CA2876365A1 - Novel process for preparation of antibody conjugates and novel antibody conjugates - Google Patents

Novel process for preparation of antibody conjugates and novel antibody conjugates Download PDF

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Publication number
CA2876365A1
CA2876365A1 CA 2876365 CA2876365A CA2876365A1 CA 2876365 A1 CA2876365 A1 CA 2876365A1 CA 2876365 CA2876365 CA 2876365 CA 2876365 A CA2876365 A CA 2876365A CA 2876365 A1 CA2876365 A1 CA 2876365A1
Authority
CA
Canada
Prior art keywords
antibody
ser
group
pro
cysteine
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA 2876365
Other languages
English (en)
French (fr)
Inventor
John Burt
Antony Godwin
George Badescu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Abzena (UK) Ltd
Original Assignee
Polytherics Ltd
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
Priority claimed from GBGB1210838.7A external-priority patent/GB201210838D0/en
Priority claimed from GB201306706A external-priority patent/GB201306706D0/en
Application filed by Polytherics Ltd filed Critical Polytherics Ltd
Publication of CA2876365A1 publication Critical patent/CA2876365A1/en
Abandoned legal-status Critical Current

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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
    • 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
    • A61K47/6851—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
    • 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 [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2863—Immunoglobulins [IG], 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 [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/32—Immunoglobulins [IG], 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Cell Biology (AREA)
  • Oncology (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)
CA 2876365 2012-06-19 2013-06-19 Novel process for preparation of antibody conjugates and novel antibody conjugates Abandoned CA2876365A1 (en)

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

Publications (1)

Publication Number Publication Date
CA2876365A1 true CA2876365A1 (en) 2013-12-27

Family

ID=48699187

Family Applications (1)

Application Number Title Priority Date Filing Date
CA 2876365 Abandoned CA2876365A1 (en) 2012-06-19 2013-06-19 Novel process for preparation of antibody conjugates and novel antibody conjugates

Country Status (16)

Country Link
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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US20150290342A1 (en) * 2012-10-24 2015-10-15 Polytherics Limited Drug-protein conjugates
NO2789793T3 (enExample) * 2012-10-24 2018-01-27
EP3964237B1 (en) 2013-03-15 2026-02-18 Regeneron Pharmaceuticals, Inc. Biologically active molecules, conjugates thereof, and therapeutic uses
KR102252925B1 (ko) 2013-08-26 2021-05-18 리제너론 파마슈티칼스 인코포레이티드 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도
EP3145552B1 (en) 2014-05-23 2020-03-04 Novartis AG Methods for making conjugates from disulfide-containing proteins
WO2015187596A2 (en) * 2014-06-02 2015-12-10 Regeneron Pharmaceuticals, Inc. Biologically active molecule conjugates, reagents and methods of manufacture, and therapeutic uses
KR102463267B1 (ko) 2014-07-24 2022-11-03 제넨테크, 인크. 적어도 하나의 트리설파이드 결합을 함유하는 단백질에서 티올 모이어티에 제제의 접합 방법
WO2016059377A1 (en) 2014-10-14 2016-04-21 Polytherics Limited Process for the conjugation of a peptide or protein with a reagent comprising a leaving group including a portion of peg
ES2960741T3 (es) * 2014-10-24 2024-03-06 Abzena Uk Ltd Conjugados y reactivos de conjugación
US10077287B2 (en) 2014-11-10 2018-09-18 Bristol-Myers Squibb Company Tubulysin analogs and methods of making and use
MA40725A (fr) * 2014-12-08 2017-10-18 Sorrento Therapeutics Inc Conjugué anticorps anti-c-met-médicament
KR20170102981A (ko) 2015-01-14 2017-09-12 브리스톨-마이어스 스큅 컴퍼니 헤테로아릴렌-가교된 벤조디아제핀 이량체, 그의 접합체, 및 제조 및 사용 방법
WO2016124781A1 (en) * 2015-02-05 2016-08-11 Ablynx N.V. Nanobody dimers linked via c-terminally engineered cysteins
KR20240142591A (ko) 2015-03-27 2024-09-30 리제너론 파아마슈티컬스, 인크. 메이탄시노이드 유도체, 이의 컨주게이트, 및 사용 방법
EP3331569A1 (en) 2015-08-07 2018-06-13 Gamamabs Pharma Antibodies, antibody drug conjugates and methods of use
CN107029242A (zh) 2015-11-03 2017-08-11 财团法人工业技术研究院 抗体药物复合物及其制造方法
MY198605A (en) 2016-01-25 2023-09-08 Regeneron Pharma Maytansinoid derivatives conjugates thereof, and methods of use
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
SG11201903605TA (en) * 2016-11-07 2019-05-30 Seattle Genetics Inc Distribution of engineered-cysteine caps
US11376317B2 (en) 2017-08-30 2022-07-05 University Of Maryland, College Park FcRn-targeted mucosal vaccination against RSV
FI3765525T3 (fi) * 2018-03-13 2023-10-16 Zymeworks Bc Inc Biparatooppisen her2-vasta-aineen ja lääkkeen konjugaatteja ja käyttömenetelmiä
US11591371B2 (en) 2018-04-02 2023-02-28 University Of Maryland, College Park FcRn-targeted mucosal vaccination against influenza infections
GB201820864D0 (en) * 2018-12-20 2019-02-06 J A Kemp Antibody-drug conjugates
CN117679532A (zh) 2019-02-15 2024-03-12 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
US12109273B2 (en) 2019-02-15 2024-10-08 Wuxi Xdc Singapore Private Limited Process for preparing antibody-drug conjugates with improved homogeneity
CN115066263A (zh) * 2019-11-18 2022-09-16 克莱奥药品有限公司 定向缀合技术
WO2021174128A1 (en) * 2020-02-26 2021-09-02 University Of Maryland, College Park Compositions and methods for mucosal vaccination against sars-cov-2
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
CN117147825A (zh) * 2022-05-29 2023-12-01 菲鹏生物股份有限公司 一种抗体缀合物及其应用

