitansinoide, conjugados de los mismos, y metodos de uso.
US10509035B2 (en) 2015-08-07 2019-12-17 Gamamabs Pharma Sa Antibodies, antibody drug conjugates and methods of use
EP3165237B1 (en) 2015-11-03 2018-12-19 Industrial Technology Research Institute Antibody-drug conjugate (adc) and method for forming the same
MX390630B (es) 2016-01-25 2025-03-21 Regeneron Pharma Derivados de maitansinoide, conjugados de los mismos y metodos de uso.
WO2017178828A1 (en) * 2016-04-14 2017-10-19 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
KR102788989B1 (ko) 2019-02-15 2025-03-31 우시 엑스디씨 싱가포르 프라이빗 리미티드 동질성이 개선된 항체-약물 콘쥬게이트의 제조방법
US12109273B2 (en) 2019-02-15 2024-10-08 Wuxi Xdc Singapore Private Limited Process for preparing antibody-drug conjugates with improved homogeneity
JP2023501720A (ja) * 2019-11-18 2023-01-18 クレオ ファーマシューティカルズ， インコーポレイテッド 指向性コンジュゲーション技術
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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
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
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
US12357701B2 (en) 2018-03-13 2025-07-15 Zymeworks Bc Inc. Anti-HER2 biparatopic antibody-drug conjugates and methods of use
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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US20150125473A1 (en) 2015-05-07
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