JP2017507995A5 - - Google Patents
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- Publication number
- JP2017507995A5 JP2017507995A5 JP2016558004A JP2016558004A JP2017507995A5 JP 2017507995 A5 JP2017507995 A5 JP 2017507995A5 JP 2016558004 A JP2016558004 A JP 2016558004A JP 2016558004 A JP2016558004 A JP 2016558004A JP 2017507995 A5 JP2017507995 A5 JP 2017507995A5
- Authority
- JP
- Japan
- Prior art keywords
- cabozantinib
- auc
- mean
- cancer
- measured
- 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.)
- Granted
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- ONIQOQHATWINJY-UHFFFAOYSA-N cabozantinib Chemical compound C=12C=C(OC)C(OC)=CC2=NC=CC=1OC(C=C1)=CC=C1NC(=O)C1(C(=O)NC=2C=CC(F)=CC=2)CC1 ONIQOQHATWINJY-UHFFFAOYSA-N 0.000 claims description 89
- 239000002176 L01XE26 - Cabozantinib Substances 0.000 claims description 81
- 229960001292 cabozantinib Drugs 0.000 claims description 81
- 239000002207 metabolite Substances 0.000 claims description 17
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 17
- 210000002381 plasma Anatomy 0.000 claims description 16
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- 206010028980 Neoplasm Diseases 0.000 claims description 10
- 201000011510 cancer Diseases 0.000 claims description 10
- AEMOLEFTQBMNLQ-AQKNRBDQSA-N D-glucopyranuronic acid Chemical group OC1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O AEMOLEFTQBMNLQ-AQKNRBDQSA-N 0.000 claims description 4
- 238000009472 formulation Methods 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 206010005949 Bone cancer Diseases 0.000 claims description 2
- 208000018084 Bone neoplasm Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 201000001342 Fallopian tube cancer Diseases 0.000 claims description 2
- 208000013452 Fallopian tube neoplasm Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 208000009018 Medullary thyroid cancer Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 2
- 210000001072 colon Anatomy 0.000 claims description 2
- 201000005787 hematologic cancer Diseases 0.000 claims description 2
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 208000023356 medullary thyroid gland carcinoma Diseases 0.000 claims description 2
- 210000004798 organs belonging to the digestive system Anatomy 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 201000000849 skin cancer Diseases 0.000 claims description 2
- 238000000034 method Methods 0.000 description 8
- WHTYLRLZUGABTR-UHFFFAOYSA-N 1-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide Chemical compound C=1C=C(F)C=CC=1NC(=O)C1(C(=O)N)CC1 WHTYLRLZUGABTR-UHFFFAOYSA-N 0.000 description 1
- -1 4-{[6,7-bis (methyloxy) quinolin-4-yl] oxy} phenyl Chemical group 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461954352P | 2014-03-17 | 2014-03-17 | |
| US61/954,352 | 2014-03-17 | ||
| PCT/US2015/021072 WO2015142928A1 (en) | 2014-03-17 | 2015-03-17 | Dosing of cabozantinib formulations |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017507995A JP2017507995A (ja) | 2017-03-23 |
| JP2017507995A5 true JP2017507995A5 (OSRAM) | 2018-04-26 |
| JP6666849B2 JP6666849B2 (ja) | 2020-03-18 |
Family
ID=52811227
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016558004A Active JP6666849B2 (ja) | 2014-03-17 | 2015-03-17 | カボザンチニブ製剤の投与 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US10159666B2 (OSRAM) |
| EP (1) | EP3119476A1 (OSRAM) |
| JP (1) | JP6666849B2 (OSRAM) |
| CN (1) | CN106255499A (OSRAM) |
| EA (1) | EA201691850A1 (OSRAM) |
| MA (1) | MA39735A (OSRAM) |
