RU2007132902A - Способ лечения рака, устойчивого к гефитинибу - Google Patents
Способ лечения рака, устойчивого к гефитинибу Download PDFInfo
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- RU2007132902A RU2007132902A RU2007132902/14A RU2007132902A RU2007132902A RU 2007132902 A RU2007132902 A RU 2007132902A RU 2007132902/14 A RU2007132902/14 A RU 2007132902/14A RU 2007132902 A RU2007132902 A RU 2007132902A RU 2007132902 A RU2007132902 A RU 2007132902A
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- Prior art keywords
- cancer
- progression
- gefitinib
- erlotinib
- egfr inhibitor
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title claims abstract 37
- 201000011510 cancer Diseases 0.000 title claims abstract 37
- 238000000034 method Methods 0.000 title claims abstract 29
- 229940121647 egfr inhibitor Drugs 0.000 claims abstract 12
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims abstract 11
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims abstract 11
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims abstract 11
- 229960001433 erlotinib Drugs 0.000 claims abstract 11
- 229960002584 gefitinib Drugs 0.000 claims abstract 11
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims abstract 11
- 230000002427 irreversible effect Effects 0.000 claims abstract 11
- NERXPXBELDBEPZ-RMKNXTFCSA-N (e)-n-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide Chemical compound C=12C=C(NC(=O)\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC(F)=C1 NERXPXBELDBEPZ-RMKNXTFCSA-N 0.000 claims abstract 4
- 229950008835 neratinib Drugs 0.000 claims abstract 4
- ZNHPZUKZSNBOSQ-BQYQJAHWSA-N neratinib Chemical compound C=12C=C(NC\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC=N1 ZNHPZUKZSNBOSQ-BQYQJAHWSA-N 0.000 claims abstract 4
- WVUNYSQLFKLYNI-AATRIKPKSA-N pelitinib Chemical group C=12C=C(NC(=O)\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC1=CC=C(F)C(Cl)=C1 WVUNYSQLFKLYNI-AATRIKPKSA-N 0.000 claims abstract 4
- 102000001301 EGF receptor Human genes 0.000 claims abstract 3
- 108060006698 EGF receptor Proteins 0.000 claims abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 3
- 239000003112 inhibitor Substances 0.000 claims abstract 2
- 230000000007 visual effect Effects 0.000 claims 4
- 206010005003 Bladder cancer Diseases 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 3
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 3
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 3
- 206010033128 Ovarian cancer Diseases 0.000 claims 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 206010038389 Renal cancer Diseases 0.000 claims 3
- 208000016624 Retinal neoplasm Diseases 0.000 claims 3
- 208000000453 Skin Neoplasms Diseases 0.000 claims 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 3
- 208000008385 Urogenital Neoplasms Diseases 0.000 claims 3
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims 3
- 210000002919 epithelial cell Anatomy 0.000 claims 3
- 201000004101 esophageal cancer Diseases 0.000 claims 3
- 201000010536 head and neck cancer Diseases 0.000 claims 3
- 208000014829 head and neck neoplasm Diseases 0.000 claims 3
- 201000010982 kidney cancer Diseases 0.000 claims 3
- 201000007270 liver cancer Diseases 0.000 claims 3
- 208000014018 liver neoplasm Diseases 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 3
- 201000011682 nervous system cancer Diseases 0.000 claims 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 3
- 201000002528 pancreatic cancer Diseases 0.000 claims 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 3
- 201000008933 retinal cancer Diseases 0.000 claims 3
- 201000000849 skin cancer Diseases 0.000 claims 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 3
- 201000005112 urinary bladder cancer Diseases 0.000 claims 3
- 230000005907 cancer growth Effects 0.000 claims 2
- 238000003384 imaging method Methods 0.000 claims 2
- 230000035772 mutation Effects 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- 230000002441 reversible effect Effects 0.000 claims 2
- 239000000107 tumor biomarker Substances 0.000 claims 2
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims 1
- 239000004473 Threonine Substances 0.000 claims 1
- 238000001514 detection method Methods 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 229930182817 methionine Natural products 0.000 claims 1
- 150000002741 methionine derivatives Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 208000016691 refractory malignant neoplasm Diseases 0.000 abstract 1
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
- A61K31/435—Heterocyclic 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines 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
- A61K31/435—Heterocyclic 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4706—4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gastroenterology & Hepatology (AREA)
- Zoology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (27)
1. Способ лечения рака, устойчивого к гефитинибу и/или эрлотинибу, включающий в себя стадии:
a. контролирования прогрессирования рака у субъекта в момент времени после начала лечения гефитинибом и/или эрлотинибом, где прогрессирование рака свидетельствует об устойчивости данного заболевания к лечению гефитинибом и/или эрлотинибом; и
b. введения субъекту, страдающему от рака, устойчивого к лечению гефитинибом и/или эрлотинибом, фармацевтической композиции, содержащей необратимый ингибитор рецептора эпидермального фактора роста (EGFR).
