CA2724740C - Formulations of 5-fluorocytosine and uses thereof - Google Patents

Formulations of 5-fluorocytosine and uses thereof Download PDF

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Publication number
CA2724740C
CA2724740C CA2724740A CA2724740A CA2724740C CA 2724740 C CA2724740 C CA 2724740C CA 2724740 A CA2724740 A CA 2724740A CA 2724740 A CA2724740 A CA 2724740A CA 2724740 C CA2724740 C CA 2724740C
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CA
Canada
Prior art keywords
formulation
weight percent
carbopol
cancer
auc
Prior art date
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Expired - Fee Related
Application number
CA2724740A
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English (en)
French (fr)
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CA2724740A1 (en
Inventor
Harry E. Gruber
Douglas Jolly
Kay Olmstead
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Forte Biosciences Inc
Original Assignee
Tocagen Inc
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Publication of CA2724740A1 publication Critical patent/CA2724740A1/en
Application granted granted Critical
Publication of CA2724740C publication Critical patent/CA2724740C/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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    • 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
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • 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
    • A61K38/43Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46Hydrolases (3)
    • A61K38/50Hydrolases (3) acting on carbon-nitrogen bonds, other than peptide bonds (3.5), e.g. asparaginase
    • 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
    • A61K38/43Enzymes; Proenzymes; Derivatives thereof
    • A61K38/51Lyases (4)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12YENZYMES
    • C12Y305/00Hydrolases acting on carbon-nitrogen bonds, other than peptide bonds (3.5)
    • C12Y305/04Hydrolases acting on carbon-nitrogen bonds, other than peptide bonds (3.5) in cyclic amidines (3.5.4)
    • C12Y305/04001Cytosine deaminase (3.5.4.1)

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Biophysics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
CA2724740A 2008-06-30 2009-06-30 Formulations of 5-fluorocytosine and uses thereof Expired - Fee Related CA2724740C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US7714208P 2008-06-30 2008-06-30
US61/077,142 2008-06-30
PCT/US2009/049322 WO2010002937A1 (en) 2008-06-30 2009-06-30 Formulations of 5-fluorocytosine and uses thereof

Publications (2)

Publication Number Publication Date
CA2724740A1 CA2724740A1 (en) 2010-01-07
CA2724740C true CA2724740C (en) 2017-02-21

Family

ID=41466310

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2724740A Expired - Fee Related CA2724740C (en) 2008-06-30 2009-06-30 Formulations of 5-fluorocytosine and uses thereof

Country Status (11)

Country Link
US (4) US9320738B2 (enExample)
EP (1) EP2306823A4 (enExample)
JP (3) JP6092514B2 (enExample)
KR (2) KR101950635B1 (enExample)
CN (2) CN102076215A (enExample)
AU (1) AU2009267052B2 (enExample)
BR (1) BRPI0915284B1 (enExample)
CA (1) CA2724740C (enExample)
IL (3) IL209385A (enExample)
MX (2) MX337213B (enExample)
WO (1) WO2010002937A1 (enExample)

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DE69940521D1 (de) 1998-10-01 2009-04-16 Univ Southern California Retrovirales genübertragungssystem und entsprechendes verwendungverfahren
CN102076215A (zh) 2008-06-30 2011-05-25 托卡根公司 5-氟胞嘧啶制剂及其用途
US8829173B2 (en) 2008-09-26 2014-09-09 Tocagen Inc. Recombinant vectors
WO2010036986A2 (en) 2008-09-26 2010-04-01 Tocagen Inc. Recombinant vectors
SG176890A1 (en) 2009-06-17 2012-01-30 Tocagen Inc Producer cells for replication competent retroviral vectors
JP2013510176A (ja) * 2009-11-06 2013-03-21 ピエール ファーブル メディカモン (1s,2r)−2−(アミノメチル)−n,n−ジエチル−1−フェニルシクロプロパンカルボキサミドの新規結晶形態
WO2012058673A2 (en) 2010-10-31 2012-05-03 Tocagen Inc. Enhanced cancer treatment and monitoring using recombinant vectors
EP2670368A4 (en) * 2011-02-03 2015-04-15 Pharmedica Ltd NEW ORAL DISSOLUTION FILMS FOR INSULIN DELIVERY FOR THE TREATMENT OF DIABETES
WO2013004658A1 (en) * 2011-07-01 2013-01-10 Transgene Sa Formulations of 5-fluorocytosine and uses thereof.
CN102579450B (zh) * 2012-02-10 2013-07-24 上海市嘉定区南翔医院 5-氟尿嘧啶在制备局限性慢性湿疹治疗药物上的应用
EP2668945A1 (de) 2012-06-01 2013-12-04 Bayer Technology Services GmbH Genotyp- bzw. Phänotyp-basierte Arzeimittelformulierungen
EP2909324B1 (en) 2012-10-25 2020-02-26 Tocagen Inc. Retroviral vector with mini-promoter cassette
US9642921B2 (en) 2012-12-20 2017-05-09 Tocagen Inc. Cancer combination therapy and recombinant vectors
EA201890640A1 (ru) 2015-09-04 2018-09-28 Токаджен Инк. Рекомбинантные векторы, содержащие пептид 2а
US20200032249A1 (en) * 2017-03-14 2020-01-30 Memorial Sloan Kettering Cancer Center Labeling, isolation, & analysis of rna from rare cell populations
US20190380965A1 (en) * 2018-06-15 2019-12-19 Hemant N. Joshi Quick Water-Dispersible Pharmaceutical Compositions of Flucytosine
US20220211783A1 (en) * 2019-02-22 2022-07-07 Candel Therapeutics, Inc. Gmci and ddri combination therapy for treating cancer
US11483244B2 (en) 2020-03-18 2022-10-25 Marvell Israel (M.I.S.L) Ltd. Packet buffer spill-over in network devices
CN111937887B (zh) * 2020-07-15 2021-09-07 南京师范大学 5-氟-2’-脱氧尿苷在抑制和/或防治螺旋藻规模化生产中褶皱臂尾轮虫的应用

