JPWO2021007245A5 - - Google Patents
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- JPWO2021007245A5 JPWO2021007245A5 JP2022500683A JP2022500683A JPWO2021007245A5 JP WO2021007245 A5 JPWO2021007245 A5 JP WO2021007245A5 JP 2022500683 A JP2022500683 A JP 2022500683A JP 2022500683 A JP2022500683 A JP 2022500683A JP WO2021007245 A5 JPWO2021007245 A5 JP WO2021007245A5
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- JP
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- Prior art keywords
- pharmaceutical composition
- composition according
- treatment
- patient
- bipolar
- Prior art date
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Description
これらの結果は、レスポンダー率および寛解率に対する統計的に有意な利益によって裏付けられており、主要アウトカムの臨床的有意味性を実証している。さらに、双極性ＩＩ型障害患者のサブグループ解析では、ルマテペロン４２ｍｇはＭＡＤＲＳ合計スコアについてプラセボよりも統計的に有意に優れていた。
本願は下記の態様も包含する。
［態様１］
双極性ＩＩ型障害の治療方法であって、該治療を必要とする患者に、遊離形態または薬学的に許容される塩形態であって重水素化形態であってもよいルマテペロンの治療有効量を投与することを含む、方法。
［態様２］
ルマテペロンがトルエンスルホン酸付加塩（例えば、一トシル酸塩または二トシル酸塩）の形態である、態様１に記載の方法。
［態様３］
塩が固体結晶塩である、態様２に記載の方法。
［態様４］
ルマテペロンが重水素化形態である、態様１～３のいずれか１つに記載の方法。
［態様５］
遊離形態または薬学的に許容される塩形態であって重水素化形態であってもよいルマテペロンが、遊離塩基６～６０ｍｇに相当する１日総用量で投与される、態様１～４のいずれか１つに記載の方法。
［態様６］
ルマテペロントシル酸塩約６０ｍｇを薬学的に許容される希釈剤または担体と組み合わせてまたは関連させて含む錠剤またはカプセル剤の１日１回投与を含む、上記のいずれかの態様に記載の方法。
［態様７］
治療されるべき状態が、双極性ＩＩ型障害におけるうつ病、または双極性ＩＩ型障害に関連するうつ病エピソード（例えば、大うつ病エピソード）である、上記のいずれかの態様に記載の方法。
［態様８］
治療の経過中に、患者が、モンゴメリー－アスバーグうつ病評価尺度（ＭＡＤＲＳ）合計スコアの改善を示し、および／または、双極性障害重症度についての臨床全般印象評価尺度（ＣＧＩ－ＢＰ－Ｓ）の改善（例えば、治療開始後８日以内での改善）を示す、上記のいずれかの態様に記載の方法。
［態様９］
治療が、高血糖症、脂質異常症、体重増加、希死念慮（suicidal ideation）もしくは希死念慮（suicidal thoughts）、またはアカシジアを包含する錐体外路症状のうち１つ以上を引き起こさない、上記のいずれかの態様に記載の方法。
［態様１０］
患者が並行して気分安定化剤の投与を受けている、上記のいずれかの態様に記載の方法。
［態様１１］
患者が以前にＳＳＲＩによる治療を受けていた（例えば、その治療は、効果的ではなかった、および／または副作用などのために中止された）、上記のいずれかの態様に記載の方法。
［態様１２］
患者が以前に非定型抗精神病薬のような抗精神病薬による治療を受けていた（例えば、その治療は、効果的ではなかった、および／または副作用などのために中止された）、上記のいずれかの態様に記載の方法。
［態様１３］
抗精神病薬が、ハロペリドールン、アリピプラゾール、クエチアピン、オランザピン、リスペリドン、ルラシドン、パリペリドン、イロペリドン、ジプラシドン、ブレクスピプラゾール（brexipiprazole）、アセナピン、クロザピンおよびゾテピンから選択される、態様１２に記載の方法。
［態様１４］
上記態様のいずれかに記載の方法で使用するための遊離形態または薬学的に許容される塩形態であって重水素化形態であってもよいルマテペロン。
These results are supported by statistically significant benefits on responder and remission rates, demonstrating the clinical significance of the primary outcome. Additionally, in a subgroup analysis of patients with bipolar II disorder, lumateperone 42 mg was statistically significantly superior to placebo for MADRS total score.
