JP2019535734A5 - - Google Patents
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- JP2019535734A5 JP2019535734A5 JP2019527188A JP2019527188A JP2019535734A5 JP 2019535734 A5 JP2019535734 A5 JP 2019535734A5 JP 2019527188 A JP2019527188 A JP 2019527188A JP 2019527188 A JP2019527188 A JP 2019527188A JP 2019535734 A5 JP2019535734 A5 JP 2019535734A5
- Authority
- JP
- Japan
- Prior art keywords
- liquid pharmaceutical
- exendin
- pharmaceutical preparation
- preparation according
- pharmaceutically acceptable
- 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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- 108010024703 exendin (9-39) Proteins 0.000 claims description 68
- WSEVKKHALHSUMB-RYVRVIGHSA-N (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid Chemical compound CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O WSEVKKHALHSUMB-RYVRVIGHSA-N 0.000 claims description 67
- 239000007788 liquid Substances 0.000 claims description 55
- 239000000203 mixture Substances 0.000 claims description 53
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 26
- 238000011282 treatment Methods 0.000 claims description 24
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 22
- 150000003839 salts Chemical class 0.000 claims description 22
- 239000000872 buffer Substances 0.000 claims description 19
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 18
- 239000008194 pharmaceutical composition Substances 0.000 claims description 17
- 208000008589 Obesity Diseases 0.000 claims description 15
- 235000020824 obesity Nutrition 0.000 claims description 14
- 238000007920 subcutaneous administration Methods 0.000 claims description 11
- 230000002496 gastric effect Effects 0.000 claims description 9
- 230000036470 plasma concentration Effects 0.000 claims description 9
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 claims description 7
- 239000001632 sodium acetate Substances 0.000 claims description 7
- 235000017281 sodium acetate Nutrition 0.000 claims description 7
- 239000000243 solution Substances 0.000 claims description 6
- 239000012929 tonicity agent Substances 0.000 claims description 5
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 4
- 229930195725 Mannitol Natural products 0.000 claims description 4
- 239000007979 citrate buffer Substances 0.000 claims description 4
- 239000008121 dextrose Substances 0.000 claims description 4
- 239000000594 mannitol Substances 0.000 claims description 4
- 235000010355 mannitol Nutrition 0.000 claims description 4
- 208000033066 hyperinsulinemic hypoglycemia Diseases 0.000 claims description 3
- 238000002360 preparation method Methods 0.000 claims description 3
- WCPGFAUEYVSQIC-XIYMWFTDSA-N CC(O)=O.CC(O)=O.CC(O)=O.CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O Chemical compound CC(O)=O.CC(O)=O.CC(O)=O.CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O WCPGFAUEYVSQIC-XIYMWFTDSA-N 0.000 claims description 2
- 239000008351 acetate buffer Substances 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 239000007951 isotonicity adjuster Substances 0.000 claims description 2
- 239000007853 buffer solution Substances 0.000 claims 5
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 2
- 239000001509 sodium citrate Substances 0.000 claims 2
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 claims 2
- HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 claims 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 1
- 229930006000 Sucrose Natural products 0.000 claims 1
- HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 claims 1
- DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 claims 1
- HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 235000011187 glycerol Nutrition 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
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- 239000002504 physiological saline solution Substances 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 description 37
