EA202191283A1 - Способы лечения устойчивого к ингибиторам cdk4/6 рака - Google Patents

Способы лечения устойчивого к ингибиторам cdk4/6 рака

Info

Publication number
EA202191283A1
EA202191283A1 EA202191283A EA202191283A EA202191283A1 EA 202191283 A1 EA202191283 A1 EA 202191283A1 EA 202191283 A EA202191283 A EA 202191283A EA 202191283 A EA202191283 A EA 202191283A EA 202191283 A1 EA202191283 A1 EA 202191283A1
Authority
EA
Eurasian Patent Office
Prior art keywords
cancer
estrogen receptor
alpha
cdk4
treatment
Prior art date
Application number
EA202191283A
Other languages
English (en)
Inventor
Хитиша Пател
Тиру БИХАНИ
Хайке Арлт
Нианджун Тао
Original Assignee
Радиус Фармасьютикалс, Инк.
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 Радиус Фармасьютикалс, Инк. filed Critical Радиус Фармасьютикалс, Инк.
Publication of EA202191283A1 publication Critical patent/EA202191283A1/ru

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
    • A61K31/13—Amines
    • 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
    • A61K31/01—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
    • 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
    • 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
    • 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
    • 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
    • C12Q2600/158—Expression markers

Landscapes

  • 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)
  • Pathology (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Genetics & Genomics (AREA)
  • Analytical Chemistry (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Biophysics (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Molecular Biology (AREA)
  • 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

В изобретении раскрыты способы лечения положительного по эстрогеновому рецептору-альфа, устойчивого к ингибиторам CDK4/6 рака у субъекта, имеющего либо эстрогеновый рецептор-альфа дикого типа и/либо мутантный эстрогеновый рецептор-альфа, причем способ предусматривает введение субъекту терапевтически эффективного количества элацестранта или его фармацевтически приемлемой соли или сольвата, причем мутантный эстрогеновый рецептор-альфа содержит одну или несколько мутаций, выбранных из группы, состоящей из D538G, Y537X1, L536X2, P535H, V534E, S463P, V392I, E380Q и их комбинаций, где X1 представляет собой S, N или C; а X2 представляет собой R или Q. В соответствии с некоторыми вариантами осуществления, устойчивый к ингибиторам CDK4/6, положительный по эстрогеновому рецептору-альфа рак выбран из группы, состоящей из рака молочной железы, рака матки, рака яичников и рака гипофиза.
EA202191283A 2018-12-06 2019-12-06 Способы лечения устойчивого к ингибиторам cdk4/6 рака EA202191283A1 (ru)

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
EA202191283A1 true EA202191283A1 (ru) 2021-10-13

Family

ID=69063871

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202191283A EA202191283A1 (ru) 2018-12-06 2019-12-06 Способы лечения устойчивого к ингибиторам cdk4/6 рака

Country Status (14)

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

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116744925A (zh) * 2020-12-14 2023-09-12 阿尔维纳斯运营股份有限公司 用四氢萘衍生物作为雌激素受体降解剂治疗乳腺癌的方法
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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9421264B2 (en) * 2014-03-28 2016-08-23 Duke University Method of treating cancer using selective estrogen receptor modulators
EP4039253A1 (en) * 2015-04-29 2022-08-10 Radius Pharmaceuticals, Inc. Methods of treating cancer
KR20230109795A (ko) * 2017-01-05 2023-07-20 래디어스 파마슈티컬스, 인코포레이티드 Rad1901-2hcl의 다형 형태
SG11202013177WA (en) * 2018-07-04 2021-01-28 Radius Pharmaceuticals Inc Polymorphic forms of rad 1901-2hcl

Also Published As

Publication number Publication date
SG11202105531XA (en) 2021-06-29
WO2020118213A1 (en) 2020-06-11
CN113164779A (zh) 2021-07-23
EP3890834A1 (en) 2021-10-13
AU2019395093A1 (en) 2021-06-24
CA3121930A1 (en) 2020-06-11
MA54388A (fr) 2021-10-13
KR20210100137A (ko) 2021-08-13
JP2022511498A (ja) 2022-01-31
JOP20210137A1 (ar) 2023-01-30
IL283659A (en) 2021-07-29
BR112021010110A2 (pt) 2021-08-24
MX2021006411A (es) 2021-07-21
US20210330612A1 (en) 2021-10-28

Similar Documents

Publication Publication Date Title
EA202191283A1 (ru) Способы лечения устойчивого к ингибиторам cdk4/6 рака
MA55145A (fr) <sup2/>? <sub2/>?g12c? ?polythérapie comprenant un inhibiteur de kraset un ou plusieurs principes pharmaceutiquement actifs supplémentaires pour le traitement de cancers
EA202092086A1 (ru) Ингибиторы аргиназы
MX2021010544A (es) Inhibidores de la proteina tirosina fosfatasa y metodos para usarlos.
EA200801041A1 (ru) Ингибиторы мек и способы их применения
EA202090497A1 (ru) Соединения и композиции для лечения гематологических нарушений
EA202192122A1 (ru) Соединения, обладающие активностью индуцирования ферроптоза, и способы их применения
EA201890878A1 (ru) Способ лечения медуллобластомы с помощью ингибитора ezh2
EA201991894A1 (ru) ПИПЕРИДИН-ЗАМЕЩЕННЫЕ ИНГИБИТОРЫ Mnk И СВЯЗАННЫЕ С НИМИ СПОСОБЫ
EA202092540A1 (ru) Комбинации для лечения рака
CY1124762T1 (el) Αναστολεις πρωτεïνης δεσμευσης creb (cbp)
JOP20210164A1 (ar) طرق وتركيبات علاج السرطان
EA202092064A1 (ru) Способы изменения состава тела
MX2022007441A (es) Inhibidores de proteína tirosina fosfatasa y sus métodos de uso.
EA202193334A1 (ru) Фармацевтические композиции, содержащие агонист fxr и фибрат, для применения при лечении холестатического заболевания печени
MX2019004872A (es) Composicion que comprende un anticuerpo de protofibrilla anti-abeta y un inhibidor de beta-secretasa bace1 para el tratamiento de enfermedad de alzheimer.
EA202192400A1 (ru) Антитела против интегрина и их применение
EA202190057A1 (ru) Солюбилизированные апиразы, способы и применение
MX2021005248A (es) Anticuerpos contra cd73 activadores de células b.
MA56508A (fr) Inhibiteur d'egfr pour le traitement du cancer
MX2021006210A (es) Metodos para diagnosticar y/o tratar una hepatopatia, nefropatia o neumopatia aguda o cronica.
MX2021006915A (es) Inhibidores de cxcr7 para el tratamiento de cancer.
EA202191256A1 (ru) Способы лечения рака на моделях, имеющих мутации esr1
CO2022001354A2 (es) Métodos para tratar o prevenir la atrofia muscular espinal
EA202191922A1 (ru) Способы и композиции для лечения злокачественных опухолей