SG10201800195XA - [6R]-MTHF – an efficient folate alternative in 5-fluorouracil based chemotherapy - Google Patents

[6R]-MTHF – an efficient folate alternative in 5-fluorouracil based chemotherapy

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Publication number
SG10201800195XA
SG10201800195XA SG10201800195XA SG10201800195XA SG10201800195XA SG 10201800195X A SG10201800195X A SG 10201800195XA SG 10201800195X A SG10201800195X A SG 10201800195XA SG 10201800195X A SG10201800195X A SG 10201800195XA SG 10201800195X A SG10201800195X A SG 10201800195XA
Authority
SG
Singapore
Prior art keywords
mthf
alternative
folate
based chemotherapy
fluorouracil
Prior art date
Application number
SG10201800195XA
Inventor
Per Lennart Lindberg
Anders Vedin
Gunnel Elisabeth Sundén
Bengt Gustavsson
Original Assignee
Isofol Medical Ab
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 Isofol Medical Ab filed Critical Isofol Medical Ab
Publication of SG10201800195XA publication Critical patent/SG10201800195XA/en

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    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/525Isoalloxazines, e.g. riboflavins, vitamin B2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/28Compounds containing heavy metals
    • A61K31/282Platinum compounds
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/33Heterocyclic compounds
    • A61K31/555Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • 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
    • A61K39/39558Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/545Medicinal preparations containing antigens or antibodies characterised by the dose, timing or administration schedule
    • 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
    • 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
    • C07K16/22Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against growth factors ; against growth regulators

Abstract

[6R]-MTHF – an efficient folate alternative in 5-fluorouracil based chemotherapy 5 The present invention relates to the treatment of solid tumors in humans such as cancer, especially colorectal cancer (CRC), which involves administering the diastereomerically pure folate adjuvant [6R]-5,10-methylenetetrahydrofolate in 5-fluorouracil (5-FU) based chemo- therapy. 10 Figure 1 15
SG10201800195XA 2017-08-24 2018-01-09 [6R]-MTHF – an efficient folate alternative in 5-fluorouracil based chemotherapy SG10201800195XA (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP17187684.0A EP3446704A1 (en) 2017-08-24 2017-08-24 [6r]-mthf - an efficient folate alternative in 5-fluorouracil based chemotherapy

Publications (1)

Publication Number Publication Date
SG10201800195XA true SG10201800195XA (en) 2019-03-28

Family

ID=59702573

Family Applications (2)

Application Number Title Priority Date Filing Date
SG11202001372TA SG11202001372TA (en) 2017-08-24 2018-01-05 [6r]-mthf - an efficient folate alternative in 5-fluorouracil based chemotherapy
SG10201800195XA SG10201800195XA (en) 2017-08-24 2018-01-09 [6R]-MTHF – an efficient folate alternative in 5-fluorouracil based chemotherapy

Family Applications Before (1)

Application Number Title Priority Date Filing Date
SG11202001372TA SG11202001372TA (en) 2017-08-24 2018-01-05 [6r]-mthf - an efficient folate alternative in 5-fluorouracil based chemotherapy

Country Status (19)

Country Link
US (2) US11013744B2 (en)
EP (3) EP3446704A1 (en)
JP (2) JP7356411B2 (en)
KR (1) KR102216031B1 (en)
CN (1) CN110290802A (en)
AU (1) AU2018320069A1 (en)
BR (1) BR112020003585A2 (en)
CA (2) CA3073555C (en)
DK (1) DK3446705T3 (en)
ES (1) ES2901621T3 (en)
HU (1) HUE057332T2 (en)
IL (1) IL272874B2 (en)
MX (1) MX2020002053A (en)
PL (1) PL3446705T3 (en)
PT (1) PT3446705T (en)
RU (1) RU2763934C2 (en)
SG (2) SG11202001372TA (en)
TW (1) TWI752147B (en)
WO (1) WO2019037898A1 (en)

