CA2855243C - Method of treating a proliferative disease - Google Patents
Method of treating a proliferative disease Download PDFInfo
- Publication number
- CA2855243C CA2855243C CA2855243A CA2855243A CA2855243C CA 2855243 C CA2855243 C CA 2855243C CA 2855243 A CA2855243 A CA 2855243A CA 2855243 A CA2855243 A CA 2855243A CA 2855243 C CA2855243 C CA 2855243C
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- CA
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- Prior art keywords
- braf inhibitor
- period
- weeks
- formula
- treatment
- 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.)
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- 201000010099 disease Diseases 0.000 title claims description 19
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims description 19
- 230000002062 proliferating effect Effects 0.000 title claims description 19
- 238000000034 method Methods 0.000 title abstract description 11
- 238000011282 treatment Methods 0.000 claims abstract description 55
- 229940125431 BRAF inhibitor Drugs 0.000 claims description 107
- 206010028980 Neoplasm Diseases 0.000 claims description 40
- 230000035772 mutation Effects 0.000 claims description 18
- 201000001441 melanoma Diseases 0.000 claims description 11
- 239000002774 b raf kinase inhibitor Substances 0.000 claims description 7
- 210000004881 tumor cell Anatomy 0.000 claims description 7
- 206010009944 Colon cancer Diseases 0.000 claims description 6
- 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 claims description 6
- 108010091528 Proto-Oncogene Proteins B-raf Proteins 0.000 claims description 6
- 102000018471 Proto-Oncogene Proteins B-raf Human genes 0.000 claims description 6
- 102100027103 Serine/threonine-protein kinase B-raf Human genes 0.000 claims description 6
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 5
- 230000001225 therapeutic effect Effects 0.000 claims description 2
- 229940121742 Serine/threonine kinase inhibitor Drugs 0.000 abstract 3
- 239000003814 drug Substances 0.000 description 10
- 241000699670 Mus sp. Species 0.000 description 7
- 229940123690 Raf kinase inhibitor Drugs 0.000 description 7
- 210000004027 cell Anatomy 0.000 description 7
- 229940079593 drug Drugs 0.000 description 7
- 102000051624 phosphatidylethanolamine binding protein Human genes 0.000 description 7
- 108700021017 phosphatidylethanolamine binding protein Proteins 0.000 description 7
- 108091000080 Phosphotransferase Proteins 0.000 description 6
- 239000003112 inhibitor Substances 0.000 description 6
- 102000020233 phosphotransferase Human genes 0.000 description 6
- 150000001875 compounds Chemical class 0.000 description 5
- 230000037361 pathway Effects 0.000 description 5
- 102000043136 MAP kinase family Human genes 0.000 description 4
- 108091054455 MAP kinase family Proteins 0.000 description 4
- 230000004044 response Effects 0.000 description 4
- 230000004083 survival effect Effects 0.000 description 4
- 229940102297 B-raf kinase inhibitor Drugs 0.000 description 3
- 101001059454 Homo sapiens Serine/threonine-protein kinase MARK2 Proteins 0.000 description 3
- 102100028904 Serine/threonine-protein kinase MARK2 Human genes 0.000 description 3
- 201000011510 cancer Diseases 0.000 description 3
- 230000003285 pharmacodynamic effect Effects 0.000 description 3
- 108010077182 raf Kinases Proteins 0.000 description 3
- 102000009929 raf Kinases Human genes 0.000 description 3
- 238000011084 recovery Methods 0.000 description 3
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 3
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 description 3
- KKVYYGGCHJGEFJ-UHFFFAOYSA-N 1-n-(4-chlorophenyl)-6-methyl-5-n-[3-(7h-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine Chemical compound N=1C=CC2=C(NC=3C(=CC=CN=3)C=3C=4N=CNC=4N=CN=3)C(C)=CC=C2C=1NC1=CC=C(Cl)C=C1 KKVYYGGCHJGEFJ-UHFFFAOYSA-N 0.000 description 2
- 101100381978 Mus musculus Braf gene Proteins 0.000 description 2
- 102100033479 RAF proto-oncogene serine/threonine-protein kinase Human genes 0.000 description 2
- 230000003213 activating effect Effects 0.000 description 2
- 230000001154 acute effect Effects 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- 230000002496 gastric effect Effects 0.000 description 2
- 230000035755 proliferation Effects 0.000 description 2
- 102200055464 rs113488022 Human genes 0.000 description 2
- 230000019491 signal transduction Effects 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 210000001685 thyroid gland Anatomy 0.000 description 2
- 238000011269 treatment regimen Methods 0.000 description 2
- 229960003862 vemurafenib Drugs 0.000 description 2
