CN114555132A - 放射性金属标记抗体的制造方法 - Google Patents

放射性金属标记抗体的制造方法 Download PDF

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Publication number
CN114555132A
CN114555132A CN202080072618.2A CN202080072618A CN114555132A CN 114555132 A CN114555132 A CN 114555132A CN 202080072618 A CN202080072618 A CN 202080072618A CN 114555132 A CN114555132 A CN 114555132A
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China
Prior art keywords
group
peptide
formula
radioactive metal
amino acid
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CN202080072618.2A
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English (en)
Chinese (zh)
Inventor
井泽彰宏
小川祐
市川浩章
河谷稔
竹森英晃
奥村侑纪
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Nihon Medi Physics Co Ltd
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Nihon Medi Physics Co Ltd
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Publication of CN114555132A publication Critical patent/CN114555132A/zh
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/0474Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
    • A61K51/0482Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group chelates from cyclic ligands, e.g. DOTA
    • 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
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/0474Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
    • A61K51/0478Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group complexes from non-cyclic ligands, e.g. EDTA, MAG3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
    • A61K51/1093Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody conjugates with carriers being antibodies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
    • A61K51/1093Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody conjugates with carriers being antibodies
    • A61K51/1096Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody conjugates with carriers being antibodies radioimmunotoxins, i.e. conjugates being structurally as defined in A61K51/1093, and including a radioactive nucleus for use in radiotherapeutic applications
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2887Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against CD20
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/32Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K19/00Hybrid peptides, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/08Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2319/00Fusion polypeptide

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
CN202080072618.2A 2019-10-18 2020-10-16 放射性金属标记抗体的制造方法 Pending CN114555132A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2019191561 2019-10-18
JP2019-191561 2019-10-18
PCT/JP2020/039076 WO2021075546A1 (ja) 2019-10-18 2020-10-16 放射性金属標識抗体の製造方法

Publications (1)

Publication Number Publication Date
CN114555132A true CN114555132A (zh) 2022-05-27

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CN202080072618.2A Pending CN114555132A (zh) 2019-10-18 2020-10-16 放射性金属标记抗体的制造方法

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US (1) US20230248854A1 (https=)
EP (1) EP4047010A4 (https=)
JP (2) JPWO2021075546A1 (https=)
KR (1) KR20220083768A (https=)
CN (1) CN114555132A (https=)
AU (1) AU2020367624A1 (https=)
BR (1) BR112022007240A2 (https=)
CA (1) CA3158344A1 (https=)
IL (1) IL292312A (https=)
MX (1) MX2022004588A (https=)
PH (1) PH12022550919A1 (https=)
TW (1) TWI875842B (https=)
WO (1) WO2021075546A1 (https=)
ZA (1) ZA202205154B (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117466980A (zh) * 2023-11-02 2024-01-30 浙江普罗亭健康科技有限公司 基于多肽链骨架应用于金属抗体标记的负载金属缀合物及其应用

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20230390425A1 (en) * 2020-10-16 2023-12-07 Nihon Medi-Physics Co., Ltd. Radioactive complexes of anti-her2 antibody, and radiopharmaceutical
WO2022149578A1 (ja) 2021-01-08 2022-07-14 日本メジフィジックス株式会社 Ac-225溶液の製造方法およびAc-225溶液を用いた医薬の製造方法
JPWO2022224980A1 (https=) * 2021-04-20 2022-10-27
EP4397320A1 (en) * 2021-08-31 2024-07-10 Nihon Medi-Physics Co., Ltd. Radioactive complex of deglycosylated antibody and radioactive pharmaceutical product
JP2023135733A (ja) * 2022-03-16 2023-09-29 Jfeエンジニアリング株式会社 ジルコニウム錯体およびその合成方法
AU2023242087A1 (en) * 2022-03-30 2024-09-12 Nihon Medi-Physics Co., Ltd. Method for producing complex
WO2024108304A1 (en) * 2022-11-23 2024-05-30 Standard Biotools Canada Inc. Dithiol chelators for metal conjugation to antibodies
WO2025235681A1 (en) * 2024-05-07 2025-11-13 Cornell University Halogenated metal chelators and uses thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107614514A (zh) * 2015-05-20 2018-01-19 国立大学法人鹿儿岛大学 利用IgG结合肽的抗体特异性修饰
CN109071606A (zh) * 2016-06-13 2018-12-21 国立大学法人鹿儿岛大学 利用IgG结合肽的位点特异性放射性同位素标记抗体

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EP3160513B1 (en) * 2014-06-30 2020-02-12 Glykos Finland Oy Saccharide derivative of a toxic payload and antibody conjugates thereof
JP7291395B2 (ja) * 2017-06-16 2023-06-15 国立大学法人 鹿児島大学 IgG結合ペプチド、及び該ペプチドによる抗体の特異的修飾
BR112020012099A2 (pt) 2017-12-18 2020-11-17 Janssen Biotech, Inc. radiomarcação de polipeptídeos
SG11202009990UA (en) * 2018-04-16 2020-11-27 Nihon Mediphysics Co Ltd Modified antibody and radioactive metal-labelled antibody

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107614514A (zh) * 2015-05-20 2018-01-19 国立大学法人鹿儿岛大学 利用IgG结合肽的抗体特异性修饰
CN109071606A (zh) * 2016-06-13 2018-12-21 国立大学法人鹿儿岛大学 利用IgG结合肽的位点特异性放射性同位素标记抗体

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
S. POTY ET AL: "The inverse electron-demand Diels–Alder reaction as a new methodology for the synthesis of 225Ac-labelled radioimmunoconjugates", 《CHEM. COMMUN.》, vol. 54, pages 2600 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117466980A (zh) * 2023-11-02 2024-01-30 浙江普罗亭健康科技有限公司 基于多肽链骨架应用于金属抗体标记的负载金属缀合物及其应用

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KR20220083768A (ko) 2022-06-20
WO2021075546A1 (ja) 2021-04-22
BR112022007240A2 (pt) 2022-07-05
CA3158344A1 (en) 2021-04-22
US20230248854A1 (en) 2023-08-10
EP4047010A4 (en) 2024-01-10
IL292312A (en) 2022-06-01
TW202128732A (zh) 2021-08-01
MX2022004588A (es) 2022-07-21
TWI875842B (zh) 2025-03-11
ZA202205154B (en) 2023-11-29
PH12022550919A1 (en) 2023-07-10
JP2025157484A (ja) 2025-10-15
EP4047010A1 (en) 2022-08-24
JPWO2021075546A1 (https=) 2021-04-22
AU2020367624A1 (en) 2022-05-19

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