AR092400A1 - Formulaciones de anticuerpos y proteinas de alta concentracion - Google Patents

Formulaciones de anticuerpos y proteinas de alta concentracion

Info

Publication number
AR092400A1
AR092400A1 ARP130103099A ARP130103099A AR092400A1 AR 092400 A1 AR092400 A1 AR 092400A1 AR P130103099 A ARP130103099 A AR P130103099A AR P130103099 A ARP130103099 A AR P130103099A AR 092400 A1 AR092400 A1 AR 092400A1
Authority
AR
Argentina
Prior art keywords
salt
antibody
protein
antibody formulation
formulation
Prior art date
Application number
ARP130103099A
Other languages
English (en)
Inventor
Ma Xinghang
Xiang Jun
Original Assignee
Bayer Healthcare Llc
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
Priority claimed from US13/601,598 external-priority patent/US8613919B1/en
Application filed by Bayer Healthcare Llc filed Critical Bayer Healthcare Llc
Publication of AR092400A1 publication Critical patent/AR092400A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39591Stabilisation, fragmentation
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183Amino acids, e.g. glycine, EDTA or aspartame
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/38Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against protease inhibitors of peptide structure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/505Medicinal preparations containing antigens or antibodies comprising antibodies
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/40Immunoglobulins specific features characterized by post-translational modification
    • C07K2317/41Glycosylation, sialylation, or fucosylation
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/90Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
    • C07K2317/94Stability, e.g. half-life, pH, temperature or enzyme-resistance

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Dermatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Endocrinology (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)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Se proporcionan formulaciones de alta concentración sin sal de anticuerpos y otras proteínas que son sustancialmente isosmóticas y de baja viscosidad. También se proporcionan procedimientos para el tratamiento de enfermedades usando las formulaciones divulgadas. Reivindicación 1: Una formulación de proteína o anticuerpo sin sal, que comprende: a) 10 mM a 30 mM de histidina; b) 50 ppm a 200 ppm de un tensioactivo no iónico; c) 88 mM a 292 mM de un azúcar o alcohol de azúcar seleccionado entre manitol, dextrosa, glucosa, trehalosa y sacarosa; d) 0 mM a 50 mM de arginina; e) 0 mM a 50 mM de lisina; f) 0 mM a 133 mM de glicina o alanina; g) 0 mM a 10 mM de metionina; y h) 20 mg/ml a 150 mg/ml de una proteína o un anticuerpo; en la que dicha formulación de proteína o anticuerpo tiene un pH que varía de pH 4,0 a pH 6,0 y en la que dicha formulación de proteína no contiene sustancialmente sal inorgánica. Reivindicación 4: La formulación de proteína o anticuerpo sin sal de cualquiera de la reivindicación 1, en la que dicho tensioactivo no iónico es un polisorbato seleccionado entre polisorbato 20 y polisorbato 80. Reivindicación 5: La formulación de proteína o anticuerpo sin sal de la reivindicación 1, en la que dicho azúcar es sacarosa. Reivindicación 7: La formulación de proteína o anticuerpo sin sal de la reivindicación 1, que comprende: a) 30 mM de histidina, b) 100 ppm de polisorbato 80, c) 292 mM de sacarosa, y d) 20 mg/ml de proteína o anticuerpo; en la que dicha formulación de proteína o anticuerpo tiene un pH que varía de pH 5,0 a pH 6,0. Reivindicación 17: Una formulación de anticuerpo anti-TFPI sin sal, que comprende: a) 10 mM a 30 mM de histidina, b) 50 ppm a 200 ppm de un tensioactivo no iónico, c) 88 mM a 292 mM de un azúcar o alcohol de azúcar seleccionado entre manitol, dextrosa, glucosa, trehalosa y sacarosa, d) 0 mM a 50 mM de arginina, e) 0 mM a 50 mM de lisina, f) 0 mM a 133 mM de glicina o alanita, g) 0 mM a 10 mM de metionina, y h) 20 mg/ml a 150 mg/ml de anticuerpo anti-TFPI; en la que dicha formulación de anticuerpo anti-TFPI tiene un pH de pH 4,0 a pH 6,0 y en la que dicha formulación de anticuerpo anti-TFPI no contiene sustancialmente sal inorgánica. Reivindicación 22: La formulación de anticuerpo anti-TFPI sin sal de la reivindicación 17, que comprende: a) 10 mM de histidina, b) 75 ppm de Tween 80, c) 234 mM de sacarosa, d) 30 mM de arginina, y e) 10 mM de metionina, y f) 100 mg/ml de anticuerpo anti-TFPI; en la que dicha formulación de anticuerpo anti-TFPI tiene un pH de 5,5. Reivindicación 23: La formulación de anticuerpo anti-TFPI sin sal de la reivindicación 17, en la que dicho anticuerpo anti-TFPI es un anticuerpo monoclonal lgG₂ humano. Reivindicación 24: La formulación de anticuerpo anti-TFPI sin sal de la reivindicación 17, en la que dicho anticuerpo monoclonal lgG₂ humano comprende una cadena ligera que comprende la secuencia de aminoácidos de SEC ID Nº 1 y una cadena pesada que comprende la secuencia de aminoácidos de SEC ID Nº 2.
ARP130103099A 2012-08-31 2013-08-30 Formulaciones de anticuerpos y proteinas de alta concentracion AR092400A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13/601,598 US8613919B1 (en) 2012-08-31 2012-08-31 High concentration antibody and protein formulations
US13/843,780 US9592297B2 (en) 2012-08-31 2013-03-15 Antibody and protein formulations

Publications (1)

Publication Number Publication Date
AR092400A1 true AR092400A1 (es) 2015-04-22

Family

ID=49162239

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP130103085A AR092388A1 (es) 2012-08-31 2013-08-29 Formulaciones de anticuerpo y proteina
ARP130103099A AR092400A1 (es) 2012-08-31 2013-08-30 Formulaciones de anticuerpos y proteinas de alta concentracion

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP130103085A AR092388A1 (es) 2012-08-31 2013-08-29 Formulaciones de anticuerpo y proteina

Country Status (26)

Country Link
US (7) US9592297B2 (es)
EP (3) EP3117837B1 (es)
JP (3) JP6462567B2 (es)
CN (2) CN114392353A (es)
AR (2) AR092388A1 (es)
AU (3) AU2013308902B2 (es)
BR (1) BR112015003838A2 (es)
CA (2) CA3129277A1 (es)
CY (1) CY1121989T1 (es)
DK (1) DK3117837T3 (es)
ES (1) ES2741575T3 (es)
HK (1) HK1210794A1 (es)
HR (1) HRP20191299T1 (es)
HU (1) HUE045652T2 (es)
IL (6) IL286784B (es)
LT (1) LT3117837T (es)
MX (2) MX369653B (es)
PL (1) PL3117837T3 (es)
PT (1) PT3117837T (es)
RS (1) RS59221B1 (es)
RU (2) RU2678097C2 (es)
SG (2) SG10201708215YA (es)
SI (1) SI3117837T1 (es)
TW (4) TW201927338A (es)
UY (1) UY34995A (es)
WO (1) WO2014036071A1 (es)

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