JPWO2020234782A5 - - Google Patents
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- JPWO2020234782A5 JPWO2020234782A5 JP2021568760A JP2021568760A JPWO2020234782A5 JP WO2020234782 A5 JPWO2020234782 A5 JP WO2020234782A5 JP 2021568760 A JP2021568760 A JP 2021568760A JP 2021568760 A JP2021568760 A JP 2021568760A JP WO2020234782 A5 JPWO2020234782 A5 JP WO2020234782A5
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- pharmaceutical composition
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- pharmaceutically acceptable
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- 150000001875 compounds Chemical class 0.000 claims description 39
- 150000003839 salts Chemical class 0.000 claims description 29
- 206010072757 chronic spontaneous urticaria Diseases 0.000 claims description 10
- 208000024376 chronic urticaria Diseases 0.000 claims description 10
- 208000028185 Angioedema Diseases 0.000 claims description 6
- 208000003251 Pruritus Diseases 0.000 claims description 6
- 208000024780 Urticaria Diseases 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- 230000009885 systemic effect Effects 0.000 claims description 6
- 229940125715 antihistaminic agent Drugs 0.000 claims description 4
- 239000000739 antihistaminic agent Substances 0.000 claims description 4
- 229940065725 leukotriene receptor antagonists for obstructive airway diseases Drugs 0.000 claims description 4
- 239000003199 leukotriene receptor blocking agent Substances 0.000 claims description 4
- 230000008034 disappearance Effects 0.000 claims description 3
- 101100365206 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) SEC9 gene Proteins 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 230000002459 sustained effect Effects 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 20
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- 210000003651 basophil Anatomy 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
Description
上記の臨床試験及び前臨床エビデンスからのデータは１０ｍｇ～２００ｍｇの１日用量の化合物（Ｉ）が、好塩基球及びマスト駆動皮膚疾患の治療に安全で且つ薬理学的に有効であることを示している。
以下の態様を包含し得る。
［１］ 慢性自発性蕁麻疹（ＣＳＵ）の治療を、そのような治療を必要する対象に行うために使用する、式（Ｉ）の化合物
［２］ 前記１日用量は約１０ｍｇ～約１００ｍｇである、上記［１］に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［３］ 前記１日用量は約１００ｍｇである、上記［１］に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［４］ 前記１日用量は約５０ｍｇである、上記［１］に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［５］ 前記１日用量は約３５ｍｇである、上記［１］に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［６］ 前記１日用量は約２５ｍｇである、上記［１］に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［７］ 前記１日用量は約２０ｍｇである、上記［１］に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［８］ 前記式（Ｉ）の化合物は、約１０ｍｇ、約３５ｍｇ、約５０ｍｇ又は約１００ｍｇの用量で１日１回投与される、上記［１］に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［９］ 前記式（Ｉ）の化合物又はその薬学的に許容される塩は、約１０ｍｇ、約２５ｍｇ、約５０ｍｇ又は約１００ｍｇの用量で１日２回投与される、上記［１］に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［１０］ 前記式（Ｉ）の化合物での治療の前に、前記対象はＣＳＵ用全身性薬剤で既に治療されたことがある、上記［１］～［９］のいずれか一項に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［１１］ 前記全身性薬剤は、Ｈ１－抗ヒスタミン薬（Ｈ１－ＡＨ）、Ｈ２－抗ヒスタミン薬（Ｈ２－ＡＨ）、及びロイコトリエン受容体拮抗薬（ＬＴＲＡ）、並びにこれらの組み合わせからなる群から選択される、上記［１０］に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［１２］ 前記式（Ｉ）の化合物での治療の前に、前記対象はＣＳＵ用全身性薬剤で治療されたことがない、上記［１］～［９］のいずれか一項に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［１３］ 前記対象は中等度から重度のＣＳＵを有する、上記［１］～［１２］のいずれか一項に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［１４］ 前記対象は以下の基準：
