CO2018010024A2 - Complejos radiofarmacéuticos - Google Patents

Complejos radiofarmacéuticos

Info

Publication number
CO2018010024A2
CO2018010024A2 CONC2018/0010024A CO2018010024A CO2018010024A2 CO 2018010024 A2 CO2018010024 A2 CO 2018010024A2 CO 2018010024 A CO2018010024 A CO 2018010024A CO 2018010024 A2 CO2018010024 A2 CO 2018010024A2
Authority
CO
Colombia
Prior art keywords
tissue
directed
chelator
complex
thorium
Prior art date
Application number
CONC2018/0010024A
Other languages
English (en)
Inventor
Lars Linden
Alan Cuthbertson
Original Assignee
Bayer Pharma AG
Bayer As
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 Bayer Pharma AG, Bayer As filed Critical Bayer Pharma AG
Publication of CO2018010024A2 publication Critical patent/CO2018010024A2/es

Links

Classifications

    • 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
    • A61K51/1027Antibodies 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 against receptors, cell-surface antigens or cell-surface determinants
    • A61K51/103Antibodies 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 against receptors, cell-surface antigens or cell-surface determinants against receptors for growth factors or receptors for growth regulators
    • 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
    • A61K51/1045Antibodies 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 against animal or human tumor cells or tumor cell determinants
    • A61K51/1051Antibodies 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 against animal or human tumor cells or tumor cell determinants the tumor cell being from breast, e.g. the antibody being herceptin
    • 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
    • A61K51/1045Antibodies 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 against animal or human tumor cells or tumor cell determinants
    • A61K51/1054Antibodies 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 against animal or human tumor cells or tumor cell determinants the tumor cell being from lung
    • 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
    • A61K51/1045Antibodies 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 against animal or human tumor cells or tumor cell determinants
    • A61K51/1063Antibodies 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 against animal or human tumor cells or tumor cell determinants the tumor cell being from stomach or intestines
    • 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
    • A61K51/1045Antibodies 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 against animal or human tumor cells or tumor cell determinants
    • A61K51/1072Antibodies 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 against animal or human tumor cells or tumor cell determinants the tumor cell being from the reproductive system, e.g. ovaria, uterus, testes or prostate
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07K16/32Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Optics & Photonics (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Cell Biology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Reproductive Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
  • Pyridine Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La invención proporciona un método para la formación de un complejo de torio dirigido a tejido, que comprende; a) formar un quelador octadentado que comprende cuatro restos de hidroxipiridinona (HOPO), sustituidos en la posición N con un grupo metilo y un resto de acoplamiento que termina en un grupo de ácido carboxílico; b) acoplar dicho quelador octadentado con al menos un resto dirigido a tejido que apunta a HER2; y c) poner en contacto dicho quelador dirigido a tejido con una solución acuosa que comprende un ion de al menos un isótopo de torio emisor alfa. También se proporcionan un método de tratamiento de una enfermedad neoplásica o hiperplásica que comprende la administración de tal complejo de torio dirigido a tejido, así como el complejo y las correspondientes formulaciones farmacéuticas.
CONC2018/0010024A 2016-03-24 2018-09-24 Complejos radiofarmacéuticos CO2018010024A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP16162123 2016-03-24
PCT/EP2017/056503 WO2017162555A1 (en) 2016-03-24 2017-03-20 Radio-pharmaceutical complexes

Publications (1)

Publication Number Publication Date
CO2018010024A2 true CO2018010024A2 (es) 2018-10-22

Family

ID=55745553

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2018/0010024A CO2018010024A2 (es) 2016-03-24 2018-09-24 Complejos radiofarmacéuticos

Country Status (19)

Country Link
US (2) US11260136B2 (es)
EP (1) EP3432936A1 (es)
JP (2) JP2019513699A (es)
CN (1) CN108778347A (es)
AR (1) AR107957A1 (es)
AU (1) AU2017239018A1 (es)
BR (1) BR112018069485A2 (es)
CA (1) CA3018607A1 (es)
CL (1) CL2018002695A1 (es)
CO (1) CO2018010024A2 (es)
IL (1) IL261329B (es)
JO (1) JOP20170072B1 (es)
MX (1) MX2018011629A (es)
PE (1) PE20190168A1 (es)
SG (2) SG11201806548UA (es)
TW (1) TWI757273B (es)
UA (1) UA125749C2 (es)
UY (1) UY37167A (es)
WO (1) WO2017162555A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020043617A1 (en) 2018-08-28 2020-03-05 Bayer As Combination of pi3k-inhibitors and targeted thorium conjugates
WO2020169537A1 (en) 2019-02-21 2020-08-27 Bayer Aktiengesellschaft Combination of pd-1/pd-l1 inhibitors and targeted thorium conjugates