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ES2286072T3 (es) 1991-03-06 2007-12-01 Emory University Sales de amidas de (-)cis 5 fluoro-2'-dedoxi-3'-tiacitidina utiles para el tratamiento de la hepatitis b.
FI980901A7 (fi) 1998-04-23 1999-10-24 Orion Yhtymae Oyj Levosimendaania säädellysti vapauttavia oraalisia koostumuksia
DE69940521D1 (de) 1998-10-01 2009-04-16 Univ Southern California Retrovirales genübertragungssystem und entsprechendes verwendungverfahren
EP1169024B1 (en) * 1999-03-31 2005-12-21 Janssen Pharmaceutica N.V. Pregelatinized starch in a controlled release formulation
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GB2368846B (en) 1999-07-08 2004-08-25 Univ California Isolated Jaagsiekte retroviruses (JSRV), gene delivery vectors, and methods of use
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AU2001268722B8 (en) 2000-06-23 2005-09-29 Teva Pharmaceutical Industries Ltd. Rapidly expanding composition for gastric retention and controlled release of therapeutic agents, and dosage forms including the composition
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CN101085355B (zh) * 2007-06-20 2012-01-25 山东大学 5-氟胞嘧啶/类水滑石纳米杂化物及其制备方法
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CN102076215A (zh) * 2008-06-30 2011-05-25 托卡根公司 5-氟胞嘧啶制剂及其用途
US8829173B2 (en) 2008-09-26 2014-09-09 Tocagen Inc. Recombinant vectors
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Also Published As

Publication number Publication date
US20110268720A1 (en) 2011-11-03
EP2306823A1 (en) 2011-04-13
JP6170896B2 (ja) 2017-07-26
US9889133B2 (en) 2018-02-13
CA2724740A1 (en) 2010-01-07
BRPI0915284A2 (pt) 2015-08-04
MX2010014256A (es) 2011-07-01
MX337213B (es) 2016-02-17
KR20110039544A (ko) 2011-04-19
WO2010002937A1 (en) 2010-01-07
US9320738B2 (en) 2016-04-26
MX366570B (es) 2019-07-12
JP2015063533A (ja) 2015-04-09
IL255813A (en) 2018-01-31
CN107029220A (zh) 2017-08-11
IL246473B (en) 2018-06-28
JP6092514B2 (ja) 2017-03-08
IL209385A (en) 2016-10-31
AU2009267052B2 (en) 2013-07-11
AU2009267052A1 (en) 2010-01-07
US20190015414A1 (en) 2019-01-17
KR101813721B1 (ko) 2017-12-29
JP2017214398A (ja) 2017-12-07
US10449194B2 (en) 2019-10-22
BRPI0915284B1 (pt) 2020-01-14
EP2306823A4 (en) 2012-09-26
US20160235751A1 (en) 2016-08-18
KR20180004279A (ko) 2018-01-10
JP2011526918A (ja) 2011-10-20
US11191764B2 (en) 2021-12-07
US20200281929A1 (en) 2020-09-10
IL209385A0 (en) 2011-01-31
CN102076215A (zh) 2011-05-25
KR101950635B1 (ko) 2019-05-20

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