| WO (1) | WO2015142928A1 (OSRAM) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101733773B1 (ko) | 2009-01-16 | 2017-05-10 | 엑셀리시스, 인코포레이티드 | Ｎ-（４-｛〔６，７-비스（메틸옥시）퀴놀린-4-일〕옥시｝페닐）-ｎ＇-（４-플루오로페닐）사이클로프로판-1,1-디카르복사미드의 말산염 및 그 결정형 |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| GEP20247677B (en) | 2011-02-10 | 2024-10-10 | Exelixis Inc | Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds |
| KR102276348B1 (ko) | 2013-03-15 | 2021-07-12 | 엑셀리시스, 인코포레이티드 | Ｎ（４〔［６,７비스（메틸옥시）퀴놀린４일］옥시〕페닐）ｎ′（４플루오로페닐）시클로프로판１,１디카복사미드의 대사물 |
| US11564915B2 (en) | 2013-04-04 | 2023-01-31 | Exelixis, Inc. | Cabozantinib dosage form and use in the treatment of cancer |
| BR112016018450A2 (pt) | 2014-02-14 | 2018-09-18 | Exelixis Inc | formas sólidas cristalinas de n-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-n'-(4-fluorofenil)ciclopropano-1,1-dicarboxamida, processos de preparo e métodos de uso |
| EA201691850A1 (ru) | 2014-03-17 | 2016-12-30 | Экселиксис, Инк. | Дозирование составов, содержащих кабозантиниб |
| MA40386A (fr) * | 2014-07-31 | 2016-02-04 | Exelixis Inc | Procédé de préparation de cabozantinib marqué au fluor-18 et d'analogues de celui-ci |
| EA034992B1 (ru) | 2014-08-05 | 2020-04-15 | Экселиксис, Инк. | Комбинации лекарственных средств для лечения множественной миеломы |
| US10654808B2 (en) * | 2015-04-07 | 2020-05-19 | Guangdong Raynovent Biotech Co., Ltd. | Tyrosine kinase inhibitor and pharmaceutical composition comprising same |
| RU2748549C2 (ru) | 2016-04-15 | 2021-05-26 | Экселиксис, Инк. | Способ лечения почечно-клеточного рака с использованием n-(4-(6,7-диметоксихинолин-4-илокси)фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, (2s)-гидроксибутандиоата |
| CN107951850A (zh) * | 2017-12-20 | 2018-04-24 | 深圳万乐药业有限公司 | 一种苹果酸卡博替尼片的制备方法 |
| CN117624045A (zh) | 2018-01-26 | 2024-03-01 | 埃克塞里艾克西斯公司 | 用于治疗激酶依赖性病症的化合物 |
| CN113292537B (zh) | 2018-06-15 | 2024-04-05 | 汉达癌症医药责任有限公司 | 激酶抑制剂的盐类及其组合物 |
| AU2024215796A1 (en) | 2023-01-31 | 2025-05-15 | Handa Oncology, Llc | Improved cabozantinib compositions and methods of use |
| WO2025079089A1 (en) * | 2023-10-09 | 2025-04-17 | Msn Laboratories Private Limited, R&D Center | Pharmaceutical composition of cabozantinib |
| WO2025196845A1 (en) * | 2024-03-22 | 2025-09-25 | Meishi Pharma Services Pvt. Ltd. | Improved formulations of cabozantinib |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2744997A1 (en) | 2003-09-26 | 2005-04-07 | Exelixis, Inc. | C-met modulators and method of use |
| AU2006231646A1 (en) | 2005-04-06 | 2006-10-12 | Exelixis, Inc. | C-Met modulators and methods of use |
| AU2007334402B2 (en) | 2006-12-14 | 2014-02-13 | Exelixis, Inc. | Methods of using MEK inhibitors |
| UY31800A (es) | 2008-05-05 | 2009-11-10 | Smithkline Beckman Corp | Metodo de tratamiento de cancer usando un inhibidor de cmet y axl y un inhibidor de erbb |
| UY32142A (es) | 2008-09-26 | 2010-05-31 | Smithkline Beckman Corp | Preparación de una quinoliniloxidifenilciclopropanodicarboxamida |
| JP5486606B2 (ja) | 2008-11-13 | 2014-05-07 | エクセリクシス， インク． | キノリン誘導体の調製方法 |
| JP2012511017A (ja) | 2008-12-04 | 2012-05-17 | エグゼリクシス， インコーポレイテッド | キノリン誘導体の調製方法 |
| KR101733773B1 (ko) * | 2009-01-16 | 2017-05-10 | 엑셀리시스, 인코포레이티드 | Ｎ-（４-｛〔６，７-비스（메틸옥시）퀴놀린-4-일〕옥시｝페닐）-ｎ＇-（４-플루오로페닐）사이클로프로판-1,1-디카르복사미드의 말산염 및 그 결정형 |
| AU2010274012A1 (en) | 2009-07-17 | 2012-02-09 | Exelixis, Inc. | Crystalline forms of N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy] -quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| SG184040A1 (en) | 2010-03-12 | 2012-10-30 | Exelixis Inc | Hydrated crystalline forms of n-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]-quinolin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
| US20120070368A1 (en) | 2010-04-16 | 2012-03-22 | Exelixis, Inc. | Methods of Using C-Met Modulators |
