JP2019527711A5 - - Google Patents
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- Publication number
- JP2019527711A5 JP2019527711A5 JP2019506721A JP2019506721A JP2019527711A5 JP 2019527711 A5 JP2019527711 A5 JP 2019527711A5 JP 2019506721 A JP2019506721 A JP 2019506721A JP 2019506721 A JP2019506721 A JP 2019506721A JP 2019527711 A5 JP2019527711 A5 JP 2019527711A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- weight
- composition according
- glycol
- rapamycin
- 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
Links
- 239000000203 mixture Substances 0.000 claims description 50
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 24
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 20
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims description 10
- 239000007788 liquid Substances 0.000 claims description 10
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims description 10
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims description 10
- 229960002930 sirolimus Drugs 0.000 claims description 10
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 9
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 5
- 239000002202 Polyethylene glycol Substances 0.000 claims description 5
- 229920001223 polyethylene glycol Polymers 0.000 claims description 5
- 206010040882 skin lesion Diseases 0.000 claims description 5
- 231100000444 skin lesion Toxicity 0.000 claims description 5
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 4
- 208000003120 Angiofibroma Diseases 0.000 claims description 4
- 239000004322 Butylated hydroxytoluene Substances 0.000 claims description 4
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 claims description 4
- 239000002033 PVDF binder Substances 0.000 claims description 4
- 208000026911 Tuberous sclerosis complex Diseases 0.000 claims description 4
- 235000010354 butylated hydroxytoluene Nutrition 0.000 claims description 4
- 229940095259 butylated hydroxytoluene Drugs 0.000 claims description 4
- 230000001815 facial effect Effects 0.000 claims description 4
- 229920002981 polyvinylidene fluoride Polymers 0.000 claims description 4
- 208000009999 tuberous sclerosis Diseases 0.000 claims description 4
- 206010027145 Melanocytic naevus Diseases 0.000 claims description 3
- 208000007256 Nevus Diseases 0.000 claims description 3
- 208000009443 Vascular Malformations Diseases 0.000 claims description 3
- RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 claims description 2
- 208000031857 Campbell de Morgan spots Diseases 0.000 claims description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 2
- 208000032541 Epidermal naevus Diseases 0.000 claims description 2
- 206010025219 Lymphangioma Diseases 0.000 claims description 2
- 201000002571 Melkersson-Rosenthal syndrome Diseases 0.000 claims description 2
- 208000003019 Neurofibromatosis 1 Diseases 0.000 claims description 2
- 208000024834 Neurofibromatosis type 1 Diseases 0.000 claims description 2
- 241000588769 Proteus <enterobacteria> Species 0.000 claims description 2
- 206010037649 Pyogenic granuloma Diseases 0.000 claims description 2
- 208000034541 Rare lymphatic malformation Diseases 0.000 claims description 2
- 206010043189 Telangiectasia Diseases 0.000 claims description 2
- 229940073669 ceteareth 20 Drugs 0.000 claims description 2
- 229940081733 cetearyl alcohol Drugs 0.000 claims description 2
- 208000010575 cherry hemangioma Diseases 0.000 claims description 2
- 239000006071 cream Substances 0.000 claims description 2
