BR112022016999A2 - Polipeptídeos de ligação modificados para conjugação de fármacos otimizada - Google Patents

Polipeptídeos de ligação modificados para conjugação de fármacos otimizada

Info

Publication number
BR112022016999A2
BR112022016999A2 BR112022016999A BR112022016999A BR112022016999A2 BR 112022016999 A2 BR112022016999 A2 BR 112022016999A2 BR 112022016999 A BR112022016999 A BR 112022016999A BR 112022016999 A BR112022016999 A BR 112022016999A BR 112022016999 A2 BR112022016999 A2 BR 112022016999A2
Authority
BR
Brazil
Prior art keywords
modified
amino acid
acid residue
reactive amino
kabat
Prior art date
Application number
BR112022016999A
Other languages
English (en)
Inventor
Brun Marie-Priscille
Duffieux Francis
Park Sunghae
Qiu Huawei
Zhou Qun
Original Assignee
Genzyme Corp
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 Genzyme Corp filed Critical Genzyme Corp
Publication of BR112022016999A2 publication Critical patent/BR112022016999A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • 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
    • A61K47/56—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • 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
    • 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
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/10—Immunoglobulins specific features characterized by their source of isolation or production
    • C07K2317/14—Specific host cells or culture conditions, e.g. components, pH or temperature
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/24—Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
    • 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
    • C07K2317/524—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
    • C07K2317/526—CH3 domain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/56—Immunoglobulins specific features characterized by immunoglobulin fragments variable (Fv) region, i.e. VH and/or VL
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • 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

Abstract

POLIPEPTÍDEOS DE LIGAÇÃO MODIFICADOS PARA CONJUGAÇÃO DE FÁRMACOS OTIMIZADA. Anticorpos modificados que são estáveis e podem ser conjugados a um ligante ou fármaco em uma relação ligante/fármaco para anticorpo acima de 3, tornando esses conjugados adequados para o tratamento de uma variedade de indicações, são fornecidos. Métodos de produção desses anticorpos modificados também são fornecidos. Em uma primeira modalidade, o anticorpo compreende um primeiro resíduo de aminoácido reativo modificado na posição 274 de acordo com a numeração do índice EU de Kabat e um segundo resíduo de aminoácido reativo modificado na posição 339, 360, 384, 385, 422 e/ou 440. Em uma segunda modalidade, o anticorpo compreende um primeiro resíduo de aminoácido reativo modificado na posição 339 de acordo com a numeração do índice EU de Kabat e um segundo resíduo de aminoácido reativo modificado na posição 290, 360, 384, 385, 422 e /ou 440. Em uma terceira modalidade, o anticorpo compreende um primeiro resíduo de aminoácido reativo modificado na posição 118 de acordo com a numeração do índice EU de Kabat e um segundo resíduo de aminoácido reativo modificado na posição 274, 339, 384, 385, 422 e/ou 440. Em uma quarta modalidade, o anticorpo compreende um primeiro resíduo de aminoácido reativo modificado na posição 384 de acordo com a numeração do índice EU de Kabat e um segundo resíduo de aminoácido reativo modificado na posição 118, 274, 290 e/ou 339. Em uma modalidade preferida, o resíduo de aminoácido reativo modificado é cisteína.
BR112022016999A 2020-02-28 2021-02-26 Polipeptídeos de ligação modificados para conjugação de fármacos otimizada BR112022016999A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202062982943P 2020-02-28 2020-02-28
PCT/US2021/019958 WO2021174034A1 (en) 2020-02-28 2021-02-26 Modified binding polypeptides for optimized drug conjugation

Publications (1)

Publication Number Publication Date
BR112022016999A2 true BR112022016999A2 (pt) 2022-10-25

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
BR112022016999A BR112022016999A2 (pt) 2020-02-28 2021-02-26 Polipeptídeos de ligação modificados para conjugação de fármacos otimizada

Country Status (14)

Country Link
US (2) US11879004B2 (pt)
EP (1) EP4110404A1 (pt)
JP (1) JP2023516952A (pt)
KR (1) KR20220148235A (pt)
CN (1) CN115515643A (pt)
AR (1) AR121462A1 (pt)
AU (1) AU2021225962A1 (pt)
BR (1) BR112022016999A2 (pt)
CA (1) CA3169521A1 (pt)
CO (1) CO2022013737A2 (pt)
IL (1) IL295590A (pt)
MX (1) MX2022010538A (pt)
TW (1) TW202200209A (pt)
WO (1) WO2021174034A1 (pt)

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Publication number Publication date
WO2021174034A1 (en) 2021-09-02
MX2022010538A (es) 2022-09-21
EP4110404A1 (en) 2023-01-04
CO2022013737A2 (es) 2022-10-21
US11879004B2 (en) 2024-01-23
US20230391849A1 (en) 2023-12-07
CA3169521A1 (en) 2021-09-02
IL295590A (en) 2022-10-01
TW202200209A (zh) 2022-01-01
JP2023516952A (ja) 2023-04-21
US20210292391A1 (en) 2021-09-23
CN115515643A (zh) 2022-12-23
AR121462A1 (es) 2022-06-08
KR20220148235A (ko) 2022-11-04
AU2021225962A1 (en) 2022-10-20

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