CN106255499A - 卡博替尼制剂的给药 - Google Patents

卡博替尼制剂的给药 Download PDF

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Publication number
CN106255499A
CN106255499A CN201580023083.9A CN201580023083A CN106255499A CN 106255499 A CN106255499 A CN 106255499A CN 201580023083 A CN201580023083 A CN 201580023083A CN 106255499 A CN106255499 A CN 106255499A
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rich
buddhist nun
card
auc
cabozantinib
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Pending
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CN201580023083.9A
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Chinese (zh)
Inventor
D·T·阿夫塔布
S·纳加纳坦
W·许
S·莱西
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Exelixis Inc
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Exelixis Inc
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia

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  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
CN201580023083.9A 2014-03-17 2015-03-17 卡博替尼制剂的给药 Pending CN106255499A (zh)

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 (1)

Publication Number Publication Date
CN106255499A true CN106255499A (zh) 2016-12-21

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CN201580023083.9A Pending CN106255499A (zh) 2014-03-17 2015-03-17 卡博替尼制剂的给药

Country Status (7)

Country Link
US (3) US10159666B2 (https=)
EP (1) EP3119476A1 (https=)
JP (1) JP6666849B2 (https=)
CN (1) CN106255499A (https=)
EA (1) EA201691850A1 (https=)
MA (1) MA39735A (https=)
WO (1) WO2015142928A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG173014A1 (en) 2009-01-16 2011-08-29 Exelixis Inc Malate salt of n- (4- { [ 6, 7-bis (methyloxy) quin0lin-4-yl] oxy}phenyl)-n' - (4 -fluorophenyl) cyclopropane-1,1-dicarboxamide, and crystalline forms therof for the treatment of cancer
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
JP2014505109A (ja) 2011-02-10 2014-02-27 エクセリクシス， インク． キノリン化合物およびそのような化合物を含有する医薬組成物の調製方法
AU2014232714B2 (en) 2013-03-15 2018-07-19 Exelixis, Inc. Metabolites of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide
EP2981263B1 (en) 2013-04-04 2022-06-29 Exelixis, Inc. Cabozantinib dosage form and use in the treatment of cancer
KR102354963B1 (ko) 2014-02-14 2022-01-21 엑셀리시스, 인코포레이티드 N-｛4-[(6,7-다이메톡시퀴놀린-4-일)옥시]페닐｝-n'-(4-플루오로페닐) 사이클로프로판-1,1-다이카복스아마이드의 결정질 고체 형태, 제조 방법 및 사용 방법
EA201691850A1 (ru) 2014-03-17 2016-12-30 Экселиксис, Инк. Дозирование составов, содержащих кабозантиниб
ES2929888T3 (es) * 2014-07-31 2022-12-02 Exelixis Inc Procedimiento para preparar cabozantinib marcado con flúor 18 y sus análogos
BR112017002318A2 (pt) 2014-08-05 2018-07-17 Exelixis, Inc. combinações de fármacos para tratar mieloma múltiplo.
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
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
UA128476C2 (uk) 2018-01-26 2024-07-24 Екселіксіс, Інк. Сполуки для лікування кіназозалежних розладів
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
TW202444365A (zh) 2023-01-31 2024-11-16 漢達生技醫藥股份有限公司 改良之卡博替尼組合物及其使用方法
WO2025079089A1 (en) * 2023-10-09 2025-04-17 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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102388024A (zh) * 2009-01-16 2012-03-21 埃克塞里艾克西斯公司 N-(4-{[6,7-双(甲基氧基)喹啉-4-基]氧基}苯基)-n’-(4-氟苯基)环丙烷-1,1-二甲酰胺的苹果酸盐及其用于癌症治疗的结晶型
CN103221035A (zh) * 2010-07-16 2013-07-24 埃克塞里艾克西斯公司 C-met调节剂药物组合物

