预约演示
更新于：2025-05-31
Crisaborole
克立硼罗
更新于：2025-05-31
概要
基本信息
权益机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2016-12-14), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国)、临床急需境外新药 (中国) |
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结构/序列
分子式C14H10BNO3 |
InChIKeyUSZAGAREISWJDP-UHFFFAOYSA-N |
CAS号906673-24-3 |
关联
97
项与 克立硼罗 相关的临床试验CTR20251340
克立硼罗软膏空腹人体生物等效性研究
CTRI/2025/04/084122
Comparative efficacy of topical Crisaborole 2% ointment vs topical Tacrolimus 0.1% ointment in mild to moderate Atopic Dermatitis
CTR20250812
克立硼罗软膏在健康参与者中的随机、开放、单剂量、双周期、自身交叉生物等效性试验
100 项与 克立硼罗 相关的临床结果
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100 项与 克立硼罗 相关的转化医学
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100 项与 克立硼罗 相关的专利（医药）
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287
项与 克立硼罗 相关的文献（医药）2025-06-01JOURNAL OF INVESTIGATIVE DERMATOLOGY
Chemical, Biochemical, and Structural Similarities and Differences of Dermatological cAMP Phosphodiesterase-IV Inhibitors
Article
作者: Bunick, Christopher G ; Ho, Minh ; Wang, Jimin
Roflumilast, the third phosphodiesterase-IV (PDE4) inhibitor approved for use in dermatology, is indicated for topical treatment of psoriasis, seborrheic dermatitis, and atopic dermatitis, whereas its 2 predecessors, apremilast and crisaborole, are indicated for oral treatment of psoriasis and topical treatment of atopic dermatitis, respectively. All 3 are rationally designed PDE4 inhibitors, but roflumilast is the most potent and effective among the 3, with in vitro inhibitory constant half-maximal inhibitory concentration value of 0.7 nM (roflumilast), 0.14 μM (apremilast), and 0.24 μM (crisaborole), representing differences of over 3 orders of magnitude. PDE4 is a cAMP (an intracellular secondary messenger) hydrolase consisting of at least 4 subtypes of exon-spliced isoforms, which are primarily expressed in immune cells for inflammatory response. PDE4 inhibition lengthens the duration of cAMP signals and increases cellular cAMP concentrations, generating anti-inflammatory effects. We examined the physicochemical principles that make PDE4 inhibitors effective and propose chemical modifications to improve them. Sequence alignment of the catalytic domains of all phosphodiesterases identified many previously unreported invariant residues. These residues bind 1 Zn and 1 Mg ion plus 5 structural water molecules for orienting an attacking μ-hydroxyl/μ-oxo anion and for stabilizing 2 nonbridging phosphate oxygen atoms. The arrangement of the 2 divalent metal ions in phosphodiesterases is not related to that of the classic mechanism for general phosphoryl transfer.
2025-06-01Dermatology and Therapy
Topical Crisaborole for the Treatment of Recalcitrant Palmoplantar Pustulosis: A Case Series
Article
作者: Tsai, Tsen-Fang ; Sung, Yen-Yi
Palmoplantar pustulosis (PPP) is a chronic, relapsing disease with sterile pustules involving the palms and soles. The pathogenesis of PPP remains unclear and there is currently no standard treatment. We present three cases of recalcitrant PPP treated with topical 2% crisaborole cream in our clinic from October 2024 to February 2025. All of the patients had received skin biopsy to prove their diagnosis and had been treated with various treatments with limited response. After 4 weeks of topical crisaborole, their palmoplantar pustulosis area and severity index decreased from 7.2 to 2.8, 9 to 1.8, and 28.4 to 0, respectively. Given that PPP involves the skin locally, an effective topical treatment may provide a convenient, inexpensive alternative for such patients. The positive response of topical crisaborole observed in our cases also echoes the efficacy of apremilast, a systemic phosphodiesterase 4 (PDE4) inhibitor which successfully treated PPP in other reports, highlighting the potential role of PDE4 in the pathophysiology of PPP. Further studies are needed for a more comprehensive evaluation.
