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WO2015145388A3 - Methods of treating colorectal cancers harboring upstream wnt pathway mutations - Google Patents

Methods of treating colorectal cancers harboring upstream wnt pathway mutations Download PDF

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Publication number
WO2015145388A3
WO2015145388A3 PCT/IB2015/052245 IB2015052245W WO2015145388A3 WO 2015145388 A3 WO2015145388 A3 WO 2015145388A3 IB 2015052245 W IB2015052245 W IB 2015052245W WO 2015145388 A3 WO2015145388 A3 WO 2015145388A3
Authority
WO
WIPO (PCT)
Prior art keywords
wnt pathway
methods
colorectal cancers
treating colorectal
pathway mutations
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/IB2015/052245
Other languages
French (fr)
Other versions
WO2015145388A2 (en
Inventor
Linda BAGDASARIAN
Feng Cong
Savina JAEGER
Margaret Elise CLAUGHLIN
Ronald Meyer
Andrea MYERS
Michael Ross PALMER
Youzhen Wang
Stephen David WOOLFENDEN
Ana VIVANCOS
Héctor PALMER
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Novartis AG
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 Novartis AG filed Critical Novartis AG
Publication of WO2015145388A2 publication Critical patent/WO2015145388A2/en
Publication of WO2015145388A3 publication Critical patent/WO2015145388A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/33—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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39558—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2863—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for growth factors, growth regulators

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Mycology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Microbiology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The present invention relates to a method of treating patients suffering from colorectal cancer, more specifically BRAF V600E -mutant or BRAF wild type, but KRAS wild type and microsatellite-unstable colorectal cancer by using a Wnt pathway inhibitor or a combination comprising a Wnt pathway inhibitor and either a BRAF inhibitor, or an EGFR inhibitor, or both. The disclosure also relates to corresponding pharmaceutical formulations, uses, methods, combinations, and related disclosure embodiments.
PCT/IB2015/052245 2014-03-27 2015-03-26 Methods of treating colorectal cancers harboring upstream wnt pathway mutations Ceased WO2015145388A2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201461971162P 2014-03-27 2014-03-27
US61/971,162 2014-03-27
US201562119939P 2015-02-24 2015-02-24
US62/119,939 2015-02-24

Publications (2)

Publication Number Publication Date
WO2015145388A2 WO2015145388A2 (en) 2015-10-01
WO2015145388A3 true WO2015145388A3 (en) 2016-01-28

Family

ID=52815064

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2015/052245 Ceased WO2015145388A2 (en) 2014-03-27 2015-03-26 Methods of treating colorectal cancers harboring upstream wnt pathway mutations

Country Status (2)

Country Link
TW (1) TW201620548A (en)
WO (1) WO2015145388A2 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20200306244A1 (en) * 2016-06-22 2020-10-01 Novartis Ag Wnt inhibitors for use in the treatment of fibrosis
US11649505B2 (en) * 2016-12-21 2023-05-16 Agency For Science, Technology And Research Kit for identifying malignancy, and uses thereof
WO2019245460A1 (en) * 2018-06-21 2019-12-26 National University Of Singapore Stratifying cancer patients harbouring oncogenic mutations in the e3 ubiquitin ligase rnf43
CN113307882B (en) * 2021-05-12 2022-12-20 东北大学 Fusion protein SZ1 and its conjugated nanomedicine for targeted therapy of colorectal cancer caused by Rspo overactivation

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120059021A1 (en) * 2008-11-11 2012-03-08 University Of Washington Compositions and methods for treating cancer and methods for predicting a response to such treatments
WO2013086260A2 (en) * 2011-12-09 2013-06-13 Oncomed Pharmaceuticals, Inc. Combination therapy for treatment of cancer
WO2013130364A1 (en) * 2012-02-28 2013-09-06 Novartis Ag Cancer patient selection for administration of wnt signaling inhibitors using rnf43 mutation status
WO2014025688A1 (en) * 2012-08-07 2014-02-13 Novartis Ag Pharmaceutical combinations comprising a b-raf inhibitor, an egfr inhibitor and optionally a pi3k-alpha inhibitor