- AMTWCFIAVKBGOD-UHFFFAOYSA-N dioxosilane;methoxy-dimethyl-trimethylsilyloxysilane Chemical compound O=[Si]=O.CO[Si](C)(C)O[Si](C)(C)C AMTWCFIAVKBGOD-UHFFFAOYSA-N 0.000 claims description 2
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 claims description 2
- 208000014402 familial multiple discoid fibromas Diseases 0.000 claims description 2
- 229940075507 glyceryl monostearate Drugs 0.000 claims description 2
- 201000011066 hemangioma Diseases 0.000 claims description 2
- WSFSSNUMVMOOMR-NJFSPNSNSA-N methanone Chemical compound O=[14CH2] WSFSSNUMVMOOMR-NJFSPNSNSA-N 0.000 claims description 2
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 claims description 2
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims description 2
- 206010030983 oral lichen planus Diseases 0.000 claims description 2
- 208000023112 overgrowth syndrome Diseases 0.000 claims description 2
- 235000019271 petrolatum Nutrition 0.000 claims description 2
- 229960004063 propylene glycol Drugs 0.000 claims description 2
- 239000008213 purified water Substances 0.000 claims description 2
- 229940083037 simethicone Drugs 0.000 claims description 2
- 235000010199 sorbic acid Nutrition 0.000 claims description 2
- 239000004334 sorbic acid Substances 0.000 claims description 2
- 229940075582 sorbic acid Drugs 0.000 claims description 2
- 239000000600 sorbitol Substances 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 208000009056 telangiectasis Diseases 0.000 claims description 2
- 230000008719 thickening Effects 0.000 claims description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 2
- 239000003871 white petrolatum Substances 0.000 claims description 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 3
- 238000003745 diagnosis Methods 0.000 claims 2
- 235000019441 ethanol Nutrition 0.000 claims 2
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 claims 2
- 229940022682 acetone Drugs 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 238000006136 alcoholysis reaction Methods 0.000 claims 1
- AKGGYBADQZYZPD-UHFFFAOYSA-N benzyl acetone Natural products CC(=O)CCC1=CC=CC=C1 AKGGYBADQZYZPD-UHFFFAOYSA-N 0.000 claims 1
- 239000002304 perfume Substances 0.000 claims 1
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 claims 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 claims 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 claims 1
- 229960003415 propylparaben Drugs 0.000 claims 1
- 229940068196 placebo Drugs 0.000 description 2
- 239000000902 placebo Substances 0.000 description 2
- 230000000699 topical effect Effects 0.000 description 2
- 206010067193 Naevus flammeus Diseases 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 208000002026 familial multiple nevi flammei Diseases 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 230000036244 malformation Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662372940P | 2016-08-10 | 2016-08-10 | |
| US62/372,940 | 2016-08-10 | ||
| PCT/US2017/046320 WO2018031789A1 (en) | 2016-08-10 | 2017-08-10 | Topical rapamycin therapy |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019527711A JP2019527711A (ja) | 2019-10-03 |
| JP2019527711A5 true JP2019527711A5 (enExample) | 2020-08-20 |
Family
ID=59684091
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019506721A Pending JP2019527711A (ja) | 2016-08-10 | 2017-08-10 | 局所ラパマイシン療法 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20190167649A1 (enExample) |
| EP (1) | EP3496712A1 (enExample) |
| JP (1) | JP2019527711A (enExample) |
| KR (1) | KR20190039220A (enExample) |
| CN (1) | CN109689053A (enExample) |
| AU (1) | AU2017311491A1 (enExample) |
| BR (1) | BR112019002689A2 (enExample) |
| CA (1) | CA3032473A1 (enExample) |
