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 (enExample) | 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 (enExample) |
| EP (1) | EP3119476A1 (enExample) |
| JP (1) | JP6666849B2 (enExample) |
| CN (1) | CN106255499A (enExample) |
| EA (1) | EA201691850A1 (enExample) |
| MA (1) | MA39735A (enExample) |
| WO (1) | WO2015142928A1 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201920110A (zh) | 2009-01-16 | 2019-06-01 | 美商艾克塞里克斯公司 | 包含n-(4-{[6,7-雙(甲氧基)喹啉-4-基]氧基}苯基)-n'-(4-氟苯基)環丙烷-1,1-二甲醯胺之蘋果酸鹽之醫藥組合物及其用途 |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| TW201309650A (zh) | 2011-02-10 | 2013-03-01 | 艾克塞里克斯公司 | 製造喹啉化合物之方法及包含該化合物之醫藥組合物 |
| GEP20196995B (en) * | 2013-03-15 | 2019-07-25 | Inc Exelixis | Metabolites of n-(4-{[6,7-bis (methyloxy)quinolin-4-yl] oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide |
| ES2927651T3 (es) | 2013-04-04 | 2022-11-10 | Exelixis Inc | Forma de dosificación de cabozantinib y uso en el tratamiento del cáncer |
| EA032757B1 (ru) | 2014-02-14 | 2019-07-31 | Экселиксис, Инк. | Кристаллические твердые формы n-{4-[(6,7-диметоксихинолин-4-ил)окси]фенил}-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, способы получения и способы применения |
| CN106255499A (zh) | 2014-03-17 | 2016-12-21 | 埃克塞里艾克西斯公司 | 卡博替尼制剂的给药 |
| EA033834B1 (ru) * | 2014-07-31 | 2019-11-29 | Exelixis Inc | Способ получения кабозантиниба, меченного фтором-18, и его аналогов |
| MA40457A (fr) | 2014-08-05 | 2017-06-14 | Exelixis Inc | Combinaison de médicaments pour traiter le myélome multiple |
| WO2016161952A1 (zh) * | 2015-04-07 | 2016-10-13 | 广东众生药业股份有限公司 | 酪氨酸激酶抑制剂及包含该酪氨酸激酶抑制剂的药物组合物 |
| US11141413B2 (en) | 2016-04-15 | 2021-10-12 | Exelixis, Inc. | Method of treating renal cell carcinoma using N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (2S)-hydroxybutanedioate |
| 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 |
| HRP20251184T1 (hr) | 2018-01-26 | 2025-12-05 | Exelixis, Inc. | Spojevi za liječenje poremećaja ovisnih o kinazi |
| TWI787523B (zh) | 2018-06-15 | 2022-12-21 | 漢達生技醫藥股份有限公司 | 達沙替尼十二烷基硫酸鹽之結晶 |
| CA3202761A1 (en) | 2020-11-25 | 2022-06-02 | Nanocopoeia, Llc | Amorphous cabozantinib particles and uses thereof |
| KR20250136810A (ko) | 2023-01-31 | 2025-09-16 | 한다 온콜로지, 엘엘씨 | 개선된 카보잔티닙 조성물 및 사용 방법 |
| AU2024358295A1 (en) * | 2023-10-09 | 2026-05-07 | Msn Laboratories Private Limited, R&D Center | Pharmaceutical composition of cabozantinib |
| TW202602441A (zh) * | 2024-03-22 | 2026-01-16 | 美時化學製藥股份有限公司 | 改良的卡博替尼（cabozantinib）之調配物 |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2210607B1 (en) | 2003-09-26 | 2011-08-17 | Exelixis Inc. | N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide for the treatment of cancer |
| WO2006108059A1 (en) | 2005-04-06 | 2006-10-12 | Exelixis, Inc. | C-met modulators and methods of use |
| WO2008076415A1 (en) | 2006-12-14 | 2008-06-26 | 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 |
| AR075084A1 (es) | 2008-09-26 | 2011-03-09 | Smithkline Beecham Corp | Metodo de preparacion de quinolinil -oxidifenil - ciclopropanodicarboxamidas e intermediarios correspondientes |
| CA2743416A1 (en) | 2008-11-13 | 2010-05-20 | Exelixis Inc. | Methods of preparing quinoline derivatives |
| US20130030172A1 (en) | 2008-12-04 | 2013-01-31 | Exelixis, Inc. | Methods of Preparing Quinoline Derivatives |
| TW201920110A (zh) | 2009-01-16 | 2019-06-01 | 美商艾克塞里克斯公司 | 包含n-(4-{[6,7-雙(甲氧基)喹啉-4-基]氧基}苯基)-n'-(4-氟苯基)環丙烷-1,1-二甲醯胺之蘋果酸鹽之醫藥組合物及其用途 |
| BR112012001118A2 (pt) | 2009-07-17 | 2016-02-23 | Exelixis Inc | formas cristalinas de n-[3-flúor-4-({6-(metilóxi)-7-[(3-morfolin-4-ilpropil)óxi]-quinolin-4-il}óxi)fenil]-n'-(4-fluorfenil)ciclopropano-1,1-dicarboxamida, composição farmacêutica com as mesmas, métodos de preparação das mesmas e tratamento de câncer |
