CA2967664A1 - Pharmaceutical formulations comprising inhibitors of human histone methyltransferase ezh2 - Google Patents

Pharmaceutical formulations comprising inhibitors of human histone methyltransferase ezh2 Download PDF

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Publication number
CA2967664A1
CA2967664A1 CA2967664A CA2967664A CA2967664A1 CA 2967664 A1 CA2967664 A1 CA 2967664A1 CA 2967664 A CA2967664 A CA 2967664A CA 2967664 A CA2967664 A CA 2967664A CA 2967664 A1 CA2967664 A1 CA 2967664A1
Authority
CA
Canada
Prior art keywords
effective amount
therapeutically effective
epz
dosage form
dissolution
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.)
Pending
Application number
CA2967664A
Other languages
English (en)
French (fr)
Inventor
Heike KEILHACK
Brett TRUITT
Yuta Suzuki
Tsukasa Murase
Futoshi SHIKATA
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eisai R&D Management Co Ltd
Epizyme Inc
Original Assignee
Eisai R&D Management Co Ltd
Epizyme Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Eisai R&D Management Co Ltd, Epizyme Inc filed Critical Eisai R&D Management Co Ltd
Publication of CA2967664A1 publication Critical patent/CA2967664A1/en
Pending legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2095Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/284Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • A61K9/2846Poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2893Tablet coating processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
CA2967664A 2014-11-17 2015-11-17 Pharmaceutical formulations comprising inhibitors of human histone methyltransferase ezh2 Pending CA2967664A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201462080985P 2014-11-17 2014-11-17
US62/080,985 2014-11-17
US201562166572P 2015-05-26 2015-05-26
US62/166,572 2015-05-26
US201562251903P 2015-11-06 2015-11-06
US62/251,903 2015-11-06
PCT/US2015/061194 WO2016081523A1 (en) 2014-11-17 2015-11-17 Method for treating cancer

Publications (1)

Publication Number Publication Date
CA2967664A1 true CA2967664A1 (en) 2016-05-26

Family

ID=56014476

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2967664A Pending CA2967664A1 (en) 2014-11-17 2015-11-17 Pharmaceutical formulations comprising inhibitors of human histone methyltransferase ezh2

Country Status (21)