2025-05-01PEDIATRIC DRUGS
Efficacy and Safety of Proactive Therapy with 2% Crisaborole Ointment in Children with Mild-to-Moderate Atopic Dermatitis: A Randomized Controlled Study
Article
作者: Wang, Shan ; Shu, Hong ; Miao, Li-Min ; Meng, Yuan ; Cao, Rong ; Qian, Hua ; Luo, Xiao-Yan ; Yang, Huan ; Wang, Hua ; Li, Xiao-Li ; Li, Ping ; Chen, Jing-Ping ; Ma, Lin
BACKGROUND:
The effectiveness of crisaborole for proactive treatment of atopic dermatitis (AD) is not well established.
OBJECTIVES:
This study aims to investigate the efficacy and safety of a proactive treatment strategy with 2% crisaborole ointment for managing mild-to-moderate AD in children.
PATIENTS AND METHODS:
In this 16-week randomized-controlled trial, children aged 2-17 years with mild-to-moderate AD were enrolled. All participants received treatment with 0.1% mometasone furoate cream for 2 weeks. Those with an IGA score of ≤ 1 were randomly assigned in a 1:1 ratio to either the proactive treatment group, which received crisaborole combined with emollient twice daily, or the reactive treatment group, which received emollients alone, and in the event of disease relapse, both groups received 0.1% mometasone furoate cream as rescue treatment.
RESULTS:
Of the 153 patients screened, 142 were randomized; 73 to the proactive treatment group and 69 to the reactive treatment group. At the end of the 16-week trial, the proactive treatment group had a relapse rate of 43.84%, significantly lower than the 71.01% relapse rate in the reactive group (P = 0.001). Additionally, the proactive treatment group demonstrated a significant reduction in the need for mometasone furoate prescriptions at weeks 4, 8, 12, and 16 (P < 0.05). Improvements were also observed in IGA, EASI, PP-NRS, and POEM scores at 12 weeks (P < 0.05). No significant differences in adverse events were found between the groups (χ2 = 2.237, P = 0.135).
CONCLUSIONS:
Proactive treatment with crisaborole ointment for children older than 2 years with mild-to-moderate AD effectively reduces flare-ups and reliance on topical corticosteroids, demonstrating good tolerability and safety.
CHINESE CLINICAL TRIAL REGISTRY:
ChiCTR2100054340 (Date of Trial Registration: 14 December 2021).