- 208000013016 Hypoglycemia Diseases 0.000 description 25
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- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 10
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Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022123899A JP2022153624A (ja) | 2016-11-21 | 2022-08-03 | エキセンディン（９－３９）の緩衝製剤 |
| JP2024100740A JP2024150450A (ja) | 2016-11-21 | 2024-06-21 | エキセンディン（９－３９）の緩衝製剤 |
| JP2025185576A JP2026048629A (ja) | 2016-11-21 | 2025-11-04 | エキセンディン（９－３９）の緩衝製剤 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662424979P | 2016-11-21 | 2016-11-21 | |
| US62/424,979 | 2016-11-21 | ||
| US201762517065P | 2017-06-08 | 2017-06-08 | |
| US62/517,065 | 2017-06-08 | ||
| PCT/US2017/062838 WO2018094404A1 (en) | 2016-11-21 | 2017-11-21 | Buffered formulations of exendin (9-39) |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022123899A Division JP2022153624A (ja) | 2016-11-21 | 2022-08-03 | エキセンディン（９－３９）の緩衝製剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019535734A JP2019535734A (ja) | 2019-12-12 |
| JP2019535734A5 true JP2019535734A5 (https=) | 2020-12-24 |
| JP7584894B2 JP7584894B2 (ja) | 2024-11-18 |
Family
ID=62145888
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019527188A Active JP7584894B2 (ja) | 2016-11-21 | 2017-11-21 | エキセンディン（９－３９）の緩衝製剤 |
| JP2022123899A Withdrawn JP2022153624A (ja) | 2016-11-21 | 2022-08-03 | エキセンディン（９－３９）の緩衝製剤 |
| JP2024100740A Pending JP2024150450A (ja) | 2016-11-21 | 2024-06-21 | エキセンディン（９－３９）の緩衝製剤 |
| JP2025185576A Pending JP2026048629A (ja) | 2016-11-21 | 2025-11-04 | エキセンディン（９－３９）の緩衝製剤 |
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| SI3456340T1 (sl) | 2007-01-08 | 2022-08-31 | The Trustees Of The University Of Pennsylvania | Antagonisti receptorja za GLP-1 za uporabo pri zdravljenju prirojenega hiperinsulinizma |
| US11311519B2 (en) | 2014-05-01 | 2022-04-26 | Eiger Biopharmaceuticals, Inc. | Treatment of hepatitis delta virus infection |
| AU2016267052B2 (en) | 2015-05-22 | 2022-01-20 | The Bot Of The Leland Stanford Junior University | Treatment of post-bariatric hypoglycemia with GLP-1 antagonists |
| US10653753B2 (en) | 2016-03-04 | 2020-05-19 | Eiger Biopharmaceuticals, Inc. | Treatment of hyperinsulinemic hypoglycemia with exendin-4 derivatives |
| EP4591853A1 (en) | 2016-11-21 | 2025-07-30 | Amylyx Pharmaceuticals, Inc. | Buffered formulations of exendin (9-39) |
| BR112019026711A2 (pt) | 2017-06-16 | 2020-06-30 | Zealand Pharma A/S | regimes de dosagem para a administração de análogos de peptídeo semelhante a glucagon- 2 (glp-2) |
| EP3628683A1 (en) * | 2018-09-28 | 2020-04-01 | Zealand Pharma A/S | Formulations of glucagon-like-peptide-2 (glp-2) analogues |
| IL314504A (en) * | 2018-10-15 | 2024-09-01 | Eiger Biopharmaceuticals Inc | Abexitide for the treatment of hyperinsulinemic hypoglycemia |
| AU2021270284A1 (en) | 2020-05-12 | 2023-01-05 | Regeneron Pharmaceuticals, Inc. | Anti-GLP1R antagonist antibodies and methods of use thereof |
| WO2022271753A1 (en) | 2021-06-21 | 2022-12-29 | Eiger Biopharmaceuticals, Inc. | Treatment of congenital hyperinsulinism with avexitide |
| US11878036B2 (en) * | 2022-05-25 | 2024-01-23 | Neuvian LLC | Vaginal care compositions and methods of improving vaginal health |
| CN116606367A (zh) * | 2022-05-31 | 2023-08-18 | 南京盛德瑞尔医药科技有限公司 | 长效Exendin-9-39及其在低血糖治疗中的应用和作为治疗低血糖的药物 |
| AU2024258693A1 (en) * | 2023-04-21 | 2025-10-09 | Amylyx Pharmaceuticals, Inc. | Glp-1r antagonism to improve nutrition following gastrointestinal surgery |
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2017
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2019
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2021
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2022
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2023
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