CA2784394C - Depot systems comprising glatiramer or a pharmacologically acceptable salt thereof - Google Patents
Depot systems comprising glatiramer or a pharmacologically acceptable salt thereof Download PDFInfo
- Publication number
- CA2784394C CA2784394C CA2784394A CA2784394A CA2784394C CA 2784394 C CA2784394 C CA 2784394C CA 2784394 A CA2784394 A CA 2784394A CA 2784394 A CA2784394 A CA 2784394A CA 2784394 C CA2784394 C CA 2784394C
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- CA
- Canada
- Prior art keywords
- glatiramer
- pharmaceutical composition
- composition according
- pharmaceutically acceptable
- acceptable salt
- 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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- 108010072051 Glatiramer Acetate Proteins 0.000 title claims abstract description 170
- YLOCGHYTXIINAI-XKUOMLDTSA-N (2s)-2-amino-3-(4-hydroxyphenyl)propanoic acid;(2s)-2-aminopentanedioic acid;(2s)-2-aminopropanoic acid;(2s)-2,6-diaminohexanoic acid Chemical compound C[C@H](N)C(O)=O.NCCCC[C@H](N)C(O)=O.OC(=O)[C@@H](N)CCC(O)=O.OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 YLOCGHYTXIINAI-XKUOMLDTSA-N 0.000 title claims abstract description 62
- 229940042385 glatiramer Drugs 0.000 title claims abstract description 58
- 150000003839 salts Chemical class 0.000 title claims description 43
- FHEAIOHRHQGZPC-KIWGSFCNSA-N acetic acid;(2s)-2-amino-3-(4-hydroxyphenyl)propanoic acid;(2s)-2-aminopentanedioic acid;(2s)-2-aminopropanoic acid;(2s)-2,6-diaminohexanoic acid Chemical compound CC(O)=O.C[C@H](N)C(O)=O.NCCCC[C@H](N)C(O)=O.OC(=O)[C@@H](N)CCC(O)=O.OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 FHEAIOHRHQGZPC-KIWGSFCNSA-N 0.000 claims abstract description 103
- 229960003776 glatiramer acetate Drugs 0.000 claims abstract description 103
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 45
- 238000007920 subcutaneous administration Methods 0.000 claims abstract description 13
- 238000007918 intramuscular administration Methods 0.000 claims abstract description 11
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- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 58
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- -1 polyalkaneanhydrides Polymers 0.000 claims description 41
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- 238000002360 preparation method Methods 0.000 claims description 22
- 230000000694 effects Effects 0.000 claims description 19
- 201000006417 multiple sclerosis Diseases 0.000 claims description 19
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims description 18
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims description 18
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- IELOKBJPULMYRW-NJQVLOCASA-N D-alpha-Tocopheryl Acid Succinate Chemical compound OC(=O)CCC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C IELOKBJPULMYRW-NJQVLOCASA-N 0.000 claims description 14
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- 235000004279 alanine Nutrition 0.000 claims description 5
- 235000013922 glutamic acid Nutrition 0.000 claims description 5
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- 229960003444 immunosuppressant agent Drugs 0.000 claims description 5
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- 239000005015 poly(hydroxybutyrate) Substances 0.000 claims description 5
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- KKGQTZUTZRNORY-UHFFFAOYSA-N fingolimod Chemical compound CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 KKGQTZUTZRNORY-UHFFFAOYSA-N 0.000 claims description 4