- SYLABBNLHCTJEF-UHFFFAOYSA-N 2-pyridin-2-yloxy-1h-benzimidazole Chemical class N=1C2=CC=CC=C2NC=1OC1=CC=CC=N1 SYLABBNLHCTJEF-UHFFFAOYSA-N 0.000 description 1
- 101150019464 ARAF gene Proteins 0.000 description 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 description 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 description 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 description 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 description 1
- 208000005623 Carcinogenesis Diseases 0.000 description 1
- 201000009030 Carcinoma Diseases 0.000 description 1
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 description 1
- 208000032612 Glial tumor Diseases 0.000 description 1
- 206010018338 Glioma Diseases 0.000 description 1
- 206010025323 Lymphomas Diseases 0.000 description 1
- 102100024193 Mitogen-activated protein kinase 1 Human genes 0.000 description 1
- 208000034578 Multiple myelomas Diseases 0.000 description 1
- 241000699660 Mus musculus Species 0.000 description 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 description 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 description 1
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 description 1
- 208000014767 Myeloproliferative disease Diseases 0.000 description 1
- 206010061309 Neoplasm progression Diseases 0.000 description 1
- 208000034176 Neoplasms, Germ Cell and Embryonal Diseases 0.000 description 1
- 206010029260 Neuroblastoma Diseases 0.000 description 1
- 108700020796 Oncogene Proteins 0.000 description 1
- 206010035226 Plasma cell myeloma Diseases 0.000 description 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 description 1
- 102000001708 Protein Isoforms Human genes 0.000 description 1
- 108010029485 Protein Isoforms Proteins 0.000 description 1
- 206010039491 Sarcoma Diseases 0.000 description 1
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 description 1
- 230000006978 adaptation Effects 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 210000003445 biliary tract Anatomy 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 210000000481 breast Anatomy 0.000 description 1
- 230000036952 cancer formation Effects 0.000 description 1
- 231100000504 carcinogenesis Toxicity 0.000 description 1
- 230000003915 cell function Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 description 1
- 230000001934 delay Effects 0.000 description 1
- 230000004069 differentiation Effects 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 description 1
- 210000003128 head Anatomy 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 201000007270 liver cancer Diseases 0.000 description 1
- 208000014018 liver neoplasm Diseases 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 208000000516 mast-cell leukemia Diseases 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 210000003739 neck Anatomy 0.000 description 1
- 230000000955 neuroendocrine Effects 0.000 description 1
- 238000011580 nude mouse model Methods 0.000 description 1
- 201000008968 osteosarcoma Diseases 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 210000002307 prostate Anatomy 0.000 description 1
- 150000003230 pyrimidines Chemical class 0.000 description 1
- 108700042226 ras Genes Proteins 0.000 description 1
- 102000027426 receptor tyrosine kinases Human genes 0.000 description 1
- 108091008598 receptor tyrosine kinases Proteins 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 208000000587 small cell lung carcinoma Diseases 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000001052 transient effect Effects 0.000 description 1
- 230000005751 tumor progression Effects 0.000 description 1
- 230000003827 upregulation Effects 0.000 description 1
- 238000011144 upstream manufacturing Methods 0.000 description 1
- 210000003932 urinary bladder Anatomy 0.000 description 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
- A61K31/495—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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161558619P | 2011-11-11 | 2011-11-11 | |
| US61/558,619 | 2011-11-11 | ||
| PCT/US2012/064269 WO2013070996A1 (en) | 2011-11-11 | 2012-11-09 | Method of treating a proliferative disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2855243A1 CA2855243A1 (en) | 2013-05-16 |
| CA2855243C true CA2855243C (en) | 2020-04-14 |
Family
ID=47279036
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2855243A Active CA2855243C (en) | 2011-11-11 | 2012-11-09 | Method of treating a proliferative disease |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US11007194B2 (enExample) |
| EP (1) | EP2776037B1 (enExample) |
| JP (1) | JP6150813B2 (enExample) |
| CN (2) | CN103917236A (enExample) |
| AU (1) | AU2012335663B2 (enExample) |
