JP2010520202A - レチノイン酸療法の効力を妨げることなくレチノイン酸療法の副作用を軽減する方法、および/又は、その効力を改善する方法 - Google Patents
レチノイン酸療法の効力を妨げることなくレチノイン酸療法の副作用を軽減する方法、および/又は、その効力を改善する方法 Download PDFInfo
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Abstract
Description
本出願は、ここにその全体を参考文献として合体させる2007年2月28日出願の出願番号60/903,937号の優先権を主張するものである。
本発明は、レチノイン酸療法の効力を妨げることなくレチノイン酸療法から生じる副作用を軽減する、および/又は、その効力を改善するためのナイアシン誘導体の利用に関する。詳しくは、直鎖ニコチン酸アルキルエステル、特にニコチン酸ミリスチル等のナイアシン誘導体は、後述するように、非限定的に、つっぱり感(tightness)/乾燥、刺痛感(ピリピリ感:stinging)、灼熱感(burning)、刺痛感(チクチク感:tingling)等が挙げられるレチノイン酸療法から生じる副作用を軽減する。又、カスパーゼ14とフィラグリンとの発現を増加させることによる皮膚細胞の分化の改善も本発明の一部である。
ビタミンA(レチノール)の天然代謝産物及び合成類似体である、レチノイドは、皮膚機能の重要な調整因子である。フィッシャー(Fisher)他著、Faseb J.、1996年、第10巻、第1002〜13頁。主要な自然発生生物活性レチノイドであるオールトランス型レチノイン酸(ビタミンA酸)は、長年に渡って、光損傷を受けた皮膚の局所治療におけるその利用可能性の研究において注目されてきた。1986年、レチノイン酸が、数ヶ月の治療後、より平滑で、皺が少なく、色素沈着の少ない皮膚を作り出することができることが報告された。クリグマン(Kligman)他著、J Am Acad Dermatol、1986年、第15巻、第836〜59頁。
例1
軽症から中程度の顔面光障害を有する対象体において皮膚バリア機能を促進するナイアシンの親油性誘導体である、ニコチン酸ミリスチル(MN)との併用でのレチノイン酸療法を調べるために臨床研究を行った。
レチノイン酸療法の耐容性と効力を評価するために、対象体を更に、ベースラインと、2,4,8及び12週間時とにおいて、効力/パフォーマンスパラメーター及び刺激感/安全性パラメーターとに関して、顔の右側および/又は左側上で臨床的に類別した。
カスパーゼ14は、表皮の成熟をコントロールするユニークなプロテーゼであることが示されている。このコントロールは、皮膚細胞分化の後期段階に関与するものとして認識されているタンパク質である、フィラグリンのタンパク質分解プロセシングから生じる。フィラグリンに対する カスパーゼ14の作用の生成物によってUVB光障害、更に水分の損失、が防止される。ここにその両方を参考文献として合体させるニコテラ(Nicotera)他著、Nature Cell Biology、第9巻、第 621〜622頁(2007年);デネッカー(Denecker)他著、Nature Cell Biology、第9巻、第666〜674頁(2007年)を参照。
Claims (16)
- レチノイン酸療法の効力の障害となることなく、レチノイン酸療法の副作用を軽減する、及び/又は、その療法の効力を改善する方法であって、前記レチノイン酸療法を受ける対象体に対して、前記副作用を軽減するのに十分な量のニコチン酸アルキルエステルを投与する工程を含む方法。
- 前記ニコチン酸アルキルエステルが、局所投与される請求項1に記載の方法。
- 前記ニコチン酸アルキルエステルが、皮膚又は経皮投与によって投与される請求項1に記載の方法。
- 前記ニコチン酸アルキルエステルが、8〜18の炭素原子の無分岐アルキル鎖を含む請求項1に記載の方法。
- 前記ニコチン酸アルキルエステルが、ニコチン酸ミリスチル、又はニコチン酸パルミトイルである請求項1に記載の方法。
- 前記ニコチン酸アルキルエステルを、前記レチノイン酸療法と同時に投与する請求項1に記載の方法。
- 前記ニコチン酸アルキルエステルを、前記レチノイン酸療法の後で投与する請求項1に記載の方法。
- 前記ニコチン酸アルキルエステルを、前記対象体に対して、角質層厚み又は皮膚バリア機能を増大させるのに十分な時間投与し、前記ニコチン酸アルキルエステルは、前記レチノイン酸療法の投与前に投与される請求項1に記載の方法。
- 前記ニコチン酸アルキルエステルを、前記対象体に対して、レチノイン酸療法に耐容する前記対象体の能力を高めるのに十分な時間投与し、前記ニコチン酸アルキルエステルは、前記レチノイン酸療法の投与前に投与される請求項1に記載の方法。
- 前記ニコチン酸アルキルエステルを、前記対象体に対して、前記レチノイン酸療法の投与の前の少なくとも1ヶ月間、投与する工程を有する請求項8に記載の方法。
- 前記ニコチン酸アルキルエステルを、前記対象体に対して、前記レチノイン酸療法の投与の前の少なくとも1ヶ月間、投与する工程を有する請求項9に記載の方法。
- 前記対象体が、哺乳動物である請求項1に記載の方法。
- 前記哺乳動物が、ヒトである請求項12に記載の方法。
- 皮膚細胞分化を改善する方法であって、それを必要とする対象体に、カスパーゼ14とフィラグリンの発現を増大させ、それらの間の相互作用を増大させて皮膚細胞分化の改善をもたらすのに十分な量のニコチン酸アルキルエステルを投与する工程を有する、皮膚細胞分化を改善する方法。