ａ）式（Ｉ）の化合物又はその薬学的に許容される塩での治療の前に、前記対象は、１６以上のＵＡＳ７スコアを有する；
ｂ）前記式（Ｉ）の化合物又はその薬学的に許容される塩での治療の前に、前記対象は、８以上のＨＳＳ７スコアを有する
の少なくとも１つに従って選択される、上記［１］～［１２］のいずれか一項に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［１５］ 前記対象は成人である、上記［１］～［１４］のいずれか一項に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［１６］ 前記対象は治療の４週目又は１２週目までに、以下のうちの：
ａ）ＵＡＳ≦６で判断される蕁麻疹及び掻痒の減少、若しくは蕁麻疹及び掻痒の完全な消失（ＵＡＳ７＝０）；又は
ｂ）皮膚科関連ＱＯＬ評価指標（ＤＬＱＩ）＝０～１；
ｃ）血管性浮腫活動性スコア（ＡＡＳ７）がゼロで判断される血管浮腫がないこと
少なくとも１つを達成する、上記［１］～［１５］のいずれか一項に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［１７］ 前記対象は、完全な蕁麻疹及び掻痒の応答（［ＵＡＳ７］＝０）及び／又は皮膚科関連ＱＯＬ評価指標（ＤＬＱＩ）＝０～１及び／又は前記治療の完了後４週目に血管性浮腫の消失の継続（ＡＡＳ７＝０）によって判断される持続的応答を達成する、上記［１］～［１６］のいずれか一項に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［１８］ 前記式（Ｉ）の化合物又はその薬学的に許容される塩は医薬製剤に配合され、前記医薬製剤は薬学的に許容される担体をさらに含む、上記［１］～［１７］のいずれか一項に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
［１９］ 前記式（Ｉ）の化合物又はその薬学的に許容される塩は、約０．５～３時間のＴ
ｍａｘ
を有する、上記［１］～［１７］のいずれか一項に記載の使用のための式（Ｉ）の化合物又はその薬学的に許容される塩。
Data from the above clinical trials and preclinical evidence indicate that daily doses of 10 mg to 200 mg of compound (I) are safe and pharmacologically effective in the treatment of basophil and mast-driven skin disorders. ing.
The following aspects may be included.
[1] A compound of formula (I) for use in treating chronic spontaneous urticaria (CSU) in a subject in need of such treatment
[2] A compound of formula (I) or a pharmaceutically acceptable salt thereof for use according to [1] above, wherein said daily dose is about 10 mg to about 100 mg.
[3] A compound of formula (I) or a pharmaceutically acceptable salt thereof for use according to [1] above, wherein said daily dose is about 100 mg.
[4] A compound of formula (I) or a pharmaceutically acceptable salt thereof for use according to [1] above, wherein said daily dose is about 50 mg.
[5] A compound of formula (I) or a pharmaceutically acceptable salt thereof for use according to [1] above, wherein said daily dose is about 35 mg.
[6] A compound of formula (I) or a pharmaceutically acceptable salt thereof for use according to [1] above, wherein said daily dose is about 25 mg.
[7] A compound of formula (I) or a pharmaceutically acceptable salt thereof for use according to [1] above, wherein said daily dose is about 20 mg.
[8] The compound of formula (I) for use according to [1] above, wherein the compound of formula (I) is administered once daily at a dose of about 10 mg, about 35 mg, about 50 mg or about 100 mg. A compound or a pharmaceutically acceptable salt thereof.
[9] The above-described [1], wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered twice daily at a dose of about 10 mg, about 25 mg, about 50 mg, or about 100 mg. A compound of formula (I) or a pharmaceutically acceptable salt thereof for use.
[10] The subject according to any one of [1] to [9] above, wherein prior to treatment with the compound of formula (I), the subject has previously been treated with a systemic agent for CSU. A compound of formula (I) or a pharmaceutically acceptable salt thereof for use.
