CA2884299A1 - Novel drug-protein conjugates - Google Patents

Novel drug-protein conjugates Download PDF

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Publication number
CA2884299A1
CA2884299A1 CA2884299A CA2884299A CA2884299A1 CA 2884299 A1 CA2884299 A1 CA 2884299A1 CA 2884299 A CA2884299 A CA 2884299A CA 2884299 A CA2884299 A CA 2884299A CA 2884299 A1 CA2884299 A1 CA 2884299A1
Authority
CA
Canada
Prior art keywords
group
conjugate
linker
auristatin
formula
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
CA2884299A
Other languages
English (en)
French (fr)
Inventor
John Burt
Antony Godwin
Mark Frigerio
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 PCT/GB2013/051593 external-priority patent/WO2013190292A2/en
Application filed by Polytherics Ltd filed Critical Polytherics Ltd
Publication of CA2884299A1 publication Critical patent/CA2884299A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6889Conjugates 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/68031Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
    • A61K47/6851Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cell Biology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Molecular Biology (AREA)
CA2884299A 2012-10-24 2013-10-11 Novel drug-protein conjugates Abandoned CA2884299A1 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201261717743P 2012-10-24 2012-10-24
US201261717710P 2012-10-24 2012-10-24
US61/717,743 2012-10-24
US61/717,710 2012-10-24
US201361811285P 2013-04-12 2013-04-12
US61/811,285 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
GBPCT/GB2013/051593 2013-06-19
PCT/GB2013/052661 WO2014064423A1 (en) 2012-10-24 2013-10-11 Drug-protein conjugates

Publications (1)

Publication Number Publication Date
CA2884299A1 true CA2884299A1 (en) 2014-05-01

Family

ID=50544085

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2884299A Abandoned CA2884299A1 (en) 2012-10-24 2013-10-11 Novel drug-protein conjugates

Country Status (18)

Country Link
US (2) US20150290342A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EP (2) EP3159013A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
JP (1) JP6328648B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
KR (1) KR102209395B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CN (1) CN104870021B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AU (1) AU2013336409B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
BR (1) BR112015008376A2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CA (1) CA2884299A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
DK (1) DK2911700T5 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ES (1) ES2623209T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IL (1) IL237672B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IN (1) IN2015DN02349A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MX (1) MX2015005122A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MY (1) MY169147A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
RU (1) RU2015119561A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SG (1) SG11201501618WA (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
WO (1) WO2014064423A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ZA (1) ZA201501642B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105658240A (zh) 2013-06-04 2016-06-08 西托姆克斯治疗公司 用于缀合可活化抗体的组合物和方法
SI3057585T1 (sl) 2013-10-15 2020-12-31 Seagen Inc. Pegilirani linkerji zdravila za izboljšano farmakokinetiko konjugata ligand-zdravilo
ES2792598T3 (es) * 2014-05-23 2020-11-11 Novartis Ag Métodos para preparar conjugados a partir de proteínas que contienen disulfuro
US10357472B2 (en) * 2014-06-12 2019-07-23 Cspc Dophen Corporation Homogenous antibody drug conjugates via enzymatic methods
EP3218009B1 (en) * 2014-10-14 2021-04-07 Polytherics Limited Process for the conjugation of a peptide or protein with a reagent comprising a leaving group including a portion of peg
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
GB201419108D0 (en) 2014-10-27 2014-12-10 Glythera Ltd Materials and methods relating to linkers for use in antibody drug conjugates
EP3165237B1 (en) 2015-11-03 2018-12-19 Industrial Technology Research Institute Antibody-drug conjugate (adc) and method for forming the same
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
ES2919323T3 (es) 2015-12-04 2022-07-26 Seagen Inc Conjugados de compuestos de tubulisina cuaternizados
WO2017161206A1 (en) 2016-03-16 2017-09-21 Halozyme, Inc. Conjugates containing conditionally active antibodies or antigen-binding fragments thereof, and methods of use
US11844839B2 (en) 2016-03-25 2023-12-19 Seagen Inc. Process for the preparation of pegylated drug-linkers and intermediates thereof
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
GB201608936D0 (en) * 2016-05-20 2016-07-06 Polytherics Ltd Novel conjugates and novel conjugating reagents
CN109311996B (zh) * 2016-06-06 2023-11-28 阿布泽纳(英国)有限公司 抗体、其用途及其缀合物
GB201614162D0 (en) * 2016-08-18 2016-10-05 Polytherics Ltd Antibodies, uses thereof and conjugates thereof
SG11201908325PA (en) 2017-03-24 2019-10-30 Seattle Genetics Inc Process for the preparation of glucuronide drug-linkers and intermediates thereof
GB201820864D0 (en) * 2018-12-20 2019-02-06 J A Kemp Antibody-drug conjugates
AU2021256223B2 (en) * 2020-04-15 2024-04-18 Shenzhen Enduring Biotech, Ltd. Antibody-drug conjugate
KR20230159463A (ko) * 2021-03-19 2023-11-21 선전 엔듀어링 바이오테크 리미티드 Cd3 및 cd19에 대해 이중 특이성을 갖는 페길화된 t 세포 인게이저
WO2023141855A1 (en) * 2022-01-27 2023-08-03 Glyco-Therapy Biotechnology Co., Ltd. Protein conjugates with multiple payloads and methods for making the same
TW202444426A (zh) * 2023-03-29 2024-11-16 美商艾克塞里克斯公司 Amhrii抗體-藥物結合物及其用途

