JOP20210137A1 - طرق علاج سرطان مقاومة لمثبطات cdk4/6 - Google Patents

طرق علاج سرطان مقاومة لمثبطات cdk4/6

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Publication number
JOP20210137A1
JOP20210137A1 JOP/2021/0137A JOP20210137A JOP20210137A1 JO P20210137 A1 JOP20210137 A1 JO P20210137A1 JO P20210137 A JOP20210137 A JO P20210137A JO P20210137 A1 JOP20210137 A1 JO P20210137A1
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Jordan
Prior art keywords
estrogen receptor
receptor alpha
cdk4
cancer
methods
Prior art date
Application number
JOP/2021/0137A
Other languages
English (en)
Inventor
Heike Arlt
Hitisha Patel
Teeru Bihani
Nianjun Tao
Original Assignee
Radius Pharmaceuticals Inc
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 Radius Pharmaceuticals Inc filed Critical Radius Pharmaceuticals Inc
Publication of JOP20210137A1 publication Critical patent/JOP20210137A1/ar

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    • A61K31/01—Hydrocarbons
    • A61K31/015—Hydrocarbons carbocyclic
    • 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
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    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/566—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol having an oxo group in position 17, e.g. estrone
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/106—Pharmacogenomics, i.e. genetic variability in individual responses to drugs and drug metabolism
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    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/158—Expression markers

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
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  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Genetics & Genomics (AREA)
  • Analytical Chemistry (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
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  • Physics & Mathematics (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

تم الكشف هنا عن طرق معالجة سرطان إيجابي ألفا لمستقبلات هرمون الاستروجين المقاوم لمثبط CDK4/6 في مريض له إما مستقبلات استروجين من النوع البري ألفا و/أو مستقبلات استروجين متحولة ألفا، وهي طريقة تشتمل على إعطاء المريض كمية فعالة علاجيًا من إيلاسيسترانت، أو ملح مقبول صيدلانيًا أو مذيب منه، حيث يشتمل مستقبل الأستروجين الطافر ألفا على طفرة واحدة أو أكثر تم اختيارها من المجموعة التي تتكون من D538G، Y537X 1، L536X 2، P535H، V534E، S463P، V392I، E380Q وتوليفات منها، حيث: X 1 هو S أو N أو C؛ وX 2 هو R أو Q. في بعض النماذج، يتم اختيار سرطان إيجابي ألفا لمستقبلات الاستروجين المقاوم لمستقبلات CDK4/6 من المجموعة التي تتكون من سرطان الثدي وسرطان الرحم وسرطان المبيض وسرطان الغدة النخامية.
JOP/2021/0137A 2018-12-06 2019-12-06 طرق علاج سرطان مقاومة لمثبطات cdk4/6 JOP20210137A1 (ar)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862776323P 2018-12-06 2018-12-06
PCT/US2019/065005 WO2020118213A1 (en) 2018-12-06 2019-12-06 Methods for treating cancer resistant to cdk4/6 inhibitors

Publications (1)

Publication Number Publication Date
JOP20210137A1 true JOP20210137A1 (ar) 2023-01-30

Family

ID=69063871

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2021/0137A JOP20210137A1 (ar) 2018-12-06 2019-12-06 طرق علاج سرطان مقاومة لمثبطات cdk4/6

Country Status (15)

Country Link
US (1) US20210330612A1 (ar)
EP (1) EP3890834A1 (ar)
JP (1) JP2022511498A (ar)
KR (1) KR20210100137A (ar)
CN (1) CN113164779A (ar)
AU (1) AU2019395093A1 (ar)
BR (1) BR112021010110A2 (ar)
CA (1) CA3121930A1 (ar)
EA (1) EA202191283A1 (ar)
IL (1) IL283659A (ar)
JO (1) JOP20210137A1 (ar)
MA (1) MA54388A (ar)
MX (1) MX2021006411A (ar)
SG (1) SG11202105531XA (ar)
WO (1) WO2020118213A1 (ar)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202237117A (zh) * 2020-12-14 2022-10-01 美商亞文納營運公司 使用四氫萘衍生物作為雌激素受體降解劑治療乳癌之方法
GB202116745D0 (en) * 2021-11-19 2022-01-05 Institute Of Cancer Res Royal Cancer Hospital Prognostic and treatment response predictive method
CN115369089A (zh) * 2022-08-11 2022-11-22 中山大学孙逸仙纪念医院 两种er阳性her-2阴性乳腺癌cdk4/6抑制剂耐药株及其构建方法和用途

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL297369B1 (en) * 2015-04-29 2024-02-01 Radius Pharmaceuticals Inc RAD for use in a method to treat mutant estrogen receptor positive breast cancer or mutant estrogen receptor positive ovarian cancer
KR102322802B1 (ko) * 2017-01-05 2021-11-04 래디어스 파마슈티컬스, 인코포레이티드 Rad1901-2hcl의 다형 형태

Also Published As

Publication number Publication date
US20210330612A1 (en) 2021-10-28
EA202191283A1 (ru) 2021-10-13
JP2022511498A (ja) 2022-01-31
KR20210100137A (ko) 2021-08-13
IL283659A (en) 2021-07-29
SG11202105531XA (en) 2021-06-29
BR112021010110A2 (pt) 2021-08-24
EP3890834A1 (en) 2021-10-13
CN113164779A (zh) 2021-07-23
AU2019395093A1 (en) 2021-06-24
MA54388A (fr) 2021-10-13
CA3121930A1 (en) 2020-06-11
WO2020118213A1 (en) 2020-06-11
MX2021006411A (es) 2021-07-21

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