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5376658A (en) 1990-05-11 1994-12-27 University Of Southern California 5,10-methylene-tetrahydrofolate as a modulator of a chemotherapeutic agent
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
KR20070019725A (en) 2004-04-02 2007-02-15 어드벤트륵스 파마슈티칼스, 인크. Use of 5,10-methylene tetrahydrofolate for the treatment of cancer
AU2005231436A1 (en) * 2004-04-02 2005-10-20 Adventrx Pharmaceuticals, Inc. Use of 5,10-methylene tetrahydrofolate for the treatment of cancer
CN1942189A (en) * 2004-04-02 2007-04-04 阿德文特克斯药物有限公司 Use of 5,10-methylene tetrahydrofolate for the treatment of cancer
AU2006320388A1 (en) * 2005-12-02 2007-06-07 Adventrx Pharmaceuticals, Inc. Stable pharmaceutical compositions of 5,10 methylenetetrahydrofolate
SI2068880T1 (en) 2006-09-18 2012-08-31 Boehringer Ingelheim Int Method for treating cancer harboring egfr mutations
WO2008109349A1 (en) 2007-03-06 2008-09-12 Adventrx Pharmaceuticals, Inc. Improved regimen for treating cancer with 5-fluorouracil, 5,10-methylenetetrahydrofolate and capecitabine
AU2008362108B2 (en) 2008-09-26 2015-09-03 Institut De Cancerologie De L'ouest Individual 5-fluorouracile dose optimization in FOLFOX treatment
EP2558122A4 (en) 2010-04-15 2014-03-05 Vegenics Pty Ltd Combination treatment with vegf-c antagonists
EP2617421A1 (en) 2012-01-20 2013-07-24 Isofol Medical AB Tetrahydrofolates in combination with EGFR-inhibitors in the use of treating cancer
EP2617422A1 (en) 2012-01-20 2013-07-24 Isofol Medical AB Anti-tumor activity of reduced folates like methylene-tetrahydrofolate, tetrahydrofolate or methyl-tetrahydrofolate
EP2837631A1 (en) * 2013-08-14 2015-02-18 Merck & Cie New stable salt of 5,10-methylene-(6R)-tetrahydrofolic acid
EP3305318A1 (en) 2016-10-05 2018-04-11 Isofol Medical AB [6r]-5,10-methylenetetrahydrofolate in 5-fluorouracil based chemotherapy

Also Published As

Publication number Publication date
EP3446705A1 (en) 2019-02-27
US20210401842A1 (en) 2021-12-30
CA3073555C (en) 2023-01-10
EP3446704A1 (en) 2019-02-27
TWI752147B (en) 2022-01-11
RU2020109130A (en) 2021-09-24
MX2020002053A (en) 2020-12-11
ES2901621T3 (en) 2022-03-23
CN110290802A (en) 2019-09-27
EP3446705B1 (en) 2021-09-22
JP2019038797A (en) 2019-03-14
RU2020109130A3 (en) 2021-09-24
AU2018320069A1 (en) 2020-03-05
HUE057332T2 (en) 2022-05-28
US20190060316A1 (en) 2019-02-28
IL272874A (en) 2020-04-30
TW201912159A (en) 2019-04-01
CA2991357A1 (en) 2019-02-24
DK3446705T3 (en) 2021-12-13
BR112020003585A2 (en) 2020-09-01
US11013744B2 (en) 2021-05-25
IL272874B1 (en) 2023-12-01
SG11202001372TA (en) 2020-03-30
RU2763934C2 (en) 2022-01-11
PT3446705T (en) 2021-12-29
IL272874B2 (en) 2024-04-01
JP7356411B2 (en) 2023-10-04
EP3672623A1 (en) 2020-07-01
KR102216031B1 (en) 2021-02-16
CA3073555A1 (en) 2019-02-28
KR20190022270A (en) 2019-03-06
WO2019037898A1 (en) 2019-02-28
PL3446705T3 (en) 2022-05-23
JP2020531490A (en) 2020-11-05

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