JP2020527607A - 非炎症性病変の処置 - Google Patents
非炎症性病変の処置 Download PDFInfo
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- JP2020527607A JP2020527607A JP2020524697A JP2020524697A JP2020527607A JP 2020527607 A JP2020527607 A JP 2020527607A JP 2020524697 A JP2020524697 A JP 2020524697A JP 2020524697 A JP2020524697 A JP 2020524697A JP 2020527607 A JP2020527607 A JP 2020527607A
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- lesions
- therapeutically effective
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- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
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- IWVCMVBTMGNXQD-UHFFFAOYSA-N terramycin dehydrate Natural products C1=CC=C2C(O)(C)C3C(O)C4C(N(C)C)C(O)=C(C(N)=O)C(=O)C4(O)C(O)=C3C(=O)C2=C1O IWVCMVBTMGNXQD-UHFFFAOYSA-N 0.000 description 1
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- 230000014616 translation Effects 0.000 description 1
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/65—Tetracyclines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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Abstract
Description
483人の対象体に約1.5mg/kg/日の(4S,4aS,5aR,12aS)−4−ジメチルアミノ−3,10,12,12a−テトラヒドロキシ−7−[(メトキシ(メチル)アミノ)−メチル]−1,11−ジオキソ−1,4,4a,5,5a,6,11,12a−オクタヒドロ−ナフタセン−2−カルボン酸アミドの一塩酸塩結晶性塩(すなわち、式I)を投与し、485人の対象体にプラセボを投与した。この研究の対象体は、中等度〜重度の顔面尋常性ざ瘡を有するがテトラサイクリンクラス抗生物質の使用を排除する障害を有しない9歳〜45歳の男性および女性を含んでいた。対象体は、合計12週間試験され、評価するために処置の3週間目、6週間目、9週間目および12週間目にクリニックへ戻された。対象体を、病変数および医師による包括的評価(Investigator’s Global Assessment)(「IGA」)スコアによって評価した。
519人の対象体に約1.5mg/kg/日の(4S,4aS,5aR,12aS)−4−ジメチルアミノ−3,10,12,12a−テトラヒドロキシ−7−[(メトキシ(メチル)アミノ)−メチル]−1,11−ジオキソ−1,4,4a,5,5a,6,11,12a−オクタヒドロ−ナフタセン−2−カルボン酸アミドの一塩酸塩結晶性塩(すなわち、式I)を投与し、515人の対象体にプラセボを投与した。この研究の対象体は、中等度〜重度の顔面尋常性ざ瘡を有するがテトラサイクリンクラス抗生物質の使用を排除する障害を有しない9歳〜45歳の男性および女性を含んでいた。対象体は、合計12週間試験され、評価するために処置の3週間目、6週間目、9週間目および12週間目にクリニックへ戻された。対象体を、(実施例1に記載したように)病変数および医師による包括的評価(「IGA」)スコアによって評価した。
プラセボと比較して、約3.0mg/kg/日、約1.5mg/kg/日、または約0.75mg/kg/日の(4S,4aS,5aR,12aS)−4−ジメチルアミノ−3,10,12,12a−テトラヒドロキシ−7−[(メトキシ(メチル)アミノ)−メチル]−1,11−ジオキソ−1,4,4a,5,5a,6,11,12a−オクタヒドロ−ナフタセン−2−カルボン酸アミドの一塩酸塩結晶性塩(すなわち、式I)を、中等度〜重度の顔面尋常性ざ瘡を有する12歳〜45歳の男性および女性の対象体約280人に投与した。対象体は、上記4つの処置クループのいずれかに1:1:1:1の比率でランダムに割り当てられた。対象体は、合計12週間試験され、処置の1週間目、2週間目、4週間目、8週目および12週間目に評価するためにクリニックへ戻された。対象体を、病変数および医師による包括的評価(「IGA」)スコアによって評価した。
Claims (30)
- (i)非炎症性病変および/またはその症状の処置、または(ii)非炎症性病変および/またはその症状の処置用医薬の調製に用いるための(4S,4aS,5aR,12aS)−4−ジメチルアミノ−3,10,12,12a−テトラヒドロキシ−7−[(メトキシ(メチル)アミノ)−メチル]−1,11−ジオキソ−1,4,4a,5,5a,6,11,12a−オクタヒドロ−ナフタセン−2−カルボン酸アミドまたはその薬学的に許容される塩の使用。
- 薬学的に許容される塩が、結晶性一塩酸塩、結晶性一メシル酸塩および結晶性一硫酸塩からなる群から選択され、好ましくは結晶性一塩酸塩である、請求項1記載の使用。
- (4S,4aS,5aR,12aS)−4−ジメチルアミノ−3,10,12,12a−テトラヒドロキシ−7−[(メトキシ(メチル)アミノ)−メチル]−1,11−ジオキソ−1,4,4a,5,5a,6,11,12a−オクタヒドロ−ナフタセン−2−カルボン酸アミドまたはその薬学的に許容される塩が、治療有効量で毎日投与される、上記請求項のいずれか1項記載の使用。
- (4S,4aS,5aR,12aS)−4−ジメチルアミノ−3,10,12,12a−テトラヒドロキシ−7−[(メトキシ(メチル)アミノ)−メチル]−1,11−ジオキソ−1,4,4a,5,5a,6,11,12a−オクタヒドロ−ナフタセン−2−カルボン酸アミドまたはその薬学的に許容される塩が、治療有効量で、少なくとも3週間、少なくとも6週間、少なくとも9週間、または少なくとも12週間投与される、上記請求項のいずれか1項記載の使用。
