JP2020510691A5 - - Google Patents
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- Publication number
- JP2020510691A5 JP2020510691A5 JP2019551311A JP2019551311A JP2020510691A5 JP 2020510691 A5 JP2020510691 A5 JP 2020510691A5 JP 2019551311 A JP2019551311 A JP 2019551311A JP 2019551311 A JP2019551311 A JP 2019551311A JP 2020510691 A5 JP2020510691 A5 JP 2020510691A5
- Authority
- JP
- Japan
- Prior art keywords
- modified release
- mpa
- composition
- dog
- activator
- 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
Links
- 239000000203 mixture Substances 0.000 claims description 138
- HPNSFSBZBAHARI-UHFFFAOYSA-N micophenolic acid Natural products OC1=C(CC=C(C)CCC(O)=O)C(OC)=C(C)C2=C1C(=O)OC2 HPNSFSBZBAHARI-UHFFFAOYSA-N 0.000 claims description 109
- 238000000034 method Methods 0.000 claims description 98
- HPNSFSBZBAHARI-RUDMXATFSA-N mycophenolic acid Chemical compound OC1=C(C\C=C(/C)CCC(O)=O)C(OC)=C(C)C2=C1C(=O)OC2 HPNSFSBZBAHARI-RUDMXATFSA-N 0.000 claims description 94
- 229960000951 mycophenolic acid Drugs 0.000 claims description 84
- 239000012190 activator Substances 0.000 claims description 61
- 210000003750 lower gastrointestinal tract Anatomy 0.000 claims description 11
- 230000000694 effects Effects 0.000 claims description 10
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims description 10
- RTGDFNSFWBGLEC-SYZQJQIISA-N mycophenolate mofetil Chemical compound COC1=C(C)C=2COC(=O)C=2C(O)=C1C\C=C(/C)CCC(=O)OCCN1CCOCC1 RTGDFNSFWBGLEC-SYZQJQIISA-N 0.000 claims description 9
- 229960004866 mycophenolate mofetil Drugs 0.000 claims description 9
- QBMSTEZXAMABFF-UEARNRKISA-N mycophenolic acid O-acyl-glucuronide Chemical compound COC1=C(C)C=2COC(=O)C=2C(O)=C1C\C=C(/C)CCC(=O)O[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O QBMSTEZXAMABFF-UEARNRKISA-N 0.000 claims description 8
- 230000001506 immunosuppresive effect Effects 0.000 claims description 5
- 239000002207 metabolite Substances 0.000 claims description 5
- 208000023275 Autoimmune disease Diseases 0.000 claims description 4
- 210000004698 lymphocyte Anatomy 0.000 claims description 4
- 206010062016 Immunosuppression Diseases 0.000 claims description 3
- 239000013543 active substance Substances 0.000 claims description 3
- 208000019838 Blood disease Diseases 0.000 claims description 2
- 206010012438 Dermatitis atopic Diseases 0.000 claims description 2
- 208000005777 Lupus Nephritis Diseases 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 201000008937 atopic dermatitis Diseases 0.000 claims description 2
- 208000014951 hematologic disease Diseases 0.000 claims description 2
- 208000018706 hematopoietic system disease Diseases 0.000 claims description 2
- 208000006454 hepatitis Diseases 0.000 claims description 2
- 231100000283 hepatitis Toxicity 0.000 claims description 2
- 230000028709 inflammatory response Effects 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 2
- 241000282472 Canis lupus familiaris Species 0.000 claims 32
- 206010063344 microscopic polyangiitis Diseases 0.000 claims 29
- 239000005862 Whey Substances 0.000 claims 5
- 102000007544 Whey Proteins Human genes 0.000 claims 5
- 108010046377 Whey Proteins Proteins 0.000 claims 5
- 240000005578 Rivina humilis Species 0.000 claims 3
- 210000004369 blood Anatomy 0.000 claims 2
- 239000008280 blood Substances 0.000 claims 2
- 241000282465 Canis Species 0.000 claims 1
- 101710088194 Dehydrogenase Proteins 0.000 claims 1
- GRSZFWQUAKGDAV-KQYNXXCUSA-N IMP Chemical compound O[C@@H]1[C@H](O)[C@@H](COP(O)(O)=O)O[C@H]1N1C(NC=NC2=O)=C2N=C1 GRSZFWQUAKGDAV-KQYNXXCUSA-N 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 235000013902 inosinic acid Nutrition 0.000 claims 1