| BR (1) | BR112014011223A8 (enExample) |
| CA (1) | CA2855243C (enExample) |
| MX (1) | MX354725B (enExample) |
| RU (1) | RU2622015C2 (enExample) |
| WO (1) | WO2013070996A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3002B1 (ar) | 2009-08-28 | 2016-09-05 | Irm Llc | مركبات و تركيبات كمثبطات كيناز بروتين |
| EP2882440B1 (en) * | 2012-08-07 | 2019-02-27 | Novartis AG | Pharmaceutical combinations comprising a b-raf inhibitor, an egfr inhibitor and optionally a pi3k-alpha inhibitor |
| MX387795B (es) * | 2016-06-03 | 2025-03-19 | Array Biopharma Inc | Combinaciones farmaceuticas. |
| US11590133B2 (en) * | 2016-12-11 | 2023-02-28 | Memorial Sloan Kettering Cancer Center | Methods and compositions for treatment of BRAF mutant cancers |
| WO2020011141A1 (zh) * | 2018-07-12 | 2020-01-16 | 深圳市塔吉瑞生物医药有限公司 | 一种二芳基吡唑化合物及包含该化合物的组合物及其用途 |
| TWI817018B (zh) | 2019-06-28 | 2023-10-01 | 美商艾瑞生藥股份有限公司 | 用於治療ｂｒａｆ相關的疾病和失調症之化合物 |
| CN114929279A (zh) * | 2020-01-07 | 2022-08-19 | 锐新医药公司 | Shp2抑制剂给药和治疗癌症的方法 |
| US12303509B2 (en) | 2020-06-09 | 2025-05-20 | Pfizer Inc. | Compounds for the treatment of BRAF-associated diseases and disorders |
| CA3257280A1 (en) | 2022-05-25 | 2023-11-30 | Msd International Gmbh | COMBINATION OF A BRAF INHIBITOR, AN EGFR INHIBITOR AND A PD-1 ANTAGONIST FOR THE TREATMENT OF COLORECTAL CANCER MSI-H/DMMR, WITH BRAF V600E MUTATION |
| ES3035530T3 (en) | 2023-03-09 | 2025-09-04 | Minneamrita Therapeutics Llc | Drug combination for the treatment of stomach cancer |
| WO2025003956A1 (en) | 2023-06-30 | 2025-01-02 | Pfizer Inc. | High drug loading formulations of encorafenib |
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| US6358932B1 (en) | 1994-05-31 | 2002-03-19 | Isis Pharmaceticals, Inc. | Antisense oligonucleotide inhibition of raf gene expression |
| US6037136A (en) | 1994-10-24 | 2000-03-14 | Cold Spring Harbor Laboratory | Interactions between RaF proto-oncogenes and CDC25 phosphatases, and uses related thereto |
| US5717100A (en) | 1995-10-06 | 1998-02-10 | Merck & Co., Inc. | Substituted imidazoles having anti-cancer and cytokine inhibitory activity |
| AR012634A1 (es) | 1997-05-02 | 2000-11-08 | Sugen Inc | Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion |
| US6514977B1 (en) | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| HUP0001880A3 (en) | 1997-05-22 | 2002-03-28 | G D Searle & Co Chicago | Substituted pyrazoles as p38 kinase inhibitors |
| GB9716557D0 (en) | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
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| RU2007138264A (ru) | 2005-03-17 | 2009-09-10 | Новартис АГ (CH) | N-[3-(1-АМИНО-5,6,7,8-ТЕТРАГИДРО-2,4,4b-ТРИАЗАФЛУОРЕН-9-ИЛ)ФЕНИЛ]БЕНЗАМИДЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ТИРОЗИН/ТРЕОНИНКИНАЗ, ПРЕЖДЕ ВСЕГО КИНАЗ В-RAF |
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| WO2011092088A1 (en) | 2010-01-27 | 2011-08-04 | Nerviano Medical Sciences S.R.L. | Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors |
| EP2560966B1 (en) | 2010-03-30 | 2021-01-06 | Verseon International Corporation | Multisubstituted aromatic compounds as inhibitors of thrombin |
| JP5938038B2 (ja) | 2010-08-03 | 2016-06-22 | ネルヴィアーノ・メディカル・サイエンシズ・ソチエタ・ア・レスポンサビリタ・リミタータ | ピラゾロフェニル−ベンゼンスルホンアミド化合物の誘導体及びその抗腫瘍薬としての使用 |
| HUE032100T2 (en) | 2011-03-21 | 2017-08-28 | Valcuria Ab | A pharmaceutical composition comprising an HDAC inhibitor and a steroid and its use |
| US20140113919A1 (en) | 2011-06-14 | 2014-04-24 | Novartis Ag | Combination of panobinostat and ruxolitinib in the treatment of cancer such as a myeloproliferative neoplasm |
| DK2782557T3 (en) | 2011-11-23 | 2018-12-10 | Array Biopharma Inc | PHARMACEUTICAL FORMULATIONS |
| RU2015121367A (ru) | 2012-11-08 | 2017-01-10 | Новартис Аг | Фармацевтическая комбинация, содержащая ингибитор b-raf и ингибитор деацетилазы гистонов, и ее применение при лечении пролиферативных заболеваний |
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| HK1198920A1 (en) | 2015-06-19 |
| AU2012335663B2 (en) | 2015-12-24 |
| AU2012335663A1 (en) | 2014-05-29 |
| RU2014117707A (ru) | 2015-12-20 |
| CN103917236A (zh) | 2014-07-09 |
| US20140275136A1 (en) | 2014-09-18 |
| RU2622015C2 (ru) | 2017-06-08 |
| EP2776037B1 (en) | 2019-01-09 |
| BR112014011223A8 (pt) | 2023-01-31 |
| MX354725B (es) | 2018-03-16 |
| BR112014011223A2 (pt) | 2017-05-09 |
| EP2776037A1 (en) | 2014-09-17 |
| CN108542906A (zh) | 2018-09-18 |
| CA2855243A1 (en) | 2013-05-16 |
| JP2014533272A (ja) | 2014-12-11 |
| JP6150813B2 (ja) | 2017-06-21 |
| US11007194B2 (en) | 2021-05-18 |
| WO2013070996A1 (en) | 2013-05-16 |
| MX2014005726A (es) | 2014-05-28 |
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