RU2762939C2 - Конъюгированные с лизином иммуноглобулины - Google Patents

Конъюгированные с лизином иммуноглобулины Download PDF

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RU2762939C2
RU2762939C2 RU2018145507A RU2018145507A RU2762939C2 RU 2762939 C2 RU2762939 C2 RU 2762939C2 RU 2018145507 A RU2018145507 A RU 2018145507A RU 2018145507 A RU2018145507 A RU 2018145507A RU 2762939 C2 RU2762939 C2 RU 2762939C2
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immunoglobulin
amino acid
residue
antigen
binding fragment
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RU2018145507A
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Russian (ru)
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RU2018145507A (ru
RU2018145507A3 (enExample
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Джаред Спайдел
Эрл АЛБОН
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Эйсай Ар Энд Ди Менеджмент Ко., Лтд.
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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
    • 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
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • 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
    • A61K47/68031—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P21/00—Preparation of peptides or proteins
    • C12P21/02—Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y203/00—Acyltransferases (2.3)
    • C12Y203/02—Aminoacyltransferases (2.3.2)
    • C12Y203/02013—Protein-glutamine gamma-glutamyltransferase (2.3.2.13), i.e. transglutaminase or factor XIII
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/40—Immunoglobulins specific features characterized by post-translational modification
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/40—Immunoglobulins specific features characterized by post-translational modification
    • C07K2317/41—Glycosylation, sialylation, or fucosylation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/51—Complete heavy chain or Fd fragment, i.e. VH + CH1
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/515—Complete light chain, i.e. VL + CL
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/52—Constant or Fc region; Isotype
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/52—Constant or Fc region; Isotype
    • C07K2317/522—CH1 domain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/52—Constant or Fc region; Isotype
    • C07K2317/524—CH2 domain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/52—Constant or Fc region; Isotype
    • C07K2317/53—Hinge
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/55—Fab or Fab'

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biotechnology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Microbiology (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
RU2018145507A 2016-06-10 2017-06-12 Конъюгированные с лизином иммуноглобулины RU2762939C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662348410P 2016-06-10 2016-06-10
US62/348,410 2016-06-10
PCT/JP2017/021672 WO2017213267A1 (en) 2016-06-10 2017-06-12 Lysine conjugated immunoglobulins

Related Child Applications (1)

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RU2021136863A Division RU2021136863A (ru) 2016-06-10 2017-06-12 Конъюгированные с лизином иммуноглобулины

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RU2018145507A RU2018145507A (ru) 2020-07-10
RU2018145507A3 RU2018145507A3 (enExample) 2020-10-15
RU2762939C2 true RU2762939C2 (ru) 2021-12-24

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RU2018145507A RU2762939C2 (ru) 2016-06-10 2017-06-12 Конъюгированные с лизином иммуноглобулины
RU2021136863A RU2021136863A (ru) 2016-06-10 2017-06-12 Конъюгированные с лизином иммуноглобулины