- 239000010410 layer Substances 0.000 description 29
- 229920000642 polymer Polymers 0.000 description 23
- CERQOIWHTDAKMF-UHFFFAOYSA-M Methacrylate Chemical compound CC(=C)C([O-])=O CERQOIWHTDAKMF-UHFFFAOYSA-M 0.000 description 15
- 239000001856 Ethyl cellulose Substances 0.000 description 8
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 8
- 229920001249 ethyl cellulose Polymers 0.000 description 8
- 235000019325 ethyl cellulose Nutrition 0.000 description 8
- 239000011241 protective layer Substances 0.000 description 6
- 229920003159 Eudragit® RS 100 Polymers 0.000 description 4
- 101710200424 Inosine-5'-monophosphate dehydrogenase Proteins 0.000 description 3
- 241000288906 Primates Species 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 description 2
- 229920003155 Eudragit® RL 100 Polymers 0.000 description 2
- 229920003134 Eudragit® polymer Polymers 0.000 description 2
- 241000282326 Felis catus Species 0.000 description 2
- 241000009328 Perro Species 0.000 description 2
- 239000011230 binding agent Substances 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 229920002678 cellulose Polymers 0.000 description 2
- 239000001913 cellulose Substances 0.000 description 2
- 229920002301 cellulose acetate Polymers 0.000 description 2
- 229920006217 cellulose acetate butyrate Polymers 0.000 description 2
- 239000007910 chewable tablet Substances 0.000 description 2
- 239000008298 dragée Substances 0.000 description 2
- BLCTWBJQROOONQ-UHFFFAOYSA-N ethenyl prop-2-enoate Chemical compound C=COC(=O)C=C BLCTWBJQROOONQ-UHFFFAOYSA-N 0.000 description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 2
- 229920000609 methyl cellulose Polymers 0.000 description 2
- 239000001923 methylcellulose Substances 0.000 description 2
- 235000010981 methylcellulose Nutrition 0.000 description 2
- 229920000058 polyacrylate Polymers 0.000 description 2
- -1 sachets Substances 0.000 description 2
- 239000002002 slurry Substances 0.000 description 2
- 239000007944 soluble tablet Substances 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 229920003139 Eudragit® L 100 Polymers 0.000 description 1
- 229920003157 Eudragit® RL 30 D Polymers 0.000 description 1
- 229920003161 Eudragit® RS 30 D Polymers 0.000 description 1
- 108010087227 IMP Dehydrogenase Proteins 0.000 description 1
- 102000006674 IMP dehydrogenase Human genes 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 238000001125 extrusion Methods 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 231100000628 reference dose Toxicity 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762470806P | 2017-03-13 | 2017-03-13 | |
| US62/470,806 | 2017-03-13 | ||
| US201762503270P | 2017-05-08 | 2017-05-08 | |
| US62/503,270 | 2017-05-08 | ||
| PCT/US2018/022266 WO2018170022A2 (en) | 2017-03-13 | 2018-03-13 | Methods and compositions for delivering mycophenolic acid active agents to non-human mammals |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020510691A JP2020510691A (ja) | 2020-04-09 |
| JP2020510691A5 true JP2020510691A5 (https=) | 2021-04-30 |
| JP7385474B2 JP7385474B2 (ja) | 2023-11-22 |
Family
ID=61911669
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019551311A Active JP7385474B2 (ja) | 2017-03-13 | 2018-03-13 | 非ヒト哺乳動物にミコフェノール酸活性剤を送達すための方法および組成物 |
Country Status (10)
| Country | Link |
|---|---|
| US (4) | US11633378B2 (https=) |
| EP (1) | EP3595639A2 (https=) |
| JP (1) | JP7385474B2 (https=) |
| KR (1) | KR20190131036A (https=) |