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4399216A (en) 1980-02-25 1983-08-16 The Trustees Of Columbia University Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US4634665A (en) 1980-02-25 1987-01-06 The Trustees Of Columbia University In The City Of New York Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US5179017A (en) 1980-02-25 1993-01-12 The Trustees Of Columbia University In The City Of New York Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US4510245A (en) 1982-11-18 1985-04-09 Chiron Corporation Adenovirus promoter system
GB8308235D0 (en) 1983-03-25 1983-05-05 Celltech Ltd Polypeptides
US5168062A (en) 1985-01-30 1992-12-01 University Of Iowa Research Foundation Transfer vectors and microorganisms containing human cytomegalovirus immediate-early promoter-regulatory DNA sequence
US4968615A (en) 1985-12-18 1990-11-06 Ciba-Geigy Corporation Deoxyribonucleic acid segment from a virus
US4880615A (en) 1988-11-25 1989-11-14 Merck & Co., Inc. Stabilized radiopharmaceutical compositions
DK0590058T3 (da) 1991-06-14 2004-03-29 Genentech Inc Humaniseret heregulin-antistof
US5624901A (en) 1994-04-15 1997-04-29 The Regents Of The University Of California 3-hydroxy-2(1H)-pyridinone chelating agents
NO312708B1 (no) 2000-02-21 2002-06-24 Anticancer Therapeutic Inv Sa Radioaktive liposomer til terapi
NO313180B1 (no) 2000-07-04 2002-08-26 Anticancer Therapeutic Inv Sa Bensökende alfapartikkel emitterende radiofarmasöytika
GB0308731D0 (en) 2003-04-15 2003-05-21 Anticancer Therapeutic Inv Sa Method of radiotherapy
US7794691B2 (en) * 2004-06-25 2010-09-14 The European Community, Represented By The European Commission Radionuclides for medical use
UA95902C2 (ru) * 2005-02-23 2011-09-26 Дженентек, Инк. Способ увеличения времени развития заболевания или выживаемости у раковых пациентов
US20090214420A1 (en) * 2005-04-01 2009-08-27 Medvet Science Pty. Ltd. Method of Diagnosis and Treatment and Agents Useful for Same
PT2511301T (pt) * 2006-08-04 2018-03-08 Medimmune Ltd Anticorpos humanos para erbb2
EP2423201B1 (en) 2006-08-15 2017-10-04 The Regents of the University of California Luminescent macrocyclic lanthanide complexes
EP2488199A1 (en) * 2009-10-14 2012-08-22 Merrimack Pharmaceuticals, Inc. Bispecific binding agents targeting igf-1r and erbb3 signalling and uses thereof
GB201002508D0 (en) * 2010-02-12 2010-03-31 Algeta As Product
GB201208309D0 (en) * 2012-05-11 2012-06-27 Algeta As Complexes
MA41176A (fr) * 2014-12-17 2017-10-24 Bayer As Complexes radio-pharmaceutiques

Also Published As

Publication number Publication date
UA125749C2 (uk) 2022-06-01
EP3432936A1 (en) 2019-01-30
IL261329A (en) 2018-10-31
CA3018607A1 (en) 2017-09-28
BR112018069485A2 (pt) 2019-07-30
PE20190168A1 (es) 2019-02-01
WO2017162555A1 (en) 2017-09-28
IL261329B (en) 2021-04-29
US11260136B2 (en) 2022-03-01
TW201736389A (zh) 2017-10-16
UY37167A (es) 2017-10-31
AR107957A1 (es) 2018-07-04
TWI757273B (zh) 2022-03-11
US20190091354A1 (en) 2019-03-28
SG11201806548UA (en) 2018-08-30
SG10202009424TA (en) 2020-11-27
CL2018002695A1 (es) 2019-01-18
US20220143229A1 (en) 2022-05-12
MX2018011629A (es) 2019-03-14
JP2019513699A (ja) 2019-05-30
AU2017239018A1 (en) 2018-08-16
CN108778347A (zh) 2018-11-09
JP2022173214A (ja) 2022-11-18
JOP20170072B1 (ar) 2022-03-14

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