JP2020533415A - ナルコレプシーの処置におけるガボキサドールの使用 - Google Patents
ナルコレプシーの処置におけるガボキサドールの使用 Download PDFInfo
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Abstract
Description
本出願は2017年9月12日に出願された米国特許仮出願第62/557,412号の優先権の利益を主張するものであり、これはその全体の参照により本明細書に包含させる。
ガボキサドールを用いたナルコレプシーの処置が提供される。
ナルコレプシーは睡眠−覚醒サイクルを制御する能力の低下が関与する慢性神経障害である。最も典型的な症状は日中の過剰な眠気、異常REM睡眠、カタプレキシー、睡眠麻痺および幻覚である。他の症状は無意識下での行動および夜間の覚醒状態を含み得る。全ての症状が全ての患者に現れるとは限らない。
ガボキサドールまたはその薬学的に許容される塩を用いたナルコレプシーの処置方法が、本明細書に記載される。本明細書に記載のナルコレプシーの処置方法は、処置を必要とする患者にガボキサドールまたはその薬学的に許容される塩を投与することを含み、ここで前記方法が1以上のナルコレプシーの症状の改善を提供するものである。本明細書に記載のナルコレプシーの処置方法はまた、処置を必要とする患者にガボキサドールまたはその薬学的に許容される塩を投与することを含み、ここで前記方法が患者の翌日機能の改善を提供するものである。ある実施態様において、処置を必要とする患者にガボキサドールまたはその薬学的に許容される塩を、1以上のCNS刺激剤、覚醒促進剤、抗うつ剤またはGABAB受容体アゴニストと組み合わせて投与することを含むナルコレプシーの処置方法が提供される。本明細書に記載のナルコレプシーの処置方法はまた、処置を必要とする患者にガボキサドールまたはその薬学的に許容される塩を、1以上のCNS刺激剤、覚醒促進剤、抗うつ剤またはGABAB受容体アゴニストと組み合わせて投与することを含み、ここで前記方法が1以上のナルコレプシーの症状の改善を提供するものである。本明細書に記載のナルコレプシーの処置方法はまた、処置を必要とする患者にガボキサドールまたはその薬学的に許容される塩を、1以上のCNS刺激剤、覚醒促進剤、抗うつ剤またはGABAB受容体アゴニストと組み合わせて投与することを含み、ここで前記方法が患者の翌日機能の改善を提供するものである。
次の実施例は、2.5〜20mgの範囲の単回経口用量後のガボキサドール一水和物の血漿濃度プロファイルおよび用量比例性を提供する。2.5〜20mgの範囲のガボキサドール一水和物カプセルの絶対的バイオアベイラビリティもまた、評価される。
ナルコレプシーを有する患者におけるガボキサドールの有効性評価
この前向き試験は、カタプレキシーを伴うまたは伴わないナルコレプシーの診断を有する18〜65歳の年齢の成人におけるナルコレプシーの症状を軽減するためのガボキサドールの用量依存的能力を評価するために使用される。具体的に、5mg、10mgおよび20mgの用量で1日1回投与されるガボキサドールはプラセボと比較され、日中の眠気指数(ESS)、覚醒維持検査(MWT)およびポリソムノグラムにより測定されるガボキサドールへの応答の程度および速度を評価する。
Claims (19)
- 処置を必要とする患者にガボキサドールまたはその薬学的に許容される塩を含む医薬組成物を投与することを含む、ナルコレプシーの処置方法。
- 0.1mg〜30mgのガボキサドールまたはその薬学的に許容される塩が患者に投与される、請求項1に記載の方法。
- ガボキサドールまたはその薬学的に許容される塩が1mg〜30mgの範囲の一日投与量で患者に投与される、請求項1に記載の方法。
- 医薬組成物が5mg〜20mgのガボキサドールを含む、請求項1に記載の方法。
- ガボキサドールまたはその薬学的に許容される塩が0.1mg/kg〜1mg/kgの範囲の用量で投与される、請求項1に記載の方法。
- 組成物が1日1回、2回、3回または隔日投与される、請求項1に記載の方法。
- CNS刺激剤、覚醒促進剤(eugeroic agent)、抗うつ剤およびGABAB受容体アゴニストから成る群から選択される化合物を投与することをさらに含む、請求項1に記載の方法。
- CNS刺激剤がアンフェタミン、右旋性アンフェタミン、メタンフェタミン、メチルフェニデート、フェンテルミン、ジエチルプロピオン、フェンジメトラジン、リスデキサンフェタミン、ベンズフェタミン、アトモキセチン、カフェインおよびエフェドリンから成る群から選択される、請求項7に記載の方法。