| CN (1) | CN110662533A (https=) |
| AU (1) | AU2018236225B2 (https=) |
| BR (1) | BR112019019003A2 (https=) |
| CA (1) | CA3054817A1 (https=) |
| MX (1) | MX2019010829A (https=) |
| WO (1) | WO2018170022A2 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11633378B2 (en) | 2017-03-13 | 2023-04-25 | Okava Pharmaceuticals, Inc. | Methods and compositions for delivering mycophenolic acid active agents to non-human mammals |
| JP2022506007A (ja) * | 2018-09-07 | 2022-01-17 | オカヴァ ファーマシューティカルズ， インコーポレイテッド | ミコフェノール酸活性剤を非ヒト哺乳動物に送達するための方法および組成物 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1203328A (en) * | 1968-06-04 | 1970-08-26 | Ici Ltd | Pharmaceutical compositions |
| US4808413A (en) | 1987-04-28 | 1989-02-28 | E. R. Squibb & Sons, Inc. | Pharmaceutical compositions in the form of beadlets and method |
| US5049394A (en) | 1987-09-11 | 1991-09-17 | E. R. Squibb & Sons, Inc. | Pharmaceutical composition containing high drug load and method for preparing same |
| ID18663A (id) * | 1996-04-12 | 1998-04-30 | Novartis Ag | Komposisi farmasi berlapis enterik |
| GB0124953D0 (en) * | 2001-10-17 | 2001-12-05 | Novartis Ag | Organic Compounds |
| US20040127403A1 (en) * | 2002-09-06 | 2004-07-01 | Francesco Parenti | Methods for treating and preventing Gram-positive bacteremias |
| AR045957A1 (es) * | 2003-10-03 | 2005-11-16 | Novartis Ag | Composicion farmaceutica y combinacion |
| GB0419355D0 (en) | 2004-08-31 | 2004-09-29 | Novartis Ag | Organic compounds |
| CN1994295A (zh) | 2006-01-06 | 2007-07-11 | 华北制药集团新药研究开发有限责任公司 | 霉酚酸盐的包有肠溶衣的药物组合物 |
| WO2008090569A1 (en) * | 2007-01-25 | 2008-07-31 | Panacea Biotec Ltd | Modified release pharmaceutical composition and a process of making the same |
| MX2010001711A (es) * | 2007-08-13 | 2010-03-11 | Panacea Biotec Ltd | Composiciones de liberacion extendida que comprenden micofenolato sodico y procedimientos de las mismas. |
| JP2011513391A (ja) * | 2008-03-05 | 2011-04-28 | パナセア バイオテック リミテッド | ミコフェノラートを含有する徐放性医薬組成物およびその方法 |
| US20110086102A1 (en) * | 2009-10-13 | 2011-04-14 | Teva Pharmaceutical Industries Ltd. | Delayed release compositions |
| KR20110091252A (ko) * | 2010-02-05 | 2011-08-11 | 서울대학교산학협력단 | 미코페놀레이트 모페틸을 함유한 서방성 면역 억제제 |
| CN102793658A (zh) * | 2012-08-23 | 2012-11-28 | 无锡福祈制药有限公司 | 一种含有麦考酚酸或麦考酚酸盐的骨架型制剂及其包衣片 |
| CN103845323B (zh) * | 2012-11-30 | 2018-02-02 | 重庆华邦制药有限公司 | 麦考酚酸及其盐肠溶制剂和制备方法 |
| US11633378B2 (en) | 2017-03-13 | 2023-04-25 | Okava Pharmaceuticals, Inc. | Methods and compositions for delivering mycophenolic acid active agents to non-human mammals |
-
2018
- 2018-03-13 US US16/493,708 patent/US11633378B2/en active Active
- 2018-03-13 CA CA3054817A patent/CA3054817A1/en active Pending
- 2018-03-13 EP EP18716395.1A patent/EP3595639A2/en not_active Withdrawn
- 2018-03-13 WO PCT/US2018/022266 patent/WO2018170022A2/en not_active Ceased
- 2018-03-13 AU AU2018236225A patent/AU2018236225B2/en not_active Ceased
- 2018-03-13 CN CN201880031161.3A patent/CN110662533A/zh active Pending
- 2018-03-13 KR KR1020197027805A patent/KR20190131036A/ko not_active Withdrawn
- 2018-03-13 BR BR112019019003A patent/BR112019019003A2/pt not_active Application Discontinuation
- 2018-03-13 JP JP2019551311A patent/JP7385474B2/ja active Active
- 2018-03-13 MX MX2019010829A patent/MX2019010829A/es unknown
- 2018-09-07 US US16/125,214 patent/US11786505B2/en active Active
-
2023
- 2023-09-06 US US18/462,235 patent/US20250049753A1/en active Pending
- 2023-10-18 US US18/489,379 patent/US20240299343A1/en not_active Abandoned
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