DK2614369T3 - Fremgangsmåde til bestemmelse af egnetheden for inhibitorer af human ezh2 i behandling - Google Patents
Fremgangsmåde til bestemmelse af egnetheden for inhibitorer af human ezh2 i behandling Download PDFInfo
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- DK2614369T3 DK2614369T3 DK11824247.8T DK11824247T DK2614369T3 DK 2614369 T3 DK2614369 T3 DK 2614369T3 DK 11824247 T DK11824247 T DK 11824247T DK 2614369 T3 DK2614369 T3 DK 2614369T3
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- DK
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- Prior art keywords
- ezh2
- mutant
- cancer
- histone
- inhibitor
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
- G01N33/6893—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids related to diseases not provided for elsewhere
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- 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
- A61K31/52—Purines, e.g. adenine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- 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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- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
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- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
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- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
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- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
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- C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
- C12Q1/6886—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
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- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
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- G—PHYSICS
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- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
- G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
- G01N33/5011—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing antineoplastic activity
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
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- G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
- G01N33/5082—Supracellular entities, e.g. tissue, organisms
- G01N33/5088—Supracellular entities, e.g. tissue, organisms of vertebrates
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- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
- G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
- G01N33/57407—Specifically defined cancers
- G01N33/57426—Specifically defined cancers leukemia
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- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
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- C12Q2600/00—Oligonucleotides characterized by their use
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- C12Q2600/00—Oligonucleotides characterized by their use
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- G01N2333/46—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans from vertebrates
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- G01N2333/90—Enzymes; Proenzymes
- G01N2333/91—Transferases (2.)
- G01N2333/91005—Transferases (2.) transferring one-carbon groups (2.1)
- G01N2333/91011—Methyltransferases (general) (2.1.1.)
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Claims (6)
1. Fremgangsmåde til bestemmelse af, hvorvidt et individ, der har eller mistænkes for at have cancer udvalgt fra lymfom og melanom, er en kandidat til behandling med en hæmmer af EZH2, hvilken fremgangsmåde omfatter; detektering af en Y64- mutant af et EZH2-polypeptid, hvis det er til stede, i en prøve, der er opnået fra individet; hvor tilstedeværelsen af Y641 -mutanten, indikerer, at individet er en kandidat til behandling med en hæmmer af EZH2.
2. Fremgangsmåde ifølge krav 1, hvor Y641 -mutanten er udvalgt fra gruppen bestående af Y641F, Y641H, Y641N og Y641S.
3. Fremgangsmåde ifølge et hvilket som helst af de foregående krav, hvor canceren er follikulært lymfom eller diffust stort B-cellelymfom (DLBCL)
4. Fremgangsmåde ifølge et hvilket som helst af de foregående krav, hvor detekteringen af Y641-mutanten af EZH2 sker ved: a. fuldgenomresekvensering, b. målområderesekvensering, der detekterer en nukleinsyre, der koder for Y641-mutanten af EZH2-polypeptidet, c. et antistof, der specifikt bindes til et polypeptid eller fragment deraf, der er karakteristisk for Y641 -mutanten af EZH2-polypeptidet; eller d. en nukleinsyresonde, der hybridiseres til en nukleinsyre, der koder for et polypeptid eller fragment deraf, der er karakteristisk for Y641-mutanten af EZH2-polypeptidet.
5. Fremgangsmåde ifølge krav 4, hvor målområderesekvenseringen omfatter amplifikation af mindst en del af nukleinsyren med mindst én PCR-primer.
