AU2013336409B2 - Drug-protein conjugates - Google Patents

Drug-protein conjugates Download PDF

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Publication number
AU2013336409B2
AU2013336409B2 AU2013336409A AU2013336409A AU2013336409B2 AU 2013336409 B2 AU2013336409 B2 AU 2013336409B2 AU 2013336409 A AU2013336409 A AU 2013336409A AU 2013336409 A AU2013336409 A AU 2013336409A AU 2013336409 B2 AU2013336409 B2 AU 2013336409B2
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AU
Australia
Prior art keywords
group
conjugate
linker
formula
integer
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Application number
AU2013336409A
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English (en)
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AU2013336409A1 (en
Inventor
George Badescu
John Burt
Mark Frigerio
Antony Godwin
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 AU2013336409A1 publication Critical patent/AU2013336409A1/en
Application granted granted Critical
Publication of AU2013336409B2 publication Critical patent/AU2013336409B2/en
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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)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cell Biology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Hematology (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Molecular Biology (AREA)
AU2013336409A 2012-10-24 2013-10-11 Drug-protein conjugates Active AU2013336409B2 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201261717710P 2012-10-24 2012-10-24
US201261717743P 2012-10-24 2012-10-24
US61/717,710 2012-10-24
US61/717,743 2012-10-24
US201361811285P 2013-04-12 2013-04-12
US61/811,285 2013-04-12
AUPCT/GB2013/051593 2013-06-19
PCT/GB2013/051593 WO2013190292A2 (en) 2012-06-19 2013-06-19 Novel process for preparation of antibody conjugates and novel antibody conjugates
PCT/GB2013/052661 WO2014064423A1 (en) 2012-10-24 2013-10-11 Drug-protein conjugates

Publications (2)

Publication Number Publication Date
AU2013336409A1 AU2013336409A1 (en) 2015-04-02
AU2013336409B2 true AU2013336409B2 (en) 2017-08-03

Family

ID=50544085

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2013336409A Active AU2013336409B2 (en) 2012-10-24 2013-10-11 Drug-protein conjugates

Country Status (18)

Country Link
US (2) US20150290342A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EP (2) EP2911700B1 (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)

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RU2015156888A (ru) 2013-06-04 2017-07-14 Сайтомкс Терапьютикс, Инк. Композиции и методы конъюгирования активируемых антител
AU2014337555C1 (en) 2013-10-15 2021-01-28 Seagen Inc. PEGylated drug-linkers for improved Ligand-Drug Conjugate pharmacokinetics
EP3145552B1 (en) * 2014-05-23 2020-03-04 Novartis AG Methods for making conjugates from disulfide-containing proteins
AU2015274506C1 (en) * 2014-06-12 2022-10-13 CSPC Megalith Biopharmaceutical Co., Ltd. Homogenous antibody drug conjugates via enzymatic methods
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
BR112017005760A2 (pt) * 2014-10-24 2017-12-12 Polytherics Ltd conjugados e reagentes de conjugação
GB201419108D0 (en) 2014-10-27 2014-12-10 Glythera Ltd Materials and methods relating to linkers for use in antibody drug conjugates
JP6486316B2 (ja) 2015-11-03 2019-03-20 財團法人工業技術研究院Industrial Technology Research Institute 抗体−薬物複合体(adc)およびそれを形成するための方法
JP2019501131A (ja) 2015-12-04 2019-01-17 シアトル ジェネティックス, インコーポレイテッド 四級化チューブリシン化合物の複合体
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
WO2017161206A1 (en) 2016-03-16 2017-09-21 Halozyme, Inc. Conjugates containing conditionally active antibodies or antigen-binding fragments thereof, and methods of use
KR20180134351A (ko) 2016-03-25 2018-12-18 시애틀 지네틱스, 인크. 페길화된 약물-링커 및 그의 중간체의 제조를 위한 공정
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
WO2017212250A1 (en) * 2016-06-06 2017-12-14 Polytherics Limited Antibodies, uses thereof and conjugates thereof
GB201614162D0 (en) * 2016-08-18 2016-10-05 Polytherics Ltd Antibodies, uses thereof and conjugates thereof
AU2018237683A1 (en) 2017-03-24 2019-10-31 Seagen 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
EP4117729A4 (en) * 2020-04-15 2023-11-15 Shenzhen Enduring Biotech, Ltd. ANTIBODY-DRUG CONJUGATE
JP2024510760A (ja) * 2021-03-19 2024-03-11 シェンチェン・エンデュアリング・バイオテック・リミテッド Cd3およびcd19に二重特異性を有するpeg化t細胞エンゲージャー
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

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Also Published As

Publication number Publication date
ES2623209T3 (es) 2017-07-10
DK2911700T3 (en) 2017-05-15
BR112015008376A2 (pt) 2017-09-26
EP2911700A1 (en) 2015-09-02
DK2911700T5 (en) 2017-05-22
KR102209395B1 (ko) 2021-01-28
JP6328648B2 (ja) 2018-05-23
IN2015DN02349A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2015-08-28
IL237672A0 (en) 2015-04-30
EP2911700B1 (en) 2017-02-08
IL237672B (en) 2018-02-28
CN104870021B (zh) 2018-03-13
SG11201501618WA (en) 2015-04-29
HK1208187A1 (en) 2016-02-26
JP2015533847A (ja) 2015-11-26
ZA201501642B (en) 2016-01-27
US20220062436A1 (en) 2022-03-03
WO2014064423A1 (en) 2014-05-01
CA2884299A1 (en) 2014-05-01
AU2013336409A1 (en) 2015-04-02
RU2015119561A (ru) 2016-12-20
EP3159013A1 (en) 2017-04-26
US20150290342A1 (en) 2015-10-15
CN104870021A (zh) 2015-08-26
MY169147A (en) 2019-02-18
KR20150103656A (ko) 2015-09-11
MX2015005122A (es) 2015-10-29

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