[11] the systemic agent is selected from the group consisting of H1-antihistamines (H1-AH), H2-antihistamines (H2-AH), and leukotriene receptor antagonists (LTRA), and combinations thereof; A compound of formula (I) or a pharmaceutically acceptable salt thereof for use according to [10] above.
[12] The use of any one of [1] to [9] above, wherein the subject has not been treated with a systemic agent for CSU prior to treatment with the compound of formula (I). A compound of formula (I) or a pharmaceutically acceptable salt thereof for
[13] The compound of formula (I) or a pharmaceutically acceptable salt thereof for use according to any one of [1] to [12] above, wherein the subject has moderate to severe CSU .
[14] The subject has the following criteria:
a) said subject has a UAS7 score of 16 or greater prior to treatment with a compound of formula (I) or a pharmaceutically acceptable salt thereof;
b) said subject has an HSS7 score of 8 or greater prior to treatment with said compound of formula (I) or a pharmaceutically acceptable salt thereof;
A compound of formula (I) or a pharmaceutically acceptable salt thereof for use according to any one of [1] to [12] above, selected according to at least one of
[15] A compound of formula (I) or a pharmaceutically acceptable salt thereof for use according to any one of [1] to [14] above, wherein the subject is an adult.
[16] The subject has, by Week 4 or Week 12 of treatment, any of the following:
a) reduction in urticaria and pruritus as judged by UAS≦6, or complete disappearance of urticaria and pruritus (UAS7=0); or
b) Dermatology-related QOL index (DLQI) = 0-1;
c) No angioedema with an angioedema activity score (AAS7) of zero
A compound of formula (I), or a pharmaceutically acceptable salt thereof, for use according to any one of [1] to [15] above, which achieves at least one.
[17] The subject has a complete urticaria and pruritus response ([UAS7] = 0) and/or a dermatology-related QOL index (DLQI) = 0-1 and/or at 4 weeks after completion of the treatment A compound of formula (I) for use according to any one of [1] to [16] above, which achieves a sustained response as judged by continued resolution of angioedema (AAS7=0); a pharmaceutically acceptable salt thereof.
[18] The above [1] to [17], wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is incorporated into a pharmaceutical preparation, and the pharmaceutical preparation further comprises a pharmaceutically acceptable carrier. A compound of formula (I) or a pharmaceutically acceptable salt thereof for use according to any one of the claims.
[19] The compound of formula (I) or a pharmaceutically acceptable salt thereof according to any one of [1] to [17] above, wherein the T max is about 0.5 to 3 hours. A compound of formula (I) or a pharmaceutically acceptable salt thereof for use.
Claims (19)
ａ）式（Ｉ）の化合物又はその薬学的に許容される塩での治療の前に、前記対象は、１６以上のＵＡＳ７スコアを有する；
ｂ）前記式（Ｉ）の化合物又はその薬学的に許容される塩での治療の前に、前記対象は、８以上のＨＳＳ７スコアを有する
の少なくとも１つに従って選択される、請求項１～１２のいずれか一項に記載の医薬組成物。 Said subjects are subject to the following criteria:
a) said subject has a UAS7 score of 16 or greater prior to treatment with a compound of formula (I) or a pharmaceutically acceptable salt thereof;
b) prior to treatment with said compound of formula (I) or a pharmaceutically acceptable salt thereof, said subject is selected according to at least one of claims 1-12 having an HSS7 score of 8 or greater; The pharmaceutical composition according to any one of
ａ）ＵＡＳ≦６で判断される蕁麻疹及び掻痒の減少、若しくは蕁麻疹及び掻痒の完全な消失（ＵＡＳ７＝０）；又は
ｂ）皮膚科関連ＱＯＬ評価指標（ＤＬＱＩ）＝０～１；
ｃ）血管性浮腫活動性スコア（ＡＡＳ７）がゼロで判断される血管浮腫がないこと
少なくとも１つを達成する、請求項１～１５のいずれか一項に記載の医薬組成物。 By Week 4 or Week 12 of treatment, the subject has any of the following:
a) reduction in urticaria and pruritus, or complete disappearance of urticaria and pruritus as judged by UAS ≤ 6 (UAS7 = 0); or b) dermatology-related QOL index (DLQI) = 0-1;
The pharmaceutical composition according to any one of claims 1 to 15, which achieves at least one of c) the absence of angioedema judged by an angioedema activity score (AAS7) of zero.