- 前記ニコチン酸アルキルエステルが、ニコチン酸ミリスチルである請求項14に記載の方法。
- 前記ニコチン酸アルキルエステルを、局所投与する請求項14に記載の方法。
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PCT/US2008/002605 WO2008106177A2 (en) | 2007-02-28 | 2008-02-27 | Method for alleviating side effects of retinoic acid therapy and/or improving efficacy without interfering with efficacy |
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US8383167B2 (en) | 2011-03-08 | 2013-02-26 | Elc Management, Llc | Method for cosmetically treating caspase-14 deficiency |
FR2975002B1 (fr) | 2011-05-12 | 2020-08-14 | Jean-Noel Thorel | Procede de traitement cosmetique de la peau en deux etapes successives |
US10076479B1 (en) | 2018-05-08 | 2018-09-18 | Avon Products, Inc. | Methods for treating skin |
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US5776699A (en) * | 1995-09-01 | 1998-07-07 | Allergan, Inc. | Method of identifying negative hormone and/or antagonist activities |
US5939082A (en) * | 1995-11-06 | 1999-08-17 | The Procter & Gamble Company | Methods of regulating skin appearance with vitamin B3 compound |
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JPN6012024123; J. Pharm. Biomed. Anal. Vol.43, No.3, 20070219, 893-899 * |
JPN6013004903; JACOBSON M.K. et al: 'Enhancement of human skin barrier integrity by nicotinic acid derivatives' J. Invest. Dermatol. Vol.122, No.3, 200403, A58 |
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RU2009135872A (ru) | 2011-04-10 |
US20100173957A1 (en) | 2010-07-08 |
PT2120917E (pt) | 2014-04-24 |
HK1143955A1 (zh) | 2011-01-21 |
EP2120917A4 (en) | 2011-09-14 |
RU2010128725A (ru) | 2012-01-20 |
NZ579416A (en) | 2011-07-29 |
JP5699414B2 (ja) | 2015-04-08 |
EP2120917A2 (en) | 2009-11-25 |
PL2120917T3 (pl) | 2014-09-30 |
DK2120917T3 (da) | 2014-04-07 |
EP2120917B1 (en) | 2014-01-22 |
ES2458566T3 (es) | 2014-05-06 |
WO2008106177A3 (en) | 2008-11-06 |
WO2008106177A2 (en) | 2008-09-04 |
CA2679315C (en) | 2013-06-25 |
RU2463046C2 (ru) | 2012-10-10 |
CN101742916A (zh) | 2010-06-16 |
AU2008219633B2 (en) | 2011-05-26 |
CN101742916B (zh) | 2015-08-19 |
AU2008219633A1 (en) | 2008-09-04 |
IL200598A (en) | 2015-07-30 |
RU2442577C2 (ru) | 2012-02-20 |
MX2009009188A (es) | 2010-03-26 |
IL200598A0 (en) | 2010-05-17 |
CA2679315A1 (en) | 2008-09-04 |
US9642845B2 (en) | 2017-05-09 |
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