2. Способ по п.1, где необратимый ингибитор EGFR выбран из группы, состоящей из EKB-569, HKI-272 и HKI-357.
3. Способ по п.1, где необратимый ингибитор EGFR связывается с остатком цистеина в положении 773 молекулы EGFR (SEQ ID NO: 1).
4. Способ по п.1, где прогрессирование рака регистрируют путем визуального наблюдения.
5. Способ по п.4, где визуальное наблюдение рака осуществляют с помощью рентгеновского излучения, срезов КТ или ЯМР-томографии.
6. Способ по п.1, где прогрессирование рака отслеживают путем детекции опухолевых биомаркеров.
7. Способ по п.1, где контролирование прогрессирования рака включает сравнение состояния рака во второй момент времени и в первый момент времени, причем второй момент времени наступает после первого, а первый момент времени может находиться до или после начала лечения гефитинибом и/или эрлотинибом, где повышенный рост раковой опухоли указывает на прогрессирование рака.
8. Способ по п.7, где с указанными ранее моментами времени сравнивают другие моменты времени.
9. Способ по п.1, где рак представляет собой эпителиально-клеточный рак.
10. Способ по п.1, где рак представляет собой рак желудочно-кишечного тракта, рак простаты, рак яичников, рак молочной железы, рак головы и шеи, рак пищевода, рак легких, немелкоклеточный рак легких, рак нервной системы, рак почек, рак сетчатки, рак кожи, рак печени, рак поджелудочной железы, рак мочеполовой системы и рак мочевого пузыря.
11. Способ лечения рака, включающий в себя стадии:
a. введения гефитиниба и/или эрлотиниба субъекту, страдающему от рака;
b. контролирования прогрессирования рака у субъекта; и
c. введения субъекту необратимого ингибитора EGFR в случае прогрессирования рака.
12. Способ по п.11, где необратимый ингибитор EGFR выбран из группы, состоящей из EKB-569, HKI-272 и HKI-357.
13. Способ по п.11, где необратимый ингибитор EGFR связывается с остатком цистеина в положении 773 молекулы EGFR (SEQ ID NO: 1).
14. Способ по п.11, где прогрессирование рака регистрируют путем визуального наблюдения.
15. Способ по п.14, где визуальное наблюдение рака осуществляют с помощью рентгеновского излучения, срезов КТ или ЯМР-томографии.
16. Способ по п.11, где прогрессирование рака контролируют путем детекции опухолевых биомаркеров.
17. Способ по п.11, где контролирование прогрессирования рака включает сравнение состояния рака во второй момент времени и в первый момент времени, причем второй момент времени наступает после первого, а первый момент времени может находиться до или после начала лечения гефитинибом и/или эрлотинибом, где повышенный рост раковой опухоли указывает на прогрессирование рака.
18. Способ по п.17, где с указанными ранее моментами времени сравнивают другие моменты времени.