Family Cites Families (11)

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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
CN107213469A (zh) 2003-11-06 2017-09-29 西雅图基因公司 能够与配体偶联的单甲基缬氨酸化合物
AU2006294554B2 (en) * 2005-09-26 2013-03-21 E. R. Squibb & Sons, L.L.C. Antibody-drug conjugates and methods of use
DK2211904T3 (en) * 2007-10-19 2016-10-24 Seattle Genetics Inc Cd19-binding agents and uses thereof
WO2009117531A1 (en) 2008-03-18 2009-09-24 Seattle Genetics, Inc. Auristatin drug linker conjugates
WO2009134952A2 (en) * 2008-04-30 2009-11-05 Immunogen, Inc Potent conjugates and hydrophilic linkers
WO2010100430A1 (en) 2009-03-04 2010-09-10 Polytherics Limited Conjugated proteins and peptides
EP2414399A1 (en) * 2009-04-01 2012-02-08 F. Hoffmann-La Roche AG Anti-fcrh5 antibodies and immunoconjugates and methods of use
UY32913A (es) * 2009-10-02 2011-04-29 Sanofi Aventis Nuevos maitansinoides y el uso de dichos maitansinoides para preparar conjugados con un anticuero
RU2620864C2 (ru) * 2012-04-25 2017-05-30 Конинклейке Филипс Н.В. Система и способ для определения местоположения градиентной катушки
JP2015521615A (ja) * 2012-06-19 2015-07-30 ポリセリックス・リミテッド 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

Also Published As

Publication number Publication date
EP2911700A1 (en) 2015-09-02
KR102209395B1 (ko) 2021-01-28
US20150290342A1 (en) 2015-10-15
CN104870021B (zh) 2018-03-13
EP3159013A1 (en) 2017-04-26
MY169147A (en) 2019-02-18
JP6328648B2 (ja) 2018-05-23
IL237672A0 (en) 2015-04-30
US20220062436A1 (en) 2022-03-03
EP2911700B1 (en) 2017-02-08
IN2015DN02349A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2015-08-28
ES2623209T3 (es) 2017-07-10
RU2015119561A (ru) 2016-12-20
IL237672B (en) 2018-02-28
SG11201501618WA (en) 2015-04-29
AU2013336409B2 (en) 2017-08-03
BR112015008376A2 (pt) 2017-09-26
JP2015533847A (ja) 2015-11-26
MX2015005122A (es) 2015-10-29
ZA201501642B (en) 2016-01-27
DK2911700T5 (en) 2017-05-22
DK2911700T3 (en) 2017-05-15
KR20150103656A (ko) 2015-09-11
HK1208187A1 (en) 2016-02-26
AU2013336409A1 (en) 2015-04-02
CN104870021A (zh) 2015-08-26
WO2014064423A1 (en) 2014-05-01

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20191011

FZDE Discontinued

Effective date: 20191011