| MX (1) | MX2019001670A (enExample) |
| RU (1) | RU2019106483A (enExample) |
| WO (1) | WO2018031789A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL302385B2 (en) | 2017-01-06 | 2024-06-01 | Palvella Therapeutics Inc | Non-aqueous preparations of mTOR inhibitors and methods of use |
| WO2019156999A1 (en) * | 2018-02-06 | 2019-08-15 | Georgetown University | TOPICAL mTOR INHIBITORS FOR CUTANEOUS PROLIFERATIVE AND VASCULAR CONDITIONS |
| JP2021530463A (ja) | 2018-07-02 | 2021-11-11 | パルヴェラ セラピューティクス、インク． | ｍＴＯＲ阻害剤の無水組成物および使用方法 |
| EP3829578A4 (en) * | 2018-08-30 | 2022-08-17 | Chemistryrx | COMPOSITIONS CONTAINING SIROLIMUS |
| CN109431997B (zh) * | 2018-12-20 | 2021-06-04 | 武汉科福新药有限责任公司 | 一种雷帕霉素局部注射制剂及其制备方法 |
| JP2022521006A (ja) | 2019-02-20 | 2022-04-04 | エイアイ・セラピューティクス・インコーポレーテッド | 局所ラパマイシン製剤ならびに顔面血管線維腫および他の皮膚疾患の治療におけるそれらの使用 |
| WO2020175131A1 (ja) * | 2019-02-27 | 2020-09-03 | 国立大学法人大阪大学 | 脈管異常治療用外用剤 |
| JP7755854B2 (ja) * | 2020-01-24 | 2025-10-17 | ノーベルファーマ株式会社 | ラパマイシン含有外用剤 |
| AU2020277132B1 (en) * | 2020-11-24 | 2021-11-04 | Aft Pharmaceuticals Limited | A Rapamycin Composition |
| AU2023203871B1 (en) * | 2023-06-20 | 2024-07-25 | Aft Pharmaceuticals Ltd | A Rapamycin Method of Treatment and Composition |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9606452D0 (en) | 1996-03-27 | 1996-06-05 | Sandoz Ltd | Organic compounds |
| EP0937082A2 (en) | 1996-07-12 | 1999-08-25 | Ariad Pharmaceuticals, Inc. | Materials and method for treating or preventing pathogenic fungal infection |
| GB9723669D0 (en) | 1997-11-07 | 1998-01-07 | Univ Aberdeen | Skin penetration enhancing components |
| AU2003259803B2 (en) | 2002-08-12 | 2007-08-02 | The Regents Of The University Of Michigan | Diagnosis and treatment of tuberous sclerosis |
| EP1853612A1 (en) | 2005-03-02 | 2007-11-14 | Wyeth | Purification of rapamycin |
| AU2007211613C1 (en) | 2006-02-02 | 2018-01-04 | Novartis Ag | Tuberous Sclerosis treatment |
| US20120022095A1 (en) | 2010-06-24 | 2012-01-26 | Teng Joyce M C | Topical rapamycin for treatment of facial angiofibromas in tuberous sclerosis |
| WO2012142145A1 (en) * | 2011-04-12 | 2012-10-18 | Dow Pharmaceutical Sciences | Methods of treating skin conditions exhibiting telangiectasia |
| CA2899206C (en) * | 2013-01-24 | 2019-07-09 | Transderm, Inc. | Compositions for transdermal delivery of mtor inhibitors |
| HUP1400075A2 (hu) * | 2014-02-14 | 2015-08-28 | Druggability Technologies Ip Holdco Jersey Ltd | Sirolimus és származékainak komplexei, elõállítása és gyógyszerészeti kompozíciói |
| KR20180081501A (ko) * | 2015-09-24 | 2018-07-16 | 드렉셀유니버시티 | 진피 장애를 치료하거나 예방하는 신규한 조성물 및 방법 |
| CN105663027B (zh) * | 2016-04-01 | 2018-12-18 | 中国人民解放军广州军区武汉总医院 | 西罗莫司外用制剂、其制备方法及用途 |
-
2017
- 2017-08-10 CA CA3032473A patent/CA3032473A1/en not_active Abandoned
- 2017-08-10 US US16/324,274 patent/US20190167649A1/en not_active Abandoned
- 2017-08-10 EP EP17755383.1A patent/EP3496712A1/en not_active Withdrawn
- 2017-08-10 WO PCT/US2017/046320 patent/WO2018031789A1/en not_active Ceased
- 2017-08-10 AU AU2017311491A patent/AU2017311491A1/en not_active Abandoned
- 2017-08-10 CN CN201780049324.6A patent/CN109689053A/zh active Pending
- 2017-08-10 KR KR1020197006896A patent/KR20190039220A/ko not_active Ceased
- 2017-08-10 JP JP2019506721A patent/JP2019527711A/ja active Pending
- 2017-08-10 RU RU2019106483A patent/RU2019106483A/ru unknown
- 2017-08-10 BR BR112019002689A patent/BR112019002689A2/pt not_active IP Right Cessation
- 2017-08-10 MX MX2019001670A patent/MX2019001670A/es unknown
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