HRP20221448T1 - Il-22 fc pripravci i postupci njihove primjene - Google Patents

Il-22 fc pripravci i postupci njihove primjene Download PDF

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Publication number
HRP20221448T1
HRP20221448T1 HRP20221448TT HRP20221448T HRP20221448T1 HR P20221448 T1 HRP20221448 T1 HR P20221448T1 HR P20221448T T HRP20221448T T HR P20221448TT HR P20221448 T HRP20221448 T HR P20221448T HR P20221448 T1 HRP20221448 T1 HR P20221448T1
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pharmaceutical preparation
fusion protein
preparation according
amino acid
seq
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HRP20221448TT
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English (en)
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Bruce Kabakoff
Cecilia WONG MAN SAI
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F. Hoffmann - La Roche Ag
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Publication of HRP20221448T1 publication Critical patent/HRP20221448T1/hr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19Cytokines; Lymphokines; Interferons
    • A61K38/20Interleukins [IL]
    • 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
    • A61K47/02Inorganic compounds
    • 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
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40Cyclodextrins; Derivatives thereof
    • 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
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6813Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin the drug being a peptidic cytokine, e.g. an interleukin or interferon
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/52Cytokines; Lymphokines; Interferons
    • C07K14/54Interleukins [IL]
    • 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
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2319/00Fusion polypeptide
    • C07K2319/30Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Dermatology (AREA)
  • Inorganic Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Toxicology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Macromonomer-Based Addition Polymer (AREA)
  • Dental Preparations (AREA)

Claims (14)

