CA3044221A1 - Intranasal nalmefene compositions and methods for the treatment of opioid overdose - Google Patents
Intranasal nalmefene compositions and methods for the treatment of opioid overdose Download PDFInfo
- Publication number
- CA3044221A1 CA3044221A1 CA3044221A CA3044221A CA3044221A1 CA 3044221 A1 CA3044221 A1 CA 3044221A1 CA 3044221 A CA3044221 A CA 3044221A CA 3044221 A CA3044221 A CA 3044221A CA 3044221 A1 CA3044221 A1 CA 3044221A1
- Authority
- CA
- Canada
- Prior art keywords
- patient
- recited
- nalmefene
- pharmaceutical formulation
- nalmefene hydrochloride
- 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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- WJBLNOPPDWQMCH-MBPVOVBZSA-N Nalmefene Chemical compound N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=C)O)CC1)O)CC1CC1 WJBLNOPPDWQMCH-MBPVOVBZSA-N 0.000 title claims abstract description 178
- 229960005297 nalmefene Drugs 0.000 title claims abstract description 178
- 238000000034 method Methods 0.000 title claims abstract description 87
- 208000012488 Opiate Overdose Diseases 0.000 title claims abstract description 69
- 238000011282 treatment Methods 0.000 title claims description 76
- 239000000203 mixture Substances 0.000 title description 133
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 261
- 238000012384 transportation and delivery Methods 0.000 claims abstract description 104
- GYWMRGWFQPSQLK-OPHZJPRHSA-N (4r,4as,7as,12bs)-3-(cyclopropylmethyl)-7-methylidene-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,9-diol;hydron;chloride Chemical compound Cl.N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=C)O)CC1)O)CC1CC1 GYWMRGWFQPSQLK-OPHZJPRHSA-N 0.000 claims description 274
- 229960000677 nalmefene hydrochloride Drugs 0.000 claims description 272
- 239000003401 opiate antagonist Substances 0.000 claims description 161
- 239000003814 drug Substances 0.000 claims description 140
- 229940079593 drug Drugs 0.000 claims description 139
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical group [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 117
- 238000010521 absorption reaction Methods 0.000 claims description 108
- 239000003623 enhancer Substances 0.000 claims description 95
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 86
- 230000036470 plasma concentration Effects 0.000 claims description 78
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical group [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 72
- 229960000686 benzalkonium chloride Drugs 0.000 claims description 66
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical group [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims description 66
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- NLEBIOOXCVAHBD-QKMCSOCLSA-N dodecyl beta-D-maltoside Chemical group O[C@@H]1[C@@H](O)[C@H](OCCCCCCCCCCCC)O[C@H](CO)[C@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 NLEBIOOXCVAHBD-QKMCSOCLSA-N 0.000 claims description 34
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- 125000001421 myristyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 7
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- 230000001939 inductive effect Effects 0.000 claims 2
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims 2
- 229940126534 drug product Drugs 0.000 abstract description 14
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- OVBJJZOQPCKUOR-UHFFFAOYSA-L EDTA disodium salt dihydrate Chemical compound O.O.[Na+].[Na+].[O-]C(=O)C[NH+](CC([O-])=O)CC[NH+](CC([O-])=O)CC([O-])=O OVBJJZOQPCKUOR-UHFFFAOYSA-L 0.000 description 34
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| US201662424378P | 2016-11-18 | 2016-11-18 | |
| US62/424,378 | 2016-11-18 | ||
| PCT/US2017/060964 WO2018093666A1 (en) | 2016-11-18 | 2017-11-09 | Compositions and methods for the treatment of opioid overdose |
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| CA3044221A1 true CA3044221A1 (en) | 2018-05-24 |
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| WO2019157099A1 (en) | 2018-02-06 | 2019-08-15 | Aegis Therapeutics, Llc | Intranasal epinephrine formulations and methods for the treatment of disease |
| US20210220346A1 (en) * | 2018-05-17 | 2021-07-22 | Aegis Therapeutics Llc | Formulations and methods for the prevention of opioid overdose |
| US20210228570A1 (en) * | 2018-06-01 | 2021-07-29 | Purdue Pharma L.P. | Compositions and methods for opioid overdose rescue |
| EP3876938A4 (en) | 2018-11-06 | 2022-08-10 | Purdue Pharma L.P. | COMPOSITIONS AND METHODS OF ADMINISTRATION OF OPIOID ANTAGONISTS |
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| US10729687B1 (en) | 2019-07-09 | 2020-08-04 | Orexo Ab | Pharmaceutical composition for nasal delivery |
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| CA3167312A1 (en) * | 2020-02-07 | 2021-08-12 | Stephen J. Lewis | Compositions and methods for attenuating opioid induced cardio and/or respiratory depression |
| CN115515621A (zh) * | 2020-05-04 | 2022-12-23 | 安福星制药公司 | 胆汁酸及其盐作为药物的经鼻递送的增强剂的安全用途 |
| PE20230382A1 (es) | 2020-05-18 | 2023-03-06 | Orexo Ab | Nueva composicion farmaceutica para administracion de farmacos |
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| IL313016A (en) | 2021-11-25 | 2024-07-01 | Orexo Ab | A pharmaceutical preparation that includes adrenaline |
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| WO2024222920A1 (zh) * | 2023-04-28 | 2024-10-31 | 成都苑东生物制药股份有限公司 | 一种用于鼻内给药的药物制剂及其制备方法 |
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| US12290596B2 (en) | 2021-08-04 | 2025-05-06 | Indivior Uk Limited | Compositions and methods for the treatment of opioid overdose |
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