DK2992874T3 - Liposom til topisk indgivelse og anvendelse deraf - Google Patents

Liposom til topisk indgivelse og anvendelse deraf Download PDF

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Publication number
DK2992874T3
DK2992874T3 DK13883388.4T DK13883388T DK2992874T3 DK 2992874 T3 DK2992874 T3 DK 2992874T3 DK 13883388 T DK13883388 T DK 13883388T DK 2992874 T3 DK2992874 T3 DK 2992874T3
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Prior art keywords
shrna
liposome
lipoplex
use according
agent
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DK13883388.4T
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English (en)
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Tatsuhiro Ishida
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Delta Fly Pharma Inc
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    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • C12N15/1137—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing against enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/713—Double-stranded nucleic acids or oligonucleotides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/69—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6905—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion
    • A61K47/6911—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion the form being a liposome
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Liposomes
    • A61K9/1271—Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Liposomes
    • A61K9/1271—Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers
    • A61K9/1272—Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers with substantial amounts of non-phosphatidyl, i.e. non-acylglycerophosphate, surfactants as bilayer-forming substances, e.g. cationic lipids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/111—General methods applicable to biologically active non-coding nucleic acids
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/10—Type of nucleic acid
    • C12N2310/14—Type of nucleic acid interfering N.A.
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    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/50—Physical structure
    • C12N2310/53—Physical structure partially self-complementary or closed
    • C12N2310/531—Stem-loop; Hairpin
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    • C12N2320/00—Applications; Uses
    • C12N2320/30—Special therapeutic applications
    • C12N2320/32—Special delivery means, e.g. tissue-specific

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  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Molecular Biology (AREA)
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  • Wood Science & Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Dispersion Chemistry (AREA)
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  • Physics & Mathematics (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (15)

1. Liposom til anvendelse ved topisk indgivelse i en fremgangsmåde til medicinsk behandling, som består af dioleylphosphatidylethanolamin (DOPE), phosphatidylcholin og kationisk lipid, hvor phosphatidylcholin omfatter mindst en umættet fedtsyrekæde, der indeholder en carbon-carbon-dobbeltbinding, og hvor den kationiske lipid er O,O'-ditetradecanoyl-N-(a-trimethylammonio-acetyl)diethanolaminchlorid (DC-6-14).
2. Liposom til anvendelse ifølge krav 1, hvor phosphatidylcholin omfatter mindst en umættet fedtsyrekæde, der indeholder en cis-konfiguration-carbon-carbon-dobbeltbinding.
3. Liposom til anvendelse ifølge krav 1, hvor phosphatidylcholin er 1,2-dio-leoyl-sn-glycero-3-phosphocholin (DOPC), palmitoyl-oleoyl-phosphatidylcho-lin (POPC) eller 1,2-dieicosenoyl-sn-glycero-3-phosphocholin (DEPC).
4. Liposom til anvendelse ifølge krav 1, hvor phosphatidylcholin er DOPC.
5. Liposom til anvendelse ifølge krav 1, som består af DOPE, DOPC og DC-6-14, eventuelt bestående af DOPE, DOPC og DC-6-14 i et molforhold på 3:2:5.
6. Sammensætning til anvendelse ved topisk indgivelse i en fremgangsmåde til medicinsk behandling, omfattende liposomet til anvendelse ifølge et hvilket som helst af kravene 1 til 5 og en aktiv forbindelse.
7. Sammensætning til anvendelse ifølge krav 6, hvor den aktive forbindelse er en nukleinsyre.
8. Sammensætning til anvendelse ifølge krav 7, hvor nukleinsyren er bundet til den udvendige membranoverflade af liposomet.
9. Antitumormiddel til anvendelse ved topisk indgivelse i en fremgangsmåde til tumorbehandling, omfattende liposomet til anvendelse ifølge et hvilket som helst af kravene 1 til 5 og shRNA (short hairpin RNA), der kan hæmme ekspression af thymidylatsynthase via RNAi.
10. Antitumormiddel til anvendelse ifølge krav 9, hvor shRNA'en er bundet til den udvendige membranoverflade af liposomet.
11. Antitumormiddel til anvendelse ifølge krav 9, hvor shRNA'en består af nu-kleotidsekvensen som vist i SEQ ID NO: 8.
12. Antitumormiddel til anvendelse ifølge krav 9, som er til anvendelse i kombination med cancer-kemoterapi eller et kemoterapeutisk middel mod cancer.
13. Kombineret produkt omfattende antitumormidlet til anvendelse ifølge et hvilket som helst af kravene 9 til 12 og et kemoterapeutisk middel mod cancer.
14. Kombineret produkt ifølge krav 13, hvor det kemoterapeutiske middel mod cancer er et antitumormiddel med TS (thymidylatsyntase)-hæmmende virkning
15. Kombineret produkt ifølge krav 14, hvor antitumormidlet med TS-hæm-mende virkning er et 5-FU-antitumor-middel eller pemetrexed-natriumhydrat.
DK13883388.4T 2013-04-30 2013-11-01 Liposom til topisk indgivelse og anvendelse deraf DK2992874T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2013095950 2013-04-30
PCT/JP2013/080367 WO2014178152A1 (ja) 2013-04-30 2013-11-01 局所投与用リポソームおよびその用途