- 覚醒促進剤がモダフィニルおよびアルモダフィニルから成る群から選択される、請求項7に記載の方法。
- ドーパミン作動性抗うつ剤、ドーパミン作動性賦活剤、セロトニン−ノルエピネフリン再取り込み阻害剤、ノルエピネフリン再取り込み阻害剤、モノアミンオキシダーゼ阻害剤、三環式抗うつ剤、四環式抗うつ剤および選択的セロトニン再取り込み阻害剤から成る群から選択される、請求項7に記載の方法。
- GABAB受容体アゴニストがナトリウムオキシベート、バクロフェンおよびフェニビュートから成る群から選択される、請求項7に記載の方法。
- ナルコレプシーと診断された患者にガボキサドールまたはその薬学的に許容される塩をナルコレプシーの1以上の症状を低減するために有効な量で投与することを含む、ナルコレプシーの処置方法。
- ナルコレプシーの症状が日中の過剰な眠気、異常REM睡眠、カタプレキシー、睡眠麻痺、幻覚、無意識下での行動および夜間の覚醒状態から選択される、請求項12に記載の方法。
- ガボキサドールまたはその薬学的に許容される塩が5mg〜30mgの範囲の量で投与される、請求項12に記載の方法。
- CNS刺激剤、覚醒促進剤、抗うつ剤およびGABAB受容体アゴニストから成る群から選択される化合物を投与することをさらに含む、請求項12に記載の方法。
- 患者の翌日機能の改善を提供する、処置を必要とする患者にガボキサドールまたはその薬学的に許容される塩を投与することを含む、ナルコレプシーの処置方法。
- 患者が日中の過剰な眠気の量の低減を示す、請求項16に記載の方法。
- ガボキサドールまたはその薬学的に許容される塩が5mg〜30mgの範囲で投与される、請求項16に記載の方法。
- CNS刺激剤、覚醒促進剤、抗うつ剤およびGABAB受容体アゴニストから成る群から選択される化合物を投与することをさらに含む、請求項16に記載の方法。
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PCT/US2018/050339 WO2019055369A1 (en) | 2017-09-12 | 2018-09-11 | USE OF GABOXADOL IN THE TREATMENT OF NARCOLEPSIA |
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US20190076409A1 (en) * | 2017-09-12 | 2019-03-14 | Ovid Therapeutics Inc. | Use of gaboxadol in the treatment of narcolepsy |
EP3883566A4 (en) | 2018-11-21 | 2022-09-07 | Certego Therapeutics Inc. | GABOXADOL FOR SUICIDE RISK REDUCTION AND RAPID DEPRESSION RELIEF |
JP2022538569A (ja) | 2019-06-28 | 2022-09-05 | ユニバーシティ オブ コペンハーゲン | 睡眠障害を伴うcns障害の治療 |
CA3182508A1 (en) | 2020-05-20 | 2021-11-25 | Certego Therapeutics Inc. | Ring deuterated gaboxadol and its use for the treatment of psychiatric disorders |
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US9682069B2 (en) * | 2015-07-17 | 2017-06-20 | Ovid Therapeutics Inc | Methods of treating Dravet syndrome |
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US20200222372A1 (en) | 2020-07-16 |
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CN111328282A (zh) | 2020-06-23 |
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