18. The pharmaceutical composition according to any one of claims 1-17, wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof has a T max of about 0.5-3 hours.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962851996P | 2019-05-23 | 2019-05-23 | |
| US62/851,996 | 2019-05-23 | ||
| PCT/IB2020/054755 WO2020234782A1 (en) | 2019-05-23 | 2020-05-20 | Methods of treating chronic spontaneous urticaria using a bruton's tyrosine kinase inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022533981A JP2022533981A (en) | 2022-07-27 |
| JPWO2020234782A5 true JPWO2020234782A5 (en) | 2023-05-26 |
| JP7568651B2 JP7568651B2 (en) | 2024-10-16 |
Family
ID=70918751
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021568760A Active JP7568651B2 (en) | 2019-05-23 | 2020-05-20 | Methods for treating chronic spontaneous urticaria using Bruton's tyrosine kinase inhibitors |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20220184074A1 (en) |
| EP (1) | EP3972604A1 (en) |
| JP (1) | JP7568651B2 (en) |
| KR (1) | KR20220012281A (en) |
| CN (1) | CN113795255A (en) |
| AU (1) | AU2020280272A1 (en) |
| BR (1) | BR112021022602A2 (en) |
| CA (1) | CA3138081A1 (en) |
| CL (1) | CL2021003032A1 (en) |
| IL (1) | IL286983A (en) |
| MX (1) | MX2021013942A (en) |
| TW (1) | TW202110450A (en) |
| WO (1) | WO2020234782A1 (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW202310841A (en) | 2021-09-03 | 2023-03-16 | 瑞士商諾華公司 | Lou064 for treating multiple sclerosis |
| MX2024007354A (en) | 2021-12-14 | 2024-06-28 | Novartis Ag | Methods of treatment using lou064. |
| TW202342048A (en) | 2022-02-28 | 2023-11-01 | 瑞士商諾華公司 | Methods of treating hidradenitis suppurativa using lou064 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9512084B2 (en) | 2013-11-29 | 2016-12-06 | Novartis Ag | Amino pyrimidine derivatives |
| WO2016079669A1 (en) * | 2014-11-19 | 2016-05-26 | Novartis Ag | Labeled amino pyrimidine derivatives |
-
2020
- 2020-05-20 CA CA3138081A patent/CA3138081A1/en active Pending
- 2020-05-20 US US17/612,778 patent/US20220184074A1/en active Pending
- 2020-05-20 KR KR1020217041089A patent/KR20220012281A/en unknown
- 2020-05-20 EP EP20729204.6A patent/EP3972604A1/en active Pending
- 2020-05-20 WO PCT/IB2020/054755 patent/WO2020234782A1/en unknown
- 2020-05-20 AU AU2020280272A patent/AU2020280272A1/en active Pending
- 2020-05-20 MX MX2021013942A patent/MX2021013942A/en unknown
- 2020-05-20 CN CN202080032000.3A patent/CN113795255A/en active Pending
- 2020-05-20 BR BR112021022602A patent/BR112021022602A2/en unknown
- 2020-05-20 JP JP2021568760A patent/JP7568651B2/en active Active
- 2020-05-21 TW TW109116854A patent/TW202110450A/en unknown
-
2021
- 2021-10-05 IL IL286983A patent/IL286983A/en unknown
- 2021-11-17 CL CL2021003032A patent/CL2021003032A1/en unknown
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