| UA108618C2 (uk) * | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| EA201290906A1 (ru) | 2010-03-12 | 2013-03-29 | Экселиксис, Инк. | Кристаллогидратные формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида |
| US20120070368A1 (en) | 2010-04-16 | 2012-03-22 | Exelixis, Inc. | Methods of Using C-Met Modulators |
| WO2012009722A1 (en) | 2010-07-16 | 2012-01-19 | Exelixis, Inc. | C-met modulator pharmaceutical compositions |
| EP2593091A1 (en) | 2010-07-16 | 2013-05-22 | Exelixis, Inc. | C-met modulator pharmaceutical compositions |
| HUE045810T2 (hu) | 2010-09-27 | 2020-01-28 | Exelixis Inc | MET és VEGF kettõs inhibitorai kasztrációrezisztens prosztatarák és oszteoblasztos csontáttétek kezelésére |
| EP2621482A1 (en) | 2010-09-27 | 2013-08-07 | Exelixis, Inc. | Dual inhibitors of met and vegf for the treatment of castration resistant prostate cancer and osteoblastic bone metastases |
| WO2012044577A1 (en) | 2010-09-27 | 2012-04-05 | Exelixis, Inc. | Dual inhibitors of met and vegf for the treatment of castration resistant prostate cancer and osteoblastic bone metastases |
| US20130252956A1 (en) | 2010-11-22 | 2013-09-26 | Howard Kallender | Methods of treating cancer |
| TW201309650A (zh) | 2011-02-10 | 2013-03-01 | 艾克塞里克斯公司 | 製造喹啉化合物之方法及包含該化合物之醫藥組合物 |
| US20120252840A1 (en) | 2011-04-04 | 2012-10-04 | Exelixis, Inc. | Method of Treating Cancer |
| EP2704717A1 (en) | 2011-05-02 | 2014-03-12 | Exelixis, Inc. | Method of treating cancer and bone cancer pain |
| 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 |
| GEP201606523B (en) | 2011-09-22 | 2016-08-10 | Exelixis Inc | Method for treating osteoporosis |
| PL2768796T3 (pl) | 2011-10-20 | 2020-05-18 | Exelixis, Inc. | Sposób wytwarzania pochodnych chinoliny |
| MX2014005458A (es) | 2011-11-08 | 2015-04-16 | Exelixis Inc | Inhibidor doble de met y del factor de crecimiento endotelial vascular (vegf) para el tratamiento del cáncer. |
| HK1207587A1 (en) | 2012-05-02 | 2016-02-05 | Exelixis, Inc. | A dual met - vegf modulator for treating osteolytic bone metastases |
| JP6513567B2 (ja) | 2012-09-07 | 2019-05-15 | エクセリクシス， インク． | 肺腺癌の治療で使用するためのｍｅｔ、ｖｅｇｆｒ、およびｒｅｔの阻害剤 |
| US20140221372A1 (en) | 2013-02-06 | 2014-08-07 | GlaxoSmithKline Intellectual Property (NO 2.) Limited | Method of administration and treatment |
| GEP20196995B (en) * | 2013-03-15 | 2019-07-25 | Inc Exelixis | Metabolites of n-(4-{[6,7-bis (methyloxy)quinolin-4-yl] oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide |
| EP2983639A1 (en) | 2013-04-04 | 2016-02-17 | Exelixis, Inc. | Drug combinations to treat cancer |
| ES2927651T3 (es) | 2013-04-04 | 2022-11-10 | Exelixis Inc | Forma de dosificación de cabozantinib y uso en el tratamiento del cáncer |
| EA032757B1 (ru) | 2014-02-14 | 2019-07-31 | Экселиксис, Инк. | Кристаллические твердые формы n-{4-[(6,7-диметоксихинолин-4-ил)окси]фенил}-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, способы получения и способы применения |
| CN106255499A (zh) | 2014-03-17 | 2016-12-21 | 埃克塞里艾克西斯公司 | 卡博替尼制剂的给药 |
| JP6696908B2 (ja) | 2014-04-25 | 2020-05-20 | エグゼリクシス， インコーポレイテッド | 肺腺癌の治療方法 |
| EA033834B1 (ru) | 2014-07-31 | 2019-11-29 | Exelixis Inc | Способ получения кабозантиниба, меченного фтором-18, и его аналогов |
| MA40457A (fr) | 2014-08-05 | 2017-06-14 | Exelixis Inc | Combinaison de médicaments pour traiter le myélome multiple |
| WO2016061253A1 (en) | 2014-10-14 | 2016-04-21 | Exelixis, Inc. | Drug combination to treat melanoma |
-
2015
- 2015-03-17 CN CN201580023083.9A patent/CN106255499A/zh active Pending
- 2015-03-17 JP JP2016558004A patent/JP6666849B2/ja active Active
- 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 US US15/126,767 patent/US10159666B2/en active Active
- 2015-03-17 MA MA039735A patent/MA39735A/fr unknown
- 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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