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- QPJVMBTYPHYUOC-UHFFFAOYSA-N methyl benzoate Chemical compound COC(=O)C1=CC=CC=C1 QPJVMBTYPHYUOC-UHFFFAOYSA-N 0.000 claims description 4
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- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims description 4
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims description 3
- 208000034530 PLAA-associated neurodevelopmental disease Diseases 0.000 claims description 3
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims description 3
- 230000001861 immunosuppressant effect Effects 0.000 claims description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 3
- 239000010452 phosphate Substances 0.000 claims description 3
- HCSBTDBGTNZOAB-UHFFFAOYSA-N 2,3-dinitrobenzoic acid Chemical compound OC(=O)C1=CC=CC([N+]([O-])=O)=C1[N+]([O-])=O HCSBTDBGTNZOAB-UHFFFAOYSA-N 0.000 claims description 2
- OBKXEAXTFZPCHS-UHFFFAOYSA-N 4-phenylbutyric acid Chemical compound OC(=O)CCCC1=CC=CC=C1 OBKXEAXTFZPCHS-UHFFFAOYSA-N 0.000 claims description 2
- NIXOWILDQLNWCW-UHFFFAOYSA-M Acrylate Chemical compound [O-]C(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-M 0.000 claims description 2
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 claims description 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 2
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- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims description 2
- OFOBLEOULBTSOW-UHFFFAOYSA-L Malonate Chemical compound [O-]C(=O)CC([O-])=O OFOBLEOULBTSOW-UHFFFAOYSA-L 0.000 claims description 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims description 2
- 229910002651 NO3 Inorganic materials 0.000 claims description 2
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 claims description 2
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-L Phosphate ion(2-) Chemical compound OP([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-L 0.000 claims description 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims description 2
- LSNNMFCWUKXFEE-UHFFFAOYSA-N Sulfurous acid Chemical compound OS(O)=O LSNNMFCWUKXFEE-UHFFFAOYSA-N 0.000 claims description 2
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- IPBVNPXQWQGGJP-UHFFFAOYSA-N acetic acid phenyl ester Natural products CC(=O)OC1=CC=CC=C1 IPBVNPXQWQGGJP-UHFFFAOYSA-N 0.000 claims description 2
- YTIVTFGABIZHHX-UHFFFAOYSA-L acetylenedicarboxylate(2-) Chemical compound [O-]C(=O)C#CC([O-])=O YTIVTFGABIZHHX-UHFFFAOYSA-L 0.000 claims description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 2
- KVSASDOGYIBWTA-UHFFFAOYSA-N chloro benzoate Chemical compound ClOC(=O)C1=CC=CC=C1 KVSASDOGYIBWTA-UHFFFAOYSA-N 0.000 claims description 2
- GHVNFZFCNZKVNT-UHFFFAOYSA-M decanoate Chemical compound CCCCCCCCCC([O-])=O GHVNFZFCNZKVNT-UHFFFAOYSA-M 0.000 claims description 2
- GHVNFZFCNZKVNT-UHFFFAOYSA-N decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 claims description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-M dihydrogenphosphate Chemical compound OP(O)([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-M 0.000 claims description 2
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/001—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
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- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Dermatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29192810P | 2010-01-04 | 2010-01-04 | |
| US61/291,928 | 2010-01-04 | ||