This application also includes the following aspects.
[Aspect 1]
A method of treating bipolar II disorder comprising administering to a patient in need thereof a therapeutically effective amount of lumateperone, which may be in free form or in a pharmaceutically acceptable salt form, which may be a deuterated form. A method comprising administering.
[Aspect 2]
A method according to aspect 1, wherein the lumateperone is in the form of a toluenesulfonic acid addition salt (eg, monotosylate or ditosylate).
[Aspect 3]
A method according to aspect 2, wherein the salt is a solid crystalline salt.
[Aspect 4]
4. The method of any one of aspects 1-3, wherein the lumateperone is in deuterated form.
[Aspect 5]
Any of aspects 1-4, wherein lumateperone in free form or in pharmaceutically acceptable salt form, which may be deuterated, is administered in a total daily dose equivalent to 6-60 mg of free base. The method described in 1.
[Aspect 6]
The method of any of the above aspects, comprising once daily administration of a tablet or capsule containing about 60 mg of lumateperontosilate in combination or associated with a pharmaceutically acceptable diluent or carrier.
[Aspect 7]
The method of any of the above aspects, wherein the condition to be treated is depression in bipolar II disorder or a depressive episode (eg, a major depressive episode) associated with bipolar II disorder.
[Aspect 8]
During the course of treatment, the patient demonstrated improvement in the Montgomery-Asberg Depression Rating Scale (MADRS) total score and/or the Clinical Global Impression Scale for Bipolar Disorder Severity (CGI-BP-S) A method according to any of the above aspects, wherein the method exhibits improvement (eg, improvement within 8 days after initiation of treatment).
[Aspect 9]
The above, wherein the treatment does not cause one or more of hyperglycemia, dyslipidemia, weight gain, suicidal ideation or suicidal thoughts, or extrapyramidal symptoms including akathisia A method according to any aspect.
[Aspect 10]
The method of any of the above embodiments, wherein the patient is concurrently receiving a mood stabilizing agent.
[Aspect 11]
A method according to any of the above aspects, wherein the patient has previously been treated with an SSRI (eg, the treatment was ineffective and/or discontinued due to side effects, etc.).
[Aspect 12]
The patient has previously been treated with an antipsychotic such as an atypical antipsychotic (e.g., the treatment was ineffective and/or was discontinued due to side effects, etc.), any of the above A method according to any one of the aspects.
[Aspect 13]
13. The method of aspect 12, wherein the antipsychotic is selected from haloperidolone, aripiprazole, quetiapine, olanzapine, risperidone, lurasidone, paliperidone, iloperidone, ziprasidone, brexipiprazole, asenapine, clozapine and zotepine.
[Aspect 14]
Lumateperone in free form or in pharmaceutically acceptable salt form, optionally in deuterated form, for use in a method according to any of the above aspects.