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EP (1) EP3468614A1 (enExample)
JP (1) JP7041077B2 (enExample)
KR (1) KR102538866B1 (enExample)
CN (1) CN109475642B (enExample)
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SG (1) SG11201810470XA (enExample)
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EP4032902A1 (en) 2015-12-18 2022-07-27 Eisai R&D Management Co., Ltd. C-terminal lysine conjugated immunoglobulins
SG11201810470XA (en) 2016-06-10 2018-12-28 Eisai R&D Man Co Ltd Lysine conjugated immunoglobulins
EP3966238A2 (en) * 2019-05-09 2022-03-16 Merus N.V. Variant domains for multimerizing proteins and separation thereof
GB201907093D0 (en) * 2019-05-20 2019-07-03 Ucl Business Plc Antibody functionalisation
CA3167317C (en) * 2020-02-12 2025-05-27 Eli Lilly And Company CRYSTALLIZATION OF ANTIBODIES OR ANTIGEN-BINDING FRAGMENTS
JP7664943B2 (ja) * 2020-03-25 2025-04-18 イーライ リリー アンド カンパニー 多重特異性結合タンパク質およびそれを開発する方法
MX2022014530A (es) 2020-05-20 2023-02-27 Janssen Biotech Inc Métodos para la conjugación específica del sitio de proteínas que contienen dominios fc glicosilados.
US20240173377A1 (en) * 2020-09-25 2024-05-30 Epivax, Inc. Retro - inverso regulatory t cell epitopes
WO2023026235A1 (en) * 2021-08-27 2023-03-02 Janssen Biotech, Inc. Anti-psma antibodies and uses thereof
CN117164701A (zh) * 2022-12-27 2023-12-05 优洛生物(上海)有限公司 一种经改造的抗体、其制备方法及其用途
IL322523A (en) 2023-02-28 2025-10-01 Eisai R&D Man Co Ltd Anti-PSMA antibodies, conjugates and methods of use
US20240337664A1 (en) * 2023-04-07 2024-10-10 Regeneron Pharmaceuticals, Inc. Characterization of crosslinking sites in antibody-drug conjugates
CN119375471A (zh) * 2023-07-26 2025-01-28 菲鹏生物股份有限公司 抗体和抗体缀合物及其用途
WO2025199464A1 (en) 2024-03-22 2025-09-25 Eisai R&D Management Co., Ltd. Anti-trop2 antibody-drug conjugates and methods of use
CN120779021A (zh) * 2024-04-08 2025-10-14 菲鹏生物股份有限公司 抗体缀合物及其用途
WO2026044149A2 (en) 2024-08-21 2026-02-26 Eisai R&D Management Co., Ltd. Synthesis of drug-linker combinations for antibody-drug conjugates
US20260139068A1 (en) 2024-08-21 2026-05-21 Eisai R&D Management Co., Ltd. Anti-cd73 antibodies, conjugates, and methods of use

Citations (5)

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RU2385879C2 (ru) * 2004-01-21 2010-04-10 Ново Нордиск Хелс Кеа Аг Способ конъюгации пептидов, опосредованной трансглутаминазой
US20130230543A1 (en) * 2010-11-05 2013-09-05 Jaume Pons Engineered polypeptide conjugates and methods for making thereof using transglutaminase
US20150017192A1 (en) * 2013-07-11 2015-01-15 Aimee Usera Site-specific chemoenzymatic protein modifications
WO2015015448A2 (en) * 2013-07-31 2015-02-05 Rinat Neuroscience Corp. Engineered polypeptide conjugates
WO2015162563A1 (en) * 2014-04-25 2015-10-29 Rinat Neuroscience Corp. Antibody-drug conjugates with high drug loading

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FI903489A7 (fi) 1988-11-11 1990-07-10 Medical Res Council Yhden osan sisältävät ligandit, näitä ligandeja sisältävät reseptorit, menetelmiä niiden valmistamiseksi sekä ligandien ja reseptorien käytt ö
WO2013176516A1 (ko) 2012-05-24 2013-11-28 한화케미칼 주식회사 트랜스글루타미나아제를 이용하여 제조한 항체-약물 결합체 및 이의 용도
EP2916872B1 (en) 2012-11-09 2019-02-27 Innate Pharma Recognition tags for tgase-mediated conjugation
WO2014159579A1 (en) 2013-03-14 2014-10-02 Abbvie Inc. MUTATED ANTI-TNFα ANTIBODIES AND METHODS OF THEIR USE
KR20160042871A (ko) * 2013-06-21 2016-04-20 이나뜨 파르마, 에스.아. 폴리펩티드의 효소적 콘쥬게이션
EP4032902A1 (en) 2015-12-18 2022-07-27 Eisai R&D Management Co., Ltd. C-terminal lysine conjugated immunoglobulins
SG11201810470XA (en) 2016-06-10 2018-12-28 Eisai R&D Man Co Ltd Lysine conjugated immunoglobulins