19. Способ по п.11, где рак представляет собой эпителиальноклеточный рак.
20. Способ по п.11, где рак представляет собой рак желудочно-кишечного тракта, рак простаты, рак яичников, рак молочной железы, рак головы и шеи, рак пищевода, рак легких, немелкоклеточный рак легких, рак нервной системы, рак почек, рак сетчатки, рак кожи, рак печени, рак поджелудочной железы, рак мочеполовой системы и рак мочевого пузыря.
21. Способ по п.11, где необратимый ингибитор EGFR вводят одновременно с обратимым ингибитором EGFR.
22. Способ по п.21, где обратимый ингибитор EGFR представляет собой гефитиниб или эрлотиниб.
23. Способ лечения рака, включающий введение субъекту, страдающему от рака и несущему мутацию в EGFR (SEQ ID NO: 1), где мутация представляет собой замену метионина в положении 790 на треонин, фармацевтической композиции, содержащей необратимый ингибитор EGFR.
24. Способ по п.23, где ингибитор EGFR выбран из группы, состоящей из EKB-569, HKI-272 и HKI-357.
25. Способ по п.23, где необратимый ингибитор EGFR связывается с остатком цистеина в положении 773 молекулы EGFR (SEQ ID NO: 1).
26. Способ по п.23, где рак представляет собой эпителиально-клеточный рак.
27. Способ по п.23, где рак представляет собой рак желудочно-кишечного тракта, рак простаты, рак яичников, рак молочной железы, рак головы и шеи, рак пищевода, рак легких, немелкоклеточный рак легких, рак нервной системы, рак почек, рак сетчатки, рак кожи, рак печени, рак поджелудочной железы, рак мочеполовой системы и рак мочевого пузыря.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US64948305P | 2005-02-03 | 2005-02-03 | |
| US60/649,483 | 2005-02-03 | ||
| US67198905P | 2005-04-15 | 2005-04-15 | |
| US60/671,989 | 2005-04-15 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2007132902A true RU2007132902A (ru) | 2009-03-10 |
| RU2405566C2 RU2405566C2 (ru) | 2010-12-10 |
Family
ID=36777922
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2007132902/14D RU2405566C9 (ru) | 2005-02-03 | 2006-02-02 | Способ лечения рака, устойчивого к гефитинибу |
| RU2007132902/14A RU2405566C2 (ru) | 2005-02-03 | 2006-02-02 | Способ лечения рака, устойчивого к гефитинибу |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2007132902/14D RU2405566C9 (ru) | 2005-02-03 | 2006-02-02 | Способ лечения рака, устойчивого к гефитинибу |
Country Status (27)
| Country | Link |
|---|---|
| US (3) | US10603314B2 (ru) |
| EP (1) | EP1848414B1 (ru) |
| JP (1) | JP2008528695A (ru) |
| KR (1) | KR101313702B1 (ru) |
| CN (8) | CN108421044A (ru) |
| AT (1) | ATE504299T1 (ru) |
| AU (1) | AU2006210572B2 (ru) |
| BR (1) | BRPI0606839B8 (ru) |
| CA (1) | CA2596714C (ru) |
| CY (2) | CY1111676T1 (ru) |
| DE (1) | DE602006021142D1 (ru) |
| DK (1) | DK1848414T3 (ru) |
| ES (1) | ES2364495T3 (ru) |
| FR (1) | FR16C1004I1 (ru) |
| HU (1) | HUS1600033I1 (ru) |
| IL (3) | IL184791A (ru) |
| LU (1) | LU93160I2 (ru) |
| MX (1) | MX2007009317A (ru) |
| NI (1) | NI200700185A (ru) |
| NO (1) | NO20074366L (ru) |
| NZ (1) | NZ556673A (ru) |
| PL (1) | PL1848414T3 (ru) |
| PT (1) | PT1848414E (ru) |
