KR102511249B1 - 신규한 안정한 항체-약물 복합체, 이의 제조방법 및 이의 용도 - Google Patents

신규한 안정한 항체-약물 복합체, 이의 제조방법 및 이의 용도 Download PDF

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KR102511249B1
KR102511249B1 KR1020167033391A KR20167033391A KR102511249B1 KR 102511249 B1 KR102511249 B1 KR 102511249B1 KR 1020167033391 A KR1020167033391 A KR 1020167033391A KR 20167033391 A KR20167033391 A KR 20167033391A KR 102511249 B1 KR102511249 B1 KR 102511249B1
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KR20170020328A (ko
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강 친
진도 위안
루 장
추빙 탄
릴리 스
카오 엘브이
레이레이 첸
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진콴텀 헬스케어 (쑤저우) 씨오., 엘티디.
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    • 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
    • A61K38/07—Tetrapeptides
    • 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
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
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    • 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
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    • 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
    • A61K47/6855—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 breast cancer cell
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    • A61K9/0012—Galenical forms characterised by the site of application
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    • C—CHEMISTRY; METALLURGY
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    • C07K—PEPTIDES
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    • 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
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    • 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
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    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • C07K2317/73—Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
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    • C07K2317/90—Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
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    • C07K2317/90—Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
    • C07K2317/94—Stability, e.g. half-life, pH, temperature or enzyme-resistance

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  • Health & Medical Sciences (AREA)
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  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
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  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Cell Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Enzymes And Modification Thereof (AREA)
KR1020167033391A 2014-04-29 2015-04-29 신규한 안정한 항체-약물 복합체, 이의 제조방법 및 이의 용도 Active KR102511249B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201410174890.8 2014-04-29
CN201410174890 2014-04-29
PCT/CN2015/077887 WO2015165413A1 (zh) 2014-04-29 2015-04-29 一种新型的稳定型抗体药物耦联物及其制备方法和用途

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Publication Number Publication Date
KR20170020328A KR20170020328A (ko) 2017-02-22
KR102511249B1 true KR102511249B1 (ko) 2023-03-20

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US (5) US11040084B2 (enExample)
EP (2) EP3517114A1 (enExample)
JP (2) JP6666264B2 (enExample)
KR (1) KR102511249B1 (enExample)
CN (2) CN106856656B (enExample)
AU (2) AU2015252518B2 (enExample)
ES (1) ES2736505T3 (enExample)
WO (1) WO2015165413A1 (enExample)

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EP3517114A1 (en) 2014-04-29 2019-07-31 Genequantum Healthcare (Suzhou) Co., Ltd. New stable antibody-drug conjugate, preparation method and use thereof
BR112019000071A2 (pt) 2016-07-07 2019-07-02 Bolt Biotherapeutics Inc conjugados adjuvantes de anticorpo
EP3937984A1 (en) 2019-03-15 2022-01-19 Bolt Biotherapeutics, Inc. Immunoconjugates targeting her2
CN114901694A (zh) * 2019-12-31 2022-08-12 启德医药科技（苏州）有限公司 抗trop2抗体、抗体-药物缀合物及其应用
WO2021136475A1 (en) * 2019-12-31 2021-07-08 Genequantum Healthcare (Suzhou) Co., Ltd. A drug conjugate and applications thereof
US20230399616A1 (en) * 2020-10-30 2023-12-14 Westlake Therapeutics (Hangzhou) Co. Limited Modified Red Blood Cells and Uses Thereof for Delivering Agents
AU2020482800B2 (en) * 2020-12-23 2025-08-21 Genequantum Healthcare (Suzhou) Co., Ltd. Novel isomeric compounds comprising a ring-opened thiosuccinimide group, an oligopeptide fragment and a chiral moiety
KR20230147105A (ko) 2021-01-28 2023-10-20 진콴텀 헬스케어 (쑤저우) 씨오., 엘티디. 리가제 융합 단백질 및 그 응용
WO2022188743A1 (en) * 2021-03-08 2022-09-15 Genequantum Healthcare (Suzhou) Co., Ltd. Anti-her2 antibody-immune agonist conjugate and applications thereof
JP7844499B2 (ja) * 2021-03-08 2026-04-13 ジーンクアンタム ヘルスケア （スーチョウ） シーオー．， エルティーディー． 抗体－免疫アゴニストコンジュゲート及びその使用
CN115197297B (zh) * 2021-04-14 2023-08-01 启德医药科技（苏州）有限公司 连接子、缀合物及其应用
US20240238440A1 (en) * 2021-04-29 2024-07-18 Hyslink Therapeutics Preparation method for and application of antibody conjugated drug
US11814394B2 (en) * 2021-11-16 2023-11-14 Genequantum Healthcare (Suzhou) Co., Ltd. Exatecan derivatives, linker-payloads, and conjugates and thereof
US20250043005A1 (en) * 2021-12-09 2025-02-06 Genequantum Healthcare (Suzhou) Co., Ltd. Antibody-cytokine fusion proteins and applications thereof
US20250213484A1 (en) * 2022-03-29 2025-07-03 Genequantum Healthcare (Suzhou) Co., Ltd. A freeze-drying process for an adc
JP7893907B2 (ja) 2022-06-02 2026-07-22 ジーンクアンタム ヘルスケア （スーチョウ） シーオー．， エルティーディー． オリゴ糖リンカー、オリゴ糖リンカーを含むリンカー－ペイロード、および糖鎖がリモデリングされた抗体薬物複合体、その製造方法と使用
KR20250068592A (ko) * 2022-06-28 2025-05-16 진콴텀 헬스케어 (쑤저우) 씨오., 엘티디. 항-fgfr3 항체 접합체 및 이의 의학적 용도
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