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Publication number Priority date Publication date Assignee Title
RU2385879C2 (ru) * 2004-01-21 2010-04-10 Ново Нордиск Хелс Кеа Аг Способ конъюгации пептидов, опосредованной трансглутаминазой
US20130230543A1 (en) * 2010-11-05 2013-09-05 Jaume Pons Engineered polypeptide conjugates and methods for making thereof using transglutaminase
US20150017192A1 (en) * 2013-07-11 2015-01-15 Aimee Usera Site-specific chemoenzymatic protein modifications
WO2015015448A2 (en) * 2013-07-31 2015-02-05 Rinat Neuroscience Corp. Engineered polypeptide conjugates
WO2015162563A1 (en) * 2014-04-25 2015-10-29 Rinat Neuroscience Corp. Antibody-drug conjugates with high drug loading

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Title
DENNLER P. et al.: Transglutaminase-based chemo-enzymatic conjugation approach yields homogeneous antibody-drug conjugates, BIOCONJUGATE CHEM. 2014, v.25, n.3, p.569-578. *
DENNLER P. et al.: Transglutaminase-based chemo-enzymatic conjugation approach yields homogeneous antibody-drug conjugates, BIOCONJUGATE CHEM. 2014, v.25, n.3, p.569-578. MINDT T.L. et al.: Modification of different IgG1 antibodies via glutamine and lysine using bacterial and human tissue transglutaminase, BIOCONJUGATE CHEM. 2008, v.19, n.1, p.271-278. JOSTEN A. et al.: Use of microbial transglutaminase for the enzymatic biotinylation of antibodies, JOURNAL OF IMMUNOLOGICAL METH., 2000, v.240, n.1-2, p.47-54. DEONARAIN M.L. et al.: Emerging formats for next-generation antibody drug conjugates, EXPERT OPIN DRUG DISCOV., 2015, v.10, n.5, p.463-481. *
DEONARAIN M.L. et al.: Emerging formats for next-generation antibody drug conjugates, EXPERT OPIN DRUG DISCOV., 2015, v.10, n.5, p.463-481. *
JOSTEN A. et al.: Use of microbial transglutaminase for the enzymatic biotinylation of antibodies, JOURNAL OF IMMUNOLOGICAL METH., 2000, v.240, n.1-2, p.47-54. *
MINDT T.L. et al.: Modification of different IgG1 antibodies via glutamine and lysine using bacterial and human tissue transglutaminase, BIOCONJUGATE CHEM. 2008, v.19, n.1, p.271-278. *

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US20210171998A1 (en) 2021-06-10
AU2017279352B2 (en) 2024-07-25
JP2019525897A (ja) 2019-09-12
PE20190340A1 (es) 2019-03-07
US10941431B2 (en) 2021-03-09
IL263329B (en) 2022-05-01
US20180044711A1 (en) 2018-02-15
RU2018145507A (ru) 2020-07-10
CL2021003383A1 (es) 2022-08-19
RU2021136863A (ru) 2022-02-01
BR112018075253A2 (pt) 2019-04-30
JOP20180118A1 (ar) 2019-01-30
KR102538866B1 (ko) 2023-06-02
PH12018502594A1 (en) 2019-10-14
AU2017279352A1 (en) 2018-12-13
MX419566B (es) 2025-01-14
NZ748605A (en) 2023-05-26
SG11201810470XA (en) 2018-12-28
CA3026991A1 (en) 2017-12-14
RU2018145507A3 (enExample) 2020-10-15
CN109475642B (zh) 2023-05-02
MY202858A (en) 2024-05-25
US11753669B2 (en) 2023-09-12
CO2018013314A2 (es) 2019-02-19
MX2018015331A (es) 2019-08-16
KR20190018159A (ko) 2019-02-21
JP7041077B2 (ja) 2022-03-23
CN109475642A (zh) 2019-03-15
IL263329A (en) 2018-12-31
WO2017213267A1 (en) 2017-12-14
EP3468614A1 (en) 2019-04-17
UA126799C2 (uk) 2023-02-08

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