| SG10201609324UA (en) | 2010-07-16 | 2017-01-27 | Exelixis Inc | C-met modulator pharmaceutical compositions |
| EP2593091A1 (en) | 2010-07-16 | 2013-05-22 | Exelixis, Inc. | C-met modulator pharmaceutical compositions |
| US20140057908A1 (en) | 2010-09-27 | 2014-02-27 | Exelixis, Inc. | Method of Treating Cancer |
| AU2011307306A1 (en) | 2010-09-27 | 2013-05-02 | Exelixis, Inc. | Dual inhibitors of MET and VEGF for the treatment of castration resistant prostate cancer and osteoblastic bone metastases |
| CA2812750C (en) | 2010-09-27 | 2020-10-06 | Exelixis, Inc. | Dual inhibitors of met and vegf for the treatment of castration-resistant prostate cancer and osteoblastic bone metastases |
| JP2013543011A (ja) | 2010-11-22 | 2013-11-28 | グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッド | 癌の治療法 |
| GEP20247677B (en) | 2011-02-10 | 2024-10-10 | Exelixis Inc | Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds |
| US20120252840A1 (en) | 2011-04-04 | 2012-10-04 | Exelixis, Inc. | Method of Treating Cancer |
| JP2014513129A (ja) | 2011-05-02 | 2014-05-29 | エクセリクシス， インク． | 癌および骨癌疼痛の治療方法 |
| TW201306842A (zh) | 2011-06-15 | 2013-02-16 | Exelixis Inc | 使用ｐｉ３ｋ／ｍｔｏｒ吡啶並嘧啶酮抑制劑及苯達莫司汀及／或利妥昔單抗治療惡性血液疾病之組合療法 |
| AU2012312364B2 (en) | 2011-09-22 | 2017-11-09 | Exelixis, Inc. | Method for treating osteoporosis |
| CN104395284A (zh) | 2011-10-20 | 2015-03-04 | 埃克塞里艾克西斯公司 | 制备喹啉衍生物的方法 |
| BR112014011009A2 (pt) | 2011-11-08 | 2017-06-06 | Exelixis Inc | inibidor duplo de met e vegf para tratar câncer |
| JP2015515988A (ja) | 2012-05-02 | 2015-06-04 | エクセリクシス， インク． | 溶骨性骨転移を治療するためのｍｅｔ−ｖｅｇｆ二重調節剤 |
| CN104703600A (zh) | 2012-09-07 | 2015-06-10 | 埃克塞里艾克西斯公司 | 用于治疗肺腺癌的met、vegfr和ret的抑制剂 |
| US20140221372A1 (en) | 2013-02-06 | 2014-08-07 | GlaxoSmithKline Intellectual Property (NO 2.) Limited | Method of administration and treatment |
| KR102276348B1 (ko) * | 2013-03-15 | 2021-07-12 | 엑셀리시스, 인코포레이티드 | Ｎ（４〔［６,７비스（메틸옥시）퀴놀린４일］옥시〕페닐）ｎ′（４플루오로페닐）시클로프로판１,１디카복사미드의 대사물 |
| BR112015025408A8 (pt) | 2013-04-04 | 2018-07-10 | Exelixis Inc | combinações de drogas para tratar câncer |
| US11564915B2 (en) | 2013-04-04 | 2023-01-31 | Exelixis, Inc. | Cabozantinib dosage form and use in the treatment of cancer |
| BR112016018450A2 (pt) | 2014-02-14 | 2018-09-18 | Exelixis Inc | formas sólidas cristalinas de n-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-n'-(4-fluorofenil)ciclopropano-1,1-dicarboxamida, processos de preparo e métodos de uso |
| EA201691850A1 (ru) | 2014-03-17 | 2016-12-30 | Экселиксис, Инк. | Дозирование составов, содержащих кабозантиниб |
| EP3134084B1 (en) | 2014-04-25 | 2021-03-17 | Exelixis, Inc. | Method of treating lung adenocarcinoma |
| MA40386A (fr) | 2014-07-31 | 2016-02-04 | Exelixis Inc | Procédé de préparation de cabozantinib marqué au fluor-18 et d'analogues de celui-ci |
| EA034992B1 (ru) | 2014-08-05 | 2020-04-15 | Экселиксис, Инк. | Комбинации лекарственных средств для лечения множественной миеломы |
| TW201625243A (zh) | 2014-10-14 | 2016-07-16 | 艾克塞里克斯公司 | 用於治療黑素瘤之藥物組合 |
-
2015
- 2015-03-17 EA EA201691850A patent/EA201691850A1/ru unknown
- 2015-03-17 WO PCT/US2015/021072 patent/WO2015142928A1/en not_active Ceased
- 2015-03-17 MA MA039735A patent/MA39735A/fr unknown
- 2015-03-17 JP JP2016558004A patent/JP6666849B2/ja active Active
- 2015-03-17 CN CN201580023083.9A patent/CN106255499A/zh active Pending
- 2015-03-17 US US15/126,767 patent/US10159666B2/en active Active
- 2015-03-17 EP EP15714340.5A patent/EP3119476A1/en not_active Withdrawn
-
2018
- 2018-11-14 US US16/190,869 patent/US20190076420A1/en not_active Abandoned
-
2020
- 2020-01-29 US US16/776,139 patent/US20200163954A1/en not_active Abandoned
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