| RU (2) | RU2405566C9 (ru) |
| SI (1) | SI1848414T1 (ru) |
| WO (1) | WO2006084058A2 (ru) |
| ZA (1) | ZA200706804B (ru) |
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| CN108421044A (zh) | 2005-02-03 | 2018-08-21 | 综合医院公司 | 治疗吉非替尼耐药性癌症的方法 |
| EP2505591A1 (en) | 2005-02-11 | 2012-10-03 | Memorial Sloan-Kettering Cancer Center | Methods and compositions for detecting a drug resistant EGFR mutant |
| MX2007012662A (es) * | 2005-04-14 | 2008-04-04 | Wyeth Corp | Uso de un inhibidor de la cinasa del receptor del factor de crecimiento epidermico (egfr) en pacientes resistentes al gefitinib. |
| BRPI0618042A2 (pt) | 2005-11-04 | 2011-08-16 | Wyeth Corp | usos de uma rapamicina e de uma herceptina, produto, pacote farmacêutico, e, composição farmacêutica |
| EP1948179A1 (en) | 2005-11-11 | 2008-07-30 | Boehringer Ingelheim International GmbH | Quinazoline derivatives for the treatment of cancer diseases |
| PL1948180T3 (pl) * | 2005-11-11 | 2013-09-30 | Boehringer Ingelheim Int | Terapia skojarzona raka polegająca na podawaniu inhibitorów EGFR/HER2 |
| CN101516376A (zh) * | 2006-09-18 | 2009-08-26 | 贝林格尔.英格海姆国际有限公司 | 用于治疗携带egfr突变的癌症的方法 |
| BRPI0717586A2 (pt) | 2006-09-18 | 2013-10-29 | Boehringer Ingelheim Int | Método para tratar câncer apresentando mutações do egfr |
| WO2008121467A2 (en) * | 2007-02-28 | 2008-10-09 | Dana-Farber Cancer Institute, Inc. | Combination therapy for treating cancer |
| US20100112687A1 (en) * | 2007-03-02 | 2010-05-06 | Mdrna, Inc. | Nucleic acid compounds for inhibiting erbb family gene expression and uses thereof |
| AU2013203111B2 (en) * | 2007-04-13 | 2015-10-08 | Beth Israel Deaconess Medical Center, Inc. | Methods for treating cancer resistant to erbb therapeutics |
| ES2529790T3 (es) * | 2007-04-13 | 2015-02-25 | Dana-Farber Cancer Institute, Inc. | Métodos de tratamiento de cáncer resistente a agentes terapéuticos de ERBB |
| US8022216B2 (en) | 2007-10-17 | 2011-09-20 | Wyeth Llc | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof |
| CN102641270A (zh) | 2008-06-17 | 2012-08-22 | 惠氏有限责任公司 | 含有hki-272和长春瑞滨的抗肿瘤组合 |
| CA2730930C (en) | 2008-07-16 | 2015-01-13 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors |
| US8669273B2 (en) | 2008-08-04 | 2014-03-11 | Wyeth Llc | Antineoplastic combinations of 4-anilino-3-cyanoquinolines and capecitabine |
| IL264349B2 (en) | 2009-04-06 | 2024-01-01 | Wyeth Llc | Regimen comprising neratinib for the treatment of cancer |
| JP5918693B2 (ja) | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Egfr阻害剤及び疾患の治療方法 |
| PL2451445T3 (pl) | 2009-07-06 | 2019-09-30 | Boehringer Ingelheim International Gmbh | Sposób suszenia BIBW2992, jego soli i stałych preparatów farmaceutycznych zawierających tę substancję czynną |
| US9556426B2 (en) | 2009-09-16 | 2017-01-31 | Celgene Avilomics Research, Inc. | Protein kinase conjugates and inhibitors |
| JP2013512882A (ja) | 2009-12-07 | 2013-04-18 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | トリプルネガティブ乳癌の治療に使用するbibw2992 |
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