- (4S,4aS,5aR,12aS)−4−ジメチルアミノ−3,10,12,12a−テトラヒドロキシ−7−[(メトキシ(メチル)アミノ)−メチル]−1,11−ジオキソ−1,4,4a,5,5a,6,11,12a−オクタヒドロ−ナフタセン−2−カルボン酸アミドまたはその薬学的に許容される塩が、約1.1mg/kg/日〜約1.8mg/kg/日、好ましくは約1.5mg/kg/日の量で投与される、上記請求項のいずれか1項記載の使用。
- 治療有効量が、経口剤形として投与される、上記請求項のいずれか1項記載の使用。
- 非炎症性病変が、尋常性ざ瘡であり、該尋常性ざ瘡が、顔面尋常性ざ瘡である、上記請求項のいずれか1項記載の使用。
- 非炎症性病変が、開放性面皰である、上記請求項のいずれか1項記載の使用。
- 非炎症性病変が、閉鎖性面皰である、上記請求項のいずれか1項記載の使用。
- (4S,4aS,5aR,12aS)−4−ジメチルアミノ−3,10,12,12a−テトラヒドロキシ−7−[(メトキシ(メチル)アミノ)−メチル]−1,11−ジオキソ−1,4,4a,5,5a,6,11,12a−オクタヒドロ−ナフタセン−2−カルボン酸アミドまたはその薬学的に許容される塩の治療有効量を含む、非炎症性病変および/またはその症状の処置に用いるための医薬。
- 薬学的に許容される塩が、結晶性一塩酸塩、結晶性一メシル酸塩および結晶性一硫酸塩からなる群から選択され、好ましくは結晶性一塩酸塩である、請求項10記載の医薬。
- 治療有効量が、毎日投与される、上記請求項のいずれか1項記載の医薬。
- 治療有効量が、少なくとも3週間、少なくとも6週間、少なくとも9週間、または少なくとも12週間投与される、上記請求項のいずれか1項記載の医薬。
- 治療有効量が、約1.1mg/kg/日〜約1.8mg/kg/日、好ましくは約1.5mg/kg/日である、上記請求項のいずれか1項記載の医薬。
- 治療有効量が、経口剤形として投与される、上記請求項のいずれか1項記載の医薬。
- 非炎症性病変が、尋常性ざ瘡であり、該尋常性ざ瘡が、顔面尋常性ざ瘡である、上記請求項のいずれか1項記載の医薬。
- 非炎症性病変が、開放性面皰である、請求項10〜16いずれか1項記載の医薬。
- 非炎症性病変が、閉鎖性面皰である、請求項10〜17いずれか1項記載の医薬。
- 非炎症性病変および/またはその症状の処置方法であって、該処置を必要とする対象体に、(4S,4aS,5aR,12aS)−4−ジメチルアミノ−3,10,12,12a−テトラヒドロキシ−7−[(メトキシ(メチル)アミノ)−メチル]−1,11−ジオキソ−1,4,4a,5,5a,6,11,12a−オクタヒドロ−ナフタセン−2−カルボン酸アミドまたはその薬学的に許容される塩の治療有効量を投与することを含む、方法。
- 薬学的に許容される塩が、結晶性一塩酸塩、結晶性一メシル酸塩および結晶性一硫酸塩からなる群から選択される、請求項19記載の方法。
- 薬学的に許容される塩が、結晶性一塩酸塩である、請求項20記載の方法。
- 治療有効量が、毎日投与される、請求項19記載の方法。
- 治療有効量が、少なくとも3週間、少なくとも6週間、少なくとも9週間、または少なくとも12週間投与される、請求項19記載の方法。
- 治療有効量が、約1.1mg/kg/日〜約1.8mg/kg/日である、請求項19記載の方法。
- 治療有効量が、約1.5mg/kg/日である、請求項24記載の方法。
- 治療有効量が、経口剤形として投与される、請求項19記載の方法。
- 非炎症性病変が、尋常性ざ瘡である、請求項19記載の方法。
- 尋常性ざ瘡が、顔面尋常性ざ瘡である、請求項27記載の方法。
- 非炎症性病変が、開放性面皰である、請求項19記載の方法。
- 非炎症性病変が、閉鎖性面皰である、請求項19記載の方法。
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- 2018-07-20 EP EP18779747.7A patent/EP3654988B1/en active Active
- 2018-07-20 WO PCT/IB2018/000938 patent/WO2019016609A1/en unknown
- 2018-07-20 BR BR112020000968-7A patent/BR112020000968A2/pt unknown
- 2018-07-20 CA CA3070663A patent/CA3070663A1/en active Pending
- 2018-07-20 ES ES18779747T patent/ES2962380T3/es active Active
- 2018-07-20 JP JP2020524697A patent/JP2020527607A/ja active Pending
- 2018-07-20 CN CN201880048978.1A patent/CN111343991A/zh active Pending
- 2018-07-20 US US16/632,121 patent/US20200222432A1/en not_active Abandoned
- 2018-07-20 AU AU2018303807A patent/AU2018303807B2/en active Active
- 2018-07-20 MX MX2020000816A patent/MX2020000816A/es unknown
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US20200222432A1 (en) | 2020-07-16 |
CA3070663A1 (en) | 2019-01-24 |
EP3654988A1 (en) | 2020-05-27 |
CN111343991A (zh) | 2020-06-26 |
EP3654988B1 (en) | 2023-09-06 |
AU2018303807B2 (en) | 2023-08-24 |
BR112020000968A2 (pt) | 2020-07-14 |
IL272124A (en) | 2020-03-31 |
KR102662461B1 (ko) | 2024-04-30 |
AU2018303807A1 (en) | 2020-02-13 |
WO2019016609A1 (en) | 2019-01-24 |
KR20200031126A (ko) | 2020-03-23 |
MA49641A (fr) | 2021-06-02 |
MX2020000816A (es) | 2020-08-17 |
ES2962380T3 (es) | 2024-03-18 |
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