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NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
TW225528B (en) 1992-04-03 1994-06-21 Ciba Geigy Ag
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
CA2216796C (en) 1995-03-30 2003-09-02 Pfizer Inc. Quinazoline derivatives
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
KR100437582B1 (en) 1995-07-06 2004-12-17 노파르티스 아게 Pyrrolopyrimidines and Processes for the Preparation Thereof
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
EA001595B1 (en) 1996-04-12 2001-06-25 Варнер-Ламберт Компани Irreversible inhibitors of tyrosine kinases.
EP0907642B1 (en) 1996-06-24 2005-11-02 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
AU4342997A (en) 1996-09-13 1998-04-02 Sugen, Inc. Use of quinazoline derivatives for the manufacture of a medicament in the reatment of hyperproliferative skin disorders
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
CO4940418A1 (en) 1997-07-18 2000-07-24 Novartis Ag MODIFICATION OF A CRYSTAL OF A DERIVATIVE OF N-PHENYL-2-PIRIMIDINAMINE, PROCESSES FOR ITS MANUFACTURE AND USE
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
UA103918C2 (en) 2009-03-02 2013-12-10 Айерем Элелси N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as wnt signaling modulators
AR077975A1 (en) 2009-08-28 2011-10-05 Irm Llc PIRAZOL PYRIMIDINE DERIVATIVES AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
JO3300B1 (en) 2012-06-06 2018-09-16 Novartis Ag Compounds and compositions for modulating egfr activity

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120059021A1 (en) * 2008-11-11 2012-03-08 University Of Washington Compositions and methods for treating cancer and methods for predicting a response to such treatments
WO2013086260A2 (en) * 2011-12-09 2013-06-13 Oncomed Pharmaceuticals, Inc. Combination therapy for treatment of cancer
WO2013130364A1 (en) * 2012-02-28 2013-09-06 Novartis Ag Cancer patient selection for administration of wnt signaling inhibitors using rnf43 mutation status
WO2014025688A1 (en) * 2012-08-07 2014-02-13 Novartis Ag Pharmaceutical combinations comprising a b-raf inhibitor, an egfr inhibitor and optionally a pi3k-alpha inhibitor

Non-Patent Citations (8)

* Cited by examiner, † Cited by third party
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GIORDANO CAPONIGRO: "Abstract 2337: Efficacy of the RAF/PI3K[alpha]/anti-EGFR triple combination LGX818 + BYL719 + cetuximab in BRAFV600E colorectal tumor models.", 6 April 2013 (2013-04-06), XP055200917, Retrieved from the Internet <URL:http://cancerres.aacrjournals.org/content/73/8_Supplement/2337.short> [retrieved on 20150708] *
ISAAC SCHAMALE: "Wnt Signaling Pathway Inhibition Enhances Efficacy of Cetuximab", OTOLARYNGOLOGY -- HEAD AND NECK SURGERY, 1 September 2013 (2013-09-01), pages 81 - 82, XP055219423, Retrieved from the Internet <URL:http://oto.sagepub.com/content/149/2_suppl/P81.3> [retrieved on 20151008] *
J. LIU ET AL: "Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES, vol. 110, no. 50, 25 November 2013 (2013-11-25), pages 20224 - 20229, XP055121007, ISSN: 0027-8424, DOI: 10.1073/pnas.1314239110 *
K. TAKADA ET AL: "Targeted Disruption of the BCL9/ -Catenin Complex Inhibits Oncogenic Wnt Signaling", SCIENCE TRANSLATIONAL MEDICINE, vol. 4, no. 148, 22 August 2012 (2012-08-22), pages 148ra117 - 148ra117, XP055150823, ISSN: 1946-6234, DOI: 10.1126/scitranslmed.3003808 *
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M. CASAS-SELVES ET AL: "Tankyrase and the Canonical Wnt Pathway Protect Lung Cancer Cells from EGFR Inhibition", CANCER RESEARCH, vol. 72, no. 16, 15 August 2012 (2012-08-15), US, pages 4154 - 4164, XP055218639, ISSN: 0008-5472, DOI: 10.1158/0008-5472.CAN-11-2848 *
T. L. BIECHELE ET AL: "Wnt/ -Catenin Signaling and AXIN1 Regulate Apoptosis Triggered by Inhibition of the Mutant Kinase BRAFV600E in Human Melanoma", SCIENCE SIGNALING, vol. 5, no. 206, 10 January 2012 (2012-01-10), US, pages ra3 - ra3, XP055218840, ISSN: 1945-0877, DOI: 10.1126/scisignal.2002274 *
X. JIANG ET AL: "Inactivating mutations of RNF43 confer Wnt dependency in pancreatic ductal adenocarcinoma", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES, vol. 110, no. 31, 11 July 2013 (2013-07-11), pages 12649 - 12654, XP055200712, ISSN: 0027-8424, DOI: 10.1073/pnas.1307218110 *

Also Published As

Publication number Publication date
TW201620548A (en) 2016-06-16
WO2015145388A2 (en) 2015-10-01

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