HK1203364A1 - Use of n-hydroxysuccinimide to improve conjugate stability - Google Patents

Use of n-hydroxysuccinimide to improve conjugate stability Download PDF

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Publication number
HK1203364A1
HK1203364A1 HK15103864.0A HK15103864A HK1203364A1 HK 1203364 A1 HK1203364 A1 HK 1203364A1 HK 15103864 A HK15103864 A HK 15103864A HK 1203364 A1 HK1203364 A1 HK 1203364A1
Authority
HK
Hong Kong
Prior art keywords
hydroxysuccinimide
nhs
conjugate stability
improve conjugate
improve
Prior art date
Application number
HK15103864.0A
Other languages
English (en)
Chinese (zh)
Inventor
Fang Liu
Godfrey W. Amphlett
Deborah H. Meshulam
Original Assignee
Immunogen, Inc.
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
Application filed by Immunogen, Inc. filed Critical Immunogen, Inc.
Publication of HK1203364A1 publication Critical patent/HK1203364A1/xx

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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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39591—Stabilisation, fragmentation
    • 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
    • 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
    • A61K47/68033—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
    • 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
    • A61K47/6857—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 the tumour determinant being from lung cancer cell
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Cell Biology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
HK15103864.0A 2011-12-13 2012-12-13 Use of n-hydroxysuccinimide to improve conjugate stability HK1203364A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161570139P 2011-12-13 2011-12-13
US61/570,139 2011-12-13
PCT/US2012/069527 WO2013090590A1 (en) 2011-12-13 2012-12-13 Use of n-hydroxysuccinimide to improve conjugate stability

Publications (1)

Publication Number Publication Date
HK1203364A1 true HK1203364A1 (en) 2015-10-30

Family

ID=48613179

Family Applications (1)

Application Number Title Priority Date Filing Date
HK15103864.0A HK1203364A1 (en) 2011-12-13 2012-12-13 Use of n-hydroxysuccinimide to improve conjugate stability

Country Status (14)

Country Link
US (1) US20140350228A1 (cg-RX-API-DMAC10.html)
EP (1) EP2790724A4 (cg-RX-API-DMAC10.html)
JP (1) JP2015504869A (cg-RX-API-DMAC10.html)
KR (1) KR20140107418A (cg-RX-API-DMAC10.html)
CN (1) CN104093425A (cg-RX-API-DMAC10.html)
AU (1) AU2012352210A1 (cg-RX-API-DMAC10.html)
BR (1) BR112014014464A8 (cg-RX-API-DMAC10.html)
CA (1) CA2859444A1 (cg-RX-API-DMAC10.html)
EA (1) EA201491173A1 (cg-RX-API-DMAC10.html)
HK (1) HK1203364A1 (cg-RX-API-DMAC10.html)
IL (1) IL233086A0 (cg-RX-API-DMAC10.html)
MX (1) MX2014007125A (cg-RX-API-DMAC10.html)
SG (2) SG11201403179QA (cg-RX-API-DMAC10.html)
WO (1) WO2013090590A1 (cg-RX-API-DMAC10.html)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7811572B2 (en) 2005-08-24 2010-10-12 Immunogen, Inc. Process for preparing purified drug conjugates
JP5784592B2 (ja) 2009-06-03 2015-09-24 イミュノジェン・インコーポレーテッド 抱合方法
EA033468B1 (ru) 2011-03-29 2019-10-31 Immunogen Inc Способы получения конъюгата "антитело-майтансиноид"
EP2904089A4 (en) 2012-10-04 2016-05-25 Immunogen Inc USE OF A PVDF MEMBRANE FOR PURIFYING CELL BINDING AGENT-CYTOTOXIC AGENT CONJUGATES
KR20160042871A (ko) * 2013-06-21 2016-04-20 이나뜨 파르마, 에스.아. 폴리펩티드의 효소적 콘쥬게이션
CN106267225B (zh) * 2015-05-29 2020-03-06 上海新理念生物医药科技有限公司 三马来酰亚胺型连接子及其应用
CN109152845B (zh) 2016-04-14 2022-07-12 宝力泰锐克斯有限公司 含有在环内包含至少两个(-ch2-ch2-o-)单元的接头的缀合物和缀合试剂
GB201615725D0 (en) 2016-09-15 2016-11-02 Polytherics Ltd Novel cytotoxic agents and conjugates thereof
CN113336823A (zh) * 2021-05-28 2021-09-03 联宁（苏州）生物制药有限公司 一种用于抗体偶联药物连接子lnd1067的合成方法
WO2025151380A1 (en) * 2024-01-08 2025-07-17 Azvlz, Inc. Functionalized conjugation crosslinkers and uses thereof

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2835829B1 (fr) * 2002-02-13 2007-09-14 Centre Nat Rech Scient Nouveau procede de preparation de biopuces a adn ou a proteines et leurs applications
DE10242076A1 (de) * 2002-09-11 2004-03-25 Fresenius Kabi Deutschland Gmbh HAS-Allergen-Konjugate
US7811572B2 (en) * 2005-08-24 2010-10-12 Immunogen, Inc. Process for preparing purified drug conjugates
WO2007059195A1 (en) * 2005-11-14 2007-05-24 University Of Southern California Integrin-binding small molecules
PT2019104E (pt) * 2007-07-19 2013-12-03 Sanofi Sa Agentes citotóxicos compreendendo novos derivados de tomaimicina e sua utilização terapêutica
CA3014224C (en) * 2009-02-05 2022-05-24 Immunogen, Inc. Condensed benzodiazepine-indoline derivatives and processes to prepare said derivatives
JP5784592B2 (ja) * 2009-06-03 2015-09-24 イミュノジェン・インコーポレーテッド 抱合方法

Also Published As

Publication number Publication date
AU2012352210A1 (en) 2014-07-24
BR112014014464A2 (pt) 2017-06-13
SG11201403179QA (en) 2014-07-30
BR112014014464A8 (pt) 2017-06-13
EA201491173A1 (ru) 2014-11-28
KR20140107418A (ko) 2014-09-04
MX2014007125A (es) 2015-04-16
WO2013090590A1 (en) 2013-06-20
EP2790724A1 (en) 2014-10-22
CA2859444A1 (en) 2013-06-20
IL233086A0 (en) 2014-07-31
CN104093425A (zh) 2014-10-08
SG10201604747WA (en) 2016-08-30
EP2790724A4 (en) 2015-08-05
JP2015504869A (ja) 2015-02-16
US20140350228A1 (en) 2014-11-27

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