BR112016013704A8 - conjugado de anticorpo-fármaco anti-trop2,fármaco antitumor e/ou anticâncer,composição farmacêutica e uso dos mesmos. - Google Patents

conjugado de anticorpo-fármaco anti-trop2,fármaco antitumor e/ou anticâncer,composição farmacêutica e uso dos mesmos. Download PDF

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Publication number
BR112016013704A8
BR112016013704A8 BR112016013704A BR112016013704A BR112016013704A8 BR 112016013704 A8 BR112016013704 A8 BR 112016013704A8 BR 112016013704 A BR112016013704 A BR 112016013704A BR 112016013704 A BR112016013704 A BR 112016013704A BR 112016013704 A8 BR112016013704 A8 BR 112016013704A8
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Prior art keywords
drug
trop2 antibody
tumor
pharmaceutical composition
antitumor
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BR112016013704A
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BR112016013704B1 (pt
BR112016013704A2 (pt
Inventor
Okajima Daisuke
Hamada Hirofumi
Hasegawa Jun
Yamaguchi Miki
Takahashi Shu
Agatsuma Toshinori
Original Assignee
Daiichi Sankyo Co Ltd
Univ Sapporo Medical
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Application filed by Daiichi Sankyo Co Ltd, Univ Sapporo Medical filed Critical Daiichi Sankyo Co Ltd
Publication of BR112016013704A2 publication Critical patent/BR112016013704A2/pt
Publication of BR112016013704A8 publication Critical patent/BR112016013704A8/pt
Publication of BR112016013704B1 publication Critical patent/BR112016013704B1/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/30Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
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    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
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    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
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    • A61K47/6859Medicinal 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 liver or pancreas cancer cell
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    • A61K47/6863Medicinal 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 stomach or intestines cancer cell
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    • 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
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    • C07K2317/92Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value

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  • Reproductive Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

o propósito da presente invenção é fornecer um fármaco antitumor que se dintingue no efeito antitumor e segurança, e que tem um excelente efeito terapêutico. é fornecido um conjugado de anticorpo-fármaco caracterizado pelo fato de que um composto antitumor representado por uma fórmula e um anticorpo anti-trop2 são ligados por um ligante tendo uma estrutura representada pela fórmula: -l1-l2-lp-nh-(ch2)n1-la-(ch2)n2-c(=o)- (em que o anticorpo anti-trop2 liga-se ao terminal de l1, e o composto antitumor liga-se ao grupo carbonila da porção -(ch2)n2-c(=o)- usando o átomo de nitrogênio do grupo amino na posição 1 como o sítio de ligação).
BR112016013704-3A 2013-12-25 2014-12-24 Conjugado de anticorpo-fármaco anti-trop2,fármaco antitumor e/ou anticâncer,composição farmacêutica e uso dos mesmos. BR112016013704B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2013-267548 2013-12-25
JP2013267548 2013-12-25
PCT/JP2014/006421 WO2015098099A1 (ja) 2013-12-25 2014-12-24 抗trop2抗体-薬物コンジュゲート

Publications (3)

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BR112016013704A2 BR112016013704A2 (pt) 2017-10-03
BR112016013704A8 true BR112016013704A8 (pt) 2018-04-17
BR112016013704B1 BR112016013704B1 (pt) 2023-07-25

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