| PCT/IL2010/000679 WO2011080733A1 (en) | 2010-01-04 | 2010-08-19 | Depot systems comprising glatiramer or a pharmacologically acceptable salt thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2784394A1 CA2784394A1 (en) | 2011-07-07 |
| CA2784394C true CA2784394C (en) | 2016-12-13 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2784394A Active CA2784394C (en) | 2010-01-04 | 2010-08-19 | Depot systems comprising glatiramer or a pharmacologically acceptable salt thereof |
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| EP (2) | EP3536333B1 (enExample) |
| JP (2) | JP5916622B2 (enExample) |
| CN (3) | CN107661490B (enExample) |
| AU (1) | AU2010337822B2 (enExample) |
| BR (1) | BR112012016459B1 (enExample) |
| CA (1) | CA2784394C (enExample) |
| CY (1) | CY1120975T1 (enExample) |
| DK (2) | DK2398488T3 (enExample) |
| ES (2) | ES2928900T3 (enExample) |
| HK (1) | HK1244430A1 (enExample) |
| HR (2) | HRP20182076T1 (enExample) |
| HU (2) | HUE040390T2 (enExample) |
| LT (2) | LT3536333T (enExample) |
| MX (3) | MX349162B (enExample) |
| PL (2) | PL2398488T3 (enExample) |
| PT (2) | PT2398488T (enExample) |
| SI (1) | SI2398488T1 (enExample) |
| SM (2) | SMT201900020T1 (enExample) |
| TR (1) | TR201818858T4 (enExample) |
| WO (1) | WO2011080733A1 (enExample) |
Families Citing this family (28)
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| USRE49251E1 (en) | 2010-01-04 | 2022-10-18 | Mapi Pharma Ltd. | Depot systems comprising glatiramer or pharmacologically acceptable salt thereof |
| US8377885B2 (en) | 2010-01-04 | 2013-02-19 | Mapi Pharma Ltd. | Depot systems comprising glatiramer or pharmacologically acceptable salt thereof |
| WO2012143924A1 (en) | 2011-04-21 | 2012-10-26 | Mapi Pharma Ltd. | Random pentapolymer for treatment of autoimmune diseases |
| ES2913942T3 (es) | 2011-09-18 | 2022-06-06 | Bio Plasmar Ltd | Macetero o vajilla biodegradable |
| WO2014128079A1 (en) * | 2013-02-19 | 2014-08-28 | Synthon B.V. | Glatiramer acetate multidose formulation |
| CN103169670B (zh) * | 2013-03-22 | 2016-07-06 | 深圳翰宇药业股份有限公司 | 一种醋酸格拉替雷微球及其制备方法 |
| WO2015015254A1 (en) * | 2013-07-29 | 2015-02-05 | Aizant Drug Research Solutions Pvt Ltd | Pharmaceutical compositions of fingolimod |
| EP3086779A4 (en) * | 2013-12-23 | 2017-12-13 | Kineta One, LLC | Sustained release depot formulations of therapeutic proteins, and uses thereof |
| EP3119413B1 (en) | 2014-03-17 | 2021-05-12 | Mapi Pharma Limited | Sublingual delivery of glatiramer acetate |
| IL295161A (en) | 2015-09-21 | 2022-09-01 | Teva Pharmaceuticals Int Gmbh | Sustained release olanzapine formulation |
| WO2018002930A1 (en) | 2016-06-30 | 2018-01-04 | Stem Cell Medicine Ltd. | Treatment of inflammatory bowel disease with long acting glatiramer and adipose-derived stem cells |
| US12097292B2 (en) | 2016-08-28 | 2024-09-24 | Mapi Pharma Ltd. | Process for preparing microparticles containing glatiramer acetate |
| JP7232752B2 (ja) * | 2016-08-28 | 2023-03-03 | マピ ファーマ リミテッド | 酢酸グラチラマーを含有する微小粒子を調製する方法 |
| SMT202500136T1 (it) * | 2016-08-31 | 2025-05-12 | Mapi Pharma Ltd | Sistemi a deposito comprendenti glatiramer acetato |
| ES2784522T3 (es) * | 2016-10-28 | 2020-09-28 | SpineThera | Composiciones farmacéuticas y usos de las mismas |
| CA3057438A1 (en) | 2017-03-20 | 2018-09-27 | Teva Pharmaceuticals International Gmbh | Sustained release olanzapine formulaitons |
| US11167003B2 (en) * | 2017-03-26 | 2021-11-09 | Mapi Pharma Ltd. | Methods for suppressing or alleviating primary or secondary progressive multiple sclerosis (PPMS or SPMS) using sustained release glatiramer depot systems |