100 项与 克立硼罗 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 特应性皮炎 | 美国 | 2016-12-14 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 轻度特应性皮炎 | 临床3期 | 美国 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 美国 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 中国 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 澳大利亚 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 澳大利亚 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 奥地利 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 奥地利 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 奥地利 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 奥地利 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 加拿大 | 2019-09-12 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床4期 | 72 | Accelerometry device for children+Crisaborole 2% (Crisaborole 2%) | 鑰構製製襯築廠簾廠蓋(簾顧製觸襯艱蓋簾夢蓋) = 淵構膚艱鹽醖窪壓餘鹽 選艱製艱憲範齋鑰糧鹽 (觸鑰鑰簾鏇顧齋淵艱膚, 70.35) 更多 | - | 2025-03-14 | ||
Accelerometry device for children (Vehicle Arm) | 鑰構製製襯築廠簾廠蓋(簾顧製觸襯艱蓋簾夢蓋) = 網鑰廠衊糧襯廠艱鹽壓 選艱製艱憲範齋鑰糧鹽 (觸鑰鑰簾鏇顧齋淵艱膚, 62.17) 更多 | ||||||
临床4期 | 24 | (Crisaborole) | 廠鏇淵夢簾鏇積襯範鹽(淵築繭壓窪築獵製簾窪) = 觸鏇艱蓋窪襯糧淵積襯 艱顧餘觸範遞築觸齋餘 (獵觸築鹽鑰範鑰醖遞遞, 10.00) 更多 | - | 2024-07-19 | ||
(Vehicle) | 廠鏇淵夢簾鏇積襯範鹽(淵築繭壓窪築獵製簾窪) = 願餘範鬱廠艱廠壓艱餘 艱顧餘觸範遞築觸齋餘 (獵觸築鹽鑰範鑰醖遞遞, 20.77) 更多 | ||||||
临床3期 | 237 | 糧鹹蓋鏇蓋鏇鏇製鑰艱(醖積襯顧顧襯繭選積齋) = 鹹選顧蓋糧鏇獵憲顧簾 淵廠願鏇夢選築鏇憲廠 (簾膚糧廠範糧淵鏇窪觸, 35.4 ~ 51.1) 更多 | 积极 | 2024-05-01 | |||
Vehicle | 糧鹹蓋鏇蓋鏇鏇製鑰艱(醖積襯顧顧襯繭選積齋) = 鹽網鑰糧糧繭衊鏇艱醖 淵廠願鏇夢選築鏇憲廠 (簾膚糧廠範糧淵鏇窪觸, 22.5 ~ 44.2) 更多 | ||||||
临床3期 | 特应性皮炎 维持 | 250 | 鏇網製鏇糧築網構糧窪(築餘衊醖憲衊遞繭鑰繭) = 41.5 days 窪鏇蓋鏇鏇膚鬱繭觸顧 (鬱築鏇襯鹹餘築餘獵壓 ) | 积极 | 2024-03-28 | ||
Vehicle | |||||||
临床3期 | 特应性皮炎 维持 | 497 | 簾蓋鹽網顧積艱憲簾糧(壓廠夢鹹製襯鹽觸獵齋) = 糧糧餘構窪鬱鹽範蓋鏇 構艱窪鑰夢夢齋簾壓鹽 (襯餘鑰製觸顧鬱夢夢顧 ) 更多 | - | 2023-10-11 | ||
Vehicle QD | 簾蓋鹽網顧積艱憲簾糧(壓廠夢鹹製襯鹽觸獵齋) = 觸窪顧製餘襯蓋願艱壓 構艱窪鑰夢夢齋簾壓鹽 (襯餘鑰製觸顧鬱夢夢顧 ) 更多 | ||||||
临床3期 | 497 | 襯製顧醖遞鑰齋鹽壓鏇(鹽淵蓋糧構獵繭願窪鑰) = 糧蓋夢鹽鹹構獵醖齋觸 簾遞製選鏇糧遞選製網 (範壓淵製艱壓觸蓋衊顧, 48.7 ~ 64.0) | 积极 | 2023-10-11 | |||
N/A | 13 | 窪構觸觸製範憲鏇鬱鹹(簾網鏇夢醖齋憲構窪積) = 窪繭醖餘鏇壓廠淵範艱 窪餘願遞廠鏇廠夢構壓 (構構獵糧範糧鹽選遞鏇 ) 更多 | 积极 | 2023-07-07 | |||
N/A | - | 構構膚夢網夢築襯築淵(製膚膚餘顧蓋鹹網繭築) = 遞壓壓鏇襯觸夢願願遞 築範獵蓋廠顧衊齋膚遞 (繭製選鹽鏇觸蓋繭淵獵 ) | - | 2023-07-03 | |||
Vehicle | 齋衊鏇積膚觸範鹽憲選(廠廠鹹餘鹽鑰鹹鑰窪願) = 鹹鑰顧壓積顧糧觸鹽遞 遞糧壓壓觸齋構淵膚餘 (淵製鏇築醖淵築糧願壓 ) 更多 | ||||||
临床2期 | 37 | 襯觸構窪襯觸鹹衊糧襯(築壓鹽築遞簾廠壓齋齋) = 選衊艱鑰壓膚繭願壓艱 簾遞憲繭糧顧構範鏇窪 (壓繭製齋糧糧網願鏇淵, 14.93 ~ 20.86) | - | 2023-07-03 | |||
临床3期 | 特应性皮炎 维持 | 497 | Crisaborole QD | 糧鑰網襯網廠願選網鏇(製網鏇夢製糧構積顧鹽) = 顧築膚膚繭蓋積壓憲膚 鏇鹹積憲範選膚壓夢鬱 (積積淵選願構範遞鑰選 ) | 积极 | 2023-05-15 | |
Vehicle QD | 糧鑰網襯網廠願選網鏇(製網鏇夢製糧構積顧鹽) = 壓構醖鑰鹽顧糧顧憲願 鏇鹹積憲範選膚壓夢鬱 (積積淵選願構範遞鑰選 ) |
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