1. Farmaceutski pripravak, naznačen time, da sadrži fuzijski protein IL-22 Fc i nosač, gdje je fuzijski protein IL-22 Fc koji sadrži polipeptid IL-22 povezan s Fc regijom pomoću veznice, pri čemu farmaceutski pripravak sadrži oko 1 mg/ml do oko 10 mg/ml fuzijskog proteina IL-22 Fc, oko 5 mM metionina, oko 10 mM natrijeva fosfata i oko 240 mM saharoze, i oko 0,02 % (m/v) polisorbata 20, pH 7,1, u konačnoj koncentraciji.
2. Farmaceutski pripravak prema patentnom zahtjevu 1, naznačen time, da je natrijev fosfat smjesa monobaznog natrijeva fosfata i dvobaznog natrijeva fosfata.
3. Farmaceutski pripravak prema patentnim zahtjevima 1 ili 2, naznačen time, da farmaceutski pripravak sadrži oko 10 mg/ml fuzijskog proteina IL-22 Fc.
4. Farmaceutski pripravak prema patentnim zahtjevima 1 ili 2, naznačen time, da farmaceutski pripravak sadrži oko 1 mg/ml fuzijskog proteina IL-22 Fc.
5. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 1 do 4, naznačen time, da: (i) farmaceutski pripravak je u obliku jedinične doze; (ii) nosač je voda; (iii) farmaceutski pripravak je stabilan tijekom jednog ili više ciklusa zamrzavanja-odmrzavanja; (iv) farmaceutski pripravak je stabilan oko 2 tjedna ili duže na temperaturi od oko 25 °C; (v) farmaceutski pripravak je stabilan oko 48 mjeseci ili dulje na temperaturi od -20 °C; (vi) farmaceutski pripravak posjeduje čistoću od oko 85 % ili više, kako je procijenjeno tekućinskom kromatografijom visoke djelotvornosti s isključenjem na osnovu veličine čestica (SE-HPLC); (vii) farmaceutski pripravak posjeduje čistoću od oko 75 % ili više, kako je procijenjeno nereduciranom (NR) kapilarnom elektroforezom u natrijevom dodecil-sulfatu bez gela (CE-SDS-NGS); (viii) farmaceutski pripravak se formulira za intravenoznu, supkutanu, intraperitonealnu ili topikalnu primjenu; (ix) farmaceutski pripravak ne sadrži konzervans; i/ili (x) farmaceutski pripravak se formulira za primjenu putem infuzije nakon razrjeđivanja izotoničnom otopinom natrijeva klorida i/ili razrjeđivačem.
6. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 1 do 5, naznačen time, da: (i) polipeptid IL-22 je glikoziliran; (ii) Fc regija nije glikozilirana; (iii) aminokiselinski ostatak na položaju 297 je Gly ili Ala kao u EU indeksu Fc regije i/ili aminokiselinski ostatak na položaju 299 je Ala, Gly ili Val kao u EU indeksu Fc regije; (iv) Fc regija sadrži CH2 i CH3 domenu IgG1 ili IgG4; i/ili (v) fuzijski protein IL-22 Fc sadrži aminokiselinski slijed koji ima najmanje 95 % identičnosti slijeda s aminokiselinskim slijedom SEQ ID NO: 8.
7. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 1 do 6, naznačen time, da fuzijski protein IL-22 Fc sadrži ili se sastoji od aminokiselinskog slijeda SEQ ID NO: 8, SEQ ID NO: 10 ili SEQ ID NO: 16.
8. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 1 do 7, naznačen time, da fuzijski protein IL-22 Fc sadrži aminokiselinski slijed SEQ ID NO: 8.
9. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 1 do 8, naznačen time, da nadalje sadrži dodatno terapeutsko sredstvo i/ili sredstvo za želiranje.
10. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 1 do 9, naznačen time, da se farmaceutski pripravak primjenjuje intravenozno, supkutano, intraperitonealno ili topikalno.
11. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 1 do 10, naznačen time, da je za uporabu kao lijek.
12. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 1 do 10, naznačen time, da je za uporabu u (i) liječenju upalne bolesti crijeva (IBD), (ii) inhibiranju mikrobne infekcije u crijevima, očuvanju vrčastih stanica u crijevu tijekom mikrobne infekcije, poboljšanju integriteta epitelnih stanica, proliferaciji epitelnih stanica, diferencijaciji epitelnih stanica, migraciji epitelnih stanica ili zacjeljivanju epitelnih rana u crijevima, (iii) liječenju akutne ozljede bubrega ili akutnog pankreatitisa, (iv) ubrzavanju ili poboljšanju zacjeljivanja rana, ili (v) sprečavanju ili liječenju kardiovaskularnog stanja.
13. Farmaceutski pripravak za uporabu prema patentnom zahtjevu 12, naznačen time, da je IBD ulcerozni kolitis ili Crohnova bolest.
14. Farmaceutski pripravak za uporabu prema patentnom zahtjevu 13, naznačen time, da je ulcerozni kolitis umjeren do teški ulcerozni kolitis.
HRP20221448TT 2018-01-26 2019-01-25 Il-22 fc pripravci i postupci njihove primjene HRP20221448T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201862622704P 2018-01-26 2018-01-26
US201862697372P 2018-07-12 2018-07-12
PCT/US2019/015268 WO2019148020A1 (en) 2018-01-26 2019-01-25 Compositions and methods of use
EP19704966.1A EP3743088B1 (en) 2018-01-26 2019-01-25 Il-22 fc compositions and methods of use

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US (1) US20200353049A1 (hr)
EP (1) EP3743088B1 (hr)
JP (1) JP7345479B2 (hr)
KR (1) KR20200125590A (hr)
CN (1) CN112020365A (hr)
AU (1) AU2019212703A1 (hr)
BR (1) BR112020015016A2 (hr)
CA (1) CA3088763A1 (hr)
DK (1) DK3743088T3 (hr)
ES (1) ES2932861T3 (hr)
HR (1) HRP20221448T1 (hr)
HU (1) HUE060435T2 (hr)
IL (1) IL276135A (hr)
LT (1) LT3743088T (hr)
MX (1) MX2020007628A (hr)
PL (1) PL3743088T3 (hr)
PT (1) PT3743088T (hr)
RS (1) RS63812B1 (hr)
SI (1) SI3743088T1 (hr)
WO (1) WO2019148020A1 (hr)

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