Claims (21)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962871170P | 2019-07-07 | 2019-07-07 | |
| US62/871,170 | 2019-07-07 | ||
| PCT/US2020/041063 WO2021007245A1 (en) | 2019-07-07 | 2020-07-07 | Novel methods |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022539821A JP2022539821A (en) | 2022-09-13 |
| JPWO2021007245A5 true JPWO2021007245A5 (en) | 2023-07-14 |
Family
ID=74066254
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022500683A Pending JP2022539821A (en) | 2019-07-07 | 2020-07-07 | New method |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US20210000822A1 (en) |
| EP (2) | EP3993798A4 (en) |
| JP (1) | JP2022539821A (en) |
| KR (1) | KR20220029744A (en) |
| CN (1) | CN114072150A (en) |
| AU (1) | AU2020311894A1 (en) |
| BR (1) | BR112022000231A2 (en) |
| CA (1) | CA3141223A1 (en) |
| IL (1) | IL289589A (en) |
| MX (1) | MX2022000143A (en) |
| WO (1) | WO2021007245A1 (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4208434A2 (en) * | 2020-09-04 | 2023-07-12 | Intra-Cellular Therapies, Inc. | Novel salts, crystals, and co-crystals |
| WO2024030835A2 (en) * | 2022-07-30 | 2024-02-08 | Intra-Cellular Therapies, Inc. | Novel salts and crystals |
| CN115671057A (en) * | 2022-10-19 | 2023-02-03 | 四川迈可隆生物科技有限公司 | Rumepilone pharmaceutical composition, long-acting microsphere sustained-release preparation and preparation method thereof |
| CN115554237B (en) * | 2022-12-08 | 2023-09-12 | 山东则正医药技术有限公司 | Rumex-pirone in-situ gel long-acting injection and preparation method and application thereof |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IE52535B1 (en) | 1981-02-16 | 1987-12-09 | Ici Plc | Continuous release pharmaceutical compositions |
| US6713471B1 (en) | 1999-06-15 | 2004-03-30 | Bristol-Myers Squibb Pharma Company | Substituted heterocycle fused gamma-carbolines |
| IL147109A0 (en) | 1999-06-15 | 2002-08-14 | Du Pont Pharm Co | Substtituted heterocycle fused gamma-carbolines |
| KR101610977B1 (en) | 2008-03-12 | 2016-04-08 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | Substituted heterocycle fused gamma-carbolines solid |
| WO2009145900A1 (en) | 2008-05-27 | 2009-12-03 | Intra-Cellular Therapies, Inc. | Methods and compositions for sleep disorders and other disorders |
| WO2011133224A1 (en) | 2010-04-22 | 2011-10-27 | Intra-Cellular Therapies, Inc. | Organic compounds |
| KR20140146192A (en) | 2012-04-14 | 2014-12-24 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | Organic compounds |
| CA2932610C (en) * | 2013-12-03 | 2023-08-22 | Intra-Cellular Therapies, Inc. | Heterocycle fused gamma-carboline compounds for use in treatment of schizophrenia |
| PL3125893T3 (en) | 2014-04-04 | 2024-02-12 | Intra-Cellular Therapies, Inc. | Deuterated heterocycle fused gamma-carbolines as antagonists of 5-ht2a receptors |
| EP3125892A4 (en) * | 2014-04-04 | 2017-12-27 | Intra-Cellular Therapies, Inc. | Organic compounds |
| WO2017117514A1 (en) * | 2015-12-31 | 2017-07-06 | Tung Roger D | Deuterated iti-007 |
| JP6686168B2 (en) | 2016-03-25 | 2020-04-22 | イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． | Organic compound |
| US11332469B2 (en) * | 2016-08-09 | 2022-05-17 | Teva Pharmaceuticals International Gmbh | Solid state forms of lumateperone ditosylate salt |
| AU2019280850B2 (en) | 2018-06-06 | 2024-08-08 | Intra-Cellular Therapies, Inc. | Novel salts and crystals |
-
2020
- 2020-07-07 EP EP20837066.8A patent/EP3993798A4/en active Pending
- 2020-07-07 EP EP22191949.1A patent/EP4134101A1/en active Pending
- 2020-07-07 US US16/922,893 patent/US20210000822A1/en not_active Abandoned
- 2020-07-07 MX MX2022000143A patent/MX2022000143A/en unknown
- 2020-07-07 CN CN202080049820.3A patent/CN114072150A/en active Pending
- 2020-07-07 AU AU2020311894A patent/AU2020311894A1/en active Pending
- 2020-07-07 WO PCT/US2020/041063 patent/WO2021007245A1/en unknown
- 2020-07-07 JP JP2022500683A patent/JP2022539821A/en active Pending
- 2020-07-07 BR BR112022000231A patent/BR112022000231A2/en unknown
- 2020-07-07 KR KR1020227003969A patent/KR20220029744A/en unknown
- 2020-07-07 CA CA3141223A patent/CA3141223A1/en active Pending
-
2022
- 2022-01-03 IL IL289589A patent/IL289589A/en unknown
-
2023
- 2023-10-25 US US18/494,754 patent/US20240066030A1/en active Pending
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