| AU2018270396B2 (en) | 2017-05-15 | 2025-03-20 | Stem Cell Medicine Ltd. | Treatment of multiple sclerosis with adipose-derived stem cells |
| CN110709091A (zh) * | 2017-05-15 | 2020-01-17 | 干细胞医药有限公司 | 使用长效格拉替雷和脂肪源性干细胞治疗多发性硬化症 |
| EP3645029B1 (en) | 2017-06-26 | 2023-01-18 | Institut Pasteur | Treatments to eliminate hiv reservoirs and reduce viral load |
| EP4171613A4 (en) * | 2020-06-29 | 2024-06-05 | Mapi Pharma Ltd. | LOW RAPID RELEASE LIRAGLUTIDE DEPOSITORY SYSTEMS |
| GB2617483B (en) * | 2020-11-02 | 2025-03-12 | Simcha Il 18 Inc | Interleukin-18 variants and methods of use |
| EP4277661A1 (en) | 2021-01-18 | 2023-11-22 | Anton Frenkel | Pharmaceutical dosage form |
| EP4285892A4 (en) * | 2021-01-29 | 2024-11-27 | Tionlab Therapeutics | CONTROLLED INITIAL RELEASE DEPOSIT COMPOSITION AND PROCESS FOR PREPARATION THEREOF |
| US11865213B2 (en) | 2021-07-05 | 2024-01-09 | Mapi Pharma Ltd. | Semaglutide depot systems and use thereof |
| CN118284414A (zh) | 2021-07-06 | 2024-07-02 | M·哈斯莱顿 | 血清素再摄取抑制剂戒断综合征的治疗 |
| WO2023170493A1 (en) * | 2022-03-07 | 2023-09-14 | Hadidi Naghmeh | Drug delivery using a parenteral pharmaceutical composition |
| WO2024054879A1 (en) * | 2022-09-06 | 2024-03-14 | Regents Of The University Of Michigan | Biodegradable polymeric particles for delivery of positively charged therapeutic agents |
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2010
- 2010-08-19 CN CN201711120362.4A patent/CN107661490B/zh active Active
- 2010-08-19 SM SM20190020T patent/SMT201900020T1/it unknown
- 2010-08-19 HR HRP20182076TT patent/HRP20182076T1/hr unknown
- 2010-08-19 HU HUE10840699A patent/HUE040390T2/hu unknown
- 2010-08-19 PT PT10840699T patent/PT2398488T/pt unknown
- 2010-08-19 CN CN2010800606327A patent/CN102686235A/zh active Pending
- 2010-08-19 WO PCT/IL2010/000679 patent/WO2011080733A1/en not_active Ceased
- 2010-08-19 TR TR2018/18858T patent/TR201818858T4/tr unknown
- 2010-08-19 HR HRP20221208TT patent/HRP20221208T1/hr unknown
- 2010-08-19 ES ES18205308T patent/ES2928900T3/es active Active
- 2010-08-19 JP JP2012546553A patent/JP5916622B2/ja active Active
- 2010-08-19 LT LTEP18205308.2T patent/LT3536333T/lt unknown
- 2010-08-19 SM SM20220422T patent/SMT202200422T1/it unknown
- 2010-08-19 MX MX2012007760A patent/MX349162B/es active IP Right Grant
- 2010-08-19 MX MX2017009179A patent/MX374215B/es unknown
- 2010-08-19 BR BR112012016459A patent/BR112012016459B1/pt active IP Right Grant
- 2010-08-19 CN CN201710417220.8A patent/CN107184954A/zh active Pending
- 2010-08-19 ES ES10840699T patent/ES2699692T3/es active Active
- 2010-08-19 EP EP18205308.2A patent/EP3536333B1/en active Active
- 2010-08-19 AU AU2010337822A patent/AU2010337822B2/en active Active
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- 2010-08-19 HU HUE18205308A patent/HUE060304T2/hu unknown
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- 2010-08-19 MX MX2020003805A patent/MX392126B/es unknown
- 2010-08-19 SI SI201031811T patent/SI2398488T1/sl unknown
- 2010-08-19 CA CA2784394A patent/CA2784394C/en active Active
- 2010-08-19 LT LTEP10840699.2T patent/LT2398488T/lt unknown
- 2010-08-19 DK DK18205308.2T patent/DK3536333T3/da active
- 2010-08-19 US US13/258,808 patent/US8796226B2/en active Active
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2015
- 2015-11-20 JP JP2015227317A patent/JP2016074696A/ja not_active Withdrawn
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2018
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- 2018-12-07 CY CY181101307T patent/CY1120975T1/el unknown
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