Country Link
US (3) US10786511B2 (enExample)
EP (2) EP4272742A1 (enExample)
JP (3) JP6829684B2 (enExample)
KR (3) KR20240035908A (enExample)
CN (2) CN107249591B (enExample)
AU (3) AU2015350108B2 (enExample)
BR (1) BR112017010166A2 (enExample)
CA (1) CA2967664A1 (enExample)
DK (1) DK3220916T3 (enExample)
EA (1) EA201791095A1 (enExample)
ES (1) ES2947819T3 (enExample)
FI (1) FI3220916T3 (enExample)
HU (1) HUE062159T2 (enExample)
IL (4) IL296080B2 (enExample)
LT (1) LT3220916T (enExample)
MX (2) MX383484B (enExample)
PL (1) PL3220916T3 (enExample)
PT (1) PT3220916T (enExample)
SG (1) SG11201703806XA (enExample)
SI (1) SI3220916T1 (enExample)
WO (1) WO2016081523A1 (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
BR112015008447A2 (pt) 2012-10-15 2017-07-04 Epizyme Inc métodos para tratar câncer
WO2015085325A1 (en) 2013-12-06 2015-06-11 Epizyme, Inc. Combination therapy for treating cancer
KR20230031963A (ko) 2014-06-17 2023-03-07 에피자임, 인코포레이티드 림프종 치료를 위한 ezh2 억제제
KR20240035908A (ko) 2014-11-17 2024-03-18 에피자임, 인코포레이티드 암을 치료하기 위한 방법
WO2016172199A1 (en) 2015-04-20 2016-10-27 Epizyme, Inc. Combination therapy for treating cancer
CA2988816A1 (en) 2015-06-10 2016-12-15 Epizyme, Inc. Ezh2 inhibitors for treating lymphoma
US10493076B2 (en) 2015-08-24 2019-12-03 Epizyme, Inc. Method for treating cancer
US11951108B2 (en) 2016-01-29 2024-04-09 Epizyme, Inc. Combination therapy for treating cancer
JP7121660B2 (ja) 2016-06-01 2022-08-18 エピザイム,インコーポレイティド 癌を処置するためのezh2阻害剤の使用
MA45406A (fr) 2016-06-17 2019-04-24 Epizyme Inc Inhibiteurs d'ezh2 pour traiter le cancer
CA3050221C (en) 2017-01-19 2021-09-28 Daiichi Sankyo Company, Limited Pharmaceutical composition used for treatment of htlv-1-associated myelopathy
WO2018183885A1 (en) 2017-03-31 2018-10-04 Epizyme, Inc. Combination therapy for treating cancer
JP2020522687A (ja) 2017-06-02 2020-07-30 エピザイム,インコーポレイティド 癌を処置するためのezh2阻害剤の使用
CA3074720A1 (en) 2017-09-05 2019-03-14 Epizyme, Inc. Combination therapy for treating cancer
BR112022012258A2 (pt) * 2019-12-20 2022-08-30 Epizyme Inc Sal cristalino de bromidreto de um inibidor de ezh2, sua preparação e composição farmacêutica útil para o tratamento de câncer
JP7628876B2 (ja) 2021-04-23 2025-02-12 日立Astemo株式会社 情報処理装置、情報処理方法、プログラムおよび記憶媒体
US20250146080A1 (en) * 2022-02-17 2025-05-08 Memorial Sloan-Kettering Cancer Center Methods for overcoming tazemetostat-resistance in cancer patients
IL316421A (en) 2022-04-27 2024-12-01 Daiichi Sankyo Co Ltd Combination of an antibody-drug conjugate with an EZH1 and/or EZH2 inhibitor

Family Cites Families (31)

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GB9119052D0 (en) 1991-09-06 1991-10-23 Boots Co Plc Pharmaceutical compositions
US6248363B1 (en) * 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
US7229774B2 (en) 2001-08-02 2007-06-12 Regents Of The University Of Michigan Expression profile of prostate cancer
US20070026064A1 (en) * 2005-07-29 2007-02-01 Yoder Steven L Pharmaceutical dosage forms having watermark-type identification and authentication inditia
US20100278921A1 (en) * 2009-04-30 2010-11-04 Fischer Cristina M Solid oral formulation of abt-263
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
JP6389036B2 (ja) 2010-09-10 2018-09-12 エピザイム インコーポレイテッド ヒトezh2の阻害剤、およびその使用方法
US20130296325A1 (en) * 2011-01-14 2013-11-07 Bristol-Myers Squibb Company HIGH DRUG LOAD TABLET FORMULATION OF [(1R), 2S]-2-AMINOPROPIONIC ACID 2-[4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-5-METHYLPYRROLO[2,1-f][1,2,4]TRIAZIN-6-YLOXY]-1-METHYLETHYL ESTER
EP3323820B1 (en) 2011-02-28 2023-05-10 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
TW201733984A (zh) 2011-04-13 2017-10-01 雅酶股份有限公司 經取代之苯化合物
CA2867282C (en) * 2012-03-12 2024-04-02 Epizyme, Inc. Inhibitors of human ezh2, and methods of use thereof
RU2699546C2 (ru) 2012-04-13 2019-09-06 Эпизайм, Инк. Комбинированная терапия для лечения рака
PL3184523T3 (pl) * 2012-04-13 2019-12-31 Epizyme Inc Bromowodorek N-((4,6-dimetylo-2-okso-1,2-dihydropirydyn-3-ylo)metylo)-5- (etylo(tetrahydro-2H-piran-4-ylo)amino)-4-metylo-4'-(morfolinometylo)-[1,1'- bifenylo]-3-karboksyamidu do zastosowania w leczeniu zaburzenia proliferacji komórkowej układu hematologicznego
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EP4324525A3 (en) 2013-10-16 2024-07-17 Epizyme, Inc. Hydrochloride salt form for ezh2 inhibition
US20160228447A1 (en) * 2013-10-18 2016-08-11 Epizyme, Inc. Method of treating cancer
WO2015085325A1 (en) 2013-12-06 2015-06-11 Epizyme, Inc. Combination therapy for treating cancer
KR20230031963A (ko) * 2014-06-17 2023-03-07 에피자임, 인코포레이티드 림프종 치료를 위한 ezh2 억제제
WO2015200650A1 (en) 2014-06-25 2015-12-30 Epizyme, Inc. Substituted benzene and 6,5-fused bicyclic heteroaryl compounds
CN106794177A (zh) 2014-10-16 2017-05-31 Epizyme股份有限公司 治疗癌症的方法
KR20240035908A (ko) 2014-11-17 2024-03-18 에피자임, 인코포레이티드 암을 치료하기 위한 방법
CA2988816A1 (en) * 2015-06-10 2016-12-15 Epizyme, Inc. Ezh2 inhibitors for treating lymphoma
MA45406A (fr) * 2016-06-17 2019-04-24 Epizyme Inc Inhibiteurs d'ezh2 pour traiter le cancer