6. Fremgangsmåde ifølge et hvilket som helst af kravene 1 til 5, hvor hæmmeren af EZH2 a. hæmmer trimethylering af H3-K27, eller b. hæmmer histonmethyltransferaseaktivitet for Y641 -mutanten af EZH2, eventuelt hvor hæmningen er selektiv hæmning.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US38168410P | 2010-09-10 | 2010-09-10 | |
PCT/US2011/051258 WO2012034132A2 (en) | 2010-09-10 | 2011-09-12 | Inhibitors of human ezh2, and methods of use thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
DK2614369T3 true DK2614369T3 (da) | 2016-05-02 |
Family
ID=45811204
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK11824247.8T DK2614369T3 (da) | 2010-09-10 | 2011-09-12 | Fremgangsmåde til bestemmelse af egnetheden for inhibitorer af human ezh2 i behandling |
Country Status (14)
Country | Link |
---|---|
US (6) | US8895245B2 (da) |
EP (1) | EP2614369B1 (da) |
JP (5) | JP6389036B2 (da) |
KR (3) | KR102373074B1 (da) |
CN (2) | CN105797158B (da) |
AU (4) | AU2011298987B2 (da) |
BR (1) | BR112013005806B1 (da) |
CA (2) | CA3176977A1 (da) |
DK (1) | DK2614369T3 (da) |
ES (1) | ES2570380T3 (da) |
HU (1) | HUE028977T2 (da) |
PL (1) | PL2614369T3 (da) |
RU (2) | RU2765155C2 (da) |
WO (1) | WO2012034132A2 (da) |
Families Citing this family (108)
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WO2011160206A1 (en) | 2010-06-23 | 2011-12-29 | Morin Ryan D | Biomarkers for non-hodgkin lymphomas and uses thereof |
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EP2614369B1 (en) * | 2010-09-10 | 2016-02-03 | Epizyme, Inc. | Method for determining the suitability of inhibitors of human ezh2 in treatment |
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JP2014534178A (ja) | 2011-09-30 | 2014-12-18 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーGlaxoSmithKline LLC | 癌の処置方法 |
US9051269B2 (en) | 2011-11-18 | 2015-06-09 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
EP2780014A4 (en) | 2011-11-18 | 2015-07-01 | Constellation Pharmaceuticals Inc | METHYLATION MODIFICATION ENZYME MODULATORS, COMPOSITIONS AND USES THEREOF |
CA2862289C (en) | 2012-02-10 | 2019-11-26 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
KR102149860B1 (ko) | 2012-02-27 | 2020-08-31 | 브리티쉬 콜롬비아 캔써 에이전시 브랜치 | 암의 후생적 결함을 교정하기 위한 작동자 단백질의 상호작용을 리프로그래밍하는 방법 |
EP3536314A1 (en) * | 2012-03-12 | 2019-09-11 | Epizyme, Inc. | Inhibitors of human ezh2, and methods of use thereof |
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BR112014025508B1 (pt) | 2012-04-13 | 2020-11-17 | Eisai R&D Management Co., Ltd. | forma de sal de um inibidor de histona metiltransferase ezh2 humana |
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CA2873779A1 (en) | 2012-05-16 | 2013-11-21 | Rana Therapeutics Inc. | Compositions and methods for modulating mecp2 expression |
BR112014028644A2 (pt) | 2012-05-16 | 2017-08-15 | Rana Therapeutics Inc | Composições e métodos para modulação da expressão de atp2a2 |
BR112014028631A2 (pt) | 2012-05-16 | 2017-10-17 | Rana Therapeutics Inc | composições e métodos para modulação da expressão da família de genes da hemoglobina |
CA2873794A1 (en) | 2012-05-16 | 2013-11-21 | Rana Therapeutics Inc. | Compositions and methods for modulating smn gene family expression |
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HUE046790T2 (hu) * | 2012-10-15 | 2020-03-30 | Epizyme Inc | A rák kezelésének módszerei |
MY180311A (en) * | 2012-10-15 | 2020-11-28 | Epizyme Inc | Substituted benzene compounds |
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US10130637B2 (en) | 2012-11-02 | 2018-11-20 | Duke University | Inhibition of histone methyltransferase for cardiac reprogramming |
EP2908843B1 (en) | 2012-11-19 | 2019-09-04 | Agency For Science, Technology And Research | Treating cancer |
UA111305C2 (uk) | 2012-12-21 | 2016-04-11 | Пфайзер Інк. | Конденсовані лактами арилу та гетероарилу |
EP2935264B1 (en) * | 2012-12-21 | 2017-10-18 | Epizyme, Inc. | 1,4-pyridone bicyclic heteroaryl compounds |
US9045455B2 (en) | 2013-03-14 | 2015-06-02 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
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2022
- 2022-10-04 AU AU2022242157A patent/AU2022242157A1/en active Pending
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2023
- 2023-08-04 JP JP2023127439A patent/JP2023153949A/ja active Pending
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