Publications (1)

Publication Number Publication Date
DK2992874T3 true DK2992874T3 (da) 2018-11-12

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ID=51843301

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Application Number Title Priority Date Filing Date
DK13883388.4T DK2992874T3 (da) 2013-04-30 2013-11-01 Liposom til topisk indgivelse og anvendelse deraf

Country Status (14)

Country Link
US (1) US9745583B2 (da)
EP (1) EP2992874B1 (da)
JP (1) JP6307070B2 (da)
KR (1) KR101831205B1 (da)
CN (1) CN105142613B (da)
AU (1) AU2013388255B2 (da)
DK (1) DK2992874T3 (da)
ES (1) ES2691494T3 (da)
HR (1) HRP20181735T1 (da)
HU (1) HUE040425T2 (da)
PL (1) PL2992874T3 (da)
PT (1) PT2992874T (da)
TW (1) TWI594768B (da)
WO (1) WO2014178152A1 (da)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9855345B2 (en) 2014-10-30 2018-01-02 Delta-Fly Pharma, Inc. Method for producing lipoplex for topical administration and antitumor agent using such lipoplex
EP3512503A4 (en) * 2016-09-14 2020-05-06 Nanyang Technological University LIPOSOMAL FORMULATIONS

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH09248182A (ja) * 1996-03-15 1997-09-22 Oyo Seikagaku Kenkyusho プラスミド包埋多重膜リポソーム
JP3910646B2 (ja) 1997-04-07 2007-04-25 第一製薬株式会社 「細胞への遺伝子導入用組成物」
EP1742661A2 (en) 2004-01-07 2007-01-17 Neopharm, Inc. Lipid compositions and use thereof
US20060216343A1 (en) 2004-11-05 2006-09-28 Steffen Panzner Pharmaceutical compositions comprising an oligonucleotide as an active agent
EP2125031B1 (en) * 2006-12-19 2017-11-01 Marina Biotech, Inc. Lipids and lipid assemblies comprising transfection enhancer elements
EP2902013A1 (en) 2008-10-16 2015-08-05 Marina Biotech, Inc. Processes and Compositions for Liposomal and Efficient Delivery of Gene Silencing Therapeutics
TW201021853A (en) 2008-11-17 2010-06-16 Enzon Pharmaceuticals Inc Releasable cationic lipids for nucleic acids delivery systems
ES2599153T3 (es) 2009-03-31 2017-01-31 Delta-Fly Pharma, Inc. Molécula de ARNi para la timidilato sintasa y uso de la misma
US20120301537A1 (en) 2011-05-23 2012-11-29 Delta-Fly Pharma, Inc. LIPOSOME CONTAINING shRNA MOLECULE TARGETING A THYMIDYLATE SYNTHASE AND USE THEREOF
JP5813461B2 (ja) 2011-10-31 2015-11-17 株式会社ミヤデン 軸状ワークの焼入装置
EP3620447B1 (en) 2012-03-29 2021-02-17 Translate Bio, Inc. Ionizable cationic lipids
BR112014029247A2 (pt) 2012-05-23 2017-06-27 Univ Ohio State nanopartícula de lipídio, composição farmacêutica, método para fazer uma nanopartícula de lipído, produto, método de tratamento de um distúrbio, e sistema de entrega

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Publication number Publication date
PL2992874T3 (pl) 2019-01-31
JPWO2014178152A1 (ja) 2017-02-23
PT2992874T (pt) 2018-11-09
TW201440813A (zh) 2014-11-01
AU2013388255A1 (en) 2015-11-12
WO2014178152A1 (ja) 2014-11-06
HUE040425T2 (hu) 2019-03-28
US9745583B2 (en) 2017-08-29
HRP20181735T1 (hr) 2018-12-28
US20160208263A1 (en) 2016-07-21
TWI594768B (zh) 2017-08-11
EP2992874A1 (en) 2016-03-09
EP2992874A4 (en) 2016-06-01
CN105142613A (zh) 2015-12-09
ES2691494T3 (es) 2018-11-27
KR101831205B1 (ko) 2018-02-22
EP2992874B1 (en) 2018-08-08
KR20150118955A (ko) 2015-10-23
CN105142613B (zh) 2018-03-16
JP6307070B2 (ja) 2018-04-04
AU2013388255B2 (en) 2017-02-16

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