Also Published As

Publication number Publication date
ES2947819T3 (es) 2023-08-21
MX2017006089A (es) 2017-12-11
IL252182B2 (en) 2023-02-01
JP2017537899A (ja) 2017-12-21
HUE062159T2 (hu) 2023-10-28
IL296080A (en) 2022-11-01
KR102338802B1 (ko) 2021-12-14
US20170360797A1 (en) 2017-12-21
US20210060030A1 (en) 2021-03-04
US12168014B2 (en) 2024-12-17
CN116650500A (zh) 2023-08-29
JP6829684B2 (ja) 2021-02-10
MX383484B (es) 2025-03-11
IL304252B1 (en) 2025-11-01
JP2021073241A (ja) 2021-05-13
EP3220916A1 (en) 2017-09-27
KR20240035908A (ko) 2024-03-18
LT3220916T (lt) 2023-07-25
BR112017010166A2 (en) 2018-02-14
JP2023062189A (ja) 2023-05-02
KR20170103768A (ko) 2017-09-13
NZ768247A (en) 2024-05-31
SG11201703806XA (en) 2017-06-29
IL304252A (en) 2023-09-01
CN107249591B (zh) 2024-01-30
EP3220916A4 (en) 2018-07-11
JP7485810B2 (ja) 2024-05-16
PL3220916T3 (pl) 2023-08-14
WO2016081523A1 (en) 2016-05-26
IL323396A (en) 2025-11-01
MX2021006734A (es) 2021-07-02
CN107249591A (zh) 2017-10-13
AU2015350108A1 (en) 2017-05-25
AU2021204706B2 (en) 2023-11-23
KR102644844B1 (ko) 2024-03-07
SI3220916T1 (sl) 2023-09-29
DK3220916T3 (da) 2023-06-26
EA201791095A1 (ru) 2017-10-31
US10786511B2 (en) 2020-09-29
AU2015350108B2 (en) 2021-04-08
FI3220916T3 (fi) 2023-06-19
IL252182B (en) 2022-10-01
KR20210156840A (ko) 2021-12-27
AU2024201171A1 (en) 2024-03-14
IL252182A0 (en) 2017-07-31
EP4272742A1 (en) 2023-11-08
EP3220916B1 (en) 2023-04-19
PT3220916T (pt) 2023-06-26
IL296080B1 (en) 2023-08-01
IL296080B2 (en) 2023-12-01
AU2021204706A1 (en) 2021-07-29
NZ731696A (en) 2024-03-22
US20250064822A1 (en) 2025-02-27

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