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2213661E (pt) 2003-09-26 2011-12-15 Exelixis Inc Moduladores de c-met e métodos de uso
US20080161305A1 (en) 2005-04-06 2008-07-03 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
UY32142A (es) 2008-09-26 2010-05-31 Smithkline Beckman Corp Preparación de una quinoliniloxidifenilciclopropanodicarboxamida
US20130197230A1 (en) 2008-11-13 2013-08-01 Jo Ann Wilson Methods of preparing quinoline derivatives
WO2010065838A1 (en) 2008-12-04 2010-06-10 Exelixis, Inc. Methods of preparing quinoline derivatives
JP2012533570A (ja) 2009-07-17 2012-12-27 エグゼリクシス， インコーポレイテッド Ｎ−［３−フルオロ−４−（｛６−（メチルオキシ）−７−［（３−モルホリン−４−イルプロピル）オキシ］−キノリン−４−イル｝オキシ）フェニル］−ｎ’−（４−フルオロフェニル）シクロプロパン−１，１−ジカルボキサミドの結晶形
UA108618C2 (uk) * 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
CA2792852A1 (en) 2010-03-12 2011-09-15 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
EP2593091A1 (en) 2010-07-16 2013-05-22 Exelixis, Inc. C-met modulator pharmaceutical compositions
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
EP2621483A1 (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
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
WO2012071321A1 (en) 2010-11-22 2012-05-31 Glaxosmithkline Llc Method of treating cancer
JP2014505109A (ja) 2011-02-10 2014-02-27 エクセリクシス， インク． キノリン化合物およびそのような化合物を含有する医薬組成物の調製方法
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
KR20140025496A (ko) 2011-05-02 2014-03-04 엑셀리시스, 인코포레이티드 암 및 뼈 암 통증의 치료방법
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
DK2768796T3 (da) 2011-10-20 2020-02-24 Exelixis Inc Fremgangsmåde til fremstilling af quinolin-derivater
JP2014532766A (ja) 2011-11-08 2014-12-08 エクセリクシス， インク． 癌を治療する、ｍｅｔ及びｖｅｇｆの二重阻害剤
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
CN114129566A (zh) 2012-09-07 2022-03-04 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
AU2014232714B2 (en) * 2013-03-15 2018-07-19 Exelixis, Inc. Metabolites of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide
BR112015025408A8 (pt) 2013-04-04 2018-07-10 Exelixis Inc combinações de drogas para tratar câncer
EP2981263B1 (en) 2013-04-04 2022-06-29 Exelixis, Inc. Cabozantinib dosage form and use in the treatment of cancer
KR102354963B1 (ko) 2014-02-14 2022-01-21 엑셀리시스, 인코포레이티드 N-｛4-[(6,7-다이메톡시퀴놀린-4-일)옥시]페닐｝-n'-(4-플루오로페닐) 사이클로프로판-1,1-다이카복스아마이드의 결정질 고체 형태, 제조 방법 및 사용 방법
EA201691850A1 (ru) 2014-03-17 2016-12-30 Экселиксис, Инк. Дозирование составов, содержащих кабозантиниб
IL248408B (en) 2014-04-25 2022-06-01 Exelixis Inc A method for treating adenocarcinoma of the lungs
ES2929888T3 (es) 2014-07-31 2022-12-02 Exelixis Inc Procedimiento para preparar cabozantinib marcado con flúor 18 y sus análogos
BR112017002318A2 (pt) 2014-08-05 2018-07-17 Exelixis, Inc. combinações de fármacos para tratar mieloma múltiplo.
WO2016061253A1 (en) 2014-10-14 2016-04-21 Exelixis, Inc. Drug combination to treat melanoma

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102388024A (zh) * 2009-01-16 2012-03-21 埃克塞里艾克西斯公司 N-(4-{[6,7-双(甲基氧基)喹啉-4-基]氧基}苯基)-n’-(4-氟苯基)环丙烷-1,1-二甲酰胺的苹果酸盐及其用于癌症治疗的结晶型
CN103221035A (zh) * 2010-07-16 2013-07-24 埃克塞里艾克西斯公司 C-met调节剂药物组合物

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DAVID C.SMITH等: "Cabozantinib in Patients With Advanced Prostate Cancer:Results of a Phase II Randomized Discontinuation Trial", 《JOURNAL OF CLINICAL ONCOLOGY》 *
F. MICHAEL YAKES等: "Cabozantinib (XL184), a Novel MET and VEGFR2 Inhibitor, Simultaneously Suppresses Metastasis, Angiogenesis, and Tumor Growth", 《MOLECULAR CANCER THERAPEUTICS》 *
ROSSELLA ELISEI等: "Cabozantinib in Progressive Medullary Thyroid Cancer", 《JOURNAL OF CLINICAL ONCOLOGY》 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

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US20200163954A1 (en) 2020-05-28
EP3119476A1 (en) 2017-01-25
JP2017507995A (ja) 2017-03-23
US10159666B2 (en) 2018-12-25
US20170087143A1 (en) 2017-03-30
MA39735A (fr) 2017-01-25
JP6666849B2 (ja) 2020-03-18
EA201691850A1 (ru) 2016-12-30
WO2015142928A1 (en) 2015-09-24
US20190076420A1 (en) 2019-03-14

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Application publication date: 20161221