Family Cites Families (8)

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Publication number Priority date Publication date Assignee Title
GB0316294D0 (en) * 2003-07-11 2003-08-13 Polytherics Ltd Conjugated biological molecules and their preparation
AU2005316844A1 (en) * 2004-11-29 2006-06-22 Seattle Genetics, Inc. Engineered antibodies and immunoconjugates
WO2009006520A1 (en) * 2007-07-03 2009-01-08 Medimmune, Llc Hinge domain engineering
PT2247620T (pt) * 2008-01-31 2016-08-23 Genentech Inc Anticorpos e imunoconjugados anti-cd79b e métodos de utilização
WO2009130602A2 (en) * 2008-04-24 2009-10-29 Celtic Pharma Peg Ltd. Factor ix conjugates with extended half-lives
WO2011060018A2 (en) * 2009-11-13 2011-05-19 Ikaria Development Subsidiary Two Llc Compositions and methods for using peptides, modified peptides, peptidomimetics and fibrin derivatives
UY33827A (es) * 2010-12-22 2012-07-31 Abbott Lab Proteínas de unión a media-inmunoglobulina y sus usos
WO2013132268A1 (en) * 2012-03-09 2013-09-12 Ucl Business Plc Chemical modification of antibodies

Also Published As

Publication number Publication date
JP2015521615A (ja) 2015-07-30
HK1204924A1 (en) 2015-12-11
IN2014DN10428A (enExample) 2015-08-21
WO2013190292A3 (en) 2014-03-20
EP2861261A2 (en) 2015-04-22
AU2013279099A1 (en) 2014-12-18
BR112014031613A2 (pt) 2017-07-25
ZA201408916B (en) 2015-11-25
US20150125473A1 (en) 2015-05-07
SG11201407600UA (en) 2014-12-30
KR20150023027A (ko) 2015-03-04
RU2015101333A (ru) 2016-08-10
CN104379178A (zh) 2015-02-25
WO2013190292A2 (en) 2013-12-27
MX2014015682A (es) 2015-07-23
